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Fludarabine (NSC 118218)

别名: FaraA; Fludarabinum; HSDB 6964; F-ara-A; HSDB6964; NSC118218; HSDB-6964; NSC 118218; F-ara A; 21679-14-1; F-Ara-A; 2-Fluoro Ara-A; (2R,3S,4S,5R)-2-(6-Amino-2-fluoro-9H-purin-9-yl)-5-(hydroxymethyl)tetrahydrofuran-3,4-diol; 9-beta-D-Arabinofuranosyl-2-fluoroadenine; Fludarabine [INN]; Fludarabina;NSC-118218 氟达拉滨;9-beta-D-呋喃阿糖基-2-氟-9H-嘌呤-6-胺;氟达那甙;氟达那苷;氟达拉宾;氟达拉宾碱;9-Β-D-阿拉伯呋喃糖-2-氟腺苷;氟达拉滨碱(BASE);9-beta-D-呋喃阿糖基-2-氟-9H-嘌;Fludarabine 氟达拉宾; 品牌 氟达拉宾对照品;氟达拉滨(杂质E);氟达拉滨碱;氟達拉濱
目录号: V1379 纯度: ≥98%
COA 产品数据 产品说明书 SDS
Fludarabine（也称为 FaraA、Fludarabinum；NSC-118218；F-ara-A、HSDB6964；NSC118218；HSDB-6964）是一种有效的 STAT1 激活抑制剂和 DNA 合成抑制剂，已被批准作为化疗药物，用于治疗白血病和淋巴瘤。
Fludarabine (NSC 118218) CAS号: 21679-14-1
产品类别: DNA(RNA) Synthesis
产品仅用于科学研究，不针对患者销售
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纯度/质量控制文件

纯度: ≥98%

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产品说明书
产品描述
氟达拉滨（也称为 FaraA、Fludarabinum；NSC-118218；F-ara-A、HSDB6964；NSC118218；HSDB-6964）是一种有效的 STAT1 激活抑制剂和 DNA 合成抑制剂，已被批准作为化疗药物，用于治疗治疗白血病和淋巴瘤。氟达拉滨是一种前药，在细胞中磷酸化为三磷酸核苷 (F-ara-ATP)，从而产生生物活性。它影响DNA合成所需的一系列酶，如DNA引物酶、DNA聚合酶、DNA连接酶I、核糖核苷酸还原酶以及DNA聚合酶δ和ε的3'-5'核酸外切酶活性。在人骨髓瘤细胞 RPMI8226 中，氟达拉滨显着抑制细胞生长并降低 Akt 磷酸化。
生物活性&实验参考方法
靶点
DNA synthesis; STAT1
Fludarabine (NSC 118218) targets ribonucleotide reductase (RR) with an IC50 of 0.2 μM [2]
Fludarabine (NSC 118218) inhibits DNA polymerase α (IC50=0.5 μM) and DNA polymerase δ (IC50=0.8 μM) [2]
Fludarabine (NSC 118218) acts as a competitive inhibitor of adenosine deaminase (ADA) with a Ki value of 1.3 μM [2]
体外研究 (In Vitro)
氟达拉滨有效抑制 RPMI 8226 细胞的增殖，IC50 为 1.54 μg/mL。 Fludarabine 对 MM.1S 和 MM.1R 细胞的 IC50 分别为 13.48 μg/mL 和 33.79 μg/mL。相比之下，U266 细胞对氟达拉滨具有耐药性，IC50 为 222.2 μg/mL。氟达拉滨治疗导致细胞周期 G1 期细胞数量增加，同时细胞周期 S 期细胞数量以时间依赖性方式减少。氟达拉滨诱导细胞周期阻滞并引发 MM 细胞凋亡。 Fludarabine 触发 caspase-8、-9 和 -3、-7 的时间依赖性裂解，然后是 PARP 裂解。氟达拉滨以时间依赖性方式增加 Bax 的表达，而 Bak 的表达不改变。暴露于氟达拉滨 12 小时后，RPMI 8226 细胞表现出膜电位损失，其中 61.05% 的细胞表达罗丹明 123 的低荧光，而未经处理的对照细胞中只有 8.62% 的细胞表达低荧光。为了提高溶解度，氟达拉滨被配制为单磷酸盐（F-ara-AMP，福达拉滨），在静脉输注后立即定量地去磷酸化为母体核苷。细胞内部发生再磷酸化，生成氟腺嘌呤阿糖苷三磷酸 (F-ara-ATP)，它是 F-ara-A 的主要细胞毒性代谢物。氟达拉滨还可以诱导单核细胞的促炎刺激，通过 ICAM-1 表达增加和 IL-8 释放来评估。氟达拉滨不影响卵巢癌细胞系的生长，但它会显着且剂量依赖性地抑制黑色素瘤细胞系的增殖。细胞测定：用氟达拉滨或对照、地塞米松敏感 (MM.1S) 和耐药 (MM.1R) 人 MM 细胞系、RPMI8226 和 U266 细胞系（5 × 105 个细胞）处理后，在磷酸盐缓冲盐水中洗涤两次(PBS) 并用 70% 冰冷乙醇固定，然后离心并悬浮于含有 100 μg/mL RNase A 的 PBS 中。37 ℃ 孵育 30 分钟后，将样品重悬于 25 μg/mL 碘化丙啶中。流式细胞术在 FACSCalibur 自动化系统上进行。根据制造商的说明，通过Annexin V-FITC细胞凋亡检测试剂盒测定细胞凋亡。对于 TUNEL（末端脱氧核苷酸转移酶介导的脱氧尿苷三磷酸缺口末端标记）测定，使用原位细胞死亡检测试剂盒通过流式细胞术分析细胞。
Fludarabine (NSC 118218)（0.1-10 μM）剂量依赖性抑制人B细胞慢性淋巴细胞白血病（B-CLL）细胞增殖，IC50=0.8 μM [1]
Fludarabine (NSC 118218)（1 μM）诱导B-CLL细胞凋亡：凋亡率提高38%（Annexin V/PI染色），caspase-3活性增强2.5倍 [1]
Fludarabine (NSC 118218)（0.5-5 μM）抑制人白血病细胞（HL-60）中的RR活性，使脱氧核糖核苷酸（dNTP）池水平降低45-68% [2]
Fludarabine (NSC 118218)（1-10 μM）抑制HeLa细胞的DNA合成，5 μM时[3H]-胸腺嘧啶掺入量减少72% [2]
Fludarabine (NSC 118218)（2-8 μM）调控免疫细胞功能：使人外周血单个核细胞（PBMCs）的TNF-α和IFN-γ分泌减少35-52% [3]
Fludarabine (NSC 118218)（1-5 μM）对成年大鼠心肌细胞无直接细胞毒性，但可减轻TNF-α诱导的心肌细胞肥大（细胞表面积减少30%）[5]
Fludarabine (NSC 118218)（0.3-3 μM）抑制人非霍奇金淋巴瘤（NHL）细胞（Raji、Daudi）生长，IC50值分别为0.7 μM和0.9 μM [4]
体内研究 (In Vivo)
用 PBS 处理的肿瘤在 25 天内迅速生长至其初始体积的约 10 倍，而在 40 mg/kg 的氟达拉滨中，肿瘤的增长不到 5 倍。 40 mg/kg Fludarabine 对 RPMI8226 肿瘤生长具有显着的抗肿瘤作用。第 10 天用 40 mg/kg 氟达拉滨治疗的 RPMI8226 肿瘤细胞凋亡细胞增加。 Fludarabine 可有效抑制 SCID 小鼠中的 RPMI8226 骨髓瘤异种移植物。[1]
Fludarabine (NSC 118218)（20 mg/kg，静脉注射，每周一次，持续3周）抑制裸鼠Raji NHL移植瘤生长：肿瘤体积减少62%，肿瘤重量较溶媒组降低58% [4]
Fludarabine (NSC 118218)（15 mg/kg，腹腔注射，每日一次，持续5天）使B-CLL转基因小鼠的循环B-CLL细胞减少70% [1]
Fludarabine (NSC 118218)（10 mg/kg，静脉注射，隔天一次，持续7天）减轻腹主动脉缩窄（AAC）诱导的大鼠心肌肥大：左心室壁厚度减少28% [5]
Fludarabine (NSC 118218)（10 mg/kg，静脉注射）使大鼠心肌组织中TNF-α和IL-6蛋白水平分别降低42%和38%，并抑制NF-κB激活 [5]
酶活实验
氟达拉滨是一种核苷类似物，由于其对淋巴细胞的强细胞毒性活性，已成功用于治疗低级别淋巴细胞恶性肿瘤，最近也用于干细胞移植的非清髓性预备方案。在本文中，我们发现氟达拉滨也可以诱导单核细胞的促炎刺激，通过增加ICAM-1的表达和IL-8的释放来评估。为了研究其中的机制，我们使用了MAPK和NF-kappaB途径的选择性抑制剂，这两种途径都与ICAM-1和IL-8的调节有关。我们的研究结果表明氟达拉滨的作用是通过激活ERK介导的，并且不依赖于p38、JNK或NF-kappaB途径。通过Western blotting分析，我们证实了氟达拉滨诱导ERK的快速激活，持续至少30分钟。此外，氟达拉滨对单核细胞的促炎激活在很大程度上被自由基清除剂n -乙酰半胱氨酸共同给予减弱，这表明活性氧参与了氟达拉滨的作用。最后，我们发现氟达拉滨不仅在单核细胞中，而且在慢性淋巴细胞白血病的非增殖淋巴细胞中诱导转录因子AP-1的激活。体内氟达拉滨的一些副作用可能归因于细胞活化/分化，而不是诱导细胞凋亡。[3]
将重组核糖核苷酸还原酶（RR）与核糖核苷酸底物（CDP、GDP）及系列浓度的Fludarabine (NSC 118218)（0.01-1 μM）在反应缓冲液中于37°C孵育60分钟。通过HPLC分离并定量脱氧核糖核苷酸产物，拟合量效抑制曲线计算IC50值 [2]
将纯化的DNA聚合酶α/δ与活化的DNA模板、dNTP底物（含[3H]-dTTP）及Fludarabine (NSC 118218)（0.1-5 μM）在检测缓冲液中混合。37°C孵育30分钟后，通过闪烁计数法测量掺入的[3H]-dTTP放射性，评估酶抑制活性 [2]
将腺苷脱氨酶（ADA）与腺苷底物及Fludarabine (NSC 118218)（0.1-10 μM）在磷酸盐缓冲液中于25°C孵育20分钟。在265 nm波长下通过分光光度法监测肌苷的生成，利用Lineweaver-Burk图确定Ki值 [2]
细胞实验
氟达拉滨或对照处理的人 MM 细胞系 RPMI8226 和 U266（5 × 10 5 细胞）对地塞米松敏感 (MM.1S) 和耐药 (MM.1R)，并用70% 冰冷乙醇，离心，悬浮于含有 100 μg/mL RNase A 的 PBS 中。37 ℃ 孵育 30 分钟后，在 25 μg/mL 碘化丙啶中进行采样。 FACSCalibur 自动化系统用于进行流式细胞术。按照制造商的说明，使用膜联蛋白 V-FITC 细胞凋亡检测试剂盒来鉴定细胞凋亡。原位细胞死亡检测试剂盒辅助流式细胞术用于分析细胞，进行 TUNEL（末端脱氧核苷酸转移酶介导的脱氧尿苷三磷酸缺口末端标记）测定。
从患者血液中分离人B-CLL细胞，接种于96孔板（1×10^5个细胞/孔）。用Fludarabine (NSC 118218)（0.1-10 μM）处理细胞72小时，MTT法评估细胞活力并计算IC50。凋亡检测采用Annexin V-FITC/PI染色，流式细胞术分析 [1]
将HL-60白血病细胞接种于6孔板（2×10^5个细胞/孔），用Fludarabine (NSC 118218)（0.5-5 μM）处理48小时。裂解细胞后，通过HPLC检测dNTP生成量以测定RR活性，[3H]-胸腺嘧啶掺入法评估DNA合成 [2]
从健康供体中分离人PBMCs，接种于24孔板（5×10^5个细胞/孔）。用LPS（1 μg/mL）刺激并加入Fludarabine (NSC 118218)（2-8 μM）处理24小时，收集培养上清液，ELISA法检测TNF-α和IFN-γ水平 [3]
分离成年大鼠心肌细胞并接种于24孔板。用Fludarabine (NSC 118218)（1-5 μM）预处理细胞1小时，随后用TNF-α（10 ng/mL）刺激48小时。相差显微镜下测量细胞表面积，免疫荧光检测NF-κB核转位 [5]
将Raji和Daudi NHL细胞接种于96孔板（5×10^3个细胞/孔），用Fludarabine (NSC 118218)（0.3-3 μM）处理72小时。比色法评估细胞增殖，软琼脂集落形成实验中接种细胞，14天后计数集落数 [4]
动物实验
溶于PBS；40 mg/kg；腹腔注射
携带RPMI 8226细胞的重症联合免疫缺陷（SCID）小鼠 皮下和播散性MM异种移植模型的建立及治疗 重症联合免疫缺陷（SCID）小鼠饲养于符合机构批准的动物实验方案的设施中。对于皮下异种移植MM RPMI 8226小鼠模型，将10 × 10⁶个RPMI 8226细胞皮下接种于3至4周龄的雌性小鼠。当肿瘤体积接近100 mm³时，将小鼠分为每组6只的实验组。连续3天，每天腹腔注射氟达拉滨或PBS（对照）。肿瘤体积采用以下公式计算：4π/3 × (肿瘤宽度/2)² × (肿瘤长度/2)，如前所述。[3]
将Raji NHL细胞（2×10^6个细胞/只）皮下注射到6-8周龄的裸鼠体内，建立异种移植瘤模型。当肿瘤体积达到100 mm³时，将小鼠随机分为载体组和氟达拉滨（NSC 118218）组（每组n=6）。氟达拉滨（NSC 118218）溶于生理盐水，每周一次静脉注射，剂量为20 mg/kg，持续3周。每隔2天测量一次肿瘤体积，并对小鼠实施安乐死以称量肿瘤重量[4]
转基因B-CLL小鼠（8-10周龄）接受溶于生理盐水的氟达拉滨（NSC 118218）治疗，剂量为15 mg/kg，每日一次，连续5天。在治疗前后采集外周血，通过流式细胞术计数B-CLL细胞[1]
雄性Wistar大鼠（200-250 g）接受腹主动脉缩窄术（AAC）以诱导心肌肥大。AAC术后两周，大鼠接受氟达拉滨（NSC 118218）（10 mg/kg，静脉注射，隔日一次，连续7天）或载体治疗。采用超声心动图评估心脏功能，并对大鼠实施安乐死，以收集心脏组织进行分子分析[5]
药代性质 (ADME/PK)
吸收、分布和排泄
口服给药后的生物利用度为55%。
117-145 mL/min [接受单次40 mg/m^2静脉注射的B细胞慢性淋巴细胞白血病患者]。
……比较狼疮性肾炎患者皮下注射和静脉注射氟达拉滨的药代动力学。……一项开放标签、随机、交叉试验，与一项I/II期试验同时进行。……政府研究医院。……5例狼疮性肾炎患者。……氟达拉滨30 mg/m^2/天，皮下注射或0.5小时静脉输注，连续3天。所有患者在每个周期的第一天均口服环磷酰胺0.5 g/m^2。分别于首次给药前及给药后0.5、1、1.5、2、4、8和24小时采集血浆样本。每隔6小时采集一次尿液样本，持续24小时。采用高效液相色谱法分析血浆和尿液中氟达拉滨的主要代谢产物氟阿拉伯呋喃糖腺嘌呤（F-ara-A）的含量。采用房室模型分析F-ara-A的药代动力学，结果表明线性二室模型最能描述其药代动力学特征。采用Wilcoxon符号秩检验比较皮下注射和静脉注射两种给药途径的药代动力学差异。皮下注射和静脉注射给药的中位（四分位间距）最大浓度分别为 0.51 (0.38-0.56) mg/L 和 0.75 (0.52-0.91) mg/L，两种给药方式的浓度-时间曲线下面积（0-24 小时）分别为 4.65 (4.17-4.98) mg·hr/L 和 4.55 (3.5-4.94) mg·hr/L，两者之间无显著差异。皮下注射后氟达拉滨的生物利用度约为静脉注射后的 105%。皮下注射和静脉注射给药的肾清除率和尿液排泄百分比差异均无统计学意义。皮下注射未观察到注射部位反应。……在狼疮性肾炎患者中，氟达拉滨的皮下注射和静脉注射似乎具有相似的药代动力学特征。皮下注射可能是一种比静脉注射更便捷的给药方式。
生物半衰期
20 小时
氟达拉滨 (NSC 118218) 在大鼠静脉注射（20 mg/kg）后，其终末半衰期 (t1/2) 为 10.5 小时 [2]
氟达拉滨 (NSC 118218) 在大鼠体内的分布容积 (Vd) 为 1.2 L/kg，总清除率 (CL) 为 80 mL/min/kg [2]
氟达拉滨 (NSC 118218) 在外周血单核细胞中迅速转化为其活性代谢物氟达拉滨三磷酸 (F-ara-ATP)，给药后 4 小时达到细胞内浓度峰值 [1]
毒性/毒理 (Toxicokinetics/TK)
肝毒性
在临床试验中，仅有少数接受氟达拉滨治疗白血病的患者出现血清酶升高。这些研究并未明确氟达拉滨与其他抗肿瘤药物在抗白血病治疗方案中的作用。已有氟达拉滨引起临床上明显的肝损伤的病例报道，但相关细节较少，且大多数患者同时接受了其他抗癌化疗药物。
氟达拉滨具有免疫抑制作用，可降低白细胞总数，特别是淋巴细胞和CD8 T细胞计数。因此，氟达拉滨治疗与慢性乙型肝炎的复发病例相关，包括一些患者在化疗前已治愈乙型肝炎，但化疗后出现乙肝表面抗原（HBsAg）阳性，并伴有活动性疾病，表现为乙肝核心抗体（anti-HBc）阳性而乙肝表面抗原（HBsAg）阴性。乙肝病毒通常在接受3至6个疗程的抗癌药物治疗后复发，最常见于化疗结束后2至4个月。由于氟达拉滨治疗后乙肝病毒复发的频率和严重程度，建议患者在治疗前进行乙肝表面抗原（HBsAg）和乙肝核心抗体（抗-HBc）筛查，并使用对乙肝病毒具有强效活性的口服核苷类抗病毒药物（如拉米夫定、替诺福韦或恩替卡韦）进行预防性抗病毒治疗。如果未进行预防性治疗，则需要密切监测并尽早开始抗病毒治疗。氟达拉滨还与机会性感染的发生有关，包括肝脏疱疹病毒和腺病毒感染。
可能性评分：E（未经证实但怀疑是临床上明显的肝损伤的原因）。
蛋白结合
19-29%
相互作用
氟达拉滨可能作为肿瘤溶解综合征的一部分升高血尿酸浓度；可能需要调整抗痛风药物（别嘌醇、秋水仙碱、丙磺舒、磺吡酮）的剂量以控制高尿酸血症和痛风；由于使用促尿酸排泄抗痛风药物存在尿酸性肾病风险，因此别嘌醇可能是预防或逆转氟达拉滨引起的高尿酸血症的首选药物。
如果同时或近期接受其他药物治疗（这些药物/引起血液疾病的药物/也会产生相同的作用），氟达拉滨的白细胞减少症和/或血小板减少症作用可能会增强；如有必要，应根据血细胞计数调整氟达拉滨的剂量。
可能会出现骨髓抑制叠加；当同时或先后使用两种或两种以上骨髓抑制剂（包括放射线）时，可能需要减少剂量。
由于可能增加致命性肺毒性的风险，不建议与氟达拉滨同时使用。 /喷司他丁/
有关氟达拉滨（共10项）的更多相互作用（完整）数据，请访问HSDB记录页面。
氟达拉滨（NSC 118218）在体外可诱导B细胞慢性淋巴细胞白血病（B-CLL）患者细胞的骨髓抑制：1 μM浓度下中性粒细胞计数降低40% [1]
氟达拉滨（NSC 118218）在人血浆中的血浆蛋白结合率为23% [2]
在接受氟达拉滨（NSC 118218）（20 mg/kg，静脉注射）治疗的大鼠中，血清ALT和AST水平升高15%（在正常范围内），未观察到明显的肾毒性（BUN、Cr未发生变化）[5]
氟达拉滨（NSC 118218） 118218)（体外浓度高达 10 μM）未诱导心肌细胞坏死，如正常的 LDH 释放所示[5]
参考文献

[1]. Eur J Haematol . 2007 Dec;79(6):486-93.

[2]. Bioorg Med Chem . 1999 Jun;7(6):1195-200.

[3]. Int Immunopharmacol . 2006 May;6(5):715-23.

[4]. Eur J Cancer . 1996 Sep;32A(10):1766-73.

[5]. Am J Physiol Heart Circ Physiol . 2007 Jun;292(6):H2935-43.
其他信息
治疗用途
氟达拉滨适用于治疗对至少一种含烷化剂的标准方案治疗无效或病情进展的B细胞慢性淋巴细胞白血病（CLL）患者。/已包含在美国产品标签中/
氟达拉滨适用于治疗非霍奇金淋巴瘤。/未包含在美国产品标签中/
磷酸氟达拉滨是一种嘌呤类似物，目前常用于治疗低级别淋巴系统恶性肿瘤。
一项研究更新旨在评估既往接受过治疗的慢性淋巴细胞白血病（CLL）患者在接受氟达拉滨挽救治疗后的长期生存情况。……从1992年9月至1995年12月，共有74例晚期复发性B细胞CLL患者入组该研究。氟达拉滨以25 mg/m²/天的剂量，连续给药5天，每次静脉输注30分钟。治疗每28天重复一次，最多6个疗程。……19例（26%）患者达到完全缓解（CR），20例（27%）患者达到部分缓解（PR），总缓解率为53%。中位总生存期为68个月，且与既往治疗次数呈显著负相关。达到CR的患者中位无进展生存期为18个月，达到PR的患者中位无进展生存期为12个月。……在本组慢性淋巴细胞白血病（CLL）患者中，单用氟达拉滨治疗的结果表明存在显著的无病生存期。这段时间窗口可用于巩固初始治疗反应，可采用生物学方法或高剂量治疗策略，例如自体骨髓移植，最终目标是根除疾病。
药物警告
注射用氟达拉非应在具有抗肿瘤治疗经验的合格医师的指导下使用。注射用氟达拉非可严重抑制骨髓功能。在急性白血病患者的剂量范围研究中，当使用高剂量时，注射用氟达拉非与严重的神经系统不良反应相关，包括失明、昏迷和死亡。这种严重的神经系统毒性发生在接受剂量约为推荐剂量四倍（96 mg/m²/天，持续5-7天）治疗的患者中，发生率为36%。据报道，接受慢性淋巴细胞白血病推荐剂量范围内治疗的患者会出现类似的严重中枢神经系统毒性，包括昏迷、癫痫发作、躁动和意识混乱。
据报道，在接受氟达拉非注射液治疗一个或多个疗程后，可能会出现危及生命甚至致命的自身免疫现象，例如溶血性贫血、自身免疫性血小板减少症/血小板减少性紫癜 (ITP)、埃文斯综合征和获得性血友病。接受氟达拉非注射液治疗的患者应接受溶血评估并密切监测。
在一项使用氟达拉非注射液联合喷司他丁（脱氧辅酶素）治疗难治性慢性淋巴细胞白血病 (CLL) 的临床研究中，致命性肺毒性的发生率高得令人无法接受。因此，不建议将注射用氟达拉滨与喷司他丁联合使用。
氟达拉滨的骨髓抑制作用可能导致微生物感染发生率增加、伤口愈合延迟和牙龈出血。牙科治疗应尽可能在开始治疗前完成，或推迟至血细胞计数恢复正常后进行。应指导患者在治疗期间保持良好的口腔卫生，包括谨慎使用普通牙刷、牙线和牙签。氟达拉滨有时还会引起口腔炎，并伴有明显的不适。
有关氟达拉滨（共26条）的更多药物警告（完整）数据，请访问HSDB记录页面。
药效学
氟达拉滨是一种用于治疗慢性淋巴细胞白血病的化疗药物。它作用于DNA聚合酶α、核糖核苷酸还原酶和DNA引物酶，导致DNA合成抑制，从而破坏癌细胞。
氟达拉滨（NSC 118218）是一种嘌呤核苷类似物（2-氟-9-β-D-阿拉伯呋喃糖基腺嘌呤），具有抗肿瘤和免疫抑制特性[2,4]。
氟达拉滨（NSC 118218）通过抑制DNA合成发挥抗肿瘤作用：其活性代谢物F-ara-ATP与脱氧腺苷三磷酸（dATP）竞争掺入DNA，导致链终止[2,4]。
氟达拉滨（NSC 118218）通过线粒体固有途径诱导恶性淋巴细胞凋亡（上调Bax，下调……）。 Bcl-2) [1]
氟达拉滨 (NSC 118218)通过抑制NF-κB介导的炎症信号通路减轻心肌肥大[5]
氟达拉滨 (NSC 118218)临床上用于治疗B细胞慢性淋巴细胞白血病和非霍奇金淋巴瘤[1,4]
*注: 文献方法仅供参考, InvivoChem并未独立验证这些方法的准确性
化学信息 & 存储运输条件
分子式
C10H12FN5O4
分子量
285.23
精确质量
285.087
元素分析
C, 42.11; H, 4.24; F, 6.66; N, 24.55; O, 22.44
CAS号
21679-14-1
相关CAS号
21679-14-1(Fludarabine free); 75607-67-9 (phosphate); 107811-61-0 (diphosphate); 1169548-80-4 (F18)
PubChem CID
657237
外观&性状
White to yellow solid powder
密度
2.2±0.1 g/cm3
沸点
747.3±70.0 °C at 760 mmHg
熔点
265-268ºC
闪点
405.8±35.7 °C
蒸汽压
0.0±2.6 mmHg at 25°C
折射率
1.876
LogP
-0.4
tPSA
139.54
氢键供体(HBD)数目
4
氢键受体(HBA)数目
9
可旋转键数目(RBC)
2
重原子数目
20
分子复杂度/Complexity
367
定义原子立体中心数目
4
SMILES
FC1=NC(=C2C(=N1)N(C([H])=N2)[C@@]1([H])[C@]([H])([C@@]([H])([C@@]([H])(C([H])([H])O[H])O1)O[H])O[H])N([H])[H]
InChi Key
HBUBKKRHXORPQB-FJFJXFQQSA-N
InChi Code
InChI=1S/C10H12FN5O4/c11-10-14-7(12)4-8(15-10)16(2-13-4)9-6(19)5(18)3(1-17)20-9/h2-3,5-6,9,17-19H,1H2,(H2,12,14,15)/t3-,5-,6+,9-/m1/s1
化学名
(2R,3S,4S,5R)-2-(6-amino-2-fluoropurin-9-yl)-5-(hydroxymethyl)oxolane-3,4-diol
别名
FaraA; Fludarabinum; HSDB 6964; F-ara-A; HSDB6964; NSC118218; HSDB-6964; NSC 118218; F-ara A; 21679-14-1; F-Ara-A; 2-Fluoro Ara-A; (2R,3S,4S,5R)-2-(6-Amino-2-fluoro-9H-purin-9-yl)-5-(hydroxymethyl)tetrahydrofuran-3,4-diol; 9-beta-D-Arabinofuranosyl-2-fluoroadenine; Fludarabine [INN]; Fludarabina;NSC-118218
HS Tariff Code
2934.99.9001
存储方式

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month
运输条件
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
溶解度数据
溶解度 (体外实验)
DMSO: 25~57 mg/mL (87.7~199.8 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
溶解度 (体内实验)
配方 1 中的溶解度: ≥ 2.5 mg/mL (8.76 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。
配方 2 中的溶解度: ≥ 2.5 mg/mL (8.76 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。
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配方 3 中的溶解度: ≥ 2.5 mg/mL (8.76 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL 澄清 DMSO 储备液添加到 900 μL 玉米油中并混合均匀。

配方 4 中的溶解度: 30% propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL

请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。
制备储备液 1 mg 5 mg 10 mg
1 mM 3.5059 mL 17.5297 mL 35.0594 mL
5 mM 0.7012 mL 3.5059 mL 7.0119 mL
10 mM 0.3506 mL 1.7530 mL 3.5059 mL

1、根据实验需要选择合适的溶剂配制储备液 (母液)：对于大多数产品，InvivoChem推荐用DMSO配置母液 (比如：5、10、20mM或者10、20、50 mg/mL浓度），个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;

2、如果您找不到您想要的溶解度信息，或者很难将产品溶解在溶液中，请联系我们;

3、建议使用下列计算器进行相关计算（摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等）;

4、母液配好之后，将其分装到常规用量，并储存在-20°C或-80°C，尽量减少反复冻融循环。

计算器
计算 重置

摩尔浓度计算器可计算特定溶液所需的质量、体积/浓度，具体如下：

  • 计算制备已知体积和浓度的溶液所需的化合物的质量
  • 计算将已知质量的化合物溶解到所需浓度所需的溶液体积
  • 计算特定体积中已知质量的化合物产生的溶液的浓度
使用摩尔浓度计算器计算摩尔浓度的示例如下所示：
假如化合物的分子量为350.26 g/mol，在5mL DMSO中制备10mM储备液所需的化合物的质量是多少？
  • 在分子量（MW）框中输入350.26
  • 在“浓度”框中输入10，然后选择正确的单位（mM）
  • 在“体积”框中输入5，然后选择正确的单位（mL）
  • 单击“计算”按钮
  • 答案17.513 mg出现在“质量”框中。以类似的方式，您可以计算体积和浓度。
计算 重置

稀释计算器可计算如何稀释已知浓度的储备液。例如，可以输入C1、C2和V2来计算V1，具体如下：

制备25毫升25μM溶液需要多少体积的10 mM储备溶液？
使用方程式C1V1=C2V2，其中C1=10mM，C2=25μM，V2=25 ml，V1未知：
  • 在C1框中输入10，然后选择正确的单位（mM）
  • 在C2框中输入25，然后选择正确的单位（μM）
  • 在V2框中输入25，然后选择正确的单位（mL）
  • 单击“计算”按钮
  • 答案62.5μL（0.1 ml）出现在V1框中
g/mol
计算 重置

分子量计算器可计算化合物的分子量 (摩尔质量)和元素组成，具体如下：

注：化学分子式大小写敏感：C12H18N3O4  c12h18n3o4
计算化合物摩尔质量（分子量）的说明：
  • 要计算化合物的分子量 (摩尔质量)，请输入化学/分子式，然后单击“计算”按钮。
分子质量、分子量、摩尔质量和摩尔量的定义：
  • 分子质量（或分子量）是一种物质的一个分子的质量，用统一的原子质量单位（u）表示。（1u等于碳-12中一个原子质量的1/12）
  • 摩尔质量（摩尔重量）是一摩尔物质的质量，以g/mol表示。
/
计算 重置

配液计算器可计算将特定质量的产品配成特定浓度所需的溶剂体积 (配液体积)

  • 输入试剂的质量、所需的配液浓度以及正确的单位
  • 单击“计算”按钮
  • 答案显示在体积框中
动物体内实验配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
第二步：请输入动物体内配方组成（配方适用于不溶/难溶于水的化合物），不同的产品和批次配方组成不同，如对配方有疑问，可先联系我们提供正确的体内实验配方。此外，请注意这只是一个配方计算器，而不是特定产品的确切配方。
+
+
+
计算 重置

计算结果:

工作液浓度： mg/mL；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度，请首先与我们联系。

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH2O，混匀澄清。

(1) 请确保溶液澄清之后，再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶；
            (2) 一定要按顺序加入溶剂 (助溶剂) 。

临床试验信息
Immunotherapy Using Tumor Infiltrating Lymphocytes for Patients With Metastatic Cancer
CTID: NCT01174121
Phase: Phase 2    Status: Recruiting
Date: 2024-12-02
TCR Reserved and Power3 Gene Knock-out Allogeneic CD19-targeting CAR-T Cell Therapy in r/r B Cell Lymphoma
CTID: NCT06323525
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2024-12-02
TCR Reserved and Power3 Gene Knock-out Allogeneic CD19-targeting CAR-T Cell Therapy in r/r B-ALL
CTID: NCT06481735
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2024-12-02
Total Body Irradiation and Astatine-211-Labeled BC8-B10 Monoclonal Antibody for the Treatment of Nonmalignant Diseases
CTID: NCT04083183
Phase: Phase 1/Phase 2    Status: Suspended
Date: 2024-12-02
A Study of Nemtabrutinib vs Chemoimmunotherapy for Participants With Previously Untreated Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma (CLL/SLL) Without TP53 Aberrations (MK-1026-008, BELLWAVE-008)
CTID: NCT05624554
Phase: Phase 3    Status: Recruiting
Date: 2024-12-02
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Cord Blood Transplant in Children and Young Adults With Blood Cancers and Non-malignant Disorders
CTID: NCT04644016
Phase: Phase 2    Status: Recruiting
Date: 2024-12-02

LN-145 or LN-145-S1 in Treating Patients With Relapsed or Refractory Ovarian Cancer, Triple Negative Breast Cancer (TNBC), Anaplastic Thyroid Cancer, Osteosarcoma, or Other Bone and Soft Tissue Sarcomas
CTID: NCT03449108
Phase: Phase 2    Status: Active, not recruiting
Date: 2024-11-29
TBio-4101 and Pembro wi/ or w/o Chemo in Recurrent/Metastatic HNSCC
CTID: NCT06236425
Phase: Phase 1    Status: Recruiting
Date: 2024-11-29
Allogenic CD19-targeting CAR-γδT Cell Therapy in r/r NHL
CTID: NCT05554939
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2024-11-29
A Study of CC-97540, CD-19-Targeted Nex-T CAR T Cells, in Participants With Severe, Refractory Autoimmune Diseases
CTID: NCT05869955
Phase: Phase 1    Status: Recruiting
Date: 2024-11-29
Consolidation of First-Line MRD+ Remission With Cema-cel in Patients With LBCL
CTID: NCT06500273
Phase: Phase 2    Status: Recruiting
Date: 2024-11-29
Most Closely Matched 3rd Party Rapidly Generated LMP, BARF1 And EBNA1 Specific CTL, EBV-Positive Lymphoma (MABEL)
CTID: NCT02287311
Phase: Phase 1    Status: Active, not recruiting
Date: 2024-11-27
US Zamto-cel Autoimmune Diseases
CTID: NCT06708845
Phase: Phase 1    Status: Not yet recruiting
Date: 2024-11-27
HLA-Mismatched Unrelated Donor Peripheral Blood Stem Cell Transplantation with Reduced Dose Post Transplantation Cyclophosphamide GvHD Prophylaxis
CTID: NCT06001385
Phase: Phase 2    Status: Recruiting
Date: 2024-11-27
Proof of Concept of TBio-4101, Lymphodepleting Chemo, IL-2 for Relapsed/Refractory Melanoma
CTID: NCT05628883
Phase: Phase 1    Status: Recruiting
Date: 2024-11-27
A Phase II Study of Adjuvant Immunotherapy Targeting KRAS G12D, KRAS G12V, or TP53 R175H for Participants With Advanced Gastrointestinal Malignancies
CTID: NCT06690281
Phase: Phase 2    Status: Not yet recruiting
Date: 2024-11-26
T Cells Expressing a Novel Fully-Human Anti-BCMA CAR for Treating Multiple Myeloma
CTID: NCT03602612
Phase: Phase 1    Status: Active, not recruiting
Date: 2024-11-26
Master Protocol to Assess Safety and Dose of First Time in Human Next Generation Engineered T Cells in NY-ESO-1 and/or LAGE-1a Positive Advanced Solid Tumors
CTID: NCT04526509
Phase: Phase 1    Status: Terminated
Date: 2024-11-26
Trial of Anti-CD19 and Anti-CD20 Bicistronic Chimeric Antigen Receptor T Cells for Treating B-Cell Malignancies
CTID: NCT05797233
Phase: Phase 1    Status: Active, not recruiting
Date: 2024-11-26
Venetoclax to Augment Epigenetic Modification and Chemotherapy
CTID: NCT05317403
Phase: Phase 1    Status: Recruiting
Date: 2024-11-26
A Phase 1/2 Study of KSQ-004EX, Autologous Tumor Infiltrating Lymphocytes Engineered to Inactivate Genes Encoding SOCS1 and Regnase-1, in Patients With Select Advanced Solid Tumors
CTID: NCT06598371
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2024-11-26
A Study of Gilteritinib (ASP2215) Combined With Chemotherapy in Children, Adolescents and Young Adults With FMS-like Tyrosine Kinase 3 (FLT3)/Internal Tandem Duplication (ITD) Positive Relapsed or Refractory Acute Myeloid Leukemia (AML)
CTID: NCT04240002
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2024-11-25
Fludarabine, Cytarabine, and Pegcrisantaspase for the Treament of Relapsed or Refractory Leukemia
CTID: NCT04526795
Phase: Phase 1    Status: Active, not recruiting
Date: 2024-11-25
GPC3 Targeted CAR-T Cell Therapy in Advanced GPC3 Expressing Hepatocellular Carcinoma (HCC)
CTID: NCT05003895
Phase: Phase 1    Status: Recruiting
Date: 2024-11-25
Autologous T-cells Genetically Engineered to Express Receptors Reactive Against KRAS Mutations in Conjunction With a Vaccine Directed Against These Antigens in Participants With Metastatic Cancer
CTID: NCT06253520
Phase: Phase 1    Status: Recruiting
Date: 2024-11-25
Prospective Randomized Study of Cell Transfer Therapy for Metastatic Melanoma Using Tumor Infiltrating Lymphocytes Plus IL-2 Following Non-Myeloablative Lymphocyte Depleting Chemo Regimen Alone or in Conjunction With 12Gy Total Body Irradiation (TBI...
CTID: NCT01319565
Phase: Phase 2    Status: Active, not recruiting
Date: 2024-11-25
CD34+ Enriched Transplants to Treat Myelodysplastic Syndrome
CTID: NCT05617625
Phase: Phase 2    Status: Suspended
Date: 2024-11-25
Administering Peripheral Blood Lymphocytes Transduced With a CD70-Binding Chimeric Antigen Receptor to People With CD70 Expressing Cancers
CTID: NCT02830724
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2024-11-25
Administering Peripheral Blood Lymphocytes Transduced With a Murine T-Cell Receptor Recognizing the G12V Variant of Mutated RAS in HLA-A*11:01 Patients
CTID: NCT03190941
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2024-11-25
The Lowest Effective Dose of Post-Transplantation Cyclophosphamide in Combination With Sirolimus and Mycophenolate Mofetil as Graft-Versus-Host Disease Prophylaxis After Reduced Intensity Conditioning and Peripheral Blood Stem Cell Transplantation
CTID: NCT05436418
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2024-11-25
Pilot Study of Reduced-Intensity Hematopoietic Stem Cell Transplant of DOCK8 Deficiency
CTID: NCT01176006
Phase: Phase 2    Status: Recruiting
Date: 2024-11-25
Phase I/II Study to Reduce Post-transplantation Cyclophosphamide Dosing for Older or Unfit Patients Undergoing Bone Marrow Transplantation for Hematologic Malignancies
CTID: NCT04959175
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2024-11-25
CD19/CD22 Bicistronic Chimeric Antigen Receptor (CAR) T Cells in Children and Young Adults With Recurrent or Refractory CD19/CD22-expressing B Cell Malignancies
CTID: NCT05442515
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2024-11-25
T Cell Receptor Gene Therapy Targeting KK-LC-1 for Gastric, Breast, Cervical, Lung and Other KK-LC-1 Positive Epithelial Cancers
CTID: NCT05035407
Phase: Phase 1    Status: Recruiting
Date: 2024-11-25
Phase 1 to Investigate the Safety, Tolerability, and Efficacy of GCC2005 in Patients With R/R NK and T-cell Malignancies
CTID: NCT06699771
Phase: Phase 1    Status: Not yet recruiting
Date: 2024-11-25
CD34+ Transplants for Leukemia and Lymphoma
CTID: NCT05565105
Phase: Phase 2    Status: Not yet recruiting
Date: 2024-11-25
A Study Comparing Anitocabtagene Autoleucel to Standard of Care Therapy in Participants With Relapsed/ Refractory Multiple Myeloma
CTID: NCT06413498
Phase: Phase 3    Status: Recruiting
Date: 2024-11-25
A Phase II Study of Allogeneic Hematopoietic Stem Cell Transplant for Subjects With VEXAS (Vacuoles, E1 Enzyme, X-linked, Autoinflammatory, Somatic) Syndrome
CTID: NCT05027945
Phase: Phase 2    Status: Recruiting
Date: 2024-11-25
A Prospective Randomized and Phase 2 Trial for Metastatic Melanoma Using Adoptive Cell Therapy With Tumor Infiltrating Lymphocytes Plus IL-2 Either Alone or Following the Administration of Pembrolizumab
CTID: NCT02621021
Phase: Phase 2    Status: Suspended
Date: 2024-11-25
Anti-CD19 Chimeric Antigen Receptor T-Cell Immunotherapy for Chronic Lymphocytic Leukemia (CLL)
CTID: NCT06364423
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2024-11-25
Donor Lymphocyte Infusion After Allogeneic Hematopoietic Cell Transplantation for High-Risk Hematologic Malignancies
CTID: NCT05327023
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2024-11-25
Optimizing PTCy Dose and Timing
CTID: NCT03983850
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2024-11-25
E7 TCR T Cells for Human Papillomavirus-Associated Cancers
CTID: NCT02858310
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2024-11-25
Allogeneic Hematopoietic Stem Cell Transplantation With JSP191-Based Conditioning in Participants With GATA2 Deficiency
CTID: NCT05907746
Phase: Phase 2    Status: Recruiting
Date: 2024-11-25
Administering Peripheral Blood Lymphocytes Transduced With a Murine T-Cell Receptor Recognizing the G12D Variant of Mutated RAS in HLA-A*11:01 Patients
CTID: NCT03745326
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2024-11-25
T Cell Receptor Immunotherapy for Patients With Metastatic Non-Small Cell Lung Cancer
CTID: NCT02133196
Phase: Phase 2    Status: Recruiting
Date: 2024-11-25
Allogeneic Hematopoietic Stem Cell Transplant for GATA2 Mutations
CTID: NCT01861106
Phase: Phase 2    Status: Recruiting
Date: 2024-11-25
Early Human Leukocyte Antigen (HLA) Matched Sibling Hematopoietic Stem Cell Transplantation
CTID: NCT04018937
Phase: Phase 2    Status: Active, not recruiting
Date: 2024-11-25
CD19/CD22 Chimeric Antigen Receptor (CAR) T Cells in Children and Young Adults With Recurrent or Refractory CD19/CD22-expressing B Cell Malignancies
CTID: NCT03448393
Phase: Phase 1    Status: Recruiting
Date: 2024-11-25
Administration of Autologous T-Cells Genetically Engineered to Express T-Cell Receptors Reactive Against Neoantigens in People With Metastatic Cancer
CTID: NCT03412877
Phase: Phase 2    Status: Recruiting
Date: 2024-11-25
Allogeneic Hematopoietic Stem Cell Transplant for Patients With Inborn Errors of Immunity
CTID: NCT04339777
Phase: Phase 2    Status: Recruiting
Date: 2024-11-25
A Phase 1/2 Trial of ADI-270 in CcRCC
CTID: NCT06480565
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2024-11-22
Study of Axicabtagene Ciloleucel Versus Standard of Care Therapy in Participants With Relapsed/Refractory Follicular Lymphoma
CTID: NCT05371093
Phase: Phase 3    Status: Recruiting
Date: 2024-11-22
TIL Therapy for Metastatic Renal Cell Carcinoma
CTID: NCT02926053
Phase: Phase 1    Status: Completed
Date: 2024-11-22
Reduced Intensity BMT for Immune Dysregulatory and Bone Marrow Failure Syndromes Using Post-Transplant Cyclophosphamide
CTID: NCT04232085
Phase: Phase 2    Status: Recruiting
Date: 2024-11-22
UF-KURE-BCMA CAR-T Cells in Patients with Relapsed or Refractory Multiple Myeloma
CTID: NCT06698744
Phase: Phase 1    Status: Not yet recruiting
Date: 2024-11-21
225Ac-DOTA-Anti-CD38 Daratumumab Monoclonal Antibody With Fludarabine, Melphalan and Total Marrow and Lymphoid Irradiation as Conditioning Treatment for Donor Stem Cell Transplant in Patients With High-Risk Acute Myeloid Leukemia, Acute Lymphoblastic Leukemia and Myelodysplastic Syndrome
CTID: NCT06287944
Phase: Phase 1    Status: Recruiting
Date: 2024-11-21
Safety Study of Rituximab (SC) Administered in Participants With CD20+ DLBCL or CD20+ Follicular NHL Grade 1 to 3A
CTID: NCT02406092
Phase: Phase 3    Status: Completed
Date: 2024-11-21
A Study to Compare the Efficacy and Safety of BMS-986393 Versus Standard Regimens in Adult Participants With Relapsed or Refractory and Lenalidomide-refractory Multiple Myeloma (QUINTESSENTIAL-2)
CTID: NCT06615479
Phase: Phase 3    Status: Not yet recruiting
Date: 2024-11-21
CRISPR-Edited Allogeneic Anti-CD19 CAR-T Cell Therapy for Relapsed/Refractory B Cell Non-Hodgkin Lymphoma (ANTLER)
CTID: NCT04637763
Phase: Phase 1    Status: Recruiting
Date: 2024-11-21
Study of KITE-197 in Participants With Relapsed or Refractory Large B-cell Lymphoma
CTID: NCT06079164
Phase: Phase 1    Status: Recruiting
Date: 2024-11-20
Allogeneic CD19-targeted CAR-γδT Cell Infusion Therapy in Relapsed/Refractory B Cell Acute Lymphoblastic Leukemia
CTID: NCT06696833
PhaseEarly Phase 1    Status: Recruiting
Date: 2024-11-20
Infusion of Expanded Cord Blood Cells in Addition to Single Cord Blood Transplant in Treating Patients With Acute Leukemia, Chronic Myeloid Leukemia, or Myelodysplastic Syndromes
CTID: NCT03399773
Phase: Phase 2    Status: Recruiting
Date: 2024-11-19
A Study Evaluating the Safety and Efficacy of Brexucabtagene Autoleucel (KTE-X19) in Adult Subjects With Relapsed/Refractory B-precursor Acute Lymphoblastic Leukemia (ZUMA-3)
CTID: NCT02614066
Phase: Phase 1/Phase 2    Status: Completed
Date: 2024-11-19
HA-1 T TCR T Cell Immunotherapy for the Treatment of Patients With Relapsed or Refractory Acute Leukemia After Donor Stem Cell Transplant
CTID: NCT03326921
Phase: Phase 1    Status: Suspended
Date: 2024-11-15
Efficacy & Safety for LN144 with Pembrolizumab with High Risk Stage IIIb-dResectable Melanoma
CTID: NCT06190249
Phase: Phase 1    Status: Suspended
Date: 2024-11-15
Autologous CAR-T Cells Targeting CSPG4 in Relapsed/Refractory HNSCC
CTID: NCT06096038
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2024-11-14
A Study to Evaluate the Safety, Tolerability, Efficacy, and Drug Levels of CC-97540 in Participants With Relapsing Forms of Multiple Sclerosis or Progressive Forms of Multiple Sclerosis
CTID: NCT06220201
Phase: Phase 1    Status: Recruiting
Date: 2024-11-14
Bendamustine With or Without Cyclophosphamide in Preventing GVHD in Patients Undergoing Stem Cell Transplant
CTID: NCT04022239
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2024-11-14
A Study of Daratumumab, Bortezomib, Lenalidomide and Dexamethasone (DVRd) Followed by Ciltacabtagene Autoleucel Versus Daratumumab, Bortezomib, Lenalidomide and Dexamethasone (DVRd) Followed by Autologous Stem Cell Transplant (ASCT) in Participants With Newly Diagnosed Multiple Myeloma
CTID: NCT05257083
Phase: Phase 3    Status: Recruiting
Date: 2024-11-14
A Study to Assess BMS-986453 in Participants With Relapsed and/or Refractory Multiple Myeloma
CTID: NCT06153251
Phase: Phase 1    Status: Recruiting
Date: 2024-11-14
CAR-T Cell Therapy for Desensitization in Kidney Transplantation
CTID: NCT06056102
Phase: Phase 1    Status: Recruiting
Date: 2024-11-14
Naive T Cell Depletion for Preventing Chronic Graft-versus-Host Disease in Children and Young Adults With Blood Cancers Undergoing Donor Stem Cell Transplant
CTID: NCT03779854
Phase: Phase 2    Status: Recruiting
Date: 2024-11-14
Study of GSK3901961 In Previously Treated Advanced (Metastatic OR Unresectable) Synovial Sarcoma/ Myxoid/Round Cell Liposarcoma, and Previously Treated Metastatic Non-Small Cell Lung Cancer
CTID: NCT06048705
Phase: Phase 1    Status: Terminated
Date: 2024-11-13
Study of GSK3845097 in Previously Treated Participants With Advanced Synovial Sarcoma and Myxoid/Round Cell Liposarcoma
CTID: NCT05943990
Phase: Phase 1    Status: Terminated
Date: 2024-11-13
Phase 2 Study of AFM13 in Combination with AB-101 in Subjects with R/R HL and CD30+ PTCL
CTID: NCT05883449
Phase: Phase 2    Status: Recruiting
Date: 2024-11-13
Optimizing Lymphodepletion to Improve Outcomes in Patients Receiving Cell Therapy With Kymriah
CTID: NCT06003179
Phase: Phase 1    Status: Withdrawn
Date: 2024-11-12
Study of HLA-Haploidentical Stem Cell Transplantation to Treat Clinically Aggressive Sickle Cell Disease
CTID: NCT03121001
Phase: Phase 2    Status: Recruiting
Date: 2024-11-12
Venetoclax With Combination Chemotherapy in Treating Patients With Newly Diagnosed or Relapsed or Refractory Acute Myeloid Leukemia
CTID: NCT03214562
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2024-11-12
Haploidentical Stem Cell Transplant with Prophylactic Natural Killer DLI for Lymphoma, Multiple Myeloma, and CLL
CTID: NCT03524235
Phase: Phase 1    Status: Completed
Date: 2024-11-12
TIL Therapy Combined With Pembrolizumab for Advanced or Metastatic Refractory Stomach and Esophageal Cancer
CTID: NCT06532799
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2024-11-12
TIL Gean Therapy Combined With Immunotherapy for Advanced or Metastatic Refractory Breast Cancer
CTID: NCT06532812
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2024-11-12
A Phase I/II Study of Trametinib and Azacitidine for Patients With Newly Diagnosed Juvenile Myelomonocytic Leukemia
CTID: NCT05849662
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2024-11-12
Study of KITE-363 or KITE-753 in Participants With Relapsed and/or Refractory B-cell Lymphoma
CTID: NCT04989803
Phase: Phase 1    Status: Recruiting
Date: 2024-11-08
Immune Cell Therapy (CAR-T) for the Treatment of Patients With HIV and B-Cell Non-Hodgkin Lymphoma
CTID: NCT05077527
Phase: Phase 1    Status: Recruiting
Date: 2024-11-08
ABBA CORD: dCBT w/ Abatacept for aGVHD Prophylaxis
CTID: NCT06680661
Phase: Phase 2    Status: Not yet recruiting
Date: 2024-11-08
A Trial Comparing Unrelated Donor BMT with IST for Pediatric and Young Adult Patients with Severe Aplastic Anemia (TransIT, BMT CTN 2202)
CTID: NCT05600426
Phase: Phase 3    Status: Recruiting
Date: 2024-11-08
Clinical Study of ARD103 CAR-T Therapy for Patients with R/R AML or MDS
CTID: NCT06680752
Phase: Phase 1/Phase 2    Status: Not yet recruiting
Date: 2024-11-08
IDP-023 g-NK Cells Plus Ocrelizumab in Patients With Progressive Multiple Sclerosis
CTID: NCT06677710
Phase: Phase 1    Status: Not yet recruiting
Date: 2024-11-07
Safety and Efficacy of Quizartinib in Children and Young Adults With Acute Myeloid Leukemia (AML), a Cancer of the Blood
CTID: NCT03793478
Phase: Phase 1/Phase 2    Status: Active, not recruiting
Date: 2024-11-07
Autologous CD8+ and CD4+ Transgenic T Cells Expressing High Affinity KRASG12V Mutation-Specific T Cell Receptors (FH-A11KRASG12V-TCR) in Treating Patients With Metastatic Pancreatic, Colorectal and Non-Small Cell Lung Cancers With KRAS G12V Mutations
CTID: NCT06043713
Phase: Phase 1    Status: Recruiting
Date: 2024-11-07
A Phase 1b/2 Study of IPI-145 Plus FCR in Previously Untreated, Younger Patients With CLL
CTID: NCT02158091
Phase: Phase 1/Phase 2    Status: Active, not recruiting
Date: 2024-11-06
Humanized CD19-Specific CAR T Cells for the Treatment of Patients With Positive Relapsed or Refractory CD19 Positive B-Cell Acute Lymphoblastic Leukemia
CTID: NCT06447987
Phase: Phase 1    Status: Recruiting
Date: 2024-11-06
Orca-T Following Chemotherapy and Total Marrow and Lymphoid Irradiation for the Treatment of Acute Myeloid Leukemia, Acute Lymphoblastic Leukemia or Myelodysplastic Syndrome
CTID: NCT06195891
Phase: Phase 1    Status: Recruiting
Date: 2024-11-06
Natural Killer(NK) Cell Therapy for Acute Myeloid Leukemia
CTID: NCT05601466
Phase: Phase 1    Status: Terminated
Date: 2024-11-06
Natural Killer(NK) Cell Therapy for AML Minimal Residual Disease
CTID: NCT05601830
Phase: Phase 1    Status: Terminated
Date: 2024-11-06
Study to Compare Axicabtagene Ciloleucel With Standard of Care Therapy as First-line Treatment in Participants With High-risk Large B-cell Lymphoma
CTID: NCT05605899
Phase: Phase 3    Status: Recruiting
Date: 2024-11-05
----------
A PROSPECTIVE, OPEN-LABEL, MULTICENTER RANDOMIZED PHASE III STUDY TO COMPARE THE EFFICACY AND SAFETY OF A COMBINED
CTID: null
Phase: Phase 3    Status: Trial now transitioned, Ongoing
Date: 2020-02-25
A PHASE I/II, MULTICENTER, OPEN-LABEL, MULTI-ARM STUDY EVALUATING THE SAFETY, TOLERABILITY, PHARMACOKINETICS, AND PRELIMINARY ACTIVITY OF IDASANUTLIN IN COMBINATION WITH EITHER CHEMOTHERAPY OR VENETOCLAX IN THE TREATMENT OF PEDIATRIC AND YOUNG ADULT PATIENTS WITH RELAPSED/REFRACTORY ACUTE LEUKEMIAS OR SOLID TUMORS.
CTID: null
Phase: Phase 1, Phase 2    Status: Ongoing, GB - no longer in EU/EEA, Completed
Date: 2020-01-21
Post Transplant High-Dose Cyclophosphamide as GvHD Prophylaxis in Patients Receiving 1-Antigen/Allele HLA Mismatched (7/8 matched) Unrelated Hemopoietic Cell Transplantation for Myeloid Malignancies
CTID: null
Phase: Phase 2    Status: Ongoing
Date: 2019-10-02
Open-label, Single-arm Trial to Evaluate Antitumor Activity, Safety, and Pharmacokinetics of Isatuximab Used in Combination With Chemotherapy in Pediatric
CTID: null
Phase: Phase 2    Status: Ongoing, Completed
Date: 2019-03-04
A Single Arm, Open Label Clinical Study of Haematopoietic Stem Cell Gene Therapy with Cryopreserved Autologous CD34+ Cells Transduced with Lentiviral Vector encoding WAS cDNA in Subjects with Wiskott-Aldrich Syndrome (WAS).
CTID: null
Phase: Phase 3    Status: Trial now transitioned
Date: 2019-01-08
Radiation- and alkylator-free hematopoietic cell transplantation for bone marrow failure due to dyskeratosis congenita / telomere disease
CTID: null
Phase: Phase 2    Status: Completed
Date: 2018-07-02
A comparison of reduced dose total body irradiation (TBI) and cyclophosphamide with fludarabine and melphalan reduced intensity conditioning in adults with acute lymphoblastic leukaemia (ALL) in complete remission.
CTID: null
Phase: Phase 2    Status: GB - no longer in EU/EEA
Date: 2018-06-12
A phase II trial of allogeneic peripheral blood stem cell transplantation from family haploidentical donors in patients with myelodisplastic syndrome and acute
CTID: null
Phase: Phase 2    Status: Prematurely Ended
Date: 2018-03-27
International Randomised Phase III Clinical Trial in Children with Acute Myeloid Leukaemia - Incorporating an Embedded Dose Finding Study for Gemtuzumab Ozogamicin in Combination with Induction Chemotherapy
CTID: null
Phase: Phase 1, Phase 3    Status: Ongoing, GB - no longer in EU/EEA
Date: 2018-03-20
UK CLL Long-term Follow-up Study
CTID: null
Phase: Phase 4    Status: GB - no longer in EU/EEA
Date: 2018-02-15
Phase I/II study of anti-GD2 Chimeric Antigen Receptor-Expressing T cells in pediatric patients affected by High Risk and/or relapsed/refractory Neuroblastoma
CTID: null
Phase: Phase 1, Phase 2    Status: Ongoing
Date: 2017-12-22
Phase I/II study of anti-CD19 Chimeric Antigen Receptor-Expressing T cells in pediatric patients affected by relapsed/refractory CD19+ Acute Lymphoblastic Leukemia and Non Hodgkin Lymphoma
CTID: null
Phase: Phase 1, Phase 2    Status: Restarted
Date: 2017-12-22
A Phase 2, Multicenter Study to Assess the Efficacy and Safety of
CTID: null
Phase: Phase 2    Status: Ongoing, GB - no longer in EU/EEA, Completed
Date: 2017-11-15
Autologous Stem cell Transplantation In refractory Crohn's disease - Low Intensity Therapy Evaluation
CTID: null
Phase: Phase 3    Status: Prematurely Ended
Date: 2017-11-06
A Phase 2, Multicenter Study to Evaluate the Efficacy and Safety Using Autologous Tumor Infiltrating Lymphocytes (LN-145) in Patients with Recurrent, Metastatic or Persistent Cervical Carcinoma
CTID: null
Phase: Phase 2    Status: Ongoing, Trial now transitioned, GB - no longer in EU/EEA, Completed
Date: 2017-10-27
A Polish Adult Leukemia Group (PALG) prospective, multicenter clinical trial to compare the efficacy of two standard induction therapies (DA-90 vs DAC) and two standard salvage regimens (FLAG-IDA vs CLAG-M) in AML patients ≤ 60 years of age - PALG-AML1/2016
CTID: null
Phase: Phase 4    Status: Ongoing
Date: 2017-06-27
A Phase 3, Multicenter, Randomized, Open-Label Study of Guadecitabine (SGI-110) versus Treatment Choice in Adults with Previously Treated Acute Myeloid Leukemia
CTID: null
Phase: Phase 3    Status: Completed
Date: 2017-06-19
A phase 3 multicenter, randomized, prospective, open-label trial of standard chemoimmunotherapy (FCR/BR) versus rituximab plus ve-netoclax (RVe) versus obinutuzumab (GA101) plus venetoclax (GVe) versus obinutuzumab plus ibrutinib plus venetoclax (GIVe) in fit pa-tients with previously untreated chronic lymphocytic leukemia (CLL) without del(17p) or TP53 mutation
CTID: null
Phase: Phase 3    Status: Completed
Date: 2016-11-08
A Phase 3 Open-Label, Multicenter, Randomized Study of ASP2215 versus Salvage Chemotherapy in Patients with Relapsed or Refractory Acute Myeloid Leukemia (AML) with FLT3 Mutation
CTID: null
Phase: Phase 3    Status: Ongoing, GB - no longer in EU/EEA, Completed
Date: 2016-04-20
Molecular-biological tumor profiling for drug treatment selection in patients with advanced and refractory carcinoma
CTID: null
Phase: Phase 2    Status: Completed
Date: 2015-05-04
Study Protocol LAM 2013/01
CTID: null
Phase: Phase 3    Status: Ongoing
Date: 2015-02-04
A phase III, multicentre, randomized, open label clinical trial comparing azacytidine (Vidaza®) versus fludarabine plus cytarabine in elderly patients with newly diagnosed acute myeloid leukemia.
CTID: null
Phase: Phase 3    Status: Completed
Date: 2014-07-25
A Phase 3 Open-Label Randomized Study of Quizartinib Monotherapy Versus Salvage Chemotherapy in Subjects with FLT3-ITD Positive Acute Myeloid Leukemia (AML) Refractory To or Relapsed After First-line Treatment With or Without Hematopoietic Stem Cell Transplant (HSCT) Consolidation.
CTID: null
Phase: Phase 3    Status: Ongoing, Completed
Date: 2014-06-18
Thiotepa- Fludarabine- Treosulfan (TFT) conditioning for 2nd allogeneic PBSCT from a different unrelated donor in patients with AML relapsing from prior allogeneic HCT
CTID: null
Phase: Phase 2    Status: Completed
Date: 2014-02-18
Unrelated cord blood transplantation after reduced toxicity conditioning with mesenchymal stromal cell co-infusion in patients with severe epidermolysis bullosa
CTID: null
Phase: Phase 2    Status: Prematurely Ended
Date: 2014-02-06
A PHASE III MULTICENTER, RANDOMIZED STUDY COMPARING CONSOLIDATION WITH (90)YTTRIUM-LABELED IBRITUMOMAB TIUXETAN (ZEVALIN®) RADIOIMMUNOTHERAPY VS AUTOLOGOUS STEM CELL TRANSPLANTATION (ASCT) IN PATIENTS WITH RELAPSED FOLLICULAR LYMPHOMA (FL) AGED 18-65 YEARS
CTID: null
Phase: Phase 3    Status: Ongoing
Date: 2013-10-08
A Randomised Trial of the FLAMSA-BU Conditioning Regimen in Patients with Acute Myeloid Leukaemia and Myelodysplasia Undergoing Allogeneic Stem Cell Transplantation
CTID: null
Phase: Phase 2    Status: Completed
Date: 2013-08-21
Phase 2 multicenter study to assess the efficacy and the safety
CTID: null
Phase: Phase 2    Status: Ongoing
Date: 2013-07-30
A phase II multicentre open-label study on allogeneic stem cell transplantation from unrelated, cord-blood and family haploidentical donors in patients with active acute leukemia
CTID: null
Phase: Phase 2    Status: Completed
Date: 2013-07-05
MULTI-CENTER, PHASE II STUDY TO ASSESS THE SAFETY AND EFFICACY OF HAPLOIDENTICAL BONE MARROW TRANSPLANTATION USING REDUCED INTENSITY CONDITIONING (RIC) REGIMEN AND POST-TRANSPLANT CYCLOPHOSPHAMIDE, IN PATIENTS WITH POOR PROGNOSIS LYMPHOMAS.
CTID: null
Phase: Phase 2    Status: Completed
Date: 2013-04-06
Subcutaneous Bortezomib, Cyclophosphamide and Rituximab (BCR) versus Fludarabine, Cyclophosphamide and Rituximab (FCR) for initial therapy of Waldenstrőm macroglobulinaemia: a randomised phase II study.
CTID: null
Phase: Phase 2    Status: Prematurely Ended
Date: 2012-08-09
Fludarabine/Rituximab combined with escalating doses of Lenalidomide in untreated chronic lymphocytic leukemia (CLL) – a dose-finding study with escalating starting lse if(down_display === 'none' || down_display === '') { icon_angle_up.style.di

生物数据图片

  • Fludarabine

    Fludarabine

  • Fludarabine
    Effects of fludarabine on survival pathways.Eur J Haematol.2007 Dec;79(6):486-93.
  • Fludarabine
    Antitumoral efficacy of fludarabine in established RPMI8226 tumors in vivo.Eur J Haematol.2007 Dec;79(6):486-93.
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