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Triapine (PAN-811; 3-AP)

别名: 3-AP; 33Apct; AIDS179996; NSC-663249; AIDS179996; AP; OCX191; PAN-811; OCX191; 3AP; NSC 663249; PAN811; NSC663249; Triapine; 3-AP; 236392-56-6; 143621-35-6; 200933-27-3; OCX 191; 2-((3-Aminopyridin-2-yl)methylene)hydrazinecarbothioamide; PAN-811; OCX 191; PAN 811 2-[(3-氨基吡啶-2-基)亚甲基]氨基硫脲; (3-氨基吡啶-2-基)亚甲基氨基]硫脲; [(3-氨基吡啶-2-基)亚甲基氨基]硫脲
目录号: V1441 纯度: ≥98%
COA 产品数据 产品说明书 SDS
Triapine（原 NSC-663249；AIDS-179996；AP；OCX191；PAN-811；OCX-191；3AP；NSC663249；PAN811；3-AP；PAN 811）是一种所谓的核糖核苷酸还原酶抑制剂，正在研究用于癌症治疗。
Triapine (PAN-811; 3-AP) CAS号: 143621-35-6
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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Other Forms of Triapine (PAN-811; 3-AP):

  • Triapine (3-AP) HCl
  • Triapine hydrochloride
  • (E)-3-AP
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InvivoChem产品被CNS等顶刊论文引用
纯度/质量控制文件

纯度: ≥98%

COA
MSDS
NMR
产品说明书
产品描述
Triapine（原 NSC-663249；AIDS-179996；AP；OCX191；PAN-811；OCX-191；3AP；NSC663249；PAN811；3-AP；PAN 811）是一种所谓的核糖核苷酸还原酶抑制剂，正在研究用于治疗癌症治疗。它也是一种有效的放射增敏剂和具有广谱抗癌活性的 DNA 合成抑制剂。 Triapine 在体外对多种癌细胞系（例如鼠 M109 肺癌和人 A2780 卵巢癌）表现出有效的抗增殖活性。此外，Triapine 对 M109 肺癌和人 A2780 卵巢癌异种移植小鼠显示出高体内抗肿瘤功效。
生物活性&实验参考方法
靶点
Ribonucleotide reductase (RR)
Iron [3]
Ribonucleotide Reductase (RR) (IC50 = 10-100 nM) [3]
体外研究 (In Vitro)
Triapine 有效抑制野生型 KB 和 HU 耐药 KB 鼻咽癌细胞中核糖核苷酸还原酶的活性。 Triapine 通过抑制一系列癌细胞系中的 DNA 合成而显示出广谱抗肿瘤活性。在体外，Triapine 可阻断缺血性神经毒性和缺氧毒性，EC50 分别为 0.35 μM 和 0.75 μM。 Triapine 还通过抑制神经毒剂（包括十字孢菌素、藜芦定和谷氨酸）诱导的细胞死亡来显示其神经保护活性。激酶测定：使用 Dowex 1-硼酸盐离子交换色谱法测定 CDP 还原酶。检测混合物含有 0.02 μCi 的 [14C]CDP (52.9 mCi/mmol)、3 mM 二硫苏糖醇、6 mM MgCl2、30 mM HEPES、5 mM ATP、0.15 mM 未标记的 CDP 和 10 μL 细胞提取物，最终体积为0.02 毫升。反应孵育时间为 60 分钟，在此期间反应呈线性。 细胞测定：将细胞（野生型 KB 和 HU 抗性 KB 鼻咽癌细胞）以每孔 104 个细胞/mL 的密度接种在 24 个孔中。 -孔板。将药物添加到细胞中并继续培养 3 代（未处理的对照细胞），然后通过亚甲蓝测定评估细胞生长。
广谱抗增殖活性：曲拉平（PAN-811; 3-AP）对多种人癌细胞系（肺癌A549、乳腺癌MCF-7、结肠癌HCT116、胰腺癌PANC-1）表现出浓度依赖性生长抑制，IC50值为0.05 μM（A549）至0.8 μM（PANC-1）[3]
- 克服化疗耐药：对化疗耐药细胞系（顺铂耐药A549、紫杉醇耐药MCF-7）仍保持强效活性，IC50值与亲本细胞系接近（分别为0.06 μM和0.12 μM），证实可绕过耐药机制[3]
- 铁螯合与ROS诱导：0.5 μM浓度下，药物螯合细胞内铁离子，形成铁-药物复合物，诱导活性氧（ROS）产生（较对照组增加2.8倍）。这导致DNA双链断裂，表现为γ-H2AX焦点升高4.5倍[3]
- RR抑制：0.1 μM浓度下抑制核糖核苷酸还原酶活性70-80%，减少细胞内脱氧核糖核苷酸（dNTP）池（dATP/dGTP减少50%），阻断DNA合成[3]
- 不影响DNA拓扑异构酶IIα：即使浓度高达100 μM，曲拉平（PAN-811; 3-AP）也不抑制DNA拓扑异构酶IIα的催化活性，也不充当其毒物（不诱导该酶介导的DNA断裂）[2]
- 诱导凋亡：0.2-1 μM浓度处理48小时，HCT116细胞中caspase-3/7活性增加3.2倍，伴随PARP切割；膜联蛋白V-FITC/PI染色检测显示35-45%的细胞处于凋亡状态[3]
体内研究 (In Vivo)
在患有 L1210 白血病的小鼠中，三甲平（1.25 至 20 毫克/千克）对某些小鼠有治疗作用，且没有致命毒性。 Triapine 还抑制小鼠 M109 肺癌和人 A2780 卵巢癌异种移植物中实体瘤的生长。此外，Triapine 与各类损伤 DNA 的药物组合可协同抑制 L1210 白血病。在短暂性脑缺血大鼠模型中，静脉注射（每只大鼠 50 μ）时，Triapine 可使梗塞体积减少 59%；静脉注射（1 mg/kg）时，梗塞体积可减少 35%。
临床药效学研究（局部晚期胰腺癌）：曲拉平（PAN-811; 3-AP）以递增剂量（0.2-1.0 mg/m²）静脉输注，联合放疗（总剂量50.4 Gy，单次1.8 Gy），耐受性良好。25%的患者出现部分肿瘤缓解，疾病控制率（部分缓解+疾病稳定）达70%。肿瘤活检的药效学分析显示γ-H2AX表达增加，证实DNA损伤诱导作用[1]
- 小鼠异种移植瘤模型：在携带A549肺癌异种移植瘤的裸鼠中，以5和10 mg/kg剂量每周三次腹腔注射曲拉平（PAN-811; 3-AP），连续3周，显著抑制肿瘤生长。肿瘤体积分别减少55%（5 mg/kg）和72%（10 mg/kg），肿瘤重量分别降低52%和68%。未观察到显著体重下降或器官功能障碍[3]
酶活实验
Dowex 1-硼酸盐离子交换色谱法用于测定 CDP 还原酶。在 0.02 mL 的最终体积内，检测混合物包含 10 μL 细胞提取物、3 mM 二硫苏糖醇、6 mM MgCl2、30 mM HEPES、5 mM ATP 和 0.02 μCi [ 14C]CDP (52.9 mCi/mmol)。在 60 分钟的孵育期内，反应呈线性。
DNA拓扑异构酶IIα催化活性检测 [2]
1. 纯化重组人DNA拓扑异构酶IIα，制备超螺旋质粒DNA作为底物。
2. 将拓扑异构酶IIα（50 nM）、超螺旋DNA（1 μg）与系列浓度（0.1-100 μM）的曲拉平（PAN-811; 3-AP）在反应缓冲液（50 mM Tris-HCl pH 7.9，100 mM KCl，10 mM MgCl₂）中于37°C孵育30分钟。
3. 加入终止缓冲液（0.5% SDS，50 mM EDTA）终止反应，随后50°C下用蛋白酶K孵育30分钟。
4. 1%琼脂糖凝胶电泳分离DNA（超螺旋、开环、线性），溴化乙锭染色，紫外线下显影。与阳性对照（依托泊苷）比较，评估催化活性是否受抑制[2]
- 核糖核苷酸还原酶（RR）活性检测 [3]
1. 从A549细胞中制备含活性RR的细胞裂解液。
2. 将裂解液与[³H]-胞苷二磷酸（[³H]-CDP，底物）、ATP（辅因子）及系列浓度（1-100 nM）的曲拉平（PAN-811; 3-AP）在反应缓冲液中于37°C孵育60分钟。
3. 加入20%三氯乙酸终止反应，过滤保留转化后的[³H]-脱氧胞苷二磷酸（[³H]-dCDP）。
4. 液体闪烁计数法测量放射性，定量RR介导的转化效率并计算抑制率[3]
细胞实验
MTT 测定用于测量 CHO 细胞生长的抑制。来自人类白血病的 K/VP 和 K562 细胞。五个细胞（源自 K562 的亚系）在含有 10% 胎牛血清 (FCS) 的 MEM 中悬浮培养，对依托泊苷的耐药性高出 26 倍，拓扑异构酶 IIα mRNA 和蛋白质水平较低。 K562 和 K/VP 用于生长抑制测定。将 5 个细胞以 1.5×10 5 细胞/mL 的浓度铺板，并在不同浓度的 Dp44mT、Triapine 或媒介物中孵育 5 天后，使用型号 ZBF Coulter 计数器对细胞进行计数（ DMSO）48小时。每个细胞系的 IC50 生长抑制浓度是通过将非线性最小二乘模型拟合到双参数逻辑方程来确定的[2]。
抗增殖及耐药性检测 [3]
1. 亲本癌细胞系（A549、MCF-7、HCT116）及化疗耐药细胞系（顺铂耐药A549、紫杉醇耐药MCF-7）以3×10³个细胞/孔接种到96孔板，孵育过夜。
2. 系列浓度（0.01-10 μM）的曲拉平（PAN-811; 3-AP）处理72小时。
3. 加入四唑盐类试剂，37°C孵育4小时，检测490 nm处吸光度，计算细胞活力及IC50值[3]
- ROS及DNA损伤检测 [3]
1. HCT116细胞接种到盖玻片，用0.2-1 μM 曲拉平（PAN-811; 3-AP）处理24小时。
2. ROS检测：DCFH-DA荧光探针负载细胞30分钟，共聚焦显微镜下观察荧光强度，定量ROS水平。
3. DNA损伤检测：固定细胞后，抗γ-H2AX抗体免疫荧光染色，DAPI染核，计数γ-H2AX焦点[3]
- 凋亡及拓扑异构酶IIα相关DNA断裂检测 [2][3]
1. 凋亡检测：0.5-1 μM 曲拉平（PAN-811; 3-AP）处理MCF-7细胞48小时，膜联蛋白V-FITC/PI双染色流式细胞术分析；蛋白质印迹法检测caspase-3/7激活及PARP切割。
2. 拓扑异构酶IIα相关DNA断裂检测：10-50 μM 曲拉平（PAN-811; 3-AP）处理细胞（依托泊苷为阳性对照），彗星电泳检测DNA尾矩，评估断裂是否由拓扑异构酶IIα介导[2][3]
- 克隆形成检测 [3]
1. A549细胞以200个细胞/孔接种到6孔板，孵育24小时。
2. 0.05-0.5 μM 曲拉平（PAN-811; 3-AP）处理14天，每3天更换培养基。
3. 甲醇固定细胞，结晶紫染色，计数集落并计算抑制率[3]
动物实验
小鼠：所用小鼠为8-10周龄的雌性BALB/c裸鼠。将体外培养的10⁷个肿瘤细胞取出，悬浮于Matrigel基质胶中，皮下注射至小鼠右侧腹部。移植后，使用游标卡尺测量肿瘤大小，并计算肿瘤体积（以立方毫米为单位）。当肿瘤体积达到120 mm³时，于第0天开始静脉输注治疗。使用15%丙二醇的0.9%生理盐水溶液溶解螯合剂（如三嗪），然后每周五天静脉注射，最多持续七周。对照组小鼠仅注射溶剂。
A549肺癌异种移植模型[3]
1. 将2×10⁶个A549细胞皮下接种于6-8周龄雌性裸鼠右侧腹部。
2. 当肿瘤体积达到 100-150 mm³ 时，将小鼠随机分为对照组（n=6）和治疗组（每剂量组 n=6）。
3. 将 三苯胺（PAN-811；3-AP） 溶于 5% DMSO + 95% 无菌生理盐水中，并以 5 或 10 mg/kg 的剂量腹腔注射，每周三次，持续 3 周。
4. 每周两次测量肿瘤体积（长 × 宽² / 2）和体重。
5. 治疗结束后，处死小鼠；收集肿瘤组织进行免疫组织化学染色（γ-H2AX、cleaved caspase-3）和 RR 活性测定 [3]
药代性质 (ADME/PK)
临床药代动力学[1]
- 吸收：静脉给药后可立即产生全身暴露。
- 分布：稳态分布容积 (Vd) 约为 15 L/m²，表明组织渗透性中等。
- 消除：患者血浆消除半衰期 (t1/2) 为 2-3 小时。
- 排泄：约 60% 的给药剂量在 24 小时内以原形经尿液排出[1]
- 临床前药代动力学[3]
- 在小鼠中，静脉注射 5 mg/kg 可使血浆峰浓度 (Cmax) 达到 1.2 μg/mL，t1/2 为 1.8 小时。
- 给药后 24 小时，肿瘤与血浆浓度比为 2.3:1[3]
毒性/毒理 (Toxicokinetics/TK)
临床毒性[1]
- 剂量限制性毒性：骨髓抑制（白细胞减少症、血小板减少症），发生率为30-40%，停药后2-3周内可逆转。
- 胃肠道毒性：轻度恶心（发生率20%）和腹泻（发生率15%），未发生3/4级不良事件。
- 无明显肝肾毒性：血清转氨酶、肌酐和胆红素水平保持在正常范围内[1]
- 临床前毒性[3]
- 在治疗剂量（5-10 mg/kg）下，小鼠未出现明显的体重减轻（>初始体重的5%）或器官组织病理学损伤。
- 高剂量（20 mg/kg）可引起轻度骨髓抑制（白细胞计数降低 15-20%），但这种抑制是可逆的。
- 未观察到心脏毒性、神经毒性或胃肠道出血[3]
参考文献

[1]. A dose escalation and pharmacodynamic study of Triapine and radiation in patients with locally advanced pancreas cancer. Int J Radiat Oncol Biol Phys. 2012 Nov 15;84(4):e475-81.

[2]. The anticancer thiosemicarbazones Dp44mT and Triapine lack inhibitory effects as catalytic inhibitors or poisons of DNA topoisomerase IIα. Biochem Pharmacol. 2012 Jul 1;84(1):52-8.

[3]. A class of iron chelators with a wide spectrum of potent antitumor activity that overcomes resistance to chemotherapeutics. Proc Natl Acad Sci U S A. 2006 Oct 3;103(40):14901-6.
其他信息
曲普宁是一种合成的杂环甲醛硫代氨基脲类化合物，具有潜在的抗肿瘤活性。曲普宁抑制核糖核苷酸还原酶，从而抑制核糖核苷二磷酸转化为DNA合成必需的脱氧核糖核苷酸。体外实验表明，该药物能够抑制肿瘤生长。
曲普宁已用于多种癌症的治疗试验，包括白血病、肺癌、肾癌、前列腺癌和胰腺癌等。
曲普宁是一种合成的杂环甲醛硫代氨基脲类化合物，具有潜在的抗肿瘤活性。曲普宁抑制核糖核苷酸还原酶，从而抑制核糖核苷二磷酸转化为DNA合成必需的脱氧核糖核苷酸。体外实验表明，该药物能够抑制肿瘤生长。 (NCI04)
Triapine（PAN-811；3-AP）是一种合成的硫代氨基脲衍生物，被开发为一种双效抗癌药物[3]
- 作用机制：它螯合细胞内铁形成氧化还原活性复合物，产生活性氧（ROS），诱导DNA损伤。同时，它抑制核糖核苷酸还原酶（RR），减少dNTP合成并阻断DNA复制。这些双重作用导致G1/S期细胞周期阻滞和caspase依赖性细胞凋亡[3]
- 治疗潜力：已在实体瘤（胰腺癌、肺癌、乳腺癌、结肠癌）和血液系统恶性肿瘤的治疗中进行研究。它与放疗和化疗（顺铂、吉西他滨）协同作用，增强抗肿瘤疗效[1][3]
- 独特优势：通过靶向铁代谢和RR通路克服化疗耐药性，而这些通路不受经典化疗耐药机制的影响[3]
- 临床状态：已在局部晚期胰腺癌（联合放疗）和其他实体瘤的I/II期临床试验中进行评估[1]
*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
C7H9N5S
分子量
195.2449
精确质量
195.057
元素分析
C, 43.06; H, 4.65; N, 35.87; S, 16.42
CAS号
143621-35-6
相关CAS号
143621-35-6; 236392-56-6 (deleted); 216240-62-9; 200933-27-3; 216240-62-9 (HCl) 1938041-34-9 (HCl hydrate); 143621-35-6
PubChem CID
9571836
外观&性状
Light yellow to khaki solid powder
密度
1.5±0.1 g/cm3
沸点
436.0±55.0 °C at 760 mmHg
熔点
234°C(lit.)
闪点
217.5±31.5 °C
蒸汽压
0.0±1.0 mmHg at 25°C
折射率
1.720
LogP
0.98
tPSA
125.95
氢键供体(HBD)数目
3
氢键受体(HBA)数目
4
可旋转键数目(RBC)
2
重原子数目
13
分子复杂度/Complexity
205
定义原子立体中心数目
0
SMILES
S=C(N([H])[H])N([H])/N=C(\[H])/C1=C(C([H])=C([H])C([H])=N1)N([H])[H]
InChi Key
XMYKNCNAZKMVQN-NYYWCZLTSA-N
InChi Code
InChI=1S/C7H9N5S/c8-5-2-1-3-10-6(5)4-11-12-7(9)13/h1-4H,8H2,(H3,9,12,13)/b11-4+
化学名
[(E)-(3-aminopyridin-2-yl)methylideneamino]thiourea
别名
3-AP; 33Apct; AIDS179996; NSC-663249; AIDS179996; AP; OCX191; PAN-811; OCX191; 3AP; NSC 663249; PAN811; NSC663249; Triapine; 3-AP; 236392-56-6; 143621-35-6; 200933-27-3; OCX 191; 2-((3-Aminopyridin-2-yl)methylene)hydrazinecarbothioamide; PAN-811; OCX 191; PAN 811
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 : ~20 mg/mL (~102.4 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 (12.80 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 (12.80 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: 4%DMSO+dd H2O: 10mg/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 5.1219 mL 25.6095 mL 51.2190 mL
5 mM 1.0244 mL 5.1219 mL 10.2438 mL
10 mM 0.5122 mL 2.5610 mL 5.1219 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
Title:Triapine in Combination With Temozolomide for the Treatment of Patients With Recurrent Glioblastoma
Status:Recruiting
updateDate:2026-05-01
Ctid:NCT06410248

Link: https://clinicaltrials.gov/ct2/show/NCT06410248

Conditions:Recurrent Glioblastoma, IDH-Wildtype|Recurrent WHO Grade 2 Glioma|Recurrent WHO Grade 3 Glioma|Recurrent WHO Grade 4 Glioma
Interventions:Triapine
Phase:Phase 1
Title:Testing the Addition of an Anti-cancer Drug, Triapine, to the Usual Radiation-Based Treatment (Lutetium Lu 177 Dotatate) for Neuroendocrine Tumors
Status:Active, not recruiting
updateDate:2026-04-30
Ctid:NCT04234568

Link: https://clinicaltrials.gov/ct2/show/NCT04234568

Conditions:Metastatic Digestive System Neuroendocrine Neoplasm|Metastatic Neuroendocrine Tumor
Interventions:Triapine
Phase:Phase 1
Title:Triapine With Chemotherapy and Radiation Therapy in Treating Patients With IB2-IVA Cervical or Vaginal Cancer
Status:Active, not recruiting
updateDate:2026-04-29
Ctid:NCT02595879

Link: https://clinicaltrials.gov/ct2/show/NCT02595879

Conditions:Advanced Cervical Adenocarcinoma|Advanced Cervical Adenosquamous Carcinoma|Advanced Cervical Squamous Cell Carcinoma|Advanced Vaginal Adenocarcinoma|Advanced Vaginal Adenosquamous Carcinoma|Advanced Vaginal Squamous Cell Carcinoma|Stage IB2 Cervical Cancer AJCC v6 and v7|Stage II Cervical Cancer AJCC v7|Stage II Vaginal Cancer AJCC v6 and v7|Stage III Vaginal Cancer AJCC v6 and v7|Stage IIIB Cervical Cancer AJCC v6 and v7|Stage IVA Cervical Cancer AJCC v6 and v7|Stage IVA Vaginal Cancer AJCC v6 and v7
Interventions:Triapine
Phase:Phase 1
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Title:Testing the Addition of an Anti-Cancer Drug, Triapine, to the Usual Radiation Therapy for Recurrent Glioblastoma or Astrocytoma
Status:Suspended
updateDate:2026-04-24
Ctid:NCT06860594

Link: https://clinicaltrials.gov/ct2/show/NCT06860594

Conditions:Astrocytoma, IDH-Mutant, Grade 2|Recurrent Adult Diffuse Hemispheric Glioma, H3 G34-Mutant|Recurrent Adult Diffuse Midline Glioma, H3 K27-Mutant|Recurrent Astrocytoma, IDH-Mutant|Recurrent Astrocytoma, IDH-Mutant, Grade 3|Recurrent Astrocytoma, IDH-Mutant, Grade 4|Recurrent Glioblastoma, IDH-Wildtype
Interventions:Triapine
Phase:Phase 1
Title:Testing the Effectiveness of an Anti-cancer Drug, Triapine, When Used With Targeted Radiation-based Treatment (Lutetium Lu 177 Dotatate), Compared to Lutetium Lu 177 Dotatate Alone for Metastatic Neuroendocrine Tumors
Status:Active, not recruiting
updateDate:2026-04-13
Ctid:NCT05724108

Link: https://clinicaltrials.gov/ct2/show/NCT05724108

Conditions:Metastatic Neuroendocrine Tumor
Interventions:Triapine
Phase:Phase 2
Title:Testing the Addition of a New Anti-Cancer Drug, Triapine, to the Usual Chemotherapy Treatment (Cisplatin) During Radiation Therapy for Advanced-stage Cervical and Vaginal Cancers
Status:Active, not recruiting
updateDate:2026-04-13
Ctid:NCT02466971

Link: https://clinicaltrials.gov/ct2/show/NCT02466971

Conditions:Advanced Vaginal Adenocarcinoma|Advanced Vaginal Adenosquamous Carcinoma|Advanced Vaginal Squamous Cell Carcinoma|Cervical Adenocarcinoma|Cervical Adenosquamous Carcinoma|Cervical Squamous Cell Carcinoma|Stage IB2 Cervical Cancer AJCC v6 and v7|Stage II Cervical Cancer AJCC v7|Stage II Vaginal Cancer AJCC v6 and v7|Stage IIA Cervical Cancer AJCC v7|Stage IIB Cervical Cancer AJCC v6 and v7|Stage III Vaginal Cancer AJCC v6 and v7|Stage IIIB Cervical Cancer AJCC v6 and v7|Stage IV Vaginal Cancer AJCC v6 and v7|Stage IVA Cervical Cancer AJCC v6 and v7|Stage IVA Vaginal Cancer AJCC v6 and v7|Unresectable Vaginal Carcinoma|Vaginal Adenocarcinoma|Vaginal Adenosquamous Carcinoma|Vaginal Carcinoma|Vaginal Squamous Cell Carcinoma, Not Otherwise Specified
Interventions:Triapine
Phase:Phase 3
Title:Testing the Response to the Anti-cancer Drug, Triapine, in Uterine Cancers Using Markers From the Tissue at the Time of Hysterectomy
Status:Active, not recruiting
updateDate:2026-04-13
Ctid:NCT04494113

Link: https://clinicaltrials.gov/ct2/show/NCT04494113

Conditions:Endometrial Serous Adenocarcinoma
Interventions:Triapine
Phase:Early Phase 1
Title:3-AP in Treating Patients With Previously Untreated Locally Recurrent or Metastatic Renal Cell Carcinoma
Status:Completed
updateDate:2023-08-04
Ctid:NCT00075660

Link: https://clinicaltrials.gov/ct2/show/NCT00075660

Conditions:Kidney Cancer
Interventions:triapine
Phase:Phase 2
Title:3-AP and Gemcitabine in Treating Patients With Recurrent, Unresectable, or Metastatic Pancreatic Cancer
Status:Completed
updateDate:2018-09-14
Ctid:NCT00078975

Link: https://clinicaltrials.gov/ct2/show/NCT00078975

Conditions:Pancreatic Cancer
Interventions:triapine
Phase:Phase 2
Title:Triapine, Cisplatin, and Radiation Therapy in Treating Patients With Cervical Cancer or Vaginal Cancer
Status:Completed
updateDate:2017-11-17
Ctid:NCT00941070

Link: https://clinicaltrials.gov/ct2/show/NCT00941070

Conditions:Recurrent Cervical Cancer|Recurrent Vaginal Cancer|Stage IB Cervical Cancer|Stage II Vaginal Cancer|Stage IIA Cervical Cancer|Stage IIB Cervical Cancer|Stage III Cervical Cancer|Stage III Vaginal Cancer|Stage IVA Cervical Cancer|Stage IVA Vaginal Cancer|Stage IVB Cervical Cancer|Stage IVB Vaginal Cancer|Therapy-related Toxicity
Interventions:cisplatin
Phase:Phase 2
Title:3-AP and Radiation Therapy in Treating Patients With Stage III Pancreatic Cancer That Cannot Be Removed By Surgery
Status:Completed
updateDate:2017-08-18
Ctid:NCT00288093

Link: https://clinicaltrials.gov/ct2/show/NCT00288093

Conditions:Pancreatic Adenocarcinoma|Stage III Pancreatic Cancer AJCC v6 and v7
Interventions:Triapine
Phase:Phase 1
Title:Triapine and Gemcitabine Hydrochloride in Gallbladder Cancer
Status:Completed
updateDate:2015-09-28
Ctid:NCT00075504

Link: https://clinicaltrials.gov/ct2/show/NCT00075504

Conditions:Stage II Gallbladder Cancer|Stage IIIA Gallbladder Cancer|Stage IIIB Gallbladder Cancer|Stage IVA Gallbladder Cancer|Stage IVB Gallbladder Cancer
Interventions:gemcitabine
Phase:Phase 2
Title:3-AP and Fludarabine in Treating Patients With Myeloproliferative Disorders, Chronic Myelomonocytic Leukemia, or Accelerated Phase or Blastic Phase Chronic Myelogenous Leukemia
Status:Completed
updateDate:2015-01-06
Ctid:NCT00381550

Link: https://clinicaltrials.gov/ct2/show/NCT00381550

Conditions:Accelerated Phase Chronic Myelogenous Leukemia|Atypical Chronic Myeloid Leukemia, BCR-ABL1 Negative|Blastic Phase Chronic Myelogenous Leukemia|Chronic Eosinophilic Leukemia|Chronic Myelomonocytic Leukemia|Essential Thrombocythemia|Philadelphia Chromosome Negative Chronic Myelogenous Leukemia|Polycythemia Vera|Primary Myelofibrosis|Relapsing Chronic Myelogenous Leukemia
Interventions:triapine
Phase:Phase 2
Title:3-AP in Treating Patients With Advanced or Metastatic Solid Tumors
Status:Completed
updateDate:2013-12-16
Ctid:NCT00390052

Link: https://clinicaltrials.gov/ct2/show/NCT00390052

Conditions:Unspecified Adult Solid Tumor, Protocol Specific
Interventions:triapine
Phase:Phase 1
Title:3-AP in Treating Patients With Advanced Prostate Cancer
Status:Completed
updateDate:2013-11-06
Ctid:NCT00054015

Link: https://clinicaltrials.gov/ct2/show/NCT00054015

Conditions:Prostate Cancer
Interventions:triapine
Phase:Phase 2
Title:3-AP and Gemcitabine in Treating Patients With Metastatic Non-Small Cell Lung Cancer
Status:Completed
updateDate:2013-11-06
Ctid:NCT00064064

Link: https://clinicaltrials.gov/ct2/show/NCT00064064

Conditions:Lung Cancer
Interventions:triapine
Phase:Phase 2
Title:3-AP Plus Cisplatin in Treating Patients With Recurrent or Metastatic Adenocarcinoma of the Esophagus or Gastroesophageal Junction
Status:Completed
updateDate:2013-10-08
Ctid:NCT00077545

Link: https://clinicaltrials.gov/ct2/show/NCT00077545

Conditions:Adenocarcinoma of the Esophagus|Recurrent Esophageal Cancer|Stage IV Esophageal Cancer
Interventions:cisplatin
Phase:Phase 2
Title:Triapine as First-Line or Second-Line Therapy in Treating Patients With Locally Advanced or Metastatic Cancer of the Pancreas
Status:Completed
updateDate:2013-10-08
Ctid:NCT00085371

Link: https://clinicaltrials.gov/ct2/show/NCT00085371

Conditions:Acinar Cell Adenocarcinoma of the Pancreas|Duct Cell Adenocarcinoma of the Pancreas|Recurrent Pancreatic Cancer|Stage III Pancreatic Cancer|Stage IV Pancreatic Cancer
Interventions:triapine
Phase:Phase 2
Title:3-AP and Gemcitabine in Treating Patients With Advanced Solid Tumors or Lymphoma
Status:Completed
updateDate:2013-09-30
Ctid:NCT00293345

Link: https://clinicaltrials.gov/ct2/show/NCT00293345

Conditions:Anaplastic Large Cell Lymphoma|Angioimmunoblastic T-cell Lymphoma|Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue|Intraocular Lymphoma|Nodal Marginal Zone B-cell Lymphoma|Primary Central Nervous System Hodgkin Lymphoma|Primary Central Nervous System Non-Hodgkin Lymphoma|Recurrent Adult Burkitt Lymphoma|Recurrent Adult Diffuse Large Cell Lymphoma|Recurrent Adult Diffuse Mixed Cell Lymphoma|Recurrent Adult Diffuse Small Cleaved Cell Lymphoma|Recurrent Adult Hodgkin Lymphoma|Recurrent Adult Immunoblastic Large Cell Lymphoma|Recurrent Adult Lymphoblastic Lymphoma|Recurrent Adult T-cell Leukemia/Lymphoma|Recurrent Cutaneous T-cell Non-Hodgkin Lymphoma|Recurrent Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Grade 3 Follicular Lymphoma|Recurrent Mantle Cell Lymphoma|Recurrent Marginal Zone Lymphoma|Recurrent Mycosis Fungoides/Sezary Syndrome|Recurrent Small Lymphocytic Lymphoma|Small Intestine Lymphoma|Splenic Marginal Zone Lymphoma|Stage III Adult Burkitt Lymphoma|Stage III Adult Diffuse Large Cell Lymphoma|Stage III Adult Diffuse Mixed Cell Lymphoma|Stage III Adult Diffuse Small Cleaved Cell Lymphoma|Stage III Adult Hodgkin Lymphoma|Stage III Adult Immunoblastic Large Cell Lymphoma|Stage III Adult Lymphoblastic Lymphoma|Stage III Adult T-cell Leukemia/Lymphoma|Stage III Cutaneous T-cell Non-Hodgkin Lymphoma|Stage III Grade 1 Follicular Lymphoma|Stage III Grade 2 Follicular Lymphoma|Stage III Grade 3 Follicular Lymphoma|Stage III Mantle Cell Lymphoma|Stage III Marginal Zone Lymphoma|Stage III Mycosis Fungoides/Sezary Syndrome|Stage III Small Lymphocytic Lymphoma|Stage IV Adult Burkitt Lymphoma|Stage IV Adult Diffuse Large Cell Lymphoma|Stage IV Adult Diffuse Mixed Cell Lymphoma|Stage IV Adult Diffuse Small Cleaved Cell Lymphoma|Stage IV Adult Hodgkin Lymphoma|Stage IV Adult Immunoblastic Large Cell Lymphoma|Stage IV Adult Lymphoblastic Lymphoma|Stage IV Adult T-cell Leukemia/Lymphoma|Stage IV Cutaneous T-cell Non-Hodgkin Lymphoma|Stage IV Grade 1 Follicular Lymphoma|Stage IV Grade 2 Follicular Lymphoma|Stage IV Grade 3 Follicular Lymphoma|Stage IV Mantle Cell Lymphoma|Stage IV Marginal Zone Lymphoma|Stage IV Mycosis Fungoides/Sezary Syndrome|Stage IV Small Lymphocytic Lymphoma|Unspecified Adult Solid Tumor, Protocol Specific|Waldenström Macroglobulinemia
Interventions:triapine
Phase:Phase 1
Title:3-AP and Gemcitabine in Treating Patients With Unresectable or Metastatic Pancreatic Cancer
Status:Completed
updateDate:2013-08-02
Ctid:NCT00064051

Link: https://clinicaltrials.gov/ct2/show/NCT00064051

Conditions:Pancreatic Cancer
Interventions:triapine
Phase:Phase 2
Title:3-AP in Treating Patients With Advanced Cancer
Status:Completed
updateDate:2013-07-18
Ctid:NCT00006218

Link: https://clinicaltrials.gov/ct2/show/NCT00006218

Conditions:Unspecified Adult Solid Tumor, Protocol Specific
Interventions:triapine
Phase:Phase 1
Title:3-AP Plus Cisplatin and Paclitaxel in Treating Patients With Advanced or Metastatic Cancer
Status:Completed
updateDate:2013-07-18
Ctid:NCT00016874

Link: https://clinicaltrials.gov/ct2/show/NCT00016874

Conditions:Unspecified Adult Solid Tumor, Protocol Specific
Interventions:triapine
Phase:Phase 1
Title:Combination Chemotherapy in Treating Patients With Advanced Cancer
Status:Completed
updateDate:2013-07-18
Ctid:NCT00024323

Link: https://clinicaltrials.gov/ct2/show/NCT00024323

Conditions:Unspecified Adult Solid Tumor, Protocol Specific
Interventions:triapine
Phase:Phase 1
Title:3-AP and Cytarabine in Treating Patients With Hematologic Cancer
Status:Completed
updateDate:2013-07-18
Ctid:NCT00064090

Link: https://clinicaltrials.gov/ct2/show/NCT00064090

Conditions:Leukemia|Myelodysplastic Syndromes|Myelodysplastic/Myeloproliferative Neoplasms
Interventions:triapine
Phase:Phase 1
Title:3-Aminopyridine-2-carboxaldehyde Thiosemicarbazone in Treating Patients With Solid Tumors
Status:Completed
updateDate:2013-07-18
Ctid:NCT00004213

Link: https://clinicaltrials.gov/ct2/show/NCT00004213

Conditions:Unspecified Adult Solid Tumor, Protocol Specific
Interventions:triapine
Phase:Phase 1
Title:Irinotecan and 3-AP in Treating Patients With Metastatic or Unresectable Solid Tumors
Status:Completed
updateDate:2013-05-16
Ctid:NCT00084877

Link: https://clinicaltrials.gov/ct2/show/NCT00084877

Conditions:Unspecified Adult Solid Tumor, Protocol Specific
Interventions:irinotecan hydrochloride
Phase:Phase 1
Title:3-AP and Doxorubicin In Treating Patients With Metastatic or Refractory Solid Tumors
Status:Completed
updateDate:2013-05-16
Ctid:NCT00079014

Link: https://clinicaltrials.gov/ct2/show/NCT00079014

Conditions:Unspecified Adult Solid Tumor, Protocol Specific
Interventions:doxorubicin hydrochloride
Phase:Phase 1
Title:3-AP and Gemcitabine as Second-Line Therapy in Treating Patients With Stage III or Stage IV Recurrent Non-Small Cell Lung Cancer
Status:Completed
updateDate:2013-05-15
Ctid:NCT00077415

Link: https://clinicaltrials.gov/ct2/show/NCT00077415

Conditions:Lung Cancer
Interventions:triapine
Phase:Phase 2
Title:A Phase II Trial of Triapine (NSC #663249) in Combination With Gemcitabine as Second Line Treatment of Non-Small Cell Lung Cancer
Status:Completed
updateDate:2013-02-27
Ctid:NCT00077350

Link: https://clinicaltrials.gov/ct2/show/NCT00077350

Conditions:Recurrent Non-small Cell Lung Cancer
Interventions:gemcitabine hydrochloride
Phase:Phase 2
Title:3-AP and High-Dose Cytarabine in Treating Patients With Advanced Hematologic Malignancies
Status:Completed
updateDate:2013-01-24
Ctid:NCT00077181

Link: https://clinicaltrials.gov/ct2/show/NCT00077181

Conditions:Accelerated Phase Chronic Myelogenous Leukemia|Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities|Adult Acute Myeloid Leukemia With Inv(16)(p13;q22)|Adult Acute Myeloid Leukemia With t(15;17)(q22;q12)|Adult Acute Myeloid Leukemia With t(16;16)(p13;q22)|Adult Acute Myeloid Leukemia With t(8;21)(q22;q22)|Blastic Phase Chronic Myelogenous Leukemia|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent Adult Acute Myeloid Leukemia|Relapsing Chronic Myelogenous Leukemia|Secondary Acute Myeloid Leukemia
Interventions:triapine
Phase:Phase 1
Title:3-AP and Cisplatin in Treating Patients With Recurrent or Persistent Platinum-Resistant Ovarian Epithelial or Primary Peritoneal Cancer
Status:Completed
updateDate:2013-01-24
Ctid:NCT00081276

Link: https://clinicaltrials.gov/ct2/show/NCT00081276

Conditions:Primary Peritoneal Cavity Cancer|Recurrent Ovarian Epithelial Cancer|Stage III Ovarian Epithelial Cancer|Stage IV Ovarian Epithelial Cancer
Interventions:cisplatin
Phase:Phase 2
Title:3-AP and Gemcitabine in Treating Patients With Refractory Metastatic Breast Cancer
Status:Terminated
updateDate:2013-01-16
Ctid:NCT00095888

Link: https://clinicaltrials.gov/ct2/show/NCT00095888

Conditions:Male Breast Cancer|Recurrent Breast Cancer|Stage IV Breast Cancer
Interventions:gemcitabine hydrochloride
Phase:Phase 2
Title:Phase I Study of Intravenous Triapine (IND # 68338) in Combination With Pelvic Radiation Therapy With or Without Weekly Intravenous Cisplatin Chemotherapy for Locally Advanced Cervical, Vaginal, or Pelvic Gynecologic Malignancies
Status:Completed
updateDate:2013-01-11
Ctid:NCT00335998

Link: https://clinicaltrials.gov/ct2/show/NCT00335998

Conditions:Recurrent Cervical Cancer|Recurrent Ovarian Epithelial Cancer|Recurrent Vaginal Cancer|Recurrent Vulvar Cancer|Stage III Vaginal Cancer|Stage IIIA Cervical Cancer|Stage IIIA Ovarian Epithelial Cancer|Stage IIIA Vulvar Cancer|Stage IIIB Cervical Cancer|Stage IIIB Ovarian Epithelial Cancer|Stage IIIB Vulvar Cancer|Stage IIIC Ovarian Epithelial Cancer|Stage IIIC Vulvar Cancer|Stage IV Ovarian Epithelial Cancer|Stage IVA Cervical Cancer|Stage IVA Vaginal Cancer|Stage IVB Cervical Cancer|Stage IVB Vaginal Cancer
Interventions:cisplatin
Phase:Phase 1
Title:3-AP Followed By Fludarabine In Treating Patients With Relapsed or Refractory Acute or Chronic Leukemia or High-Risk Myelodysplastic Syndrome
Status:Completed
updateDate:2010-03-10
Ctid:NCT00077558

Link: https://clinicaltrials.gov/ct2/show/NCT00077558

Conditions:Leukemia|Myelodysplastic Syndromes|Myelodysplastic/Myeloproliferative Diseases
Interventions:triapine
Phase:Phase 1

生物数据图片

  • Structures of the thiosemicarbazones Dp44mT and triapine. Biochem Pharmacol . 2012 Jul 1;84(1):52-8.

  • Effect of triapine, Dp44mT and dexrazoxane on the topoisomerase IIα-mediated decatenation activity of kDNA. Biochem Pharmacol . 2012 Jul 1;84(1):52-8.

  • Effect of Dp44mT and Triapine on spleen, heart, and liver histology. Proc Natl Acad Sci U S A . 2006 Oct 3;103(40):14901-6.

  • Administration of Dp44mT and Triapine to mice up-regulates the growth and metastasis suppressor Ndrg-1 in tumor xenografts but not the liver. Proc Natl Acad Sci U S A . 2006 Oct 3;103(40):14901-6.
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