Regorafenib mesylate 中文名称: 瑞戈非尼甲磺酸盐

别名: 利拉非尼甲磺酸盐

目录号: V44486 纯度: ≥98%

COA 产品数据产品说明书 SDS

Regorafenib (BAY 73-4506) 甲磺酸盐是一种口服生物可利用的多靶点受体酪氨酸激酶（酪氨酸激酶）抑制剂，分别抑制 VEGFR1/2/3、PDGFRβ、Kit、RET 和 Raf-1 的 IC50。

Regorafenib mesylate CAS号: 835621-08-4
产品类别: New3

产品仅用于科学研究，不针对患者销售

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Nature 2025, 643(8070):192-200.

Nature 2024 Dec 18.

Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nat Neurosci 2024, 27:1468-1474.

Science Adv 2025, 11(33):eadr5199.

Nat Metab 2024, 6: 1108-1127.

Cell Stem Cell 2024, 31:106-126.e13.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

STTT 2023,8(1):91.

Cell Reports 2023,42(4):112313

Science Trans Med 2023, 15: eadd7872.

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Cancer Discov 2022,12(4):1106-1127.

Immunity 2023,56(3):620-634.e11.

Immunity 2024,57:2651-2668.e12.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

产品描述
生物活性&实验参考方法
化学信息
溶解度数据
计算器
临床试验信息
相关产品

产品描述

Regorafenib (BAY 73-4506) 甲磺酸盐是一种口服生物可利用的多靶点受体酪氨酸激酶（酪氨酸激酶）抑制剂，分别抑制 VEGFR1/2/3、PDGFRβ、Kit、RET 和 Raf-1 的 IC50。 13/4.2/46、22、7、1.5 和 2.5 nM。甲磺酸瑞戈非尼显示出非常有效的抗肿瘤和抗血管生成活性。

生物活性&实验参考方法

体外研究 (In Vitro)	在 GIST 882、甲状腺 TT、MDA-MB-231、HepG2、A375 和 SW620 细胞中，甲磺酸瑞戈非尼（0–10 μM，96 小时）具有抗增殖作用 [1]。除了抑制 FGFR 和 pERK1/2 之外，甲磺酸瑞格非尼（0-3000 nM，30 分钟）还可以防止 VEGFR2、TIE2 和 PDGFR-β 自身磷酸化[1]。甲磺酸瑞戈非尼以浓度依赖性方式抑制 Hep3B 细胞生长，IC50 为 5 μM。然后，Hep3B 细胞中的瑞戈非尼会上调 JNK 靶点磷酸化的 c-Jun，但总 c-Jun 不会上调 [2]。
体内研究 (In Vivo)	Regorafenib mesylate（10 mg/kg，口服，单剂量或每日服用 4 天）可减少大鼠 GS9L 胶质母细胞瘤模型中的肿瘤血管和肿瘤发展 [1]。甲磺酸瑞戈非尼（0-100 mg/kg，口服，每日一次 × 9）在 Colo-205、MDA-MB-231 和 786-O 模型中表现出抗肿瘤和抗血管生成作用 [1]。
细胞实验	细胞增殖测定[1] 细胞类型： GIST 882、甲状腺 TT、MDA-MB-231、HepG2、A375 和 SW620 细胞测试浓度： 10 μM 和 5 nM 孵育时间： 96 小时实验结果： GIST 882、甲状腺 TT、MDA- For MB -231、HepG2、A375 和 SW620 细胞，IC50 值为 45 ± 20、34 ± 8、401 ± 88、560 ± 200、900、967 ± 287 nM。分别。蛋白质印迹分析[1] 细胞类型： NIH-3T3/VEGFR2 细胞、(CHO)-TIE2 细胞、HAoSMCs 细胞、MCF-7 细胞测试浓度：0、10、30、100、300、1000、3000 nM 孵育时间：30 分钟实验结果：抑制 VEGFR2、TIE2 和 PDGFR-β 的自身磷酸化，IC50 值分别为 3、31 和 90 nM，抑制 FGF10 刺激的 MCF-7 乳腺癌 (BC) 细胞中的 FGFR 信号传导，并显示抑制磷酸化 FGFR 底物 2 (pFRS2) 和下游信号激酶 pERK1/2。
动物实验	动物/疾病模型：大鼠 GS9L 胶质母细胞瘤异种移植模型[1] 剂量： 10 mg/kg 给药途径：口服（po）单次给药或每日一次，连续4天实验结果：抑制大鼠 GS9L 胶质母细胞瘤模型中的肿瘤血管生成和肿瘤生长。动物/疾病模型：雌性无胸腺NCr nu/nu（裸鼠），多种异种移植模型，包括源自CRC（Colo-205）、BC（MDA-MB-231）和RCC（786-O）肿瘤的模型[1] 剂量：0、3、10、30、100 mg/kg 给药途径：po（灌胃）qd × 9 实验结果：有效抑制Colo-205、MDA-MB-231和786-O模型的生长。显著降低肿瘤MVA，有效抑制RAF/MEK/ERK信号级联反应，并显著抑制肿瘤细胞增殖。
药代性质 (ADME/PK)	吸收、分布和排泄 Cmax = 2.5 μg/mL；Tmax = 4 小时；AUC = 70.4 μgh/mL；稳态 Cmax = 3.9 μg/mL；稳态 AUC = 58.3 μgh/mL；与口服溶液相比，片剂的平均相对生物利用度为 69% 至 83%。服用 120 mg 放射性标记口服溶液后 12 天内，约 71% 的放射性标记剂量经粪便排出（47% 为母体化合物，24% 为代谢物），19% 的剂量经尿液排出（17% 为葡萄糖醛酸苷）。瑞戈非尼经肠肝循环，在 24 小时给药间隔内观察到多个血浆浓度峰值。代谢/代谢物瑞戈非尼由 CYP3A4 和 UGT1A9 代谢。在人血浆中稳态测定的瑞戈非尼主要循环代谢物为M-2（N-氧化物）和M-5（N-氧化物和N-去甲基），二者均具有与瑞戈非尼相似的体外药理活性和稳态浓度。M-2和M-5的蛋白结合率很高（分别为99.8%和99.95%）。瑞戈非尼是P-糖蛋白抑制剂，而其活性代谢物M-2（N-氧化物）和M-5（N-氧化物和N-去甲基）是P-糖蛋白的底物。生物半衰期瑞戈非尼，口服160 mg = 28小时（14-58小时）；M-2代谢物，口服160 mg = 25小时（14-32小时）；M-5代谢物，口服160 mg = 51小时（32-72小时）；
毒性/毒理 (Toxicokinetics/TK)	肝毒性在瑞戈非尼的大型临床试验中，血清转氨酶水平升高较为常见，发生率达39%至45%，其中3%至6%的患者转氨酶水平超过正常值上限（ULN）的5倍以上。此外，已有数例瑞戈非尼治疗期间出现临床表现明显的肝损伤的报道，这些损伤通常较为严重，偶有致命性，估计发生率约为0.3%。因此，建议常规监测肝酶。瑞戈非尼引起的肝损伤可表现为多种不同的模式或表型。部分患者在开始服用瑞戈非尼后数日内出现急性肝坏死，血清转氨酶和乳酸脱氢酶水平升高，伴有轻度黄疸，但INR延长并出现肝功能衰竭的体征。这种损伤可能较为严重，但通常具有自限性，且恢复迅速且完全。其他患者表现为类似急性病毒性肝炎的临床模式，伴有肝细胞性（或混合性）血清酶升高和黄疸，黄疸可持续较长时间，且在一些病例中甚至导致死亡。自身免疫和免疫过敏反应并不常见。此外，罕见的瑞戈非尼相关肝损伤病例表现为类似肝窦阻塞综合征或假性肝硬化，伴有明显的肝脏结节和腹水，但最终可改善或消退。最后，瑞戈非尼与其他多激酶抑制剂（舒尼替尼、伊马替尼、索拉非尼）一样，也与高氨血症昏迷发作有关，通常在开始用药后的几天或几周内出现，停药后可迅速逆转。可能性评分：B（极有可能引起临床上明显的肝损伤）。妊娠和哺乳期影响 ◉ 哺乳期用药概述目前尚无瑞戈非尼在哺乳期临床应用的信息。由于瑞戈非尼与血浆蛋白的结合率高达99.5%，因此其在乳汁中的含量可能很低。然而，其一种代谢物的半衰期长达70小时，可能会在婴儿体内蓄积。制造商建议在瑞戈非尼治疗期间以及末次给药后 2 周内停止母乳喂养。 ◉ 对母乳喂养婴儿的影响截至修订日期，未找到相关的已发表信息。 ◉ 对泌乳和母乳的影响截至修订日期，未找到相关的已发表信息。蛋白结合瑞戈非尼与人血浆蛋白的结合率很高 (99.5%)。
参考文献	[1]. Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity. Int J Cancer, 2011, 129(1), 245-255. [2]. Fluoro-Bay 43-9006 (Regorafenib) effects on hepatoma cells: growth inhibition, quiescence, and recovery. J Cell Physiol, 2013, 228(2), 292-297.
其他信息	瑞戈非尼是一种吡啶甲酰胺类化合物，由4-[4-({[4-氯-3-(三氟甲基)苯基]氨基甲酰基}氨基)-3-氟苯氧基]吡啶-2-羧酸与甲胺缩合而成。用于治疗既往接受过化疗、抗EGFR或抗VEGF治疗的转移性结直肠癌患者。它具有抗肿瘤、酪氨酸激酶抑制和肝毒性等作用。它是一种芳香醚、吡啶甲酰胺、单氯苯类、(三氟甲基)苯类、单氟苯类和苯脲类化合物。瑞戈非尼是一种口服的多激酶抑制剂，用于治疗转移性结直肠癌、晚期胃肠道间质瘤和肝细胞癌。瑞戈非尼于2012年9月27日获得FDA批准。2017年4月，瑞戈非尼的适应症扩展至治疗肝细胞癌。无水瑞戈非尼是一种激酶抑制剂。其作用机制包括作为激酶抑制剂、细胞色素P450 2C9抑制剂、乳腺癌耐药蛋白抑制剂、UGT1A9抑制剂和UGT1A1抑制剂。瑞戈非尼是一种口服多激酶抑制剂，用于治疗难治性转移性结直肠癌、肝细胞癌和胃肠道间质瘤。瑞戈非尼治疗期间常伴有血清转氨酶升高，并有罕见但有时严重甚至致命的临床表现明显的肝损伤病例。无水瑞戈非尼是瑞戈非尼的无水形式，瑞戈非尼是一种口服生物利用度高的小分子药物，具有潜在的抗血管生成和抗肿瘤活性。瑞戈非尼可与血管内皮生长因子受体（VEGFR）2和3以及Ret、Kit、PDGFR和Raf激酶结合并抑制其活性，从而抑制肿瘤血管生成和肿瘤细胞增殖。VEGFR是受体酪氨酸激酶，在肿瘤血管生成中发挥重要作用；受体酪氨酸激酶RET、KIT和PDGFR以及丝氨酸/苏氨酸特异性Raf激酶参与肿瘤细胞信号传导。瑞戈非尼是瑞戈非尼的水合物形式，是一种口服生物利用度高的小分子药物，具有潜在的抗血管生成和抗肿瘤活性。瑞戈非尼可与血管内皮生长因子受体（VEGFR）2和3以及Ret、Kit、PDGFR和Raf激酶结合并抑制其活性，从而抑制肿瘤血管生成和肿瘤细胞增殖。VEGFR是受体酪氨酸激酶，在肿瘤血管生成中发挥重要作用；受体酪氨酸激酶RET、KIT和PDGFR以及丝氨酸/苏氨酸特异性Raf激酶参与肿瘤细胞信号传导。另见：瑞戈非尼一水合物（活性成分）。药物适应症瑞戈非尼适用于治疗既往接受过氟尿嘧啶、奥沙利铂和伊立替康类化疗、抗VEGF治疗以及（如果KRAS野生型）抗EGFR治疗的转移性结直肠癌（CRC）患者。瑞戈非尼也适用于治疗既往接受过甲磺酸伊马替尼和苹果酸舒尼替尼治疗的局部晚期、不可切除或转移性胃肠道间质瘤（GIST）患者。瑞戈非尼也适用于治疗既往接受过索拉非尼治疗的肝细胞癌 (HCC) 患者。 FDA 标签 Stivarga 适用于以下成年患者的单药治疗：既往接受过或不适合接受现有疗法（包括氟尿嘧啶类化疗、抗 VEGF 疗法和抗 EGFR 疗法）治疗的转移性结直肠癌 (CRC) 患者；既往接受过伊马替尼和舒尼替尼治疗后病情进展或不耐受的不可切除或转移性胃肠道间质瘤 (GIST) 患者；既往接受过索拉非尼治疗的肝细胞癌 (HCC) 患者。治疗所有恶性肿瘤（造血和淋巴组织肿瘤除外）作用机制瑞戈非尼是一种小分子抑制剂，可抑制多种膜结合和细胞内激酶，这些激酶参与正常的细胞功能以及肿瘤发生、肿瘤血管生成和肿瘤微环境维持等病理过程。在体外生化或细胞实验中，瑞戈非尼及其主要的人源活性代谢物M-2和M-5在临床应用浓度下可抑制RET、VEGFR1、VEGFR2、VEGFR3、KIT、PDGFR-α、PDGFR-β、FGFR1、FGFR2、TIE2、DDR2、TrkA、Eph2A、RAF-1、BRAF、BRAFV600E、SAPK2、PTK5和Abl的活性。在体内模型中，瑞戈非尼在大鼠肿瘤模型中表现出抗血管生成活性，并在包括一些人类结直肠癌在内的多种小鼠异种移植模型中表现出抑制肿瘤生长和抗转移活性。

*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	C21H15CLF4N4O3.CH4O3S
分子量	578.9211
精确质量	578.065
CAS号	835621-08-4
相关CAS号	Regorafenib;755037-03-7;Regorafenib monohydrate;1019206-88-2;Regorafenib-d3;1255386-16-3
PubChem CID	11167602
外观&性状	Typically exists as solid at room temperature
LogP	6.81
tPSA	155.1
氢键供体(HBD)数目	3
氢键受体(HBA)数目	8
可旋转键数目(RBC)	5
重原子数目	33
分子复杂度/Complexity	686
定义原子立体中心数目	0
SMILES	C1(C(NC)=O)=NC=CC(OC2=CC=C(NC(=O)NC3=CC=C(Cl)C(C(F)(F)F)=C3)C(F)=C2)=C1.S(C)(=O)(O)=O
InChi Key	FNHKPVJBJVTLMP-UHFFFAOYSA-N
InChi Code	InChI=1S/C21H15ClF4N4O3/c1-27-19(31)18-10-13(6-7-28-18)33-12-3-5-17(16(23)9-12)30-20(32)29-11-2-4-15(22)14(8-11)21(24,25)26/h2-10H,1H3,(H,27,31)(H2,29,30,32)
化学名	4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide
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)	May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
溶解度 (体内实验)	注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。注射用配方 (IP/IV/IM/SC等) 注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline) 生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。注射用配方 2:* DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline) 注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil) 示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。 View More 注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)] 20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。注射用配方 5:* 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline) 注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline) 注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) 注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil) 注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline) 口服配方口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠) 口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素) 示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。 View More 口服配方 3: 溶解于 PEG400 (聚乙二醇400) 口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素) 口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素) 口服配方 6: 做成粉末与食物混合注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。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。

溶解度 (体外实验)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

溶解度 (体内实验)

注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。

注射用配方
(IP/IV/IM/SC等)

注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)
*生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。
注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil)
示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。

View More

注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil)
注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)

口服配方

口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。

View More

口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合

注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。

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	1.7274 mL	8.6368 mL	17.2735 mL
	5 mM	0.3455 mL	1.7274 mL	3.4547 mL
	10 mM	0.1727 mL	0.8637 mL	1.7274 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

质量

浓度

体积

分子量*

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

参见示例

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。

浓度 (起始)

体积 (起始)

浓度 (终)

体积 (终)

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

分子式

分子量

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。

配液体积

质量

配液浓度

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）

给药剂量 mg/kg

动物平均体重 g

每只动物给药体积 μL

动物数量

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。

% DMSO

% Tween 80

% ddH₂O

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。

注意： (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

A Trial to Evaluate Multiple Regimens in Newly Diagnosed and Recurrent Glioblastoma
CTID: NCT03970447
Phase: Phase 2/Phase 3 Status: Recruiting
Date: 2024-12-02

Regorafenib for Recurrent Grade 2 and 3 Meningioma (MIRAGE Trial)
CTID: NCT06275919
Phase: Phase 2 Status: Recruiting
Date: 2024-11-29

Phase Ib / Regorafenib With Conventional Chemotherapy/Newly Diagnosed Patients/ Multimetastatic Ewing Sarcoma
CTID: NCT05830084
Phase: Phase 1 Status: Recruiting
Date: 2024-11-29

An Open Label Study Evaluating the Efficacy and Safety of Etrumadenant (AB928) Based Treatment Combinations in Participants With Metastatic Colorectal Cancer.
CTID: NCT04660812
Phase: Phase 1/Phase 2 Status: Active, not recruiting
Date: 2024-11-25

Botensilimab, Balstilimab and Regorafenib or Botensilimab and Balstilimab for the Treatment of Advanced or Metastatic Microsatellite Stable Colorectal Cancer
CTID: NCT06575725
Phase: Phase 2 Status: Withdrawn
Date: 2024-11-21

View More

A Study of Continued Treatment With Regorafenib in Participants With Solid Tumors Who Have Participated in Other Bayer Studies
CTID: NCT06246643
Phase: Phase 2 Status: Active, not recruiting
Date: 2024-11-20

Evaluation of Treatment PERSOnalization Based on Its Therapeutic Monitoring in Patients with Metastatic Colorectal Cancer Treated with REgorafenib
CTID: NCT04874207
Phase: Phase 4 Status: Active, not recruiting
Date: 2024-11-15

Regorafenib in Patients with Progressive, Recurrent/Metastatic Adenoid Cystic Carcinoma
CTID: NCT02098538
Phase: Phase 2 Status: Completed
Date: 2024-11-12

Safety and Efficacy of SYHA1813 Single Agent or in Combination With Different Regimens in Unresectable Locally Advanced or Metastatic Solid Tumors.
CTID: NCT06682611
Phase: Phase 1/Phase 2 Status: Not yet recruiting
Date: 2024-11-12

A Study Using Regorafenib as Second or Third Line Therapy in Metastatic Medullary Thyroid Cancer
CTID: NCT02657551
Phase: Phase 2 Status: Active, not recruiting
Date: 2024-11-12

TAPUR: Testing the Use of Food and Drug Administration (FDA) Approved Drugs That Target a Specific Abnormality in a Tumor Gene in People With Advanced Stage Cancer
CTID: NCT02693535
Phase: Phase 2 Status: Recruiting
Date: 2024-11-12

An Observational Study Called STAR-T to Learn More About the Sequential Treatment With Regorafenib and TAS-102 in Adults With Metastatic Colorectal Cancer Under Real World Conditions
CTID: NCT05839951
Phase: Status: Active, not recruiting
Date: 2024-11-12

An Open-Label Study to Enable Continued Treatment Access for Subjects Previously Enrolled in Studies of Ruxolitinib
CTID: NCT02955940
Phase: Phase 2 Status: Active, not recruiting
Date: 2024-11-06

A Real-World Study to Learn More About the Order of Different Treatments and Their Effects in People With Metastatic Colorectal Cancer Receiving Their Third and Fourth Line of Treatment
CTID: NCT06137170
Phase: Status: Active, not recruiting
Date: 2024-11-01

A Study of Coformulated Favezelimab/Pembrolizumab (MK-4280A) Versus Standard of Care in Subjects With Previously Treated Metastatic PD-L1 Positive Colorectal Cancer (MK-4280A-007)-China Extension Study
CTID: NCT05600309
Phase: Phase 3 Status: Active, not recruiting
Date: 2024-10-30

A Study of Coformulated Favezelimab/Pembrolizumab (MK-4280A) Versus Standard of Care in Subjects With Previously Treated Metastatic PD-L1 Positive Colorectal Cancer (MK-4280A-007)
CTID: NCT05064059
Phase: Phase 3 Status: Active, not recruiting
Date: 2024-10-30

Study of Lenvatinib (MK-7902/E7080) in Combination With Pembrolizumab (MK-3475) Versus Standard of Care in Participants With Metastatic Colorectal Cancer (MK-7902-017/E7080-G000-325/LEAP-017)
CTID: NCT04776148
Phase: Phase 3 Status: Completed
Date: 2024-10-29

ctDNA-Guided Sunitinib And Regorafenib Therapy for GIST
CTID: NCT05366816
Phase: Phase 2 Status: Recruiting
Date: 2024-10-26

Safety and Efficacy of NEO212 in Patients with Astrocytoma IDH-mutant, Glioblastoma IDH-wildtype or Brain Metastasis
CTID: NCT06047379
Phase: Phase 1/Phase 2 Status: Recruiting
Date: 2024-10-16

A Study Evaluating the Activity of Anti-cancer Treatments Targeting Tumor Molecular Alterations/characteristics in Advanced / Metastatic Tumors.
CTID: NCT04116541
Phase: Phase 2 Status: Recruiting
Date: 2024-10-16

An Observational Study to Learn More About the Long-Term Responses to Treatment With Regorafenib in Patients With Metastatic Colorectal Cancer in the United States
CTID: NCT06029010
Phase: Status: Active, not recruiting
Date: 2024-10-15

A Phase 2 Randomized, Open-Label Study of RRx-001 vs Regorafenib in Subjects With Metastatic Colorectal Cancer
CTID: NCT02096354
Phase: Phase 2 Status: Completed
Date: 2024-10-15

Sotorasib and Panitumumab Versus Investigator's Choice for Participants With Kirsten Rat Sarcoma (KRAS) p.G12C Mutation
CTID: NCT05198934
Phase: Phase 3 Status: Active, not recruiting
Date: 2024-10-15

Regorafenib and Pembrolizumab in Treating Participants With Advanced or Metastatic Colorectal Cancer
CTID: NCT03657641
Phase: Phase 1/Phase 2 Status: Active, not recruiting
Date: 2024-10-10

An Investigational Immunotherapy Study of BMS-986288 Alone and in Combination With Nivolumab in Advanced Solid Cancers
CTID: NCT03994601
Phase: Phase 1/Phase 2 Status: Completed
Date: 2024-10-08

[18F]FLT-PET as a Predictive Imaging Biomaker of Treatment Responses to Regorafenib
CTID: NCT02175095
Phase: N/A Status: Completed
Date: 2024-10-04

Regorafenib in Combination with Pembrolizumab or Pembrolizumab for MSI-H Colorectal Cancer
CTID: NCT06006923
Phase: Phase 2 Status: Recruiting
Date: 2024-10-02

Regorafenib, With Cetuximab or Panitumumab, for the Treatment of Unresectable, Locally Advanced, or Metastatic Colorectal Cancer
CTID: NCT04117945
Phase: Phase 2 Status: Active, not recruiting
Date: 2024-09-27

Botensilimab, Balstilimab and Regorafenib for the Treatment of Patients with Microsatellite Stable Metastatic Colorectal Cancer Who Have Progressed on Prior Chemotherapy
CTID: NCT05672316
Phase: Phase 1/Phase 2 Status: Active, not recruiting
Date: 2024-09-25

Regorafenib Alone or in Combination With Hypofractionated/Low-dose Radiotherapy Plus Toripalimab for Metastatic Colorectal Cancer
CTID: NCT05963490
Phase: Phase 2 Status: Recruiting
Date: 2024-09-24

Assessing a Regorafenib-irinotecan Combination Versus Regorafenib Alone in Metastatic Colorectal Cancer Patients
CTID: NCT03829462
Phase: Phase 3 Status: Active, not recruiting
Date: 2024-09-20

Regorafenib and Nivolumab in Mismatch Repair (MMR) Refractory Colorectal Cancer
CTID: NCT03712943
Phase: Phase 1 Status: Completed
Date: 2024-09-19

Study Of Intrabucally Administered Electromagnetic Fields and Regorafenib
CTID: NCT04327700
Phase: Phase 2 Status: Terminated
Date: 2024-09-19

Regorafenib in Metastatic Colorectal Cancer
CTID: NCT02466009
Phase: Phase 2 Status: Completed
Date: 2024-09-04

Regorafenib Followed by Nivolumab in Patients With Hepatocellular Carcinoma (GOING)
CTID: NCT04170556
Phase: Phase 1/Phase 2 Status: Completed
Date: 2024-09-03

GSL Synthetase Inhibitor Plus Immune Checkpoint Inhibitor and/or Regorafenib in Previously Treated pMMR/MSS CRC.
CTID: NCT06558773
Phase: Phase 2 Status: Not yet recruiting
Date: 2024-08-21

An Investigational Immuno-therapy Study Of Nivolumab In Combination With Trametinib With Or Without Ipilimumab In Participants With Previously Treated Cancer of the Colon or Rectum That Has Spread
CTID: NCT03377361
Phase: Phase 1/Phase 2 Status: Active, not recruiting
Date: 2024-08-19

Neoadjuvant Regorafenib in Combination With Nivolumab and Short-course Radiotherapy in Stage II-III Rectal Cancer
CTID: NCT04503694
Phase: Phase 2 Status: Recruiting
Date: 2024-08-13

Regorafenib, Ipilimumab and Nivolumab for the Treatment of Chemotherapy Resistant Microsatellite Stable Metastatic Colorectal Cancer
CTID: NCT04362839
Phase: Phase 1 Status: Active, not recruiting
Date: 2024-08-05

Regorafenib and Durvalumab for the Treatment of High-Risk Liver Cancer
CTID: NCT05194293
Phase: Phase 2 Status: Recruiting
Date: 2024-07-30

Cadonilimab Combined With Regorafenib as A Third-line Treatment in Patients With MSS CRLM
CTID: NCT06455254
Phase: Phase 2 Status: Recruiting
Date: 2024-07-30

A Trial to Learn Whether Regorafenib in Combination With Nivolumab Can Improve Tumor Responses and How Safe it is for Participants With Solid Tumors
CTID: NCT04704154
Phase: Phase 2 Status: Completed
Date: 2024-07-23

The Finnish National Study to Facilitate Patient Access to Targeted Anti-cancer Drugs
CTID: NCT05159245
Phase: Phase 2 Status: Recruiting
Date: 2024-07-15

Clinical Study of Regorafenib and Nivolumab Plus Chemotherapy
CTID: NCT05394740
Phase: Phase 1/Phase 2 Status: Active, not recruiting
Date: 2024-07-08

Study of XL092 + Atezolizumab vs Regorafenib in Subjects With Metastatic Colorectal Cancer
CTID: NCT05425940
Phase: Phase 3 Status: Active, not recruiting
Date: 2024-07-05

Circulating Cell-Free Tumor DNA Testing in Guiding Treatment for Patients With Advanced or Metastatic Colorectal Cancer
CTID: NCT03844620
Phase: Phase 2 Status: Active, not recruiting
Date: 2024-06-28

Efficacy of Ginseng for Patients on Regorafenib
CTID: NCT02581059
Phase: Phase 2 Status: Terminated
Date: 2024-06-26

Phase 2 Study to Evaluate the Efficacy of Regorafenib in Specific GIST Mutation Subsets (KIT Exon 17, 18, or 14 Mutation and SDHB Deficient GIST) in the Post-imatinib Second-line Setting.
CTID: NCT06087263
Phase: Phase 2 Status: Recruiting
Date: 2024-06-21

Combined TACE, TKI/Anti-VEGF and ICIs as Conversion Therapy for Advanced Hepatocellular Carcinoma
CTID: NCT05717738
Phase: Status: Recruiting
Date: 2024-06-13

Regorafenib in Combination With Venetoclax and Azacitidine for the Treatment of Patients With Relapsed or Refractory Acute Myeloid Leukemia
CTID: NCT06454409
Phase: Phase 1 Status: Not yet recruiting
Date: 2024-06-12

Phase II Study of Regorafenib as Maintenance Therapy
CTID: NCT03793361
Phase: Phase 2 Status: Active, not recruiting
Date: 2024-06-04

An Observational Study to Learn More About Treatment With Regorafenib in People With Advanced Gastrointestinal Stromal Tumors in the United States
CTID: NCT06321055
Phase: Status: Completed
Date: 2024-05-31

Regorafenib in Combination With Multimodal Metronomic Chemotherapy for Chemo-resistant Metastatic Colorectal Cancers
CTID: NCT06425133
Phase: Phase 2 Status: Not yet recruiting
Date: 2024-05-24

FaR-RMS: An Overarching Study for Children and Adults With Frontline and Relapsed RhabdoMyoSarcoma
CTID: NCT04625907
Phase: Phase 1/Phase 2 Status: Recruiting
Date: 2024-05-23

Panitumumab, Regorafenib, or TAS-102, in Treating Patients With Metastatic and/or Unresectable RAS Wild-Type Colorectal Cancer
CTID: NCT03992456
Phase: Phase 2 Status: Active, not recruiting
Date: 2024-05-21

RegoNivo vs Standard of Care Chemotherapy in AGOC
CTID: NCT04879368
Phase: Phase 3 Status: Active, not recruiting
Date: 2024-05-16

T-Cell Therapy (ECT204) in Adults With Advanced HCC
CTID: NCT04864054
Phase: Phase 2 Status: Recruiting
Date: 2024-05-06

Regorafenib Plus Pembrolizumab in Patients With Advanced or Spreading Liver Cancer Who Have Been Previously Treated With PD-1/PD-L1 Immune Checkpoint Inhibitors
CTID: NCT04696055
Phase: Phase 2 Status: Completed
Date: 2024-05-01

Regorafenib and XmAb20717 in Treatment of High-risk Patients With Colorectal Cancer With Radiographic Occult Molecular Residual Disease After End of Established Definitive Therapy (RX-CROME)
CTID: NCT05900648
Phase: Phase 2 Status: Withdrawn
Date: 2024-04-29

A Phase I Dose Finding Study in Children With Solid Tumors Recurrent or Refractory to Standard Therapy
CTID: NCT02085148
Phase: Phase 1 Status: Completed
Date: 2024-04-22

Regorafenib Combined With Fulvestrant in Recurrent Low-Grade Serous Ovarian Cancer
CTID: NCT05113368
Phase: Phase 2 Status: Recruiting
Date: 2024-04-11

A Clinical Study of Regorafenib in Participants Who Have Been Treated in Previous Bayer-sponsored Regorafenib Studies That Have Been Completed
CTID: NCT03890731
Phase: Phase 2 Status: Completed
Date: 2024-04-02

HAIC Combined With Cadonilimab and Regorafenib as 2nd-line Treatment for ICC
CTID: NCT06335927
Phase: Phase 2 Status: Recruiting
Date: 2024-03-28

Combination of LTC004 and Regorafenib to Treat Patients With Advanced/Metastatic CRC
CTID: NCT06322563
Phase: Phase 2 Status: Not yet recruiting
Date: 2024-03-21

A Study of Nivolumab Combined With FOLFOX and Regorafenib in People Who Have HER2-Negative Esophagogastric Cancer
CTID: NCT04757363
Phase: Phase 2 Status: Active, not recruiting
Date: 2024-03-19

Study of Regorafenib in Patients With Advanced Myeloid Malignancies
CTID: NCT03042689
Phase: Phase 1 Status: Completed
Date: 2024-03-08

Serial Measurements of Molecular and Architectural Responses to Therapy (SMMART) PRIME Trial
CTID: NCT03878524
Phase: Phase 1 Status: Terminated
Date: 2024-03-04

A Study of Nivolumab-relatlimab Fixed-dose Combination Versus Regorafenib or TAS-102 in Participants With Later-lines of Metastatic Colorectal Cancer
CTID: NCT05328908
Phase: Phase 3 Status: Active, not recruiting
Date: 2024-03-01

A Clinical Study of BioTTT001 in Combination With Toripalimab and Regorafenib in Patients With Colorectal Cancer
CTID: NCT06283134
Phase: Phase 1 Status: Not yet recruiting
Date: 2024-02-29

A Clinical Study of T3011 in Combination With Toripalimab and Regorafenib in Patients With Colorectal Cancer
CTID: NCT06283303
Phase: Phase 1 Status: Not yet recruiting
Date: 2024-02-29

A Trial of Cadonilimab Plus Regorafenib in Patients With Hepatocellular Carcinoma Who Failed Camrelizumab Combined With Apatinib
CTID: NCT06280105
Phase: Phase 2 Status: Not yet recruiting
Date: 2024-02-28

Immune Checkpoint Therapy vs Target Therapy in Reducing Serum HBsAg Levels in Patients With HBsAg+ Advanced Stage HCC
CTID: NCT03899428
Phase: Phase 2 Status: Recruiting
Date: 2024-02-28

Chidamide + Regorafenib in Hepatocellular Carcinoma (HCC)
CTID: NCT05770882
Phase: Phase 1/Phase 2 Status: Recruiting
Date: 2024-02-23

Efficacy and the Safety of Regorafenib in Patients Aged More Than 70 Years With a Metastatic Colorectal Adenocarcinoma .
CTID: NCT02788006
Phase: Phase 2 Status: Completed
Date: 2024-02-23

The Purpose of This Trial is to Determine if Regorafenib Plus Durvalumab (MEDI4736) is Safe and Effective in Treatment of Chemo Refractory Advanced Biliary Tract Cancers
CTID: NCT04781192
Phase: Phase 1/Phase 2 Status: Recruiting
Date: 2024-02-23

Regorafenib With Temozolomide With or Without RT in MGMT-Methylated, IDH Wild-type GBM Patients
CTID: NCT06095375
Phase: Phase 1 Status: Recruiting
Date: 2024-02-12

Regorafenib in Patients With Relapsed Glioblastoma. IOV-GB-1-2020 REGOMA-OSS
CTID: NCT04810182
Phase: Status: Completed
Date: 2024-02-08

The Drug Rediscovery Protocol (DRUP Trial)
CTID: NCT02925234
Phase: Phase 2 Status: Recruiting
Date: 2024-01-24

Regorafenib in Good Performance Status Patients With Newly Diagnosed Metastatic Colorectal Adenocarcinoma
CTID: NCT02023333
Phase: Phase 2 Status: Active, not recruiting
Date: 2024-01-22

Regorafenib in Patients With Refractory Primary Bone
A Phase 3 Multicenter, Randomized, Open-label, Active-controlled Study of Sotorasib and Panitumumab Versus Investigator’s Choice (Trifluridine and Tipiracil, or Regorafenib) for the Treatment of Previously Treated Metastatic Colorectal Cancer Subjects with KRAS p.G12C Mutation
CTID: null
Phase: Phase 3 Status: Restarted, Trial now transitioned, Ongoing
Date: 2022-01-26

GCAR-7213: GBM AGILE Global Adaptive Trial Master Protocol: An International, Seamless Phase II/III Response Adaptive Randomization Platform Trial Designed To Evaluate Multiple Regimens In Newly Diagnosed and Recurrent Glioblastoma (GBM), Version 3.2, Amendment 2.2, 14Apr2021
CTID: null
Phase: Phase 2, Phase 3 Status: Trial now transitioned, Completed
Date: 2021-12-07

A Phase 3 study of MK-4280A (coformulated favezelimab [MK-4280] plus
CTID: null
Phase: Phase 3 Status: Trial now transitioned, Temporarily Halted, Completed
Date: 2021-10-08

The Finnish National Study to Facilitate Patient Access to Targeted Anti-cancer Drugs to determine the Efficacy in Treatment of Advanced Cancers with a Known Molecular Profile
CTID: null
Phase: Phase 2 Status: Trial now transitioned
Date: 2021-10-06

A randomized, phase IIb study of adjuvant durvalumab (MEDI4736)
CTID: null
Phase: Phase 2 Status: Trial now transitioned
Date: 2021-09-27

Evaluation of treatment PERSOnalization based on its therapeutic monitoring in patients with metastatic colorectal cancer treated with regorafenib
CTID: null
Phase: Phase 2 Status: Trial now transitioned
Date: 2021-04-27

A Phase 3 Randomized Study of Lenvatinib in Combination with Pembrolizumab Versus Standard of Care in Participants with Metastatic Colorectal Cancer Who Have Received and Progressed On or After or Became Intolerant to Prior Treatment
CTID: null
Phase: Phase 3 Status: Ongoing, Completed
Date: 2021-04-14

A Study Of Nivolumab In Combination With Trametinib With Or Without Ipilimumab In Participants With Previously Treated Metastatic Colorectal Cancers
CTID: null
Phase: Phase 1, Phase 2 Status: Restarted, Ongoing, Completed
Date: 2021-04-12

A phase II trial of neoadjuvant REGorafenib in combination with nIvolumab and short-course radiotherapy iN stage II-III rectAl cancer
CTID: null
Phase: Phase 2 Status: Trial now transitioned
Date: 2021-03-09

REGOMAIN – A randomized, placebo-controlled, double-blinded, multicentre, comparative phase II study of the efficacy of regorafenib as maintenance treatment in patients with high grade bone sarcomas (HGBS) at diagnosis or relapse and without complete remission after standard treatment
CTID: null
Phase: Phase 2 Status: Trial now transitioned
Date: 2021-01-07

A Multi-indication, Single-treatment Arm, Open-label Phase 2 Study of Regorafenib and Nivolumab in Combination with dose in Patients with Recurrent or Metastatic Solid Tumors
CTID: null
Phase: Phase 2 Status: Ongoing, GB - no longer in EU/EEA, Completed
Date: 2020-12-16

An Open-Label Study of Regorafenib in Combination with Pembrolizumab in Patients with Advanced or Metastatic Hepatocellular Carcinoma (HCC) after PD-1/PD-L1 Immune Checkpoint Inhibitors
CTID: null
Phase: Phase 2 Status: Temporarily Halted, Completed
Date: 2020-12-11

Randomized phase II study of PAnitumumab REchallenge followed by REgorafenib versus the reverse sequence in RAS and BRAF WILD-TYPE chemorefractory metastatic colorectal cancer patients.
CTID: null
Phase: Phase 2 Status: Trial now transitioned
Date: 2020-09-24

Regorafenib in combination with metronomic cyclophosphamide, capecitabine, and low-dose aspirin in metastatic colorectal cancer carcinoma
CTID: null
Phase: Phase 2 Status: Completed
Date: 2020-08-19

A randomized, phase II study comparing the sequences of regorafenib and trifluridine/tipiracil, after failure of standard therapies in patients with metastatic colorectal cancer
CTID: null
Phase: Phase 2 Status: Ongoing, Prematurely Ended
Date: 2020-07-23

A PHASE Ib/II, OPEN-LABEL, MULTICENTER, RANDOMIZED UMBRELLA STUDY EVALUATING THE EFFICACY AND SAFETY OF MULTIPLE IMMUNOTHERAPY-BASED TREATMENT COMBINATIONS IN PATIENTS WITH METASTATIC COLORECTAL CANCER (MORPHEUS-CRC)
CTID: null
Phase: Phase 1, Phase 2 Status: GB - no longer in EU/EEA, Prematurely Ended
Date: 2020-03-27

Gender-related response to Tyrosine Kinase-Inhibitor drugs in hepatocellular carcinoma
CTID: null
Phase: Phase 4 Status: Prematurely Ended
Date: 2020-03-20

The GOING Study: Regorafenib followed by Nivolumab in patients with Hepatocellular Carcinoma progressing under sorafenib
CTID: null
Phase: Phase 2 Status: Ongoing
Date: 2020-01-14

REGOSTA – A randomized, placebo-controlled, double-blinded, multicentre study evaluating the efficacy and safety of regorafenib as maintenance therapy after first-line treatment in patients with bone sarcomas
CTID: null
Phase: Phase 3 Status: Trial now transitioned
Date: 2019-03-14

A single arm, open-label, multicenter Phase 2 study of regorafenib in participants who have been treated in a previous Bayer-sponsored regorafenib study (monotherapy or combination treatment) that has reached the primary completion endpoint or the main data analysis, or has been stopped prematurely.
CTID: null
Phase: Phase 2 Status: GB - no longer in EU/EEA, Completed
Date: 2019-02-20

Safety, tolerability and efficacy of regorafenib in combination with FOLFIRINOX in patients with RAS-mutated metastatic colorectal cancer: a dose-escalation, phase I/II trial - FOLFIRINOX-R
CTID: null
Phase: Phase 1, Phase 2 Status: Ongoing
Date: 2018-12-04

A randomised phase II trial assessing REGorafenib combined with IRInotecan as second-line treatment in patients with metastatic gastro-oesophageal adenocarcinomas.
CTID: null
Phase: Phase 2 Status: Prematurely Ended
Date: 2018-11-09

Efficacy of regorafenib as maintenance therapy in non-adipocytic soft tissue sarcoma having received first-line doxorubicin-based chemotherapy
CTID: null
Phase: Phase 2 Status: Completed
Date: 2018-08-14

A randomized phase III trial assessing a regorafenib-irinotecan combination (REGIRI) versus regorafenib alone in metastatic colorectal cancer patients after failure of standard therapies, according to the A/A genotype of Cyclin D1
CTID: null
Phase: Phase 3 Status: Trial now transitioned
Date: 2018-08-06

An International, Multicenter, Open-label, Randomized, Phase 3 Study of BLU-285 vs Regorafenib in Patients with Locally Advanced Unresectable or Metastatic Gastrointestinal Stromal Tumor (GIST)
CTID: null
Phase: Phase 3 Status: GB - no longer in EU/EEA, Completed
Date: 2018-04-23

A phase I/II study of Regorafenib plus Avelumab in digestive tumors
CTID: null
Phase: Phase 1, Phase 2 Status: Ongoing
Date: 2018-03-14

A multi-center, open-label, non-randomized, phase I dose escalation study of regorafenib (BAY 73-4506) in pediatric subjects with solid malignant tumors that are recurrent or refractory to standard therapy.
CTID: null
Phase: Phase 1 Status: Ongoing, Completed
Date: 2018-01-15

Predictive value of in-vitro testing anti-cancer therapy sensitivity on tumorspheres from patients with metastatic colorectal cancer
CTID: null
Phase: Phase 2 Status: Completed
Date: 2017-07-10

Phase II randomized study of maintenance Regorafenib vs Placebo in no progression patients after first-line platinum and fluoropyrimidines based chemotherapy in HER2 negative locally advanced/metastatic gastric or gastroesophagel junction cancer (a-MANTRA Study)
CTID: null
Phase: Phase 2 Status: Completed
Date: 2017-04-04

A randomized phase II study between regorafenib and continuing biologic treatment to multi treated patients with colorectal cancer.
CTID: null
Phase: Phase 2 Status: Prematurely Ended
Date: 2016-09-07

A Phase III, open-label, multicenter, three-arm, randomized study to investigate the efficacy and safety of cobimetinib plus atezolizumab and atezolizumab monotherapy vs. regorafenib in patients with previously treated unresectable locally advanced or metastatic colorectal adenocarcinoma
CTID: null
Phase: Phase 3 Status: Prematurely Ended, Completed
Date: 2016-08-18

A randomized phase 2 study comparing different dose-approaches of induction treatment (first cycle) of regorafenib in metastatic colorectal cancer (mCRC) patients
CTID: null
Phase: Phase 2 Status: Completed
Date: 2016-06-09

The effects of the proton pump inhibitor esomeprazole on the bioavailability of regorafenib in patients with a metastatic colorectal cancer (mCRC) or gastrointestinal stromal tumour (GIST).
CTID: null
Phase: Phase 4 Status: Completed
Date: 2016-05-19

A randomised phase II trial of imatinib alternating with
CTID: null
Phase: Phase 2 Status: Ongoing, GB - no longer in EU/EEA, Prematurely Ended, Completed
Date: 2016-01-19

Phase II, single arm, non-randomized and multicenter clinical trial of regorafenib as a single agent in the first-line setting for patients with metastatic and/or unresectable KIT/PDGFR Wild Type GIST
CTID: null
Phase: Phase 2 Status: Ongoing, Completed
Date: 2015-10-13

PHASE II STUDY EVALUATION OF EFFICACITY AND TOLERANCE OF REGORAFENIB FOR 70 YEARS OLD AND MORE PATIENTS WITH A METASTATIC COLORECTAL ADENOCARCIMA
CTID: null
Phase: Phase 2 Status: Completed
Date: 2015-09-04

Phase II study on Regorafenib in advanced Solitary Fibrous Tumor
CTID: null
Phase: Phase 2 Status: Completed
Date: 2015-07-28

Regorafenib monotherapy as second-line treatment of patients with RAS-mutant advanced colorectal cancer: a multicentre, single-arm, two-stage, phase 2 study.
CTID: null
Phase: Phase 2 Status: Completed
Date: 2015-06-19

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

Regorafenib in relapsed glioblastoma. REGOMA study Randomized, controlled open‐label phase II clinical trial
CTID: null
Phase: Phase 2 Status: Completed
Date: 2015-04-24

A Randomized, Double-Blind Study of Ruxolitinib or Placebo in
CTID: null
Phase: Phase 2 Status: Completed, Prematurely Ended
Date: 2015-04-21

Phase II randomized study of maintenance regorafenib vs placebo in no progression patients after first-line platinum and fluoropyrimidines based chemotherapy in HER2 negative locally advanced/metastatic gastric or gastroesophagel junction cancer.
CTID: null
Phase: Phase 2 Status: Prematurely Ended
Date: 2014-12-24

REgorafenib’s Liquid BiopsY (RELY): A multicenter translational biomarker phase II trial of regorafenib in patients with non-resectable pretreated colorectal cancer.
CTID: null
Phase: Phase 2 Status: Completed
Date: 2014-12-17

Phase III study of RegorAfenib VErsus placebo as maintenance therapy in RAS wiLd type metastatic coLOrectal cancer
CTID: null
Phase: Phase 3 Status: Ongoing, Prematurely Ended
Date: 2014-12-01

An Open-Label Phase II Study of regorafenib In Patients With Metastatic Solid Tumors Who Have Progressed After Standard Therapy - RESOUND
CTID: null
Phase: Phase 2 Status: Ongoing
Date: 2014-11-25

A combined Phase IIa / IIb study of the efficacy, safety, and tolerability of repeated topical doses of regorafenib eye drops, in treatment-naïve subjects with neovascular age related macular degeneration
CTID: null
Phase: Phase 2 Status: Prematurely Ended
Date: 2014-07-02

Phase II study of Regorafenib as single agent for the treatment of patients with metastatic colorectal cancer (mCRC) with any RAS or BRAF mutation previously treated with FOLFOXIRI plus bevacizumab.
CTID: null
Phase: Phase 2 Status: Completed
Date: 2014-06-11

Activity of Regorafenib in combination with modified Gemcitabine - Oxaliplatin Chemotherapy (mGEMOX) in patients with advanced Biliary Tract Cancer (BTC): A Phase Ib-II trial
CTID: null
Phase: Phase 1, Phase 2 Status: Ongoing
Date: 2014-05-27

A Randomized Phase II, placebo-controlled , multicenter study evaluating efficacy and safety of regorafenib in patients with metastatic bone sarcomas.
CTID: null
Phase: Phase 2 Status: Trial now transitionelse if(down_display === 'none' || down_display === '') { icon_angle_up.style.