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Regorafenib

产品编号 T1792 CAS 755037-03-7

别名: BAY 73-4506, 瑞戈非尼, Fluoro-Sorafenib, 瑞格非尼

Regorafenib (BAY 73-4506) 是一种多靶点受体酪氨酸激酶抑制剂，抑制 RET、C-RAF、VEGFR2、c-Kit、VEGFR1 和 PDGFRβ (IC50=1.5/2.5/4.2/7/13/22 nM)，具有口服活性。Regorafenib 具有抗肿瘤和抗血管生成活性。

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Regorafenib, CAS 755037-03-7

规格	价格/CNY	货期
5 mg	￥ 192	现货
10 mg	￥ 298	现货
25 mg	￥ 515	现货
50 mg	￥ 788	现货
100 mg	￥ 1,230	现货
200 mg	￥ 1,850	现货
500 mg	￥ 3,130	现货
1 mL * 10 mM (in DMSO)	￥ 358	现货

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其他形式的 Regorafenib:

选择批次

纯度: 99.95%

纯度: 99.87%

纯度: 98%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor that inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ and is orally active. Regorafenib has antitumor and anti-angiogenic activity.
靶点活性	B-Raf (V600E):19 nM (cell free), c-Kit:7 nM (cell free), Raf-1:2.5 nM (cell free), VEGFR1:13 nM (cell free), RET:1.5 nM (cell free), VEGFR2:4.2 nM (cell free)
体外活性	方法：人肝癌细胞 Hep3B、PLC/PRF/5 和 HepG2 用 Regorafenib (0-10 μM) 处理 72 h，使用 MTT 方法检测细胞活力。结果：Regorafenib 浓度依赖性降低 Hep3B 细胞活力，IC50 约为 5 μM。PLC/PRF/5 细胞的敏感性与 Hep3B细胞相似。但 HepG2 细胞更敏感，IC50 约为 1 μM。[1] 方法：肿瘤细胞 NIH-3T3/VEGFR2、CHO/TIE2、HAoSMC/PDGFR-β 和 MCF-7/FGFR 用 Regorafenib (10-3000 nM) 处理 1 h，使用 Western Blot 方法检测靶点蛋白表达水平。结果：Regorafenib 抑制 p-VEGFR2、p-TIE2、p-PDGFR-β 和 p-FGFR。[2]
体内活性	方法：为检测体内抗肿瘤活性，将 Regorafenib (3-100 mg/kg) 口服给药给携带肿瘤 Colo-205 或 MDA-MB-231 的 NCr nu/nu 小鼠，每天一次，持续九天。结果：Regorafenib 抑制肿瘤生长。Colo-205 模型中，Regorafenib 在 10 mg/kg 的剂量下，第 14 天的 TGI 达到 75%。MDA-MB-231 模型，Regorafenib 在低至 3 mg/kg 的剂量下是高效的，导致 81% 的显著TGI。[2] 方法：为检测体内抗肿瘤活性，将 Regorafenib (3-10 mg/kg) 口服给药给携带肿瘤 HT-29 或 MDA-MB-231 的 NMRI nu/nu 小鼠，每天一次，持续二十七天。结果：Regorafenib 剂量依赖性抑制 HT-29 和 MDA-MB-231 肿瘤生长。[3]
激酶实验	In vitro assays using recombinant VEGFR2 (murine aa785–aa1367), VEGFR3 (murine aa818–aa1363), PDGFR-b (aa561–aa1106), RAF-1 (aa305–aa648) and BRAFV600E (aa409–aa765) kinase domains were performed as previously described. Initial in vitro kinase inhibition profiling was performed at a fixed 1 μM compound concentration under Millipore standard conditions [10 μM adenosine-50'- triphosphate (ATP) concentration]. Inhibitory concentration of 50% (IC50) values were determined from selected responding kinases, e.g., VEGFR1 and RET. TIE2 kinase inhibition was measured with a homogeneous time-resolved fluorescence (HTRF) assay using a recombinant fusion protein of glutathione-S-transferase, the intracellular domain of TIE2 and the peptide biotin-Ahx-EPKDDAYPLYSDFG as substrate.
细胞实验	Each cell line was seeded at 0.3×10^5 cells/2ml of DMEM containing 10% FBS in 35 mm tissue culture dishes. The cells were incubated for 24 h to allow attachment, and then the medium was replaced by fresh culture medium containing Regorafenib at increasing concentrations (1 μM, 2.5 μM, 5 μM, 7.5 μM and 10 μM). In these experimental conditions, the cells were allowed to grow for 72 or 96 h. Time-course experiments on Hep3B cells were performed with 7.5 μM of Regorafenib at short (15, 60, 180 min.), middle (24, 48, 72 and 96 h) or long times (up to seven days). When the cells were treated for long times the drug was replaced with a fresh one. Each experiment included a control with the equivalent concentration of DMSO (solvent control) as the one used for adding Regorafenib. Each experiment was performed in triplicate and repeated 3 times. Subsequent analyses were performed at specific Regorafenib concentrations and incubation times [2].
动物实验	Female athymic NCr nu/nu mice, kept in accordance with Federal guidelines, were subcutaneously inoculated with 5×10^6 Colo-205 or MDAMB-231 cells or implanted with 1 mm^3 786-O tumor fragments. When tumors reached a volume of ~100 mm^3, regorafenib or vehicle control was administered orally qd×21 in the 786-O model, and qd×9 in the Colo-205 and MDA-MB231 models, respectively, at doses of 100, 30, 10, and 3 mg/kg. Paclitaxel was administered intravenously at 10 mg/kg in ethanol/Cremophor ELV/saline (12.5%/12.5%/75%) every 2 days×5. Tumor size (volume) was estimated twice weekly (l×w^2)/2, and the percentage of tumor growth inhibition (TGI) was obtained from terminal tumor weights (1-T/C100). Mice were weighed every other day starting from the first day of treatment. The general health status of the mice was monitored daily [1].

别名	BAY 73-4506, 瑞戈非尼, Fluoro-Sorafenib, 瑞格非尼
分子量	482.82
分子式	C21H15ClF4N4O3
CAS No.	755037-03-7

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 90 mg/mL (186.4 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0712 mL	10.3558 mL	20.7117 mL	51.7791 mL
	5 mM	0.4142 mL	2.0712 mL	4.1423 mL	10.3558 mL
	10 mM	0.2071 mL	1.0356 mL	2.0712 mL	5.1779 mL
	20 mM	0.1036 mL	0.5178 mL	1.0356 mL	2.589 mL
	50 mM	0.0414 mL	0.2071 mL	0.4142 mL	1.0356 mL
	100 mM	0.0207 mL	0.1036 mL	0.2071 mL	0.5178 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Carr BI, et al. Fluoro-Sorafenib (Regorafenib) effects on hepatoma cells: growth inhibition, quiescence, and recovery. J Cell Physiol. 2013 Feb;228(2):292-7. 2. Wilhelm SM, et al. 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 Jul 1;129(1):245-55. 3. Zopf D, et al. Pharmacologic activity and pharmacokinetics of metabolites of regorafenib in preclinical models. Cancer Med. 2016 Nov;5(11):3176-3185. 4. Duan F, Huang R, Zhang F, et al. Biphasic modulation of insulin signaling enables highly efficient hematopoietic differentiation from human pluripotent stem cells[J]. Stem cell research & therapy. 2018 Jul 27;9(1):205.

文献引用

1. Huang M, Chen M, Qi M, et al. Perivascular cell‐derived extracellular vesicles stimulate colorectal cancer revascularization after withdrawal of antiangiogenic drugs. Journal of Extracellular Vesicles. 2021, 10(7): e12096. 2. Duan F, Huang R, Zhang F, et al. Biphasic modulation of insulin signaling enables highly efficient hematopoietic differentiation from human pluripotent stem cells. Stem Cell Research & Therapy. 2018 Jul 27;9(1):205 3. Wang C, Huang M, Lin Y, et al.ENO2-derived phosphoenolpyruvate functions as an endogenous inhibitor of HDAC1 and confers resistance to antiangiogenic therapy.Nature Metabolism.2023: 1-22.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Regorafenib 755037-03-7 Angiogenesis Apoptosis Autophagy MAPK Tyrosine Kinase/Adaptors Raf VEGFR c-RET PDGFR c-Kit HUVECs Vascular endothelial growth factor receptor Colo-205 FGFR SCFR RET NIH-3T3 antiangiogenic Antitumorigenic inhibit HAoSMCs BAY 73-4506 Platelet-derived growth factor receptor tumor Inhibitor Hep3B cell 瑞戈非尼 CD117 Fluoro-Sorafenib Raf kinases Fibroblast growth factor receptor 瑞格非尼 786-O inhibitor

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Regorafenib

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

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剂量换算

体内实验配液计算器

技术支持

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