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Regorafenib hydrochloride

酪氨酸激酶抑制剂，Regorafenib Hydrochloride 是一种多靶点抑制剂，靶作用于 VEGFR1/2/3，PDGFRβ，Kit，RET 和 Raf-1，IC50 值分别为 13/4.2/46，22，7，1.5 和 2.5 nM。

目录号: PC16046 纯度: ≥98%

CAS No. :835621-07-3

商品编号	规格	价格	会员价
PC16046-10mg	10mg	¥637.00	请登录
PC16046-50mg	50mg	¥980.00	请登录
PC16046-100mg	100mg	¥1568.00	请登录
PC16046-200mg	200mg	¥2450.00	请登录
PC16046-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥980.00	请登录

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中文名称	Regorafenib hydrochloride
中文别名	瑞戈非尼;REGORAFENIB 盐酸盐;盐酸盐瑞格菲尼;瑞戈菲尼;瑞格非尼盐酸盐;瑞戈非尼盐酸盐;盐酸瑞格非尼;瑞格菲尼盐酸盐;瑞戈非尼一水物;瑞格菲尼一水合物
英文名称	Regorafenib hydrochloride
英文别名	Regorafenib (Hydrochloride);BAY73-4506 hydrochloride;4-[4-[[[[4-Chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-2-pyridinecarboxamide hydrochloride;Regafenib HCL;Regafenib hydrochloride;2-Pyridinecarboxamide,4-[4-[[[[4-chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-, monohydrochloride;4-[4-({[4-Chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methyl-2-pyridinecarboxamide hydrochloride (1:1);4-(4-(3-(4-Chloro-3-(trifluoromethyl)phenyl)ureido)-3-fluorophenoxy)-N-methylpicolinamide hydr;2-Pyridinecarboxamide, 4-[4-[[[[4-chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluoro phenoxy]-N-methyl-, monoh;2-Pyridinecarboxamide, 4-[4-[[[[4-chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-flu...;4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide hydrochloride;Regorafenib Hydrochloride
Cas No.	835621-07-3
分子式	C₂₁H₁₅N₄O₃F₄Cl^.HCl
分子量	519.28
包装储存	Sealed and stored at 4℃，, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性

Regorafenib Hydrochloride (BAY 73-4506 hydrochloride) is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC₅₀s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.

性状

Solid

IC50 & Target[1][2]

VEGFR1

13 nM (IC₅₀)

VEGFR2

4.2 nM (IC₅₀)

VEGFR3

46 nM (IC₅₀)

PDGFRβ

22 nM (IC₅₀)

Braf

28 nM (IC₅₀)

BRaf

19 nM (IC₅₀)

Raf-1

2.5 nM (IC₅₀)

体外研究(In Vitro)

Regorafenib potently inhibits VEGFR2 autophosphorylation in NIH-3T3/VEGFR2 cells with an IC₅₀ of 3 nM. In HAoSMCs, regorafenib inhibits PDGFR-β autophosphorylation after stimulation with PDGF-BB, with an IC₅₀ of 90 nM. Regorafenib inhibits the proliferation of VEGF165-stimulated HUVECs, with an IC₅₀ of 3 nM. Regorafenib causes a concentration-dependent decrease in Hep3B cell growth, having an IC₅₀ of 5 μM. Regorafenib subsequently increases the levels of phospho-c-Jun, a JNK target, but not total c-Jun in Hep3B cells.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Regorafenib effectively inhibits growth of the Colo-205 xenografts in the dose range of 10-100 mg/kg reaching a TGI of 75% at day 14 at the 10 mg/kg dose. In the MDA-MB-231 model, regorafenib is highly efficacious at a dose as low as 3 mg/kg, resulting in a significant TGI of 81%, which increases to 93% at doses of 10 and 30 mg/kg, where tumor stasis is reached.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

Sealed and stored at 4℃，, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. 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, 129(1), 245-255. [Information]

[2]. Heng DY, et al. Targeted therapy for metastatic renal cell carcinoma: current treatment and future directions. Ther Adv Med Oncol, 2010, 2(1), 39-49. [Information]

[3]. Carr BI, et al. Fluoro-Sorafenib (Regorafenib) effects on hepatoma cells: growth inhibition, quiescence, and recovery. J Cell Physiol, 2013, 228(2), 292-297. [Information]

溶解度数据

体外研究:

DMSO : ≥ 5.6 mg/mL (10.78 mM)

H₂O : < 0.1 mg/mL (insoluble)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9257 mL	9.6287 mL	19.2574 mL
5 mM	0.3851 mL	1.9257 mL	3.8515 mL
10 mM	0.1926 mL	0.9629 mL	1.9257 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 50% PEG300 50% saline
Solubility: 2 mg/mL (3.85 mM); Suspended solution; Need ultrasonic

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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