Regorafenib Hydrochloride | BAY 73-4506 hydrochloride;Stivarga | VEGFR

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Regorafenib HCl/瑞戈非尼盐酸盐 {[allProObj[0].p_purity_real_show]}

货号：A481225 同义名： BAY 73-4506 hydrochloride; Stivarga

Regorafenib HCl can inhibit many kinases including RET (IC50 = 1.5 nM), Raf-1 (IC50 = 2.5 nM), VEGFR2 (IC50 = 4.2 nM), VEGFR1 (IC50 = 13 nM), PDGFRβ (IC50 = 22 nM) and VEGFR3 (IC50 = 46 nM).

Regorafenib HCl/瑞戈非尼盐酸盐化学结构
CAS号：835621-07-3

Regorafenib HCl/瑞戈非尼盐酸盐 3D分子结构
CAS号：835621-07-3

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Regorafenib HCl/瑞戈非尼盐酸盐纯度/质量文件产品仅供科研

货号：A481225 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: 更多 >

VEGFR 亚型比较

产品名称	VEGFR1 ↓ ↑	VEGFR2 ↓ ↑	VEGFR3 ↓ ↑	其他靶点	纯度
Motesanib Diphosphate	++++ VEGFR1, IC50: 2 nM	++++ VEGFR2/Flk1, IC50: 3 nM VEGFR2, IC50: 3 nM	+++ VEGFR3, IC50: 6 nM	PDGFR,RET	99% (HPLC)
Tivozanib	++ VEGFR1, IC50: 30 nM	+++ VEGFR2, IC50: 6.5 nM	++ VEGFR3, IC50: 15 nM		99%+
Brivanib	+ VEGFR1, IC50: 380 nM	++ VEGFR2, IC50: 25 nM Flk1, IC50: 25 nM			99%+
Regorafenib	+++ VEGFR1, IC50: 13 nM	+++ VEGFR2, IC50: 4.2 nM	+ VEGFR3, IC50: 46 nM	RET	98%
Pazopanib	+++ VEGFR1, IC50: 10 nM	++ VEGFR2, IC50: 30 nM	+ VEGFR3, IC50: 47 nM	PDGFR,FGFR,c-Kit	99%
Sitravatinib	+++ VEGFR1 (FLT1), IC50: 6 nM	+++ VEGFR2 (KDR), IC50: 5 nM	++++ VEGFR3 (FLT4), IC50: 2 nM		99%+
Foretinib	+++ VEGFR1/FLT1, IC50: 6.8 nM	++++ KDR, IC50: 0.86 nM	++++ VEGFR3/FLT4, IC50: 2.8 nM	Tie-2	99%+
MGCD-265 analog	++++ VEGFR1, IC50: 3 nM	++++ VEGFR2, IC50: 3 nM	++++ VEGFR3, IC50: 4 nM	Tie-2	99%+
Lactate	+++ VEGFR1/FLT1, IC50: 10 nM	+++ VEGFR2/Flk1, IC50: 13 nM	+++ VEGFR3/FLT4, IC50: 8 nM	FLT3,c-Kit	85%
AEE788	+ FLT1, IC50: 59 nM	+ KDR, IC50: 77 nM		EGFR	98+%
Linifanib	++++ VEGFR1/FLT1, IC50: 3 nM	++++ VEGFR2/KDR, IC50: 4 nM	+ VEGFR3/FLT4, IC50: 190 nM	FLT3	99%+
Vatalanib 2HCl	+ VEGFR1/FLT1, IC50: 77 nM	++ VEGFR2/Flk1, IC50: 270 nM VEGFR2/KDR, IC50: 37 nM	+ VEGFR3/FLT4, IC50: 660 nM	c-Fms,c-Kit	99%+
Axitinib	++++ VEGFR1/FLT1, IC50: 0.1 nM	++++ VEGFR2/Flk1, IC50: 0.18 nM VEGFR2/KDR, IC50: 0.2 nM			98%
Dovitinib	+++ VEGFR1/FLT1, IC50: 10 nM	+++ VEGFR2/Flk1, IC50: 13 nM	+++ VEGFR3/FLT4, IC50: 8 nM	FLT3,c-Kit	99%+
ZM 306416	+ VEGFR1, IC50: 0.33 μM			Src	99%+
KRN-633	+ VEGFR1, IC50: 170 nM	+ VEGFR2, IC50: 160 nM	+ VEGFR3, IC50: 125 nM	c-Kit,BTK	98%
OSI-930	+++ FLT1, IC50: 8 nM	+++ KDR, IC50: 9 nM			99%+
Lenvatinib	++ VEGFR1/FLT1, IC50: 22 nM	++++ VEGFR2/KDR, IC50: 4.0 nM	+++ VEGFR3/FLT4, IC50: 5.2 nM		98%
NVP-BAW2881	+ hVEGFR1, IC50: 820 nM	+++ mVEGF2, IC50: 165 nM hVEGFR2, IC50: 9 nM	+ hVEGFR3, IC50: 420 nM		99%
Cediranib	+++ VEGFR1/FLT1, IC50: 5 nM	++++ VEGFR2/KDR, IC50: 0.5 nM		c-Kit	99%+
Nintedanib	++ VEGFR1, IC50: 34 nM	+++ VEGFR2, IC50: 13 nM	+++ VEGFR3, IC50: 13 nM	FLT3	99+%
BMS-794833		++ VEGFR2, IC50: 15 nM			99%+
SKLB1002		++ VEGFR2, IC50: 32 nM			99%
Cabozantinib S-malate		++++ VEGFR2/KDR, IC50: 0.035 nM			99+%
Ki8751		++++ VEGFR2, IC50: 0.9 nM		c-Kit	99%
SU 5402		++ VEGFR2, IC50: 20 nM			98%
Rivoceranib Mesylate		++++ VEGFR2, IC50: 1 nM		RET	98+%
Ponatinib		++++ VEGFR2, IC50: 1.5 nM			98%
LY2874455		+++ VEGFR2, IC50: 7 nM			99%+
ZM323881 HCl		++++ VEGFR2, IC50: <2 nM			98%
AZD2932		+++ VEGFR-2, IC50: 8 nM		c-Kit	99%
Cabozantinib		++++ VEGFR2/KDR, IC50: 0.035 nM			98%
Sorafenib		++ VEGFR2/Flk1, IC50: 90 nM VEGFR2, IC50: 90 nM			99%
CYC-116		++ VEGFR2, Ki: 44 nM		FLT3	99%+
Golvatinib		++ VEGFR2, IC50: 16 nM			99%+
Sunitinib		+ VEGFR2 , IC50: 80 nM		FLT3	98%
RAF265		++ VEGFR2, EC50: 30 nM			99%+
PD173074					99%+
BFH772		++++ VEGFR2, IC50: 3 nM			98%
Semaxinib		+ VEGFR2/Flk1, IC50: 1.23 μM			98%
Vandetanib		++ VEGFR2, IC50: 40 nM	+ VEGFR3, IC50: 110 nM	EGFR	99%
SAR131675			++ VEGFR3, IC50: 23 nM		99%+
ENMD-2076		+ VEGFR2/KDR, IC50: 58.2 nM	++ VEGFR3/FLT4, IC50: 15.9 nM	FLT3,RET	98%
Telatinib		+++ VEGFR2, IC50: 6 nM	++++ VEGFR3, IC50: 4 nM	c-Kit	99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Regorafenib HCl/瑞戈非尼盐酸盐生物活性

描述	Regorafenib Hydrochloride (BAY 73-4506 hydrochloride) is a multi-target inhibitor of VEGFR1/2/3, PDGFRβ, Kit, RET, and Raf-1, with IC50 values of 13/4.2/46, 22, 7, 1.5, and 2.5 nM, respectively^[1].

Regorafenib HCl/瑞戈非尼盐酸盐动物研究

Animal study

Regorafenib effectively suppresses the growth of Colo-205 xenografts within the dosage range of 10-100 mg/kg, achieving a tumor growth inhibition (TGI) of 75% by day 14 at the 10 mg/kg dose. In the MDA-MB-231 model, regorafenib exhibits high efficacy even at a low dose of 3 mg/kg, leading to a notable TGI of 81%. This efficacy escalates to 93% at doses of 10 and 30 mg/kg, reaching tumor stasis^[1].

Regorafenib HCl/瑞戈非尼盐酸盐参考文献

[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.

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

Regorafenib HCl/瑞戈非尼盐酸盐实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.93mL

0.39mL

0.19mL

9.63mL

1.93mL

0.96mL

19.26mL

3.85mL

1.93mL

Regorafenib HCl/瑞戈非尼盐酸盐技术信息

CAS号	835621-07-3
分子式	C₂₁H₁₆Cl₂F₄N₄O₃
分子量	519.28
SMILES Code	O=C(NC)C1=NC=CC(OC2=CC=C(NC(NC3=CC=C(Cl)C(C(F)(F)F)=C3)=O)C(F)=C2)=C1.[H]Cl

别名	BAY 73-4506 hydrochloride; Stivarga
运输	蓝冰
InChI Key	ACSWJKPZXNIVMY-UHFFFAOYSA-N
Pubchem ID	66577009

存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,2-8°C

溶解方案

动物实验：配制的工作液建议现用现配，短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在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。

方案一

动物实验配方

IP 2% DMSO+2% Tween80+40% PEG300+water 5 mg/mL clear

PO 0.5% CMC-Na 53 mg/mL suspension

Regorafenib HCl/瑞戈非尼盐酸盐 {[allProObj[0].p_purity_real_show]}

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