CAS:755037-03-7Regorafenib

您的位置 : 首页 / Protein Tyrosine Kinase/RTK / c-RET / Regorafenib

Regorafenib 瑞格非尼 Cat No. FB02029Cas No. 755037-03-7

Synonyms: Fluoro-Sorafenib;BAY-734506

Regorafenib is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13/4.2/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively.

规格	价格	促销价格	库存

18817579266

立即询价

咨询

18817579266

立即询价

实验数据

储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0712 mL
- 10.3559 mL
- 20.7118 mL
- 5 mM
- 0.4142 mL
- 2.0712 mL
- 4.1424 mL
- 10 mM
- 0.2071 mL
- 1.0356 mL
- 2.0712 mL
计算器摩尔计算器总药量计算器工作液计算器

技术信息

CAS号

755037-03-7

储存条件

粉末: -20°C 3 年

液体: -80°C 12 月

分子式

C21H15ClF4N4O3

运输

蓝冰

分子量

482.82

别名

Fluoro-Sorafenib;BAY-734506

溶解度

DMSO	460.0 mg/mL (952.7 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+30% PEG300+water	2 mg/mL	clear
PO	0.5% CMC-Na	50 mg/mL	suspension

靶点数据

生物活性

靶点 c-Kit

IC50:7nM C-Raf

IC50:2.5nM c-RET

IC50:1.5nM PDGFRβ

IC50:22nM VEGFR1

IC50:13nM 更多
描述Regorafenib strongly prevents VEGFR2 autophosphorylation in NIH-3T3/VEGFR2 cells with IC50 of 3 nM. In HAoSMCs, regorafenib suppress PDGFR-β autophosphorylation after stimulation with PDGF-BB, with an IC50 of 90 nM. Regorafenib also inhibits FGFR signaling in MCF-7 breast cancer (BC) cells stimulated with FGF10. Regorafenib very potently inhibited the mutant receptors KIT and RET, with IC50 of approximately 20 nM and 10 nM, respectively. Regorafenib inhibits the proliferation of VEGF-stimulated HUVECs, with an IC50 of approximately 3 nM. Regorafenib prevents the proliferation of FGF2-stimulated HUVECs and of PDGF-BB-stimulated HAoSMCs with IC50 of 127 nM and 146 nM, respectively. Regorafenib targets both tumor cell proliferation and tumor vasculature through inhibition of receptors of tyrosine kinases (VEGFR, KIT, RET, FGFR, and PDGFR) and serine/threonine kinases (Raf and p38MAPK). Regorafenib suppresses growth of human Hep3B, PLC/PRF/5 and HepG2 cells in a concentration- and time-dependent manner.

靶点	Description	IC50
c-Kit		IC50:7nM
C-Raf		IC50:2.5nM
c-RET		IC50:1.5nM
PDGFRβ		IC50:22nM
VEGFR1		IC50:13nM
VEGFR2		IC50:4.2nM
VEGFR3		IC50:46nM