Sorafenib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的口服 Raf 抑制剂，对 Raf-1、wt Braf 和 BRaf V599E 的 IC50 分别为 6、22 和 38 nM。

A potent, orally available Raf inhibitor with IC50 of 6, 22, and 38 nM for Raf-1, wt Braf, and BRaf V599E, respectively; Also demonstrates potent inhibition of certain proangiogenic RTKs, including VEGFR-2, PDGFR-β, VEGFR-3, Flt-3, c-Kit (IC50<100 nM); Exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis.Kidney Cancer Approved(In Vitro):Sorafenib (BAY 43-9006) also inhibits BRAFwt (IC50=22 nM), BRAFV599E (IC50=38 nM), VEGFR-2 (IC50=90 nM), VEGFR-3 (IC50=20 nM), PDGFR-β (IC50=57 nM), c-KIT (IC50=68 nM), and Flt3 (IC50=58 nM) in biochemical assays. In MDA-MB-231 breast cancer cells, Sorafenib completely blocks activation of the MAPK pathway. Cells are preincubated with Sorafenib (0.01 to 3 μM), and dose-dependent inhibition of basal MEK 1/2 and ERK 1/2 phosphorylation (IC50, 40 and 100 nM, respectively). (In Vivo):Sorafenib demonstrates broad oral antitumor efficacy in panel of human tumor xenograft models. Sorafenib is given orally at 7.5 to 60 mg/kg. There is no lethality and no increase in weight loss in any treated group relative to the corresponding control group. Daily oral administration of Sorafenib (30 to 60 mg/kg) produces complete tumor stasis during treatment in five of the six models. The survival rate is 73.3 % in Diethyl nitrosamine (DENA) group and 83.3 % in Sorafenib group compared to 100 % in the normal control group. DENA group shows a significant increase in liver index (1.51-fold increase, p<0.05) compared to normal control group, while treatment with Sorafenib shows significant decrease (p<0.05) in liver index when compared to DENA group. The liver index in Sorafenib group significantly decreases to lower than its value in the normal control.

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Bay 43-9006 | Bay 43-9006

MAPK/ERK Signaling

Raf

B-Raf|B-Raf(V599E)|Raf-1|VEGFR2/Flk1|VEGFR3

Cancer

Kidney Cancer

284461-73-0

464.825

C21H16ClF3N4O3

>98% (HPLC)

DMSO: ≥ 45 mg/mL

CNC(=O)C1=NC=CC(OC2=CC=C(NC(=O)NC3=CC(=C(Cl)C=C3)C(F)(F)F)C=C2)=C1

2-Pyridinecarboxamide, 4-[4-[[[[4-chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]phenoxy]-N-methyl-

(-20℃)

With Ice Pack

≥ 2 years