Vemurafenib

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

Vemurafenib (PLX-4032;RG7204;RO5185426) 是一种有效的选择性 B-RAF V600E 抑制剂，IC50 为 30 nM。

Vemurafenib (PLX-4032;RG7204;RO5185426) is a potent, selective B-RAF V600E inhibitor with IC50 of 30 nM, displays similar potency for c-RAF-1 (IC50=48 nM), and has selectivity against many other kinases, including wild type B-RAF (IC50=100nM); potently inhibits proliferation of a panel of tumor cell lines, selectively blocks the RAF/MEK/ERK pathway in BRAF mutant cells; causes tumor regressions and improves animal survival in tumor xenograft models of BRAF(V600E)-expressing melanoma.Skin Cancer Approved(In Vitro):Vemurafenib (PLX4032) selectively blocks the RAF/MEK/ERK pathway in BRAF mutant cells. RG7204 is a potent inhibitor of proliferation in those expressing RAFV600E but not BRAFWT in 17 melanoma cell lines. Vemurafenib (RG7204) induces MEK and ERK phosphorylation at high concentrations in CHL-1 cells. Ectopic expression of EGFR in melanoma cells is sufficient to cause resistance to PLX4032.(In Vivo):Vemurafenib (PLX4032, 20, 25, 75 mg/kg, p.o.) causes dose-dependent inhibition of tumor growth, with higher exposures resulting in tumor regression of BRAF mutant xenografts. RG7204 (12.5, 25, and 75 mg/kg, p.o.) significantly inhibits tumor growth and induced tumor regression in mice bearing LOX tumor xenografts.

Vemurafenib (PLX4032) selectively blocks the RAF/MEK/ERK pathway in BRAF mutant cells. RG7204 is a potent inhibitor of proliferation in those expressing RAFV600E but not BRAFWT in 17 melanoma cell lines. Vemurafenib (RG7204) induces MEK and ERK phosphorylation at high concentrations in CHL-1 cells. Ectopic expression of EGFR in melanoma cells is sufficient to cause resistance to PLX4032.

Vemurafenib (PLX4032, 20, 25, 75 mg/kg, p.o.) causes dose-dependent inhibition of tumor growth, with higher exposures resulting in tumor regression of BRAF mutant xenografts. RG7204 (12.5, 25, and 75 mg/kg, p.o.) significantly inhibits tumor growth and induced tumor regression in mice bearing LOX tumor xenografts.

PLX-4032 | RG7204 | RO5185426

MAPK/ERK Signaling

Raf

ACK1|BLK|B-Raf|B-Raf(V600E)|BRK|C-Raf|CSK|FGR|FRK(PTK5)|Lck|LynB|MAP4K5(KHS1)|MNK2|NEK11|Src|SRMS|WNK3|Yes1|c-Raf-1

Cancer

Skin Cancer

918504-65-1

489.9221

C23H18ClF2N3O3S

>98% (HPLC)

DMSO: 6.2 mg/mL

CCCS(=O)(NC1=CC=C(F)C(C(C2=CNC3=NC=C(C4=CC=C(Cl)C=C4)C=C32)=O)=C1F)=O

1-Propanesulfonamide, N-[3-[[5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]carbonyl]-2,4-difluorophenyl]-

(-20℃)

With Ice Pack

≥ 2 years