Belvarafenib

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

Belvarafenib (HM95573、GDC5573) 是一种新型有效的选择性 RAF 抑制剂。

Belvarafenib (HM95573, GDC5573) is a novel potent, selective RAF inhibitor with IC50 of 41 nM, 7 nM and 2 nM for?BRAF WT, BRAF V600E and CRAF, respectively;?inhibits cell proliferation of A375 (BRAF V600E) and SK-MEL-30 (NRAS Q61K) with IC50 of 57 and 24 nM, also inhibits the phosphorylations of MEK and ERK downstream kinases in mutant BRAF and mutant NRAS melanoma cells;?shows the excellent antitumor activity in mouse models xenografted with both of BRAF mutation cell lines (e.g. A375 and SK-MEL-28) and NRAS mutation cell lines.(In Vitro):Belvarafenib (Example 116) is a potent and pan RAF inhibitor with antineoplastic activity. The IC50 values of Belvarafenib are 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv600E and C-RAF respectively. It also shows high inhibitory activity for FMS, DDR1 and DDR2 kinases, with IC50s of 10 nM, 23 nM and 44 nM, respectively.

Belvarafenib (Example 116) is a potent and pan RAF inhibitor with antineoplastic activity. The IC50 values of Belvarafenib are 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv600E and C-RAF respectively. It also shows high inhibitory activity for FMS, DDR1 and DDR2 kinases, with IC50s of 10 nM, 23 nM and 44 nM, respectively.

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HM95573 | GDC5573

MAPK/ERK Signaling

Raf

Raf

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1446113-23-0

478.93

C23H16ClFN6OS

>98% (HPLC)

In Vitro:?DMSO : 12.5 mg/mL (26.10 mM)

FC1=C(Cl)C=CC=C1NC2=NC=CC3C(NC(C4=CSC5=C4N=CN=C5N)=O)=CC(C)=CC23

4-amino-N-[1-(3-chloro-2-fluoroanilino)-6-methylisoquinolin-5-yl]thieno[3,2-d]pyrimidine-7-carboxamide

(-20℃)

With Ice Pack

≥ 2 years