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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Raf-AZ304
AZ304

Chemical Structure : AZ304

CAS No.: 942507-42-8

AZ304 (AZ 304;AZ-304)

货号: PC-63581Not For Human Use, Lab Use Only.

AZ304 is a novel potent, dual BRAF inhibitor targeting the kinase domains of wild type BRAF, V600E mutant BRAF and wild type CRAF with IC50 of 79 nM, 38 nM and 68 nM, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

AZ304 is a potent, dual BRAF inhibitor targeting the kinase domains of wild type BRAF, V600E mutant BRAF and wild type CRAF with IC50 of 79 nM, 38 nM and 68 nM, respectively.
AZ304 also potentlt inhibits p38 and CSF1R with IC50 of 6 and 35 nM, has no activity for MAP3K7, CSK, IGF1R, EGFR, FGFR, CDK2, CDK4, JAK2, SRC (IC50>5 uM).
AZ304 potently reduces p-ERK with mean EC50 of 65 nM in the V600E mutant BRAF containing melanoma cell line A375, EC50 of 60 nM in wild type BRAF melanoma cell line SK-MEL-31.
AZ304 inhibits cell proliferation in mutant BRAF, wt BRAF/RAS and mutant RAS with IC50 of 0.08-7.72 uM, 0.43-11.7 uM 0.9-16.66 uM, respectively.
Cetuximab enhances the potency of AZ304 independently of BRAF mutational status in vivo.

物理化学性质&存储条件

分子量 451.53
分子式 C27H25N5O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-(2-cyanopropan-2-yl)-N-(3-((7-methoxyquinazolin-4-yl)amino)-4-methylphenyl)benzamide

参考文献

1. Ma R, et al. Br J Cancer. 2018 May 14. doi: 10.1038/s41416-018-0086-x.

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