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AZ304
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
AZ304图片
CAS NO:942507-42-8
包装与价格：
包装价格(元)
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AZ304 是一种 ATP 竞争性双 BRAF 激酶抑制剂，有效抑制野生型 BRAF、V600E 突变型 BRAF 和野生型 CRAF，IC50 分别为 79 nM、38 nM 和 68 nM。 AZ304 对其他激酶也有显着影响，例如 p38 (IC50, 6 nM)、CSF1R (IC50, 35 nM)。抗肿瘤活性。
Cas No.942507-42-8
Canonical SMILESO=C(NC1=CC=C(C)C(NC2=C3C=CC(OC)=CC3=NC=N2)=C1)C4=CC=CC(C(C)(C#N)C)=C4
分子式C27H25N5O2
分子量451.52
溶解度Soluble in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

AZ304 is a dual inhibitor of BRAF that effectively inhibits wild-type BRAF, mutant BRAF (V600E) and wild-type CRAF with IC50 values of 79 nM, 38 nM and 68 nM, respectively.AZ304 significantly inhibits other kinases, such as p38 (IC50, 6 nM), CSF1R (IC50, 35 nM).Has anti-tumor activity.

AZ304 (1 nM-100 μM) potently reduces ERK phosphorylation (p-ERK), with a mean EC50 of 65 nM in the V600E mutant BRAF containing melanoma cell line A375, and EC50s of 52 nM, 60 nM in the wild type BRAF melanoma cell line SK-MEL-31 with and without EGF[1]. AZ304 also potently inhibits p-p38 in both BRAF genetic statuses cell lines[1].
AZ304 (0, 0.1, 1, 10, 100 μM, 48 and 72 hours) dose-dependently inhibits the growth of RKO, HT-29, DiFi, and Caco-2, with GI50s of 4.539 μM, 3.896 μM, 4.987 μM, 1.763 μM (48 hours) and 0.5032 μM, 0.3887 μM, 0.6354 μM, 0.3772 μM (72 hours), respectively[1].
AZ304 (2 μM, 36 and 48 hours) decreases BRAF, p-ERK, p-AKT and p-mTOR levels, increases p-EGFR in both BRAF V600E mutant and BRAF wild type cells. AZ304 down-regulates p-EGFR, inhibits p-ERK, more potently suppresses BRAF, ERK, AKT and mTOR signalling pathways in combination with C225[1].

Reference:

[1]. Ma R, et al. AZ304, a novel dual BRAF inhibitor, exerts anti-tumour effects in colorectal cancer independently of BRAF genetic status. Br J Cancer. 2018 May;118(11):1453-1463.


 
 
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