AZ304 是一种 BRAF 双重抑制剂，有效抑制野生型 BRAF，突变型 BRAF (V600E) 和野生型 CRAF，IC₅₀ 值分别为 79 nM，38 nM 和 68 nM。AZ304 对其他激酶有显著抑制作用，如 p38 (IC₅₀，6 nM)，CSF1R (IC₅₀，35 nM)。具有抗肿瘤活性。

AZ304 is an ATP-competitive dual BRAF kinase inhibitor, potently inhibits wild type BRAF, V600E mutant BRAF and wild type CRAF, with IC 50 s of 79 nM, 38 nM and 68 nM, respectively. AZ304 also has significant effect on other kinases, such as p38 (IC 50 , 6 nM), CSF1R (IC 50 , 35 nM). Anti-tumor activity.

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BRaf 38 nM (IC50) BRAF 79 nM (IC50

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.AZ304 also potently inhibits p-p38 in both BRAF genetic statuses cell lines.
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.
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 c

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[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.

In Vitro: DMSO : 125 mg/mL (276.84 mM; Need ultrasonic)配制储备液