AZ304,942507-42-8

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AZ304

CAS No. : 942507-42-8

MCE 国际站：AZ304

产品活性：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。

研究领域：MAPK/ERK Pathway  |  Autophagy

作用靶点：Raf  |  Autophagy

In Vitro: 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 combination with C225.

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