产品说明书

AZ304

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Chemical Structure| 942507-42-8 同义名 : -
CAS号 : 942507-42-8
货号 : A802126
分子式 : C27H25N5O2
纯度 : 99%+
分子量 : 451.52
MDL号 : MFCD31812677
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(265.77 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 AZ304 is a dual BRAF inhibitor, with IC50 values of 38, 79, 68, 6 and 35nM for BRAFV600E, BRAF, CRAF, p38 and CSF1R, respectively, exerting potent inhibitory effects on both wild type and V600E mutant forms of the serine/threonine-protein kinase BRAF. AZ304 at concentration<1μM effectively inhibited a panel of human cancer cell lines with different BRAF and RAS genetic statuses, by suppressing ERK phosphorylation. The anti-proliferative activity of AZ304 cannot be retained by EGF in CRC cell lines with different BRAF mutation status. Oral gavage with 10mg/kg AZ304, twice daily, for 10 days, exhibited anti-tumour activity in RKO and Caco-2 xenograft model. And combination of Cetuximab with AZ304 could enhance this anti-tumour activity[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.21mL

0.44mL

0.22mL

11.07mL

2.21mL

1.11mL

22.15mL

4.43mL

2.21mL
参考文献

[1]Ma R, Xu L, 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.

[2]Ma R, Xu L, Qu X, Che X, Zhang Y, Fan Y, Li C, Guo T, Hou K, Hu X, Drew L, Shen M, Cheung T, Liu Y. 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. doi: 10.1038/s41416-018-0086-x. Epub 2018 May 14. PMID: 29755114; PMCID: PMC5988692.