EZM0414 | SETD2 | Probechem Biochemicals

Chemical Structure : EZM0414

CAS No.: 2411748-50-8

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EZM0414 (EZM 0414)

货号: PC-73322Not For Human Use, Lab Use Only.

EZM 0414 is a potent, selective and orally bioavailable inhibitor of histone methyltransferase SETD2 with biochemical IC50 of 18 nM, >10,000-fold selectivity over other HMTases.

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5 mg	￥2980	In stock
10 mg	￥4880	In stock
25 mg	￥7980	In stock
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生物&药学活性

EZM 0414 is a potent, selective and orally bioavailable inhibitor of histone methyltransferase SETD2 with biochemical IC50 of 18 nM, >10,000-fold selectivity over other HMTases.
EZM 0414 reduced global tri-methylation of H3K36 (H3K36me3, IC50=34 nM) in t(4;14) bearing MM cell lines, with no effect on global di-methyl H3K36 (H3K36me2) levels.
EZM 0414 demonstrated broad anti-proliferative effects of EZM0414 in a panel of MM cell lines with enhanced sensitivity in cells harboring the (4;14) chromosomal translocation, as well as in a panel of DLBCL cell lines representing both GCB and ABC subtypes.
EZM 0414 suppressed tumor volume and inhibited H3K36me3 level in human MM and DLBCL xenograft models.

物理化学性质&存储条件

分子量	400.498
分子式	C22H29FN4O2
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	N-((1R,3S)-3-(4-acetylpiperazin-1-yl)cyclohexyl)-7-fluoro-4-methyl-1H-indole-2-carboxamide

参考文献

1. Alford JS, et al. ACS Med Chem Lett. 2022 Jun 7;13(7):1137-1143.

EZM0414 (EZM 0414)

生物&药学活性

物理化学性质&存储条件

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EZM0414 (EZM 0414)

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