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Chemical Structure : EZM0414
CAS No.: 2411748-50-8
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $298 | In stock | |
| 10 mg | $488 | In stock | |
| 25 mg | $798 | In stock | |
| 100 mg | Get quote |
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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.
| M.Wt | 400.498 | |
| Formula | C22H29FN4O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
N-((1R,3S)-3-(4-acetylpiperazin-1-yl)cyclohexyl)-7-fluoro-4-methyl-1H-indole-2-carboxamide |
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1. Alford JS, et al. ACS Med Chem Lett. 2022 Jun 7;13(7):1137-1143.
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