EPZ-011989

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

EPZ-011989 (EPZ011989) 是一种有效的、选择性的、口服生物可利用的 EZH2 抑制剂，Ki 小于 3 nM。

EPZ-011989 (EPZ011989)?is a potent, selective, orally bioavailable inhibitor of EZH2 with Ki of < 3 nM; equipotently inhibits mutant and wild-type EZH2, displays >15-fold selectivity over EZH1 and >3000-fold selectivity over other HMTs; demonstrates significant tumor growth inhibition in a mouse xenograft model of human B cell lymphoma.Blood Cancer Preclinical.

Cell Proliferation Assay Cell Line:WSU-DLCL2 cells Concentration:0-10 μM Incubation Time:11 days Result:Demonstrated an average lowest cytotoxic concentration (LCC) in WSU-DLCL2 cells of 208 nM.

Animal Model:SCID mice Dosage:125, 250, 500, and 1000 mg/kg Administration:Oral; single, twice-daily (BID)for 7 days or twice-daily (BID)for 21 days Result:Provided coverage over the LCC for 24 h (1000 mg/kg ), while the 250 and 500 mg/kg doses provided coverage over this value for approximately 8 h.Observed complete ablation of the methyl mark by the end of day 7.

EPZ011989

Chromatin/Epigenetic

HMTase

EZH2

Cancer

Blood cancer

1598383-40-4

605.8105

C35H51N5O4

>98% (HPLC)

DMSO: ≥ 33 mg/mL

O=C(NCC1=C(C)C=C(C)NC1=O)C2=CC(C#CCN3CCOCC3)=CC(N(CC)[C@H]4CC[C@H](N(CCOC)C)CC4)=C2C

Benzamide, N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-3-[ethyl[trans-4-[(2-methoxyethyl)methylamino]cyclohexyl]amino]-2-methyl-5-[3-(4-morpholinyl)-1-propyn-1-yl]-

(-20℃)

With Ice Pack

≥ 2 years