EPZ-011989 trifluoroacetate

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

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。

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.

EPZ-011989 trifluoroacetate inhibits mutant and wild-type EZH2 with an Ki value of <3 nM.EPZ-011989 trifluoroacetate reduces cellular H3K27 methylation with an IC50 value of 94 nM.EPZ-011989 trifluoroacetate (0-10 μM; 11 days) has anti-proliferation effect in WSU-DLCL2 cells. 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.

EPZ-011989 trifluoroacetate (oral; 30-1000 mg/kg; single or bid; for 7 days or 21 days) can elicit robust methyl mark inhibition and antitumor activity. 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. Showed robust tumor growth inhibition, methyl mark reduction and extended total and free plasma exposure time.

EPZ011989 trifluoroacetate

Chromatin/Epigenetic

HMTase

HMTase

Cancer

Blood cancer

1598383-41-5

719.8339

C37H52F3N5O6

>98% (HPLC)

DMSO: ≥ 34 mg/mL

COCCN([C@@H]1CC[C@@H](N(C2=CC(C#CCN3CCOCC3)=CC(C(NCC4=C(C)C=C(C)NC4=O)=O)=C2C)CC)CC1)C.OC(C(F)(F)F)=O.OC(C(F)(F)F)=O

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]-, 2,2,2-trifluoroacetate (1:x)

(-20℃)

With Ice Pack

≥ 2 years