貨號	規格	價格	上海	北京	武漢	南京
S81367-5mg	99.7%	￥540.00 S81367-5mg ￥540.00 現貨	8 8	-	-	-
S81367-10mg	99.7%	￥810.00 S81367-10mg ￥810.00 現貨	5 5	-	-	-
S81367-50mg	99.7%	￥2550.00 S81367-50mg ￥2550.00 現貨	2 2	-	-	-

產品介紹

EPZ011989 is a potent and orally active Zeste Homolog 2 (EZH2) inhibitor with metabolic stability. EPZ011989 has inhibitory inhibition for EZH2 with a Ki value of <3 nM. EPZ011989 shows robust methyl mark inhibition and anti-tumor activity. EPZ011989 can be used for the research of various cancers

產品描述：

靶點：

Ki: <3 nM (EZH2); IC50: 94 nM (H3K27 methylation inhibition);HistoneMethyltransferase

體外研究：

EPZ011989 inhibits mutant and wild-type EZH2 with an Ki value of <3 nM. EPZ011989 reduces cellular H3K27 methylation with an IC50 value of 94 nM. EPZ011989 (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.

體內研究：

EPZ011989 (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.

參考文獻：

1. Campbell JE, et al. EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity. ACS Med Chem Lett. 2015 Mar 4;6(5):491-495.

溶解性：

soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	1.651 ml	8.253 ml	16.507 ml
5 mM	0.33 ml	1.651 ml	3.301 ml
10 mM	0.165 ml	0.825 ml	1.651 ml
50 mM	0.033 ml	0.165 ml	0.33 ml

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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