产品
编 号：F190443
分子式：C35H51N5O4
分子量：605.81
分子式：C35H51N5O4
分子量：605.81
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
询价
询价
10mg
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询价
50mg
询价
询价
100mg
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询价
结构图
CAS No: 1598383-40-4
产品详情
生物活性：
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. EPZ011989 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
体内研究：
EPZ011989 (oral; 30-1000 mg/kg; single or bid; for 7 days or 21 days) 可引起强大的甲基标记抑制和抗肿瘤活性。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.
Animal Model:Rat
Dosage:30, 100, and 300 mg/kg
Administration:Oral, single
Result:dose (mg/kg) route t1/2 (h) tmax (h)Cmax (ng/mL) AUCinf (h*ng/mL) time above LCC (h)
30p.o.4.722409704
100p.o.3.92.7160056008
300p.o.3.72.729001000010
体外研究：
EPZ011989 抑制突变型和野生型 EZH2，Ki 值为 EPZ011989 相关抗体:Cell Proliferation AssayCell 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.
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. EPZ011989 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
体内研究：
EPZ011989 (oral; 30-1000 mg/kg; single or bid; for 7 days or 21 days) 可引起强大的甲基标记抑制和抗肿瘤活性。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.
Animal Model:Rat
Dosage:30, 100, and 300 mg/kg
Administration:Oral, single
Result:dose (mg/kg) route t1/2 (h) tmax (h)Cmax (ng/mL) AUCinf (h*ng/mL) time above LCC (h)
30p.o.4.722409704
100p.o.3.92.7160056008
300p.o.3.72.729001000010
体外研究：
EPZ011989 抑制突变型和野生型 EZH2，Ki 值为 EPZ011989 相关抗体:Cell Proliferation AssayCell 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.
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