产品
编 号：F190444
分子式：C37H52F3N5O6
分子量：719.83
分子式：C37H52F3N5O6
分子量：719.83
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CAS No: 1598383-41-5
产品详情
生物活性：
EPZ-011989 trifluoroacetate is a potent and orally active Zeste Homolog 2 (EZH2) inhibitor with metabolic stability. EPZ-011989 trifluoroacetate has inhibitory inhibition for EZH2 with a Ki value of <3 nM. EPZ-011989 trifluoroacetate shows robust methyl mark inhibition and anti-tumor activity. EPZ-011989 trifluoroacetate can be used for the research of various cancers. EPZ011989 (trifluoroacetate) 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：
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.
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：
EPZ-011989 trifluoroacetate inhibits mutant and wild-type EZH2 with an Ki value of EPZ011989 trifluoroacetate 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.
EPZ-011989 trifluoroacetate is a potent and orally active Zeste Homolog 2 (EZH2) inhibitor with metabolic stability. EPZ-011989 trifluoroacetate has inhibitory inhibition for EZH2 with a Ki value of <3 nM. EPZ-011989 trifluoroacetate shows robust methyl mark inhibition and anti-tumor activity. EPZ-011989 trifluoroacetate can be used for the research of various cancers. EPZ011989 (trifluoroacetate) 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：
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.
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：
EPZ-011989 trifluoroacetate inhibits mutant and wild-type EZH2 with an Ki value of EPZ011989 trifluoroacetate 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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