Quisinostat

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

Quisinostat (JNJ-26481585) 是一种新型第二代 HDAC 抑制剂，对 HDAC1 具有最高效力，IC50 为 0.11 nM，对 HDAC 2、4、10 和 11 具有中等效力。

Quisinostat (JNJ-26481585) is a novel second-generation HDAC inhibitor with highest potency for HDAC1 with IC50 of 0.11 nM, modest potent to HDACs 2, 4, 10, and 11; greater than 30-fold selectivity against HDACs 3, 5, 8, and 9 and lowest potency to HDACs 6 and 7. Phase 2.(In Vitro):Quisinostat inhibits HDAC isozymes in vitro.Quisinostat (30-1000 nM; 24 hours) is a potent pan-HDAC inhibitor in tumor cells.Quisinostat has a broad spectrum antiproliferative activity against solid and hematologic cancer cell lines and induces apoptosis.(In Vivo):Quisinostat (40 mg/kg; p.o.; once daily; for 3 days) acts as a potent HDAC1 inhibitor p21waf1,cip1 ZsGreen tumors in vivo.Quisinostat induces continuous H3 acetylation in tumor tissue in vivo.Quisinostat (10 mg/kg; once daily; i.p.; for 14 days) strongly inhibits the growth of large pre-established HCT116 colon xenografts.

Quisinostat inhibits HDAC isozymes in vitro.Quisinostat (30-1000 nM; 24 hours) is a potent pan-HDAC inhibitor in tumor cells.?Quisinostat has a broad spectrum antiproliferative activity against solid and hematologic cancer cell lines and induces apoptosis. Western Blot Analysis Cell Line:Human A2780 ovarian carcinoma cellsConcentration:30 nM, 100 nM, 300 nM, 1000 nM Incubation Time:24 hours Result:Induced H3 and H4 acetylation at concentrations as low as 30 to 100 nM.

Quisinostat (40 mg/kg; p.o.; once daily; for 3 days) acts as a potent HDAC1 inhibitor that inhibits p21waf1,cip1 ZsGreen tumors in vivo.Quisinostat induces continuous H3 acetylation in tumor tissue in vivo.Quisinostat (10 mg/kg; once daily; i.p.; for 14 days) strongly inhibits the growth of large pre-established HCT116 colon xenografts. Animal Model:NMRI nude mice, with HCT116 colon carcinoma cells xenografts Dosage:10 mg/kg Administration: Intraperitoneal injection, once daily, for 14 days Result:Strongly inhibited the growth of large pre-established HCT116 colon xenografts.

(JNJ-26481585)

Cell Cycle/DNA Damage

HDAC

HDAC1| HDAC10| HDAC11| HDAC2| HDAC3| HDAC4| HDAC5| HDAC8

Cancer

——

875320-29-9

394.476

C21H26N6O2

>98% (HPLC)

DMSO:79 mg/mL (200.26 mM); Ethanol:<1 mg/mL (<1 mM); Water:<1 mg/mL (<1 mM)

O=C(C1=CN=C(N2CCC(CNCC3=CN(C)C4=C3C=CC=C4)CC2)N=C1)NO

N-hydroxy-2-(4-((((1-methyl-1H-indol-3-yl)methyl)amino)methyl)piperidin-1-yl)pyrimidine-5-carboxamide

(-20℃)

With Ice Pack

≥ 2 years