Quisinostat 2HCl

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) 2HCl 是一种新型第二代 HDAC 抑制剂，对 HDAC1 具有最高效力，在无细胞测定中 IC50 为 0.11 nM。

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

JNJ-26481585 inhibits HDAC isozymes in vitro.JNJ-26481585 (30-1000 nM; 24 hours) is a potent pan-HDAC inhibitor in tumor cells.JNJ-26481585 has broad spectrum antiproliferative activity against solid and hematologic cancer cell lines and induces apoptosis. Western Blot Analysis Cell Line:Human A2780 ovarian carcinoma cells Concentration: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.

JNJ-26481585 (40 mg/kg; p.o.; once daily, for 3 days) as a potent HDAC1 inhibitor p21waf1,cip1 ZsGreen tumors in vivo.JNJ-26481585 induces continuous H3 acetylation in tumor tissue in vivo.JNJ-26481585 (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.

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Metabolic Enzyme/Protease

Retinoid Receptor

HDAC1| HDAC10| HDAC11| HDAC2| HDAC4

Cancer

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875320-31-3

467.39

C21H28Cl2N6O2

>98% (HPLC)

In Vitro:?DMSO : 31.25 mg/mL (66.86 mM)

Cl.Cl.CN1C=C(CNCC2CCN(CC2)C2=NC=C(C=N2)C(=O)NO)C2=CC=CC=C12

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(-20℃)

With Ice Pack

≥ 2 years