Bioactivity | Quisinostat dihydrochloride (JNJ-26481585 dihydrochloride) is an orally available, potent pan-HDAC inhibitor with IC50s of 0.11 nM, 0.33 nM, 0.64 nM, 0.46 nM, and 0.37 nM for HDAC1, HDAC2, HDAC4, HDAC10 and HDAC11, respectively. Quisinostat dihydrochloride has a broad spectrum antitumoral activity[1]. |
Invitro | JNJ-26481585 inhibits HDAC isozymes in vitro[1].JNJ-26481585 (30-1000 nM; 24 hours) is a potent pan-HDAC inhibitor in tumor cells[1].JNJ-26481585 has broad spectrum antiproliferative activity against solid and hematologic cancer cell lines and induces apoptosis[1]. Western Blot Analysis[1] Cell Line: |
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[1].JNJ-26481585 induces continuous H3 acetylation in tumor tissue in vivo[1].JNJ-26481585 (10 mg/kg; once daily; i.p.; for 14 days) strongly inhibits the growth of large pre-established HCT116 colon xenografts[1]. Animal Model: |
Name | Quisinostat dihydrochloride |
CAS | 875320-31-3 |
Formula | C21H28Cl2N6O2 |
Molar Mass | 467.39 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
Reference | [1]. Arts J, et al. JNJ-26481585, a novel "second-generation" oral histone deacetylase inhibitor, shows broad-spectrum preclinical antitumoral activity. Clin Cancer Res. 2009 Nov 15;15(22):6841-51. |