| Identification | Back Directory | [Name]
JNJ26854165(Quisinostat) 2HCl | [CAS]
875320-31-3 | [Synonyms]
Quisinostat 2HCl
JNJ26854165 2HCL
JNJ-26481585 2HCl
Quisinostat dihydrochloride
JNJ 26481585 dihydrochloride
JNJ26854165(Quisinostat) 2HCl
Quisinostat 2HCl, 98%, a new type HDAC inhibitor
JNJ 26481585 dihydrochloride - Quisinostat dihydrochloride | [Molecular Formula]
C21H28Cl2N6O2 | [MOL File]
875320-31-3.mol | [Molecular Weight]
467.392 |
| Hazard Information | Back Directory | [Uses]
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]. | [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: | NMRI nude mice, with HCT116 colon carcinoma cells xenografts[1] | | Dosage: | 10 mg/kg | | Administration: | Intraperitoneal injection, once daily, for 14 days | | Result: | Strongly inhibited the growth of large pre-established HCT116 colon xenografts. |
| [IC 50]
HDAC1: 0.11 nM (IC50); HDAC2: 0.33 nM (IC50); HDAC3: 4.86 nM (IC50); HDAC4: 0.64 nM (IC50); HDAC5: 3.69 nM (IC50); HDAC6: 76.8 nM (IC50); HDAC7: 119 nM (IC50); HDAC8: 4.26 nM (IC50); HDAC9: 32.1 nM (IC50); HDAC10: 0.46 nM (IC50); HDAC11: 0.37 nM (IC50) | [References]
[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. DOI:10.1158/1078-0432.CCR-09-0547 |
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