|
|
| | JNJ26854165(Quisinostat) 2HCl Basic information |
| Product Name: | JNJ26854165(Quisinostat) 2HCl | | Synonyms: | JNJ26854165(Quisinostat) 2HCl;JNJ 26481585 dihydrochloride;JNJ-26481585 2HCl;JNJ 26481585 dihydrochloride - Quisinostat dihydrochloride;JNJ26854165 2HCL;Quisinostat 2HCl, 98%, a new type HDAC inhibitor;Quisinostat 2HCl;Quisinostat dihydrochloride | | CAS: | 875320-31-3 | | MF: | C21H27ClN6O2 | | MW: | 430.94 | | EINECS: | | | Product Categories: | | | Mol File: | 875320-31-3.mol |  |
| | JNJ26854165(Quisinostat) 2HCl Chemical Properties |
| solubility | DMSO:46.7(Max Conc. mg/mL);99.9(Max Conc. mM) | | form | A crystalline solid | | color | White to yellow |
| | JNJ26854165(Quisinostat) 2HCl Usage And Synthesis |
| 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 |
| | JNJ26854165(Quisinostat) 2HCl Preparation Products And Raw materials |
|