InformationQuisinostat (JNJ-26481585) 2HCl is a novel second-generationHDACinhibitor with highest potency for HDAC1 withIC50of 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.TargetsHDAC1 (Cell-free assay); HDAC2 (Cell-free assay); HDAC11 (Cell-free assay); HDAC10 (Cell-free assay); HDAC4 (Cell-free assay) 97,0.11 nM; 0.33 nM; 0.37 nM; 0.46 nM; 0.64 nMIn vitroJNJ-26481585 exhibits broad spectrum antiproliferative activity in solid and hematologic cancer cell lines, such as all lung, breast, colon, prostate, brain, and ovarian tumor cell lines, with IC50 ranging from 3.1-246 nM, which is more potent than vorinostat, R306465, panobinostat, CRA-24781, or mocetinostat in various human cancer cell lines tested. A recent study shows that JNJ-26481585 promotes myeloma cell death at low nanomolar concentrations by resulting in Mcl-1 depletion and Hsp72 induction.In vivoIn an HDAC1-responsive A2780 ovarian tumor screening model, JNJ-26481585 dosing at its maximal tolerated dose (10 mg/kg i.p. and 40 mg/kg p.o.) for 3 days leads to an HDAC1-regulated fluorescence , which predicts tumor growth inhibition. Furthermore, JNJ-26481585 also shows more potent inhibitory effects on the growth of C170HM2 colorectal liver metastases than 5-fluorouracil/Leucovorin.Cell Research(from reference)Cell lines：NCL-H2106, Colo699 and LNCAP cells Concentrations：0-300 nM Incubation Time：24 hours. Specification: 0.98 Molecular Formula: C21H28Cl2N6O2 Molecular Weight: 467.39 PubChem CID: 122129987 Related Documents: https://ald-pub-files.oss-cn-shanghai.aliyuncs.com/aladdinsci/pdp/sds/1/Q412686-SCI_bddd8e67e1e8101ffe9361599c4300f1.pdf
- UPC:
- 51312503
- Condition:
- New
- Availability:
- 2 weeks
- Weight:
- 0.96 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- Q412686-5mg
- CAS:
- 875320-31-3
- Product Size:
- 5mg
