中文名：奎西諾司他（JNJ-26481585）2HCl
英文名：Quisinostat (JNJ-26481585) 2HCl
英文別名：N-hydroxy-2-(4-(((1-methyl-1H-indol-3-yl)methylamino)methyl)piperidin-1-yl)pyrimidine-5-carboxamide dihydrochloride
純度：10mM in DMSO
貨號：Q408865
包裝：1ml
Cas號：875320-31-3
存儲溫度：-80℃儲存
產(chǎn)品介紹：
Information
Quisinostat (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 lo
In?vitro
JNJ-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?vivo
In 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?Data
cell?lines：
Concentrations：0-300 nM
Incubation?Time：24 hours
Powder?Purity:≥99%
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關(guān)鍵字： N-hydroxy-2-(4-(((1-methyl-1H-indol-3-yl)methylamino)methyl)piperidin-1-yl)pyrimidine-5-carboxamide dihydrochloride
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