Purinostat

Chemical Structure : Purinostat

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货号: PC-20479Not For Human Use, Lab Use Only.

Purinostat is a potent, highly selective class I and IIb HDAC inhibitor with IC50 of 0.81, 1.4, 1.7, and 3.8 nM for class I HDAC1, 2, 3, and 8, and 11.5, 1.1 nM for class IIb HDAC 6 and 10, respectively.

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生物&药学活性

Purinostat is a potent, highly selective class I and IIb HDAC inhibitor with IC50 of 0.81, 1.4, 1.7, and 3.8 nM for class I HDAC1, 2, 3, and 8, and 11.5, 1.1 nM for class IIb HDAC 6 and 10, respectively.
Purinostat mesylate displays much weaker activity against HDAC IIa and IV (HDAC4,5,7,9 11) with IC50 of 426-3,349 nM, also has no significant inhibitory activity on 89 kinase enzymes involved in tumor regulation.
Purinostat mesylate showed approximately 100-fold higher than Chidamide (Tucidinostat, Cat. PC-35344) inhibition on HDAC1, 2, 8, and 10 subtypes.
Purinostat mesylate showed better inhibitory effects than LBH589 (Panobinostat, Cat. PC-42468) against various hematologic tumor cell lines with IC50 values at nanomolar or subnanomolar.
Purinostat mesylate effectively increased the levels of Ac-H3, Ac-H4, and decreased HSP90 in a concentration-dependent manner in vitro of Ph+ leukemia cell lines, consistent with the BCR-ABL downregulation, p-SRC and STAT5 were also significantly suppressed.
Purinostat mesylate (5 mg/kg) exerted the robust antitumor activity on BL-2 secondary transplantation mouse model of Ph+ B-ALL.
Purinostat mesylate showed potent antileukemia effects in BCR-ABL(T315I)–induced primary B-ALL mice.

物理化学性质&存储条件

分子量	490.53
分子式	C23H26N10O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	2-(((2-(4-aminophenyl)-9-methyl-6-morpholino-9H-purin-8-yl)methyl)(methyl)amino)-N-hydroxypyrimidine-5-carboxamide methanesulfonate

参考文献

1. Yang L, et al. Clin Cancer Res. 2019 Dec 15;25(24):7527-7539.

2. Chen Y, et al. J Med Chem 2016;59:5488–504.

Purinostat

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Purinostat

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