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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Isocitrate Dehydrogenase (IDH)-GSK864
GSK864

Chemical Structure : GSK864

CAS No.: 1816331-66-4

GSK864 (GSK 864;GSK-864)

货号: PC-45645Not For Human Use, Lab Use Only.

GSK864 is a compound structurally related to GSK321 with improved in vivo pharmacokinetic properties, inhibits IDH1 mutants R132C, R132H, and R132G with IC50 values of 8.8, 15.2 and 16.6 nM, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GSK864 is a compound structurally related to GSK321 with improved in vivo pharmacokinetic properties, inhibits IDH1 mutants R132C, R132H, and R132G with IC50 values of 8.8, 15.2 and 16.6 nM, respectively.
GSK864 shows the similar activity (2-HG production in R132C IDH1 mutant HT1080 fibrosarcoma cells, EC50 of 320 nM).
GSK864 reduces leukemic blasts in vivo.

物理化学性质&存储条件

分子量 558.6033
分子式 C30H31FN6O4
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

DMSO: ≥ 100 mg/mL

Chemical Name/SMILES

(S)-1-(4-fluorobenzyl)-N3-(4-methoxy-3,5-dimethylphenyl)-7-methyl-5-(1H-pyrrole-2-carbonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine-3,7-dicarboxamide

参考文献

1. Okoye-Okafor UC, et al. Nat Chem Biol. 2015 Nov;11(11):878-86.

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