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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Isocitrate Dehydrogenase (IDH)-GSK321
GSK321

Chemical Structure : GSK321

CAS No.: 1816331-63-1

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GSK321 (GSK-321, GSK 321)

货号: PC-70088Not For Human Use, Lab Use Only.

GSK321 is a highly potent, selective inhibitor of mutant IDH1 with IC50s of 4.6/3.8/2.9 nM for R132H/R132C/R132G respectively.

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5 mg ￥1380 In stock
10 mg ￥2180 In stock
25 mg ￥3780 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GSK321 is a highly potent, selective inhibitor of mutant IDH1 with IC50s of 4.6/3.8/2.9 nM for R132H/R132C/R132G respectively.
GSK321 shows modest activity against WT IDH1 (IC50=46 nM) and exhibits no inhibitory activity against IDH2.
GSK321 inhibits intracellular 2-HG production in HT1080 cells (EC50= 85 nM).

物理化学性质&存储条件

分子量 501.5624
分子式 C28H28FN5O3
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

(R)-1-(4-fluorobenzyl)-N-(3-((S)-1-hydroxyethyl)phenyl)-7-methyl-5-(1H-pyrrole-2-carbonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine-3-carboxamide

参考文献

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

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