CAS NO: | 1816272-18-0 |
包装: | 10mg |
市场价: | 13050元 |
Cas No. | 1816272-18-0 | ||||||||||||||||||||||||||||||||
别名 | GSK321 | ||||||||||||||||||||||||||||||||
分子式 | C28H28FN5O3 | ||||||||||||||||||||||||||||||||
分子量 | 501.55 | ||||||||||||||||||||||||||||||||
储存条件 | Store at -20°C | ||||||||||||||||||||||||||||||||
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. | ||||||||||||||||||||||||||||||||
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request | ||||||||||||||||||||||||||||||||
产品描述 | IC50: 2.9 (R132G), 3.8 (R132C), 4.6 (R132H) and 46 nM (WT IDH1)[1] (S,R)-WT IDH1 Inhibitor 2 (GSK321) is a potent, selective mutantIDH1inhibitor withIC50values of 2.9, 3.8, 4.6 and 46 nM for R132G, R132C, R132H and WT IDH1, respectively, and >100-fold selectivity over IDH2. (S,R)-WT IDH1 Inhibitor 2 induces decrease in intracellular 2-HG, abrogation of the myeloid differentiation block and induction of granulocytic differentiation at the level of leukemic blasts and more immature stem-like cells. (S,R)-WT IDH1 Inhibitor 2 can be used for research of acute myeloid leukemia (AML) and other cancers[1]. (S,R)-WT IDH1 Inhibitor 2 (GSK321; 0.1-10000 nM; 24 h) inhibits intracellular 2-HG production in HT1080 cells with an EC50value of 85 nM[1]. Cell Viability Assay[1]
Cell Cycle Analysis[1]
Western Blot Analysis[1]
(S,R)-WT IDH1 Inhibitor 2 (GSK321; 150 mg/kg; i.p.; daily, for 15 d; male CD-1 mice with IDH1 mutant AML xenograft) reduces leukemic blasts in vivo[1].
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