CAS NO: | 1448347-49-6 |
规格: | 98% |
分子量: | 582.96 |
包装 | 价格(元) |
1mg | 电议 |
5mg | 电议 |
25mg | 电议 |
AG-120(Ivosidenib)
mutant IDH1 inhibitor
CAS:1448347-49-6
分子式:C28H22ClF3N6O3
分子量:582.96
纯度:98%
存储:Sealed in dry,2-8°C
Background:
AG-120 is an IDH1 inhibitor.
Isocitrate dehydrogenase (IDH) is a metabolic enzyme interconverting isocitrate and α-ketoglutarate (α-KG), but cancer-associated mutations of IDH1 and IDH2 confer a neomorphic activity, which allows reduction of α-KG to the oncometabolite 2-HG.
In vitro: TF-1 cells or primary human AML patient samples expressing mutant IDH1 were treated with AG-120, and the results showed that in TF-1 IDH1-R132H cells, AG-120 was able to decrease the intracellular 2-HG levels, inhibit growth factor independent proliferation and restore erythropoietin-induced differentiation [1].
Ex vivo: Previous ex-vivo study showed that the pharmacological inhibition of mutant IDH1 enzyme with AG-120 in primary human blast cells led to an effective way to lower intracellular 2-HG levels and induced myeloid differentiation [1].
参考文献:
[1] Erica Hansen et al. AG-120, an Oral, Selective, First-in-Class, Potent Inhibitor of Mutant IDH1, Reduces Intracellular 2HG and Induces Cellular Differentiation in TF-1 R132H Cells and Primary Human IDH1 Mutant AML Patient Samples Treated Ex Vivo. Blood 2014 124:3734.