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CAS No.: 10538-99-5

LY 345899, a Folate analog, is an inhibitor of methylene tetrahydrofolate dehydrogenase MTHFD1 (IC50 = 96 nM, Ki = 18 nM) and MTHFD2 (IC50 = 96 nM).

规格	价格	促销价格	库存	数量

400-920-2911

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描述MTHFD2 is a mitochondrial methylenetetrahydrofolate dehydrogenase and cyclohydrolase involved in one-carbon metabolism. It is responsible for the oxidation of methylene-THF to 10-formyl-THF in mitochondria, which is highly overexpressed in cancer cells and embryonic cells. LY345899, a Folate analog, is a MTHFD inbhibitor with IC₅₀ values of 96 nM and 663 nM for MTHFD1 and MTHFD2, respectively^[1]. LY345899 treatment for 72 hours caused a decrease in the cell viability of the CRC cells with highly expressed MTHFD2 (LoVo, SW620, HCT116). LY345899 (1 μM; 14 days) significantly reduced cell colony formation among these CRC cells. Further, LY345899 treatment decreased cellular NADPH/NADP+ and GSH/GSSG levels. Accordingly, LY345899 treatment for 48 hours obviously enhanced cell death under hypoxia or detached conditions. In SW620-based xenograft mice, LY345899 (5 mg/kg or 10 mg/kg; i.p.; 5 d/wk) showed potent antitumor activity in vivo, which was evident by the reduced SW620 cell or PDX-based tumor growth and tumor weight^[2].
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实验方案

技术信息

CAS号

10538-99-5

储存条件

分子式

C20H21N7O7

运输

蓝冰

分子量

471.42

别名

溶解度

DMSO	120.0 mg/mL (254.5 mM) warming

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