纯度:>98% by HPLC;NMR (Conforms)
分子式:C28H31F3N4O6S
分子量:608.63
溶剂:DMSO (>40 mg/ml)
性状:Pale yellow solid
存储:-20°C
Activity (short version):MTHFD2 inhibitor
Function / Pharmacology:Potent (IC50 = 6.3 nM) and selective (>90-fold over MTHFD1) inhibitor of the mitochondrial enzyme methylenetetrahydrofolate dehydrogenase 2 (MTHFD2), a key enzyme in one carbon metabolism in purine or thymidine biosynthesis.1 It almost completely inhibited tumor growth in an MDA-MB-231 mouse xenograft model. DS18561882 treatment of triple-negative breast cancer cells lead to significant reduction of cancer cell proliferation but not apoptosis; however, in combination with Chk1 inhibitors it led to apoptotic cell death.2 In combination with enzalutamide, it significantly inhibited castration resistant prostate cancer cells in vitro and in vivo.3