Chemical Name: N-[4-[8-[(3S)-3,4-Dimethylpiperazin-1-yl]-7-methyl-5-oxo-2,4-dihydro-1H-chromeno[3,4-c]pyridine-3-carbonyl]-2-(trifluoromethoxy)phenyl]methanesulfonamide. Alternate Names: DS18
MTHFD2 inhibitor
Molecular Weight:
608.63
Purity:
>98% by HPLC NMR (Conforms)
Form:
Pale yellow solid
CAS Number:
[2227149-22-4]
Formula:
C28H31F3N4O6S
Application Notes:
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
* VAT and and shipping costs not included. Errors and price changes excepted