DS18561882 also inhibited MTHFD1 (IC50=0.57).DS18561882 had good oral drug kinetics.DS18561882 is a potent isozyme-selective methylene tetrahydrofolate dehydrogenase 2 (MTHFD2) inhibitor with IC50 value of 0.0063.

DS18561882 (0-150 nM) gives the lowest GI50 value (140 nM) against the MDA-MB-231 cell line.

DS18561882 (oral;10mg /kg, 30mg /kg, 100mg /kg or 300mg /kg) had good oral drug kinetics, including ACU(64.6, 264, 726ug. H /ml).;Cmax (11.4, 56.5, 90.1 ° g/ml).T1/2 (2.21, 2.16, 2.32 hours) at 30 mg/kg;100 mg/kg;200 mg/kg, respectively.DS18561882 was suspended in 0.5% (W/V) methyl cellulose 400 solution.DS18561882 (oral;30, 100 or 300 mg/kg;Tumor growth inhibition was inhibited in a dose-dependent manner and was completely inhibited in mice at a dose of 300 mg/kg (TGI: 67%).

2227149-22-4

C28H31F3N4O6S

608.63

DS18561882

DMSO:250 mg/mL (410.76 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years