DS18561882

DS18561882 is a highly potent, isozyme-selective methylenetetrahydrofolate dehydrogenase 2 (MTHFD2) inhibitor with an IC 50 value of 0.0063 μM. DS18561882 also has inhibitory effect on MTHFD1 ( IC 50 =0.57 μM). DS18561882 exhibits a good oral pharmacokinetic profile In Vitro DS18561882 (0-150 nM) gives the lowest GI 50 value (140 nM) against the MDA-MB-231 cell line. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo DS18561882 (oral administration; 30, 100 or 300 mg/kg; twice daily) inhibits tumor growth inhibition with a dose-dependent manner, the tumor is completely inhibited (TGI: 67%) at the dose of 300 mg/kg in mice . DS18561882 (oral administration; 10, 30, 100, or 300 mg/kg) has a good oral pharmacokinetic profile, including ACU (64.6, 264, 726 μg.h/ml ); C max (11.4, 56.5, 90.1 μg/ml); t 1/2 (2.21, 2.16, 2.32 hours) for 30 mg/kg; 100mg/kg; 200 mg/kg, respectively . DS18561882 is suspended in a 0.5% (w/v) methyl cellulose 400 solution in this article . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Five week old female BALB/cAJcl-nu/nu mice with MDA-MB-231 luc tumor cells (4 × 10 6 cells/mouse) Dosage: 30, 100 or 300 mg/kg Administration: Oral administration; 30, 100 or 300 mg/kg; twice daily; until day 11 Result: Suppressed tumor growth in a dose-dependent manner. Form:Solid IC50& Target:IC50: 0.0063 μM (MTHFD2),0.57 μM (MTHFD1)

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