DS18561882 是一种高效的，对酶具有高选择性的亚甲基四氢叶酸脱氢酶 2 ( MTHFD2) 抑制剂，IC50 值为 0.0063 μM。DS18561882 抑制 MTHFD2 的 IC50 值是0.57 μM。DS18561882 具有良好的口服药代动力学特性。
货号:ajcx15596
CAS:2227149-22-4
分子式:C28H31F3N4O6S
分子量：608.63
溶解度:DMSO: 250 mg/mL (410.76 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

DS18561882 is a highly potent, isozyme-selective methylenetetrahydrofolate dehydrogenase 2 (MTHFD2) inhibitor with an IC50 value of 0.0063 μM. DS18561882 also has inhibitory effect on MTHFD1 (IC50=0.57 μM). DS18561882 exhibits a good oral pharmacokinetic profile[1].

DS18561882 (0-150 nM) gives the lowest GI50 value (140 nM) against the MDA-MB-231 cell line[1].

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[1].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 ); Cmax (11.4, 56.5, 90.1 μg/ml); t1/2 (2.21, 2.16, 2.32 hours) for 30 mg/kg; 100mg/kg; 200 mg/kg, respectively[1].DS18561882 is suspended in a 0.5% (w/v) methyl cellulose 400 solution in this article[1]. Animal Model: Five week old female BALB/cAJcl-nu/nu mice with MDA-MB-231 luc tumor cells (4 × 106 cells/mouse)[1]

[1]. Kawai J, et al. Discovery of a Potent, Selective, and Orally Available MTHFD2 Inhibitor (DS18561882) with In Vivo Anti-Tumor Activity. J Med Chem. 2019 Oct 22.