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 MTHFD1 的 IC₅₀ 值是 0.57 μM。DS18561882 具有良好的口服药代动力学特性。

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.

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IC50: 0.0063 μM (MTHFD2); 0.57 μM (MTHFD1)

DS18561882 (0-150 nM) gives the lowest GI50 value (140 nM) against the MDA-MB-231 cell line.
has not independently confirmed the accuracy of these methods. They are for reference only.

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.
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

[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.

In Vitro: DMSO : 150 mg/mL (246.46 mM; Need ultrasonic)配制储备液