DS18561882

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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 IC50 value of 0.0063 μM. DS18561882 also has inhibitory effect on MTHFD1 (IC50=0.57 μM). DS18561882 exhibits a good oral pharmacokinetic profile.

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

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 ); 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.DS18561882 is suspended in a 0.5% (w/v) methyl cellulose 400 solution in this article.Animal Model:Five week old female BALB/cAJcl-nu/nu mice with MDA-MB-231 luc tumor cells (4 × 106 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.

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Cell Cycle/DNA Damage

DHFR

DHFR

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2227149-22-4

608.63

C28H31F3N4O6S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 150 mg/mL (246.46 mM; 超声助溶 )

C[C@H]1CN(CCN1C)c1ccc2c3CCN(Cc3c(=O)oc2c1C)C(=O)c1ccc(NS(C)(=O)=O)c(OC(F)(F)F)c1

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(-20℃)

With Ice Pack

≥ 2 years