产品
编 号：F279869
分子式：C28H31F3N4O6S
分子量：608.63
分子式：C28H31F3N4O6S
分子量：608.63
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
结构图
CAS No: 2227149-22-4
产品详情
生物活性：
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.
体内研究：
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.
体外研究：
DS18561882 (0-150 nM) gives the lowest GI50 value (140 nM) against the MDA-MB-231 cell line.
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.
体内研究：
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.
体外研究：
DS18561882 (0-150 nM) gives the lowest GI50 value (140 nM) against the MDA-MB-231 cell line.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备