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DS18561882

Cat.No.E1154

DS18561882 is a potent and isozyme-selective inhibitor of methylenetetrahydrofolate dehydrogenase 2 (MTHFD2), demonstrating an IC50 of 0.0063 μM. It also inhibits MTHFD1 with an IC50 of 0.57 μM. This compound displays favorable oral pharmacokinetic properties.
DS18561882 Chemical Structure

Chemical Structure

Molecular Weight: 608.63

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Chemical Information, Storage & Stability

Molecular Weight 608.63 Formula

C28H31F3N4O6S

 Storage (From the date of receipt)
CAS No. 2227149-22-4 Download SDF Storage of Stock Solutions

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Mechanism of Action

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. This compound (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. It is suspended in a 0.5% (w/v) methyl cellulose 400 solution in this article.
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