DS18561882

Modify Date: 2025-08-27 12:21:59

DS18561882 Structure
DS18561882 structure
Common Name DS18561882
CAS Number 2227149-22-4 Molecular Weight 608.63
Density N/A Boiling Point N/A
Molecular Formula C28H31F3N4O6S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of DS18561882


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].

 Names

Name DS18561882

 DS18561882 Biological Activity

Description 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].
Related Catalog
Target

IC50: 0.0063 μM (MTHFD2); 0.57 μM (MTHFD1)[1]

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

[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.

 Chemical & Physical Properties

Molecular Formula C28H31F3N4O6S
Molecular Weight 608.63
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