DS18561882

Catalog No.E1154

Technical Data

Formula	C28H31F3N4O6S
Molecular Weight	608.63	CAS No.	2227149-22-4
Solubility (25°C)*	In vitro


* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Biological Activity

Description	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.
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.

Description

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.

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.

Protocol (from reference)

References

https://pubmed.ncbi.nlm.nih.gov/31638799/

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.