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Chemical Structure : DS18561882
CAS No.: 2227149-22-4
Catalog No.: PC-73018Not For Human Use, Lab Use Only.
DS18561882 (DS 18561882, DS18) is a potent, isozyme-selective, orally available MTHFD2 inhibitor with IC50 of 6.3 nM, >800-fold selectivity over MTHFD1.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $358 | In stock | |
| 10 mg | $528 | In stock | |
| 25 mg | $858 | In stock | |
| 100 mg | Get quote |
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DS18561882 (DS 18561882, DS18) is a potent, isozyme-selective, orally available MTHFD2 inhibitor with IC50 of 6.3 nM, >800-fold selectivity over MTHFD1.
DS18561882 showed the strongest cell growth inhibition (GI50=140 nM) against MDA-MB-231 human breast cancer cell line.
DS18561882 demonstrated tumor growth inhibition in a mouse xenograft model upon oral administration.
DS18 specifically inhibits MTHFD2 activity and induces cell cycle arrest in HCC38 breast cancer cells.
DS18 induces apoptosis synergistically when combined with Chk1 inhibitors Y2606368 and GDC0575.
DS18561882 +Chk1 inhibitors induces DNA DSBs in vitro, dramatically inhibits tumorigenesis in triple negative-PDX model.
| M.Wt | 608.63 | |
| Formula | C28H31F3N4O6S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(S)-N-(4-(8-(3,4-Dimethylpiperazin-1-yl)-7-methyl-5-oxo-1,3,4,5-tetrahydro-2H-chromeno[3,4-c]pyridine-3-carbonyl)-2-(trifluoromethoxy)phenyl)methanesulfonamide |
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1. Junya Kawai, et al. J Med Chem. 2019 Nov 27;62(22):10204-10220.
2. Lee J, et al. Biochem Biophys Res Commun. 2021 Dec 20;584:7-14.
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