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DS18561882 | MTHFD2 inhibitor

CAS:
2227149-22-4
Catalog Number:
10-4188
Activity:
MTHFD2 inhibitor
Chemical Names:
N-[4-[8-[(3S)-3,4-Dimethylpiperazin-1-yl]-7-methyl-5-oxo-2,4-dihydro-1H-chromeno[3,4-c]pyridine-3-carbonyl]-2-(trifluoromethoxy)phenyl]methanesulfonamide
Alternate Name:
DS18
Molecular Weight:
608.63
Molecular Formula:
C28H31F3N4O6S
Solubility:
Soluble in DMSO (at least 40 mg/ml)
Physical Properties:
Pale yellow solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

DS18562881 (2227149-22-4) is a potent (IC50 = 6.3 nM) and selective (>90-fold over MTHFD1) inhibitor of the mitochondrial enzyme methylenetetrahydrofolate dehydrogenase 2 (MTHFD2), a key enzyme in one carbon metabolism in purine or thymidine biosynthesis.1 It almost completely inhibited tumor growth in an MDA-MB-231 mouse xenograft model. DS18561882 treatment of triple-negative breast cancer cells lead to significant reduction of cancer cell proliferation but not apoptosis; however, in combination with Chk1 inhibitors it led to apoptotic cell death.2 In combination with enzalutamide, it significantly inhibited castration resistant prostate cancer cells in vitro and in vivo.3

References/Citations:

  1. Kawai et al. (2019), Discovery of a Potent, Selective, and Orally Available MTHFD2 Inhibitor (DS18561882) with In Vivo Antitumor Activity; J. Med. Chem. 62 10204
  2. Lee et al. (2021), A novel oral inhibitor for one-carbon metabolism and checkpoint kinase 1 inhibitor as a rational combination treatment for breast cancer; Biochem. Biophys, Res. Commun. 584 7
  3. Zhao et al. (2022), PPFIA4 promotes castration-resistant prostate cancer by enhancing mitochondrial metabolism through MTHFD2; J. Exp. Clin. Cancer Res. 41 125
DS18561882 | MTHFD2 inhibitor is also available in the Cellular Metabolism Library.
CAS:
2227149-22-4
Catalog Number:
10-4188
Activity:
MTHFD2 inhibitor
Chemical Names:
N-[4-[8-[(3S)-3,4-Dimethylpiperazin-1-yl]-7-methyl-5-oxo-2,4-dihydro-1H-chromeno[3,4-c]pyridine-3-carbonyl]-2-(trifluoromethoxy)phenyl]methanesulfonamide
Alternate Name:
DS18
Molecular Weight:
608.63
Molecular Formula:
C28H31F3N4O6S
Solubility:
Soluble in DMSO (at least 40 mg/ml)
Physical Properties:
Pale yellow solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

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