DS18561882 | MTHFD2 inhibitor
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $100.00 | ||
| 25 mg | $375.00 |
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:
- 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
- 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
- Zhao et al. (2022), PPFIA4 promotes castration-resistant prostate cancer by enhancing mitochondrial metabolism through MTHFD2; J. Exp. Clin. Cancer Res. 41 125
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
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:
- 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
- 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
- Zhao et al. (2022), PPFIA4 promotes castration-resistant prostate cancer by enhancing mitochondrial metabolism through MTHFD2; J. Exp. Clin. Cancer Res. 41 125
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1-855-FOCUS21
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