DS18561882 |
| カタログ番号GC38906 |
DS18561882は、IC50値が0.0063μMの高いポテンシャルを持つアイソザイム選択的メチレンテトラヒドロ葉酸デヒドロゲナーゼ2（MTHFD2）阻害剤です。また、MTHFD1にも抑制効果があります（IC50=0.57μM）。DS18561882は良好な経口薬物動態プロファイルを示します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2227149-22-4
Sample solution is provided at 25 µL, 10mM.
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DS18561882 is a novel, orally active, specific inhibitor of methylenetetrahydrofolate dehydrogenase (MTHFD2), exhibiting an IC50 value of 0.0063 μM[1].
DS18561882(0-10μM; 72h) specifically inhibits MTHFD2 activity and induces cell cycle arrest in HCC38 breast cancer cells, however, it did not induce cell death. Combinatory treatment of Chk1 inhibitor and DS18561882 induces apoptosis synergistically [2]. DS18561882(50 µM; 5days) together with pemetrexed increased the antitumor sensibilities and provided therapeutic advantages in the treatment of Lung adenocarcinoma (LUAD) cells[3].
DS18561882(oral administration; 30, 100 or 300 mg/kg; twice daily) inhibited tumor growth in MDA-MB-231luc tumor mice in a dose-dependent manner, and the tumor was completely suppressed at a dose of 300 mg/kg[1]. DS18561882(100mg/kg; p.o.) can significantly impede the progression of castration-resistant prostate cancer (CRPC) induced by elevated PPFIA4 expression[4].
[1]. Kawai J, Toki T, et,al. Discovery of a Potent, Selective, and Orally Available MTHFD2 Inhibitor (DS18561882) with in Vivo Antitumor Activity. J Med Chem. 2019 Nov 27;62(22):10204-10220. doi: 10.1021/acs.jmedchem.9b01113. Epub 2019 Nov 18. PMID: 31638799.
[2]. Lee J, Chen X, et,al. 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. 2021 Dec 20;584:7-14. doi: 10.1016/j.bbrc.2021.11.001. Epub 2021 Nov 2. PMID: 34753066.
[3]. Zhao R, Feng T, et,al. PPFIA4 promotes castration-resistant prostate cancer by enhancing mitochondrial metabolism through MTHFD2. J Exp Clin Cancer Res. 2022 Apr 5;41(1):125. doi: 10.1186/s13046-022-02331-3. PMID: 35382861; PMCID: PMC8985307.
Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)
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