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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Antifolate-DS18561882
DS18561882

Chemical Structure : DS18561882

CAS No.: 2227149-22-4

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DS18561882 (DS 18561882, DS18)

货号: 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.

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5 mg ￥1980 In stock
10 mg ￥2980 In stock
25 mg ￥4880 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 608.63
分子式 C28H31F3N4O6S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
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

参考文献

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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