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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Glutaminase-IPN60090
IPN60090

Chemical Structure : IPN60090

CAS No.: 1853164-83-6

IPN60090 (IACS-6274, IACS6274, IPN 60090 )

货号: PC-21821Not For Human Use, Lab Use Only.

IPN60090 (IACS-6274) is a potent, selective glutaminase-1 (GLS-1) inhibitor with IC50 of 31 nM, inhibits proliferation of A549 cells with IC50 of 26 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

IPN60090 (IACS-6274) is a potent, selective glutaminase-1 (GLS-1) inhibitor with IC50 of 31 nM, inhibits proliferation of A549 cells with IC50 of 26 nM.
IPN60090 (IACS-6274) displays no activity observed against GLS-2 (IIC50>50 uM), shows no significant inhibition of the hERG channel or common cytochrome P450 enzymes, as well as a 97-member Eurofins DiscoverX kinase panel.
IPN60090 (IACS-6274) demonstrates robust in vivo target engagement when orally dosed to this model at doses of 25-100 mg/kg twice daily, at both 4 days and 28 days, inhibits tumor growth in Ru337 PDX subcutaneous mouse tumor model.
IPN60090 can specifically bind to the ZSWIM4 protein, exerts a significant chemosensitizing effect in both EOC cells and PDO models.

物理化学性质&存储条件

分子量 532.53
分子式 C24H27F3N8O3
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

4-[(3,3-Difluorocyclobutyl)oxy]-N-[6-[(3R)-3-fluoro-4-[4-[(methylamino)carbonyl]-1H-1,2,3-triazol-1-yl]butyl]-3-pyridazinyl]-6-methyl-2-pyridineacetamide

参考文献

1. Soth MJ, et al. J Med Chem. 2020 Nov 12;63(21):12957-12977.

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