Chemical Structure : IPN60090
CAS No.: 1853164-83-6
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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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.
分子量 | 532.53 | |
分子式 | C24H27F3N8O3 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
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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 |
1. Soth MJ, et al. J Med Chem. 2020 Nov 12;63(21):12957-12977.
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