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IDH305

Chemical Structure : IDH305

CAS No.: 1628805-46-8

IDH305 (IDH-305;IDH 305)

Catalog No.: PC-60164Not For Human Use, Lab Use Only.

IDH 305 (IDH305) is a potent, selective, brain penetrant mutant IDH1 inhibitor with IC50 of 18 and 28 nM for IDH1 R132H and R132C.

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Biological Activity

IDH305 (IDH-305) is a potent, selective, brain penetrant mutant IDH1 inhibitor with IC50 of 18 and 28 nM for IDH1 R132H and R132C.
IDH305 exhibits >200 fold selectivity over WT IDH1 (IC50=6.14 uM), and no activtiy against IDH2 mutants.
IDH305 inhibits EGF-independent proliferation of HCT116-IDH1R132H+/- cells with IC50 of 20 nM.
IDH305 exhibits in vivo correlation of 2-HG reduction and efficacy in IDH1 mutant xenograft tumor model.

Physicochemical Properties

M.Wt 490.463
Formula C23H22F4N6O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(R)-4-((S)-1-fluoroethyl)-3-(2-(((S)-1-(4-methyl-2'-(trifluoromethyl)-[3,4'-bipyridin]-6-yl)ethyl)amino)pyrimidin-4-yl)oxazolidin-2-one

References

1. Cho YS, et al. ACS Med Chem Lett. 2017 Sep 18;8(10):1116-1121.

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