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Mutant IDH1-IN-1

Chemical Structure : Mutant IDH1-IN-1

CAS No.: 1355326-21-4

Mutant IDH1-IN-1

Catalog No.: PC-43052Not For Human Use, Lab Use Only.

Mutant IDH1-IN-1 is a potent, mutant-selective IDH1 inhibitor with with IC50s of 4, 42, 80 and 143 nM against mutant IDH1 R132C/R132C, IDH1 R132H/R132H, IDH1 R132H/WT and wild type IDH1, respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

Mutant IDH1-IN-1 is a potent, mutant-selective IDH1 inhibitor with with IC50s of 4, 42, 80 and 143 nM against mutant IDH1 R132C/R132C, IDH1 R132H/R132H, IDH1 R132H/WT and wild type IDH1, respectively; inhibits 2HG production in R132H IDH1-expressing HEK-293 cells with IC50 of 81.5 nM.

Physicochemical Properties

M.Wt 498.5912
Formula C30H31FN4O2
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
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Solubility

DMSO: ≥ 45 mg/mL

Chemical Name/SMILES

1H-Benzimidazole-1-acetamide, N-[2-(cyclohexylamino)-1-(2-methylphenyl)-2-oxoethyl]-N-(3-fluorophenyl)-

References

1. Deng G, et al. J Biol Chem. 2015 Jan 9;290(2):762-74.

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