Product Data Sheet

Crelosidenib (gentisate)

Catalog No. A75814

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Crelosidenib (gentisate) is a selective oral inhibitor of mutant isocitrate dehydrogenase (IDH) enzymes, specifically targeting IDH1 R132H (IC50 of 6.27 nM), IDH1 R132C (IC50 of 3.71 nM), IDH2 R140Q (IC50 of 36.9 nM), and IDH2 R172K (IC50 of 11.5 nM). It demonstrates decreased activity against wild-type IDH enzymes. Crelosidenib is primarily utilized in research focusing on metabolic dysregulation and oncogenic pathways associated with IDH mutations in various cancers.
Chemical Information
Catalog NumA75814
M. Wt812.86
FormulaC42H48N6O11
Purity>98%
Storageat -20 °C 3 years (powder form); at -20 °C 6 months (Solution base)
CAS No.2759438-85-0
SynonymsLY3410738 (gentisate); Mutant IDH1-IN-6 (gentisate)
SMILESOC(C1=C(C=CC(O)=C1)O)=O.O=C2OCC3=CN=C(N=C3N2CC)N[C@@H](C)C(C=C4)=CC=C4[C@@H](N5CCN(CC5)C(C=C)=O)CC6CC6.OC(C7=C(C=CC(O)=C7)O)=O
Biological Activity
DescriptionCrelosidenib (gentisate) is a selective oral inhibitor of mutant isocitrate dehydrogenase (IDH) enzymes, specifically targeting IDH1 R132H (IC50 of 6.27 nM), IDH1 R132C (IC50 of 3.71 nM), IDH2 R140Q (IC50 of 36.9 nM), and IDH2 R172K (IC50 of 11.5 nM). It demonstrates decreased activity against wild-type IDH enzymes. Crelosidenib is primarily utilized in research focusing on metabolic dysregulation and oncogenic pathways associated with IDH mutations in various cancers.
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SHIPPING AND STORAGE
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