Mutant IDH1-IN-7
Mutant IDH1-IN-7 is a highly selective Isocitrate Dehydrogenase 1 (IDH1) R132H (IC50 = 0.26 μM, Kd = 2.1 μM)/R132C (IC50 = 1.1 μM) inhibitor. Mutant IDH1-IN-7 has no inhibitory effect on wild-type IDH1, IDH2-wt, and IDH2 R140Q. Mutant IDH1-IN-7 inhibits 2-Hydroxyglutarate (2-HG) production in U87-MG R132H cells (EC50 = 0.55 μM). Mutant IDH1-IN-7 exhibits moderate antiproliferative effects on U87-MG R132H and HT-1080 cells.
For research use only. We do not sell to patients.
- Formula: C27H28N4O3
- Molecular Weight:456.54
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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R132H IDH1 0.26 μM (IC50) |
R132H IDH1 2.1 μM (Kd) |
R132C IDH1 1.1 μM (IC50) |
Mutant IDH1-IN-7 (Compound 13e) (10-40 μM, 72 h) exhibits moderate antiproliferative activity against U87-MG IDH1 R132H and HT-1080 cells while displaying significantly lower potency in U87-MG and L02 cells[1].
Mutant IDH1-IN-7 (5 μM, 1 h) shows no inhibitory effect on wild-type IDH1, IDH2-wt and IDH2 R140Q, with IC50 values > 40 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 456.54
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Formula C27H28N4O3
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SMILES
CC1=CC=C(C=C1)NC(CN2C(N/C(C2=O)=C\C3=CC=CN3C4=CC(CC(C)C)=CC=C4)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Mutant IDH1-IN-7 Related Classifications
HY-175213 Related Classifications
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