IHMT-IDH1-053
IHMT-IDH1-053 (compound 16) is a highly selectivity and irreversible IDH1-mutant inhibitor with an IC50 of 4.7 nM for IDH1 R132H. IHMT-IDH1-053 displays high selectivity against IDH1 mutants over IDH1 wt and IDH2 wt/mutants. IHMT-IDH1-053 inhibits 2-hydroxyglutarate (2-HG) production in IDH1 R132H mutant transfected 293T cells (IC50=28 nM). IHMT-IDH1-053 binds to the IDH1 R132H protein in the allosteric pocket adjacent to the NAPDH binding pocket through a covalent bond with residue Cys269. IHMT-IDH1-053 inhibits the proliferation of HT1080 cell line and primary AML cells which both bear IDH1 R132 mutants.
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- CAS. Nr.: 3049485-80-2
- Formel: C25H33FN6O4S
- Molecular Weight:532.63
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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R132H IDH1 4.7 μM (IC50) |
IDH1 wt |
IDH2 wt |
Chemical Information
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CAS. Nr. 3049485-80-2
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Molecular Weight 532.63
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Formel C25H33FN6O4S
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SMILES
C[C@H](NC1=NC=C(F)C(N2C(OC[C@@H]2C(C)C)=O)=N1)C3=CC=C(N4CCC(NS(C=C)(=O)=O)CC4)C=C3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
IHMT-IDH1-053 Related Classifications
HY-149359 Related Classifications
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