Crelosidenib
Mutant IDH1-IN-6 is a potent, selective and orally active mutant isocitrate dehydrogenase (IDH) inhibitor with IC50s of 6.27 nM, 3.71 nM, 36.9 nM and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q and IDH2 R172K mutant enzymes, respectively. Mutant IDH1-IN-6 is less active at inhibiting the IDH wild-type enzymes.
For research use only. We do not sell to patients.
- CAS No.: 2230263-60-0
- Formula: C28H36N6O3
- Molecular Weight:504.62
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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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IDH1 |
IDH2 |
Mutant IDH1-IN-6 (example 2) inhibits production of 2-hydroxyglutarate in HT1080 cells with an IC50 of 1.28 nM, indicating the inhibition of mutant IDHl R132C in cells. aKG, a metabolite generated by wild-type IDHl is not affected by Mutant IDH1-IN-6, indicating Mutant IDH1-IN-6 is selective for mutant IDHl over wild type IDHl in cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Athymic nude mice (20-22 g) injected with TB08 cells[1]
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Dosage:1 mg/kg, 2 mg/kg, 4 mg/kg, 8 mg/kg, 16 mg/kg, 32 mg/kg
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Administration:Oral gavage; twice daily; for 3 days
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Result:Inhibitied of 2-hydroxyglutarate in IDHl mutant xenograft mice.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2230263-60-0
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Molecular Weight 504.62
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Formula C28H36N6O3
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SMILES
O=C1OCC2=CN=C(N[C@H](C3=CC=C([C@@H](N4CCN(C(C=C)=O)CC4)CC5CC5)C=C3)C)N=C2N1CC
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Synonyms
LY3410738; Mutant IDH1-IN-6
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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)
Crelosidenib Related Classifications
HY-131312 Related Classifications
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