IDH1 Inhibitor 9
IDH1 Inhibitor 9 (compound 11S) is a potent IDH1 inhibitor with IC50 values of 124.4, 95.7 nM for IDH1 R132H, IDH1 R132C, respectively. IDH1 Inhibitor 9 induces apoptosis and cell cycle arrest at the S phase. IDH1 Inhibitor 9 shows anti-tumor activity.
For research use only. We do not sell to patients.
- CAS No.: 3037967-71-5
- Formula: C26H30N4O3
- Molecular Weight:446.54
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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 124.4 nM (IC50) |
R132C IDH1 95.7 nM (IC50) |
IDH1 Inhibitor 9 (compound 11S) (2, 4, 8, 10 µM) induces apoptosis and cell cycle arrest at the S phase in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT-1080 cells
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Concentration:2, 4, 8 µM
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Incubation Time:48 h
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Result:Induced apoptosis in a dose-dependent manner.
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Cell Line:HT-1080 cells
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Concentration:2, 4, 8, 10 µM
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Incubation Time:24 h
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Result:Induced cell cycle arrest at the S phase with the percentage of cells in the S phase ranged from 22.4 to 51.6 % with increasing concentrations from 2 to 10 μM.
Pharmacokinetic Parameters (SD rats)[1].
| Parameters | iv (0.5 mg/kg) | po (5 mg/kg) |
| T1/2 (h) | 1.46 ± 0.12 | 2.13 ± 0.18 |
| Tmax (h) | 0.03 ± 0.00 | 0.19 ± 0.00 |
| Cmax (ng/mL) | 766.5 ± 143.1 | 478 ± 76 |
| AUC(0-t) (hr* ng/mL) | 236 ± 283.0 | 369.7 ± 93.2 |
| CL (mL/h/kg) | 1637 ± 212 | 10103 ± 3310 |
| F % | - | 16.8 ± 4.7 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:4-5 weeks, Female nude mice (HT-1080 xenograft mouse model)[1]
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Dosage:20, 40 mg/kg
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Administration:I.p.; every 2 days for 8 days
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Result:Suppressed tumor growth without evident loss in body weight.
Chemical Information
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CAS No. 3037967-71-5
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Molecular Weight 446.54
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Formula C26H30N4O3
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SMILES
OC1=CC(OC)=C(C/C=C(C)/C)C=C1C2=NC(N3CCNCC3)=NC(C4=CC=C(O)C=C4)=C2
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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)
IDH1 Inhibitor 9 Related Classifications
HY-162631 Related Classifications
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