Mutant IDH1 inhibitor
Based on 2 publication(s) in Google Scholar
Mutant IDH1 inhibitor is a potent mutant IDH1 R132H inhibitor with IC50 of < 72 nM.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.08%
- CAS. Nr.: 1429180-08-4
- Formel: C25H34N6O3
- Molecular Weight:466.58
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Chemical Information
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Lösungsmittel & Löslichkeit
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Publications Citing Use of MedChemExpress (MCE) Mutant IDH1 inhibitor
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Biologische Aktivität
IC50: < 72 nM (mutant IDH1 R132H)
Mutant IDH1 inhibitor is a potent IDH1 R132H inhibitor, and used for the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1429180-08-4
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Appearance Solid
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Molecular Weight 466.58
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Formel C25H34N6O3
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Color White to light yellow
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SMILES
CC(C)[C@@H](COC1=O)N1C2=NC(N[C@@H](C)C3=CC=C(CN4CCN(C(C)=O)CC4)C=C3)=NC=C2
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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J Med Chem
Differentiating Inhibition Selectivity and Binding Affinity of Isocitrate Dehydrogenase 1 Variant Inhibitors. [Abstract]2023 Apr 13;66(7):5279-5288. PMID: 36952395 -
Sci Rep
Assessing inhibitors of mutant isocitrate dehydrogenase using a suite of pre-clinical discovery assays. [Abstract]2017 Oct 6;7(1):12758. PMID: 28986582
Mutant IDH1 inhibitor purchased from MedChemExpress. Usage Cited in: Sci Rep. 2017 Oct 6;7(1):12758. [Abstract]
Represented western blot of an isothermal dose-response at melting temperature of 59°C demonstrating cellular mIDH1 enzyme thermal stabilization with mIDH1 inhibitors.
Lösungsmittel & Löslichkeit
DMSO : ≥ 34 mg/mL (72.87 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Protokoll
Day 1: cells are seeded in 384-well plates in triplicates for both the cell proliferation and 2HG assay, and incubated at 37°C, 95% Rh, 5% CO2 overnight. Day 2: compounds are serially diluted 1 :3 (10 point dilution from 10 mM solutions in DMSO) and delivered to the cell assay plates via acoustic dispenser, with final concentration ranging from 30 μM to 1.5 nM. The plates are returned to the incubator after treatment and incubated for 48 hours. Day 4 Proliferation assay: CTG is added to the assay plates and luminescence signal is read on the plate reader. Day 4 2HG assay : Extraction sample preparation consisted of aspirating all media from the assay plates, adding 70 μL of 90% methanol in water, dry ice incubation for 15 minutes, centrifuging at 2000 rpm for 30 min to ensure all particulates have settled, and transferring 30 μL of the supernatant into LC-MS ready plates. LC-MS analysis follows.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
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- Italian - IT (251 KB)
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Handling Instructions (2659 KB)
Verweise
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1433 mL | 10.7163 mL | 21.4326 mL | 53.5814 mL |
| 5 mM | 0.4287 mL | 2.1433 mL | 4.2865 mL | 10.7163 mL | |
| 10 mM | 0.2143 mL | 1.0716 mL | 2.1433 mL | 5.3581 mL | |
| 15 mM | 0.1429 mL | 0.7144 mL | 1.4288 mL | 3.5721 mL | |
| 20 mM | 0.1072 mL | 0.5358 mL | 1.0716 mL | 2.6791 mL | |
| 25 mM | 0.0857 mL | 0.4287 mL | 0.8573 mL | 2.1433 mL | |
| 30 mM | 0.0714 mL | 0.3572 mL | 0.7144 mL | 1.7860 mL | |
| 40 mM | 0.0536 mL | 0.2679 mL | 0.5358 mL | 1.3395 mL | |
| 50 mM | 0.0429 mL | 0.2143 mL | 0.4287 mL | 1.0716 mL | |
| 60 mM | 0.0357 mL | 0.1786 mL | 0.3572 mL | 0.8930 mL |
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