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Submit ReviewIvosidenib
Description: Potent inhibitor of mutant isocitrate dehydrogenase (mIDH1)
Chemical Name: (2S)-N-{(1S)-1-(2-Chlorophenyl)-2-[(3,3-difluorocyclobutyl)amino]-2-oxoethyl}-1(4-cyanopyridin-2-yl)-N-(5-fluoropyridin-3-yl)-5-oxopyrrolidine-2-carboxamide
Purity: ≥98% (HPLC)
Biological Activity for Ivosidenib
Ivosidenib is a potent inhibitor of mutant isocitrate dehydrogenase enzyme 1 (mIDH1), with activity against a variety of mutant IDH1 enzymes (IC50 range = 5-19 nM). Reduces intracellular 2-HG (Cat. No. 6122) by 96% at 0.5 μM. Increases sensitivity of melanoma to Temozolomide (Cat. No. 2706) in vivo and inhibits wild-type IDH1 in low magnesium and low nutrient levels. Ivosidenib also inhibits growth of tumors in cell and animal models of pancreatic cancer and inhibits invasion and migration of chondrosarcoma cells in vitro.
Technical Data for Ivosidenib
| M. Wt | 582.96 |
| Formula | C28H22ClF3N6O3 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1448347-49-6 |
| PubChem ID | 71657455 |
| InChI Key | WIJZXSAJMHAVGX-DHLKQENFSA-N |
| Smiles | N([C@H](C(NC1CC(F)(F)C1)=O)C2=C(Cl)C=CC=C2)(C(=O)[C@H]3N(C(=O)CC3)C4=CC(C#N)=CC=N4)C=5C=C(F)C=NC5 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Ivosidenib
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 58.3 | 100 | |
| ethanol | 58.3 | 100 |
Preparing Stock Solutions for Ivosidenib
The following data is based on the product molecular weight 582.96. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.72 mL | 8.58 mL | 17.15 mL |
| 5 mM | 0.34 mL | 1.72 mL | 3.43 mL |
| 10 mM | 0.17 mL | 0.86 mL | 1.72 mL |
| 50 mM | 0.03 mL | 0.17 mL | 0.34 mL |
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Product Datasheets for Ivosidenib
References for Ivosidenib
References are publications that support the biological activity of the product.
Popovici-Muller et al (2018) Discovery of AG-120 (ivosidenib): a first-in-class mutant IDH1 inhibitor for the treatment of IDH1 mutant cancers. ACS Med.Chem.Lett. 9 300 PMID: 29670690
Zarei et al (2022) Wild-type IDH1 inhibition enhances chemotherapy response in melanoma. J.Exp.Clin.Cancer Res. 41 283 PMID: 36153582
If you know of a relevant reference for Ivosidenib, please let us know.
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Keywords: Ivosidenib, Ivosidenib supplier, mutant, IDH1, isocitrate, dehydrogenase, potent, inhibitors, inhibits, melanoma, pancreatic, cancer, invasion, migration, Isocitrate, 1, (IDH1), 7761, Tocris Bioscience
Citations for Ivosidenib
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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