Idasanutlin (RG7388)
Idasanutlin; also known as RG7388 and RO5503781, is a highly potent and selective MDM2 antagonist with potential anticancer activity. RG7388 binds to MDM2 blocking the interaction between the MDM2 protein and the transcriptional activation domain of the tumor suppressor protein p53. By preventing the MDM2-p53 interaction, p53 is not enzymatically degraded and the transcriptional activity of p53 is restored. This may lead to p53-mediated induction of tumor cell apoptosis. MDM2, a zinc finger nuclear phosphoprotein and negative regulator of the p53 pathway, is often overexpressed in cancer cells and has been implicated in cancer cell proliferation and survival.
1: Ding Q, Zhang Z, Liu JJ, Jiang N, Zhang J, Ross TM, Chu XJ, Bartkovitz D, Podlaski F, Janson C, Tovar C, Filipovic ZM, Higgins B, Glenn K, Packman K, Vassilev LT, Graves B. Discovery of RG7388, a Potent and Selective p53-MDM2 Inhibitor in Clinical Development. J Med Chem. 2013, 56 (14), 5979–5983.
PubMed PMID: 23808545.
PubMed PMID: 23808545.
| Chemical | |
|---|---|
| CAS Num | 1229705-06-9 |
| Chemical Formula | C31H29Cl2F2N3O4 |
| Molecular Weight | 616.48247 |
| IUPAC Chemical Name | 4-((2R,3S,4R,5S)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-neopentylpyrrolidine-2-carboxamido)-3-methoxybenzoic acid. |
| Exact Mass | 615.15032 |
| Elemental Analysis | C, 60.40; H, 4.74; Cl, 11.50; F, 6.16; N, 6.82; O, 10.38 |
| Synonym | RG7388; RG 7388; RG-7388; RO5503781; RO-5503781; RO 5503781; Idasanutlin. |
| Solubility | Soluble in DMSO, not in water |
| SMILES Code | O=C(O)C1=CC=C(NC([C@@H]2N[C@@H](CC(C)(C)C)[C@](C#N)(C3=CC=C(Cl)C=C3F)[C@H]2C4=CC=CC(Cl)=C4F)=O)C(OC)=C1 |
| Biological | |
| Targets and Effects | N/A |
| Pathways | Apoptosis |
| Physical | |
| Appearance | Solid powder |
| Purity | >98% (or refer to the Certificate of Analysis) |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| Storage Condition | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Shelf Life | >2 years if stored properly |
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