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SAR405838
- MI-77301
- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C29H34Cl2FN3O3
- MW: 562.5
Description
SAR405838 (MI-77301) is a potent inhibitor of the MDM2–p53 protein–protein interaction with a reported Ki value of 0.88 nM. It binds MDM2 with high affinity, prevents sequestration and degradation of wild-type p53, and thereby restores p53 transcriptional activity.
In cells retaining functional p53, SAR405838 induces accumulation of p53 and its downstream effectors, leading to cell-cycle arrest and/or apoptosis. It has demonstrated pharmacodynamic activity and tumor-growth inhibition in leukemia and solid-tumor xenograft models and is useful for studying MDM2 dependence and p53 reactivation.
Key Features
- High-affinity MDM2–p53 interaction inhibitor
- Ki: 0.88 nM
- Activates wild-type p53 signaling
- Induces cell-cycle arrest or apoptosis
- Orally bioactive in xenograft models
Applications
- MDM2 and p53 pathway research
- Protein–protein interaction assays
- p53 target-gene studies
- Apoptosis and cell-cycle analysis
- Wild-type p53 tumor models
More Information
| Parent CAS No. | 1303607-60-4 |
|---|---|
| Chemical Name | (2'S,3R,4'S,5'R)-6-Chloro-4'-(3-chloro-2-fluorophenyl)-N-((1r,4R)-4-hydroxycyclohexyl)-2'-neopentyl-2-oxospiro[indoline-3,3'-pyrrolidine]-5'-carboxamide |
| SMILES | C1C=C2[C@@]3([C@@H](C4C=CC=C(Cl)C=4F)[C@H](C(=O)N[C@H]4CC[C@H](O)CC4)N[C@H]3CC(C)(C)C)C(=O)NC2=CC=1Cl |&1:3,4,13,17,20,25,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C29H34Cl2FN3O3/c1-28(2,3)14-22-29(19-12-7-15(30)13-21(19)34-27(29)38)23(18-5-4-6-20(31)24(18)32)25(35-22)26(37)33-16-8-10-17(36)11-9-16/h4-7,12-13,16-17,22-23,25,35-36H,8-11,14H2,1-3H3,(H,33,37)(H,34,38)/t16?,17?,22-,23-,25+,29+/m0/s1 |
| InChiKey | IDKAKZRYYDCJDU-AEPXTFJPSA-N |
| CID | 53476877 |
| Short Description | MDM2 inhibitor |
References
- S Wang et al. SAR405838: an optimized inhibitor of MDM2-p53 interaction that induces complete and durable tumor regression. Cancer Res. 2014 Oct 15;74(20):5855-65.
- J Jung et al. TP53 mutations emerge with HDM2 inhibitor SAR405838 treatment in de-differentiated liposarcoma. Nat Commun. 2016 Aug 31;7:12609.
- M de Jonge et al. A phase I study of SAR405838, a novel human double minute 2 (HDM2) antagonist, in patients with solid tumours. Eur J Cancer. 2017 May;76:144-151.
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