MI-773 (SAR-405838)
featured

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 206069

CAS#: 1303607-60-4

Description: MI-773, also known as SAR405838, is an orally available spiro-oxindole HDM2 (human double minute 2) antagonist with potential antineoplastic activity. Upon oral administration, the p53-HDM2 protein-protein interaction inhibitor MI-773 binds to HDM2, preventing the binding of the HDM2 protein to the transcriptional activation domain of the tumor suppressor protein p53. By preventing this HDM2-p53 interaction, the proteosome-mediated enzymatic degradation of p53 is inhibited and the transcriptional activity of p53 is restored, which may result in the restoration of p53 signaling and lead to the p53-mediated induction of tumor cell apoptosis. HDM2, a zinc finger protein and a negative regulator of the p53 pathway, is often overexpressed in cancer cells. It has been implicated in cancer cell proliferation and survival. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)


Price and Availability

Size
Price

5mg
USD 340
Size
Price

10mg
USD 600
Size
Price

MI-773 (SAR-405838), purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

img

Theoretical Analysis

MedKoo Cat#: 206069
Name: MI-773 (SAR-405838)
CAS#: 1303607-60-4
Chemical Formula: C29H34Cl2FN3O3
Exact Mass: 561.19613
Molecular Weight: 562.51
Elemental Analysis: C, 61.92; H, 6.09; Cl, 12.60; F, 3.38; N, 7.47; O, 8.53


Synonym: SAR-405838; SAR 405838; SAR405838; MI-773; MI773; MI 773

IUPAC/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 Code: O=C([C@H](N[C@H]1CC(C)(C)C)[C@H](C2=CC=CC(Cl)=C2F)[C@@]31C(NC4=C3C=CC(Cl)=C4)=O)N[C@H]5CC[C@H](O)CC5


Technical Data

Appearance:
Solid powder

Purity:
>98%

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).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>5 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

  
 
 
 


References

1: Hoffman-Luca CG, Yang CY, Lu J, Ziazadeh D, McEachern D, Debussche L, Wang S.
1. Significant Differences in the Development of Acquired Resistance to the MDM2
Inhibitor SAR405838 between In Vitro and In Vivo Drug Treatment. PLoS One. 2015
Jun 12;10(6):e0128807. doi: 10.1371/journal.pone.0128807. eCollection 2015.
PubMed PMID: 26070072; PubMed Central PMCID: PMC4466389.

2: Hoffman-Luca CG, Ziazadeh D, McEachern D, Zhao Y, Sun W, Debussche L, Wang S.
Elucidation of Acquired Resistance to Bcl-2 and MDM2 Inhibitors in Acute Leukemia
In Vitro and In Vivo. Clin Cancer Res. 2015 Jun 1;21(11):2558-68. doi:
10.1158/1078-0432.CCR-14-2506. Epub 2015 Mar 9. PubMed PMID: 25754349.

3: Wang S, Sun W, Zhao Y, McEachern D, Meaux I, Barrière C, Stuckey JA, Meagher
JL, Bai L, Liu L, Hoffman-Luca CG, Lu J, Shangary S, Yu S, Bernard D, Aguilar A,
Dos-Santos O, Besret L, Guerif S, Pannier P, Gorge-Bernat D, Debussche L.
SAR405838: an optimized inhibitor of MDM2-p53 interaction that induces complete
and durable tumor regression. Cancer Res. 2014 Oct 15;74(20):5855-65. doi:
10.1158/0008-5472.CAN-14-0799. Epub 2014 Aug 21. PubMed PMID: 25145672; PubMed
Central PMCID: PMC4247201.