Binds MDM2 (Ki = 0.88 nM)

MI-77301 – 1 mg

Brand:
Cayman
CAS:
1303607-60-4
Storage:
-20
UN-No:
Non-Hazardous - /

The protein p53, often called the ‘guardian of the genome,’ is a transcription factor that is activated in response to cellular stress (low oxygen levels, heat shock, DNA damage, etc.) and acts to prevent further proliferation of the stressed cell by promoting cell cycle arrest or apoptosis. Its role as a tumor suppressor is evident by the observation that approximately 50% of human tumors have mutated or non-functional p53. Mdm2, a key negative regulator of p53, which is over-expressed in many human tumors, functions by binding to and targeting p53 for proteasomal degradation. MI-77301 binds to MDM2 with a Ki value of 0.88 nM and blocks the MDM2-p53 interaction.{29885} It activates wild-type p53 in vitro and in xenograft tumor tissue of leukemia and solid tumors, leading to p53-dependent cell cycle arrest and/or apoptosis.{29885} In an SJSA-1 xenograft model of osteosarcoma, a single dose of 200 mg/kg MI-77301 induces complete tumor regression in mice by upregulating the pro-apoptotic protein PUMA.{29885}  

 

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Description

Binds MDM2 (Ki = 0.88 nM), blocking MDM2-p53 protein-protein interaction, leading to p53-dependent cell cycle arrest and/or apoptosis; induces tumor regression in a SJSA-1 xenograft model of osteosarcoma by upregulating the pro-apoptotic protein PUMA

Formal name: (2’S,3R,4’S,5’R)-6-chloro-4’-(3-chloro-2-fluorophenyl)-2’-(2,2-dimethylpropyl)-1,2-dihydro-N-(trans-4-hydroxycyclohexyl)-2-oxo-spiro[3H-indole-3,3’-pyrrolidine]-5’-carboxamide

Synonyms:  SAR405838

Molecular weight: 562.5

CAS: 1303607-60-4

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Cell Cycle||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|p53 Signaling||Research Area|Cancer|Transcription Factors|p53

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