A selective MDM2 inhibitor that blocks the binding of MDM2 to p53 (IC50 = 30 nM); activates the p53 pathway in SJSA1 osteosarcoma cells and inhibits the growth of xenografts in nude mice

RG7388 – 1 mg

Brand:
Cayman
CAS:
1229705-06-9
Storage:
-20
UN-No:
De Minimis - 3077 / 9

RG7388 is a non-imidazoline, selective MDM2 inhibitor that blocks the binding of MDM2 to p53 (IC50 = 30 nM).{33578} By inhibiting MDM2, RG7388 activates the p53 pathway in SJSA1 osteosarcoma cells and inhibits the growth of xenografts in nude mice.{33578,33579} RG7388 is orally available and prolonged daily administration results in loss of MDM2 and p21 protein, growth inhibition, and apoptosis in SJSA1 xenograft tumors.{33579} Like other MDM2 inhibitors, RG7388 competitively inhibits multi-drug resistance protein 1 (MRP1) and reverse MRP1-mediated multidrug resistance in cancer cells in a p53-independent manner.{33577}  

 

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Description

A selective MDM2 inhibitor that blocks the binding of MDM2 to p53 (IC50 = 30 nM); activates the p53 pathway in SJSA1 osteosarcoma cells and inhibits the growth of xenografts in nude mice

Formal name: 4-[[[(2R,3S,4R,5S)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-(2,2-dimethylpropyl)-2-pyrrolidinyl]carbonyl]amino]-3-methoxy-benzoic acid

Synonyms:  Idasanutlin|Ro 5503781

Molecular weight: 616.5

CAS: 1229705-06-9

Purity: ≥98%

Formulation: A crystalline solid

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

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