An inhibitor of the MDM2-p53 interaction (IC50 = 0.018 µM); inhibits proliferation in cancer cell lines expressing wild-type p53 (IC50s = 0.18-2.2 µM) and cell lines expressing mutant p53 (IC50s = 5.7-20.3 µM); prevents and reduces tumor growth in an SJSA-1 mouse xenograft model at 50 and 100 mg/kg per day

RG-7112 – 25 mg

Brand:
Cayman
CAS:
939981-39-2
Storage:
-20
UN-No:
Non-Hazardous - /

RG-7112 is an inhibitor of mouse double-minute 2 protein (MDM2; IC50 = 0.018 µM), an E3 ubiquitin ligase that ubiquitinates the tumor suppressor p53 and also acts as a negative regulator of p53 transcriptional activity.{42617} RG-7112 binds to the p53 binding pocket of MDM2. It increases the levels of p53 and its transcriptional targets in SJSA-1 osteosarcoma cells.{42617,42618} It inhibits proliferation in cancer cell lines expressing wild-type p53 (IC50s = 0.18-2.2 µM) and cell lines expressing mutant p53 (IC50s = 5.7-20.3 µM). RG-7112 also prevents and reduces tumor growth in an SJSA-1 mouse xenograft model when administered at doses of 50 and 100 mg/kg per day, respectively.{42618} However, it inhibits thrombopoiesis in vivo, decreasing platelet counts in rats when administered at doses of 50 and 100 mg/kg and in cynomolgus monkeys at doses of 10 and 20 mg/kg.{42619}  

 

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SKU: 25673 - 25 mg Category:

Description

An inhibitor of the MDM2-p53 interaction (IC50 = 0.018 µM); inhibits proliferation in cancer cell lines expressing wild-type p53 (IC50s = 0.18-2.2 µM) and cell lines expressing mutant p53 (IC50s = 5.7-20.3 µM); prevents and reduces tumor growth in an SJSA-1 mouse xenograft model at 50 and 100 mg/kg per day, respectively; decreases platelet counts in rats at 50 and 100 mg/kg and in cynomolgus monkeys at 10 and 20 mg/kg

Formal name: [(4S,5R)-4,5-bis(4-chlorophenyl)-2-[4-(1,1-dimethylethyl)-2-ethoxyphenyl]-4,5-dihydro-4,5-dimethyl-1H-imidazol-1-yl][4-[3-(methylsulfonyl)propyl]-1-piperazinyl]-methanone

Synonyms:  RO5045337

Molecular weight: 727.8

CAS: 939981-39-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Ubiquitin Ligase System||Research Area|Cancer|Cell Signaling|p53 Signaling||Research Area|Cancer|Transcription Factors|p53||Research Area|Cell Biology|Proteolysis|Ubiquitin/Proteasome System

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