939981-39-2 Usage
Description
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. 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. 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. 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.
Uses
RG 7112 is MDM2 antagonist. It can be used in biological study of single mouse analysis on evaluation of alternative in vivo drug screening methodology.
Check Digit Verification of cas no
The CAS Registry Mumber 939981-39-2 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 9,3,9,9,8 and 1 respectively; the second part has 2 digits, 3 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 939981-39:
(8*9)+(7*3)+(6*9)+(5*9)+(4*8)+(3*1)+(2*3)+(1*9)=242
242 % 10 = 2
So 939981-39-2 is a valid CAS Registry Number.
939981-39-2Relevant articles and documents
Deconstruction of a nutlin: Dissecting the binding determinants of a potent protein-protein interaction inhibitor
Fry, David C.,Wartchow, Charles,Graves, Bradford,Janson, Cheryl,Lukacs, Christine,Kammlott, Ursula,Belunis, Charles,Palme, Stefan,Klein, Christian,Vu, Binh
supporting information, p. 660 - 665 (2013/07/26)
Protein-protein interaction (PPI) systems represent a rich potential source of targets for drug discovery, but historically have proven to be difficult, particularly in the lead identification stage. Application of the fragment-based approach may help tow