1260251-31-7 Usage
Description
Birinapant is a bivalent mimetic of the Diablo homolog known as second mitochondria-derived activator of caspase (Smac). It is an antagonist of cellular inhibitor of apoptosis 1 (cIAP1, or BIRC2), cIAP2 (BIRC3), and XIAP (BIRC4), binding each at nanomolar concentrations. Birinapant causes rapid cIAP1 degradation, caspase activation, PARP cleavage, and NF-κB activation in breast cancer cells. It shows in vivo antitumor activity, inducing apoptosis in several types of cancer xenografts in mice.
Uses
Birinapant is a bivalent SMAC mimetic compound antagonist of TRAF2 associated cIAP1 and cIAP2.
Enzyme inhibitor
This rotationally symmetric SMAC mimetic antagonist and anticancer agent (FW = 806.94 g/mol; CAS 1260251-31-7) targets cellular Inhibitor of Apoptosis Protein (or cIAP1; Kd of <1 nM), arguably the most potent mammalian caspase inhibitor, showing single-agent efficacy due to its panIAP antagonism and causing rapid cIAP1 degradation, caspase activation, PARP cleavage, and NF-κB activation. When administered in combination with TNF-α, Birinapant is effective against a melanoma cell line with acquired resistance to BRAF inhibitors
Check Digit Verification of cas no
The CAS Registry Mumber 1260251-31-7 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,2,6,0,2,5 and 1 respectively; the second part has 2 digits, 3 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 1260251-31:
(9*1)+(8*2)+(7*6)+(6*0)+(5*2)+(4*5)+(3*1)+(2*3)+(1*1)=107
107 % 10 = 7
So 1260251-31-7 is a valid CAS Registry Number.
1260251-31-7Relevant articles and documents
Process Development and Synthesis of Birinapant: Large Scale Preparation and Acid-Mediated Dimerization of the Key Indole Intermediate
Deng, Yijun,Xie, Qiuzhe,LaPorte, Matthew G.,Chasnoff, Anna T. A.,Mortensen, Mark A.,Patra, Debasis,Putrelo, Seth A.,Antonovich, Robert S.,Cao, Hong,Yan, Jun,Cooper, Arthur J.,Rippin, Susan R.,Alexander, Matthew D.,Kumar, Pavan Tirunahari,Hendi, Mukta S.,Lee, Yu-Hua,Haimowitz, Thomas,Condon, Stephen M.
, p. 242 - 252 (2016/03/04)
Birinapant/TL32711 (1) is a novel bivalent antagonist of the inhibitor of apoptosis (IAP) family of proteins which is currently in clinical development for the treatment of cancer and hepatitis B virus (HBV) infection. In this report, we present a detaile
SMAC Mimetic
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Page/Page column 15, (2011/01/12)
A SMAC mimetic and pharmaceutical compositions thereof and methods of use.