Imatinib-13C, d3

Imatinib-13C, d3 (STI571-13C, d3) is 13C labeled Imatinib. Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively[1][2][3][4]. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV[5].

Product Specifications

Product Name Alternative

STI571-13C, d3; CGP-57148B-13C, d3

UNSPSC

12352005

Target

Autophagy; Bcr-Abl; c-Kit; Isotope-Labeled Compounds; PDGFR; SARS-CoV

Related Pathways

Anti-infection; Autophagy; Others; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Smiles

O=C(C1=CC=C(CN2CC[N]CC2)C=C1)NC3=CC=C(C)C(NC4=NC(C5=CN=CC=C5)=CC=N4)=C3.C[13C]([2H])([2H])[2H]

Molecular Formula

C29 13CH31D3N7O

Molecular Weight

512.65

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[2]Heinrich MC, et al. Inhibition of c-kit receptor tyrosine kinase activity by STI 571, a selective tyrosine kinase inhibitor. Blood. 2000 Aug 1;96 (3) :925-32.|[3]Guida T, et al. Sorafenib inhibits imatinib-resistant KIT and platelet-derived growth factor receptor beta gatekeeper mutants. Clin Cancer Res. 2007 Jun 1;13 (11) :3363-9.|[4]Iqbal N, et al. Imatinib: a breakthrough of targeted therapy in cancer. Chemother Res Pract. 2014;2014:357027.|[5]Okuda K, et al. ARG tyrosine kinase activity is inhibited by STI571.Blood. 2001 Apr 15;97 (8) :2440-8|[6]Yao JC, et al. Clinical and in vitro studies of imatinib in advanced carcinoid tumors. Clin Cancer Res. 2007 Jan 1;13 (1) :234-40.|[7]Sun XC, et al. Depletion of telomerase RNA inhibits growth of gastrointestinal tumors transplanted in mice. World J Gastroenterol. 2013 Apr 21;19 (15) :2340-7.|[8]Yildiz C, et al. Effect of imatinib on growth of experimental endometriosis in rats. Eur J Obstet Gynecol Reprod Biol. 2016 Feb;197:159-63.|[9]Jeanne M Sisk, et al. Coronavirus S Protein-Induced Fusion Is Blocked Prior to Hemifusion by Abl Kinase Inhibitors. J Gen Virol. 2018 May;99 (5) :619-630.|[10]Coleman CM, et al, Frieman MB. Abelson Kinase Inhibitors Are Potent Inhibitors of Severe Acute Respiratory Syndrome Coronavirus and Middle East Respiratory Syndrome Coronavirus Fusion. J Virol. 2016;90 (19) :8924‐8933. Published 2016 Sep 12.