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
CAS Number
[152459-95-5]
Product Name Alternative
STI571; CGP-57148B
UNSPSC
12352005
Hazard Statement
H361
Target
Autophagy; Bcr-Abl; c-Kit; PDGFR; SARS-CoV
Type
Reference compound
Related Pathways
Anti-infection; Autophagy; Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/Imatinib.html
Concentration
10mM
Purity
99.95
Solubility
DMSO : 12.5 mg/mL (ultrasonic)
Smiles
CN(CC1)CCN1CC2=CC=C(C(NC3=CC=C(C)C(NC4=NC(C5=CC=CN=C5)=CC=N4)=C3)=O)C=C2
Molecular Formula
C29H31N7O
Molecular Weight
493.60
Precautions
H361
References & Citations
[1]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.|[2]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.|[3]Iqbal N, et al. Imatinib: a breakthrough of targeted therapy in cancer. Chemother Res Pract. 2014;2014:357027.|[4]Okuda K, et al. ARG tyrosine kinase activity is inhibited by STI571.Blood. 2001 Apr 15;97 (8) :2440-8|[5]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.|[6]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.|[7]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.|[8]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.|[9]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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Launched
Citation 01
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