Imatinib (220127-57-1) is a tyrosine kinase inhibitor specific for abl (IC50 = 0.038 μM)1, PDGF-R (IC50 = 0.3 μM)1 and c-kit (IC50 = 0.1 μM)2. It is a clinically useful anti-cancer drug approved for the treatment of chronic myelogenous leukemia, gastrointestinal stromal tumors as well as several other cancers.
References/Citations:
1) Buchdunger, et al.(1996) Inhibition of the Abl Protein-Tyrosine Kinase in Vitro and in Vivo by a 2-Phenylpyrimidine Derivative; Cancer Res. 56 100
2) Heinrich et al (2000) Inhibition of c-kit receptor tyrosine kinase activity by STI 571, a selective tyrosine kinase inhibitor. Blood 96 925
3) Morioka et al. (2016) Effect of Collagen Type 1 or Human Fibronectin on Imatinib Cytotoxicity in Oral Squamous Cell Carcinoma; Pharmacology and Pharmacy, 7 255 [Focus Biomolecules Citation]
4) Hazekawa et al. (2017) Assessment of cytotoxicity of imatinib for oral squamous cell carcinoma by a real-time cell analysis system; E. J. Bio., 13 56 [ Focus Biomolecules Citation]
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