Imatinib methanesulfonate
Catalog #:
IN0128
| IN0128-100mg | USD102.0 |
| IN0128-1g | USD390.0 |
Synonyms: Gleevec, CGP57148B, STI571
IUPAC Name:
4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3- ylpyrimidin-2-yl)amino]phenyl]benzamide
Functional Activity:
Imatinib is a 2-phenylaminopyrimidine derivative that functions as a specific inhibitor of a number of tyrosine kinase enzymes. It occupies the TK active site, leading to a decrease in activity.
There are a large number of TK enzymes in the body, including the insulin receptor. Imatinib is specific for the TK domain in abl (the Abelson proto-oncogene), c-kit and PDGF-R (platelet-derived growth factor receptor).
Imatinib is a drug used to treat certain types of cancer. It is used in treating chronic myelogenous leukemia (CML), gastrointestinal stromal tumors (GISTs) and a number of other malignancies. It is the first member of a new class of agents that act by inhibiting particular tyrosine kinase enzymes, instead of non-specifically inhibiting rapidly dividing cells.
Technical Data:
M.Wt: 589.71
Formula: C30H35 N7O4S
Solubility: Soluble in DMSO and water
Purity: >99%
Storage: Store at -20°C
CAS No.: 220127-57-1
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References for Imatinib:
1. Candelaria, M., Arias-Bonfill, D., Chavez-Blanco, A., Chanona, J., Cantu, D., Perez, C., and Duenas-Gonzalez, A. Lack in efficacy for imatinib mesylate as second-line treatment of recurrent or metastatic cervical cancer expressing platelet-derived growth factor receptor alpha. Int J Gynecol Cancer, 19: 1632-1637, 2009.
2. Yardley, D. A., Burris, H. A., 3rd, Markus, T., Spigel, D. R., Greco, F. A., Mainwaring, M., Waterhouse, D. M., Webb, C. D., and Hainsworth, J. D. Phase II trial of docetaxal plus imatinib mesylate in the treatment of patients with metastatic breast cancer. Clin Breast Cancer, 9: 237-242, 2009.
3. Shen, T., Kuang, Y. H., Ashby, C. R., Lei, Y., Chen, A., Zhou, Y., Chen, X., Tiwari, A. K., Hopper-Borge, E., Ouyang, J., and Chen, Z. S. Imatinib and nilotinib reverse multidrug resistance in cancer cells by inhibiting the efflux activity of the MRP7 (ABCC10). PLoS One, 4: e7520, 2009.
4. Druker, B. J. Perspectives on the development of imatinib and the future of cancer research. Nat Med, 15: 1149-1152, 2009.
5. Matsue, K., Matsuo, K., Fujiwara, H., Iwama, K., Hayama, B. Y., Kimura, S., Yamakura, M., and Takeuch, M. Diminished alpha2-plasmin inhibitor activity associated with the use of imatinib mesylate in patients with Philadelphia chromosome-positive haematologic cancer. Thromb Haemost, 101: 1170-1171, 2009.
6. Dorr, D. A., Burdon, R., West, D. P., Lagman, J., Georgopoulos, C., Belknap, S. M., McKoy, J. M., Djulbegovic, B., Edwards, B. J., Weitzman, S. A., Boyle, S., Tallman, M. S., Talpaz, M., Sartor, O., and Bennett, C. L. Quality of reporting of serious adverse drug events to an institutional review board: a case study with the novel cancer agent, imatinib mesylate. Clin Cancer Res, 15: 3850-3855, 2009.
