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- STI571 (Imatinib, Gleevec) | Abl/cKit/PDGFR inhibitor
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- Tyrosine Kinase
- ABL/SRC
- STI571 (Imatinib, Gleevec) | Abl/cKit/PDGFR inhibitor
- Home
- Molecular Target
- Tyrosine Kinase
- PDGFR family
- STI571 (Imatinib, Gleevec) | Abl/cKit/PDGFR inhibitor
Product Description
Imatinib is an orally-available, aminopyrimidine-based inhibitor of Abl, c-Kit, and PDGFR with cellular phosphorylation inhibition IC50 value of 0.1 uM. [1]
Focused studies on c-Kit show that Imatinib inhibits activity of both wild-type and mutant c-Kit, as well as c-Kit-dependent activation of Akt. [2] Furthermore, Imatinib completely suppresses activation of MAPK and the antiapoptotic effect of c-Kit activation.
Studies on the PDGF receptors show that Imatinib preferentially inhibits the both a and b isoforms, but not the closely related c-Fms, Flt3, KDR, Flt1, and TEK tyrosine kinases. [3] In addition, Imatinib inhibits stem cell factor-mediated cellular signalling, including ligand-stimulated receptor autophosphorylation and inositol phosphate formation.
Technical information:
| Chemical Formula: | C29H31N7O.CH4SO3 | |
| CAS #: | 220127-57-1 | |
| Molecular Weight: | 589.4 | |
| Purity: | >99% | |
| Appearance: | White | |
| Chemical Name: | 4-[(4-Methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]benzamide Methanesulfonate | |
| Solubility: | Up to 22 mM in DMSO | |
| Synonyms: | STI-571, STI 571, STI571, Imatinib mesylate, Gleevec, Glivec |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Capdeville et al., Glivec (STI571, imatinib), a rationally developed, targeted anticancer drug. Nat. Rev. Drug. Disc. 2002, 1, 493-502. Pubmed ID: 12120256 |
| 2. | Heinrich et al., Inhibition of c-kit receptor tyrosine kinase activity by STI 571, a selective tyrosine kinase inhibitor. Blood, 2000, 96(3), 925-932. Pubmed ID: 10910906 |
| 3. | Buchdunger et al., Abl protein-tyrosine kinase inhibitor STI571 inhibits in vitro signal transduction mediated by c-kit and platelet-derived growth factor receptors. J. Pharmacol. Exp. Ther. 2000, 295(1), 139-145. Pubmed ID: 10991971 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
