Imatinib mesylate

Biological Activity

Imatinib mesylate is a potent and selective v-Abl tyrosine kinase inhibitor (IC₅₀ = 38 nM). Also inhibits PDGFR and c-kit. Exhibits selectivity for v-Abl over a panel of other tyrosine and serine/threonine protein kinases. Selectively inhibits PDGF-stimulated growth of v-abl-transformed PB-3 cells and v-sis-transformed BALB/c 3T3 cells in vitro. Exhibits antitumor effects in mice bearing AMuLV or BABL/c 3T3 v-sis cells. Inhibits replication of SARS-CoV and MERS-CoV in vitro (EC₅₀ values are 9.823 and 17.689 μM, respectively).

External Portal Information

Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of Imatinib is reviewed on the chemical probes website.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Transient inhibition of p53 homologs protects ovarian function from two distinct apoptotic pathways triggered by anticancer therapies
   SY Kim, DM Nair, M Romero, VA Serna, AJ Koleske, TK Woodruff, T Kurita
   Cell Death Differ., 2018;0(0):.
2. Inhibition of the Abl protein-tyrosine kinase in vitro and in vivo by a 2-phenylaminopyrimidine derivative.
   Buchdunger et al.
   Cancer Res., 1996;56:100
3. Inhibition of c-kit tyrosine kinase by ima. mesylate induces apoptosis in mast cells in rheumatoid synovia: a potential approach to the treatment of arthritis.
   Juurikivi et al.
   Ann.Rheum.Dis., 2005;64:1126
4. Imatinib treatments have long-term impact on placentation and embryo survival
   W Salem, K Li, C Krapp, SA Ingles, MS Bartolomei, K Chung, RJ Paulson, RA Nowak, LK McGinnis
   Sci Rep, 2019;9(1):2535.
5. Parity predisposes breasts to the oncogenic action of PAPP-A and activation of the collagen receptor DDR2
   E Slocum, A Craig, A Villanueva, D Germain
   Breast Cancer Res., 2019;21(1):56.
6. Repurposing of clinically developed drugs for treatment of Middle East Respiratory Syndrome coronavirus infection.
   Dyall et al.
   Antimicrob.Agents Chemother., 2014;58:4885

Product Datasheets