Imatinib mesylate
Biological Activity
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.
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.
Compound Libraries
Imatinib mesylate is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
M. Wt | 589.71 |
Formula | C29H31N7O.CH4O3S |
Storage | Store at +4°C |
Purity | ≥98% (HPLC) |
CAS Number | 220127-57-1 |
PubChem ID | 123596 |
InChI Key | YLMAHDNUQAMNNX-UHFFFAOYSA-N |
Smiles | CS(O)(=O)=O.CN1CCN(CC1)CC2=CC=C(C(NC3=CC=C(C(NC4=NC=CC(C5=CN=CC=C5)=N4)=C3)C)=O)C=C2 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
water | 58.97 | 100 | |
DMSO | 58.97 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 589.71. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.7 mL | 8.48 mL | 16.96 mL |
5 mM | 0.34 mL | 1.7 mL | 3.39 mL |
10 mM | 0.17 mL | 0.85 mL | 1.7 mL |
50 mM | 0.03 mL | 0.17 mL | 0.34 mL |
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References
References are publications that support the products' biological activity.
Buchdunger et al (1996) Inhibition of the Abl protein-tyrosine kinase in vitro and in vivo by a 2-phenylaminopyrimidine derivative. Cancer Res. 56 100 PMID: 8548747
Juurikivi et al (2005) Inhibition of c-kit tyrosine kinase by imatinib mesylate induces apoptosis in mast cells in rheumatoid synovia: a potential approach to the treatment of arthritis. Ann.Rheum.Dis. 64 1126 PMID: 16014680
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Citations for Imatinib mesylate
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