All AbMole products are for research use only, cannot be used for human consumption.
Imatinib Mesylate, the mesylate salt of imatinib, is a tyrosine kinase inhibitor with antineoplastic activity. Imatinib binds to an intracellular pocket located within tyrosine kinases (TK), thereby inhibiting ATP binding and preventing phosphorylation and the subsequent activation of growth receptors and their downstream signal transduction pathways. This agent inhibits TK encoded by the bcr-abl oncogene as well as receptor TKs encoded by the c-kit and platelet-derived growth factor receptor (PDGFR) oncogenes. Inhibition of the bcr-abl TK results in decreased proliferation and enhanced apoptosis in malignant cells of Philadelphia-positive (Ph+) hematological malignancies such as CML and ALL; effects on c-kit TK activity inhibit mast-cell and cellular proliferation in those diseases overexpressing c-kit, such as mastocytosis and gastrointestinal stromal tumor (GIST).
Int J Mol Sci. 2024 Mar 26;25(7):3693.
FL118 Is a Potent Therapeutic Agent against Chronic Myeloid Leukemia Resistant to BCR-ABL Inhibitors through Targeting RNA Helicase DDX5
Imatinib Mesylate purchased from AbMole
BMC Biol. 2021 May 20;19(1):108.
Very long intergenic non-coding (vlinc) RNAs directly regulate multiple genes in cis and trans
Imatinib Mesylate purchased from AbMole
Sci Rep. 2020 Feb 4;10(1):1794.
A CRISPR/Cas13-based Approach Demonstrates Biological Relevance of Vlinc Class of Long Non-Coding RNAs in Anticancer Drug Response
Imatinib Mesylate purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | T cells |
| Preparation method | Cell proliferation assays. T cells, 1 × 105 in 200 μL/well of 96-well microtiter plates (Corning, Corning, NY), were stimulated with DCs or phytohemagglutinin M (PHA-M; 10 μg/mL, Sigma) or PDGF or both (R&D Systems, Minneapolis, MN) in a final volume of 0.2 mL/well. The cells were incubated with graded concentrations of imatinib mesylate, incubated for 4 days, pulsed with 2.0 μCi (0.074 MBq) tritiated thymidine (Amersham, Arlington Heights, IL) per well, and incubated for further 12 hours when they were harvested, and incorporated radioactivity was then quantified. |
| Concentrations | 0~20μM |
| Incubation time | 4 days |
| Animal Experiment | |
|---|---|
| Animal models | DTH in mice |
| Formulation | 10% DMSO |
| Dosages | 50 mg/kg for 21 consecutive days |
| Administration | intraperitoneal injections |
| Molecular Weight | 589.7 |
| Formula | C29H31N7O.CH4SO3 |
| CAS Number | 220127-57-1 |
| Solubility (25°C) | DMSO 60 mg/mL Water 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Src-bcr-Abl Products |
|---|
| Risvodetinib
Risvodetinib (IkT-148009) is an orally active, selective and brain-penetrant protein tyrosine kinase inhibitor, displaying excellent target efficacy against c-Abl1, c-Abl2/Arg with IC50 values of 33 nM, 14 nM, respectively. |
| SI-2 hydrochloride
SI-2 hydrochloride is a highly promising SRC-3 inhibitor (PPI) with acceptable oral availability, with IC50 values of 3-20 nM for breast cancer cell death. |
| KB SRC 4
KB SRC 4 is a potent, and highly selective c-Src inhibitor, with a Ki of 44 nM and a Kd of 86 nM, and shows no inhibition on c-Abl up to 125 μM; KB SRC 4 has antitumor activity. |
| Hydroxymethyl dasatinib
Hydroxymethyl dasatinib (M24), a benzylhydroxy metabolite of Dasatinib, exhibits an IC50 of 46.7nM in K562 CML cells. |
| Asciminib hydrochloride
Asciminib (ABL001) hydrochloride is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC50 of 0.25 nM. |
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