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).
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 |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
Related Src-bcr-Abl Products |
---|
Osteogenic Growth Peptide (10-14)
Osteogenic Growth Peptide (10-14) (OGP(10-14)), the C-terminal truncated pentapeptide of osteogenic growth peptide (OGP), retains the full OGP-like activity. |
Abl Cytosolic Substrate
Abl Cytosolic Substrate is a substrate for Abelson tyrosine kinase (Abl ). |
Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH
Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH is a high-affinity pentapeptide to bind to the src SH2 domain (IC50≈1 µM). |
p60c-src substrate II
p60c-src substrate II is an efficient pentapeptide substrate for the tyrosine kinase pp60c-src. |
Caffeic acid-pYEEIE
Caffeic acid-pYEEIE, a non-phosphopeptide inhibitor, exhibits potent binding affinity for the GST-Lck-SH2 domain. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.