Imatinib is a number of tyrosine kinase enzymes specific inhibitor. It act by specifically inhibiting a certain enzyme that is characteristic of a particular cancer cell, rather than non-specifically inhibiting and killing all rapidly dividing cells, and served as a model for other targeted therapy modalities through tyrosine kinase inhibition. In chronic myelogenous leukemia, the Philadelphia chromosome leads to a fusion protein of abl with bcr (breakpoint cluster region), termed bcr-abl. As this is now a constitutively active tyrosine kinase, it is used to decrease bcr-abl activity. It is being used as an experimental agent to suppress platelet-derived growth factor (PDGF) by inhibiting its receptor (PDGF-Rβ).
BMC Biol. 2023 Nov 24;21(1):271.
Evidence for widespread existence of functional novel and non-canonical human transcripts
Imatinib 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 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 purchased from AbMole
Nat Commun. 2019 Dec 20;10(1):5799.
Novel approach reveals genomic landscapes of single-strand DNA breaks with nucleotide resolution in human cells.
Imatinib purchased from AbMole
Biochem Biophys Res Commun. 2019 May 14;512(4):786-792.
CircRNA_000543 knockdown sensitizes nasopharyngeal carcinoma to irradiation by targeting miR-9/platelet-derived growth factor receptor B axis.
Imatinib purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | BON-1 cells and NCI-H727 cells |
| Preparation method | Seeding BON-1 cells and NCI-H727 cells into flat-bottomed 96-well plates in triplicate and allowing to adhere overnight in 10% fetal bovine serum-supplemented DMEM or RPMI 1640 complete medium, respectively; the medium is then exchanged for serum-free medium (negative control) or serum-free medium containing serial dilutions of Imatinib. Determing the number of metabolically active cells by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay, and measuring absorbance in a Packard Spectra microplate reader at 540 nm.after 48 hours (control cultures do not reach confluence), calculating growth inhibition using the following formula: inhibition rate = (1 − a / b) × 100%, where a and b are the absorbance values of the treated and control groups, respectively. |
| Concentrations | ~100 μM |
| Incubation time | 48 hours |
| Animal Experiment | |
|---|---|
| Animal models | SCLC6, SCLC61, SCLC 74 and SCLC108 small cell lung cancers are injected into Swiss mice (nu/nu, female |
| Formulation | Imatinib is diluted in water. |
| Dosages | 70 or 100 mg/kg |
| Administration | Administered via i.p. |
| Molecular Weight | 493.6 |
| Formula | C29H31N7O |
| CAS Number | 152459-95-5 |
| Solubility (25°C) | DMSO 5 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.
[2] Simone Claudiani, et al. The argument for using imatinib in CML
[3] Cornelius F Waller. Imatinib Mesylate
[4] Meinolf Suttorp, et al. Pharmacology and pharmacokinetics of imatinib in pediatric patients
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