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. 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.
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.
|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.|
|Incubation time||48 hours|
|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.|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO 5 mg/mL|
|Related c-Kit Products|
Ripretinib (DCC-2618) is an orally bioavailable, selective KIT and PDGFR-alpha inhibitor.
Pexidartinib (PLX3397) is an oral, potent mutil-targeted receptor tyrosine kinase inhibitor of CSF-1R, Kit, and Flt3 with IC50 of 20 nM, 10 nM and 160 nM, respectively.
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