Imatinib

Biological Activity

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).

Product Citations

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  Patent. US2025127716A1 2025-04-24.

  Patent. US2025127716A1
  Imatinib purchased from AbMole

• 

  Patent. US2025127716A1 2025 Apr 24; .

  Patent. US2025127716A1
  Imatinib purchased from AbMole

• 

  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 purchased from AbMole

• 

  Discover Oncology. 2024 Jun 15.

  Lycorine attenuated proliferation and induced apoptosis on imatinib-resistant K562 cell by inhibiting autophagy
  Imatinib purchased from AbMole

• 

  BMC Biol. 2023 Nov 24;21(1):271.

  Evidence for widespread existence of functional novel and non-canonical human transcripts
  Imatinib purchased from AbMole

• 

  Patent. WO2023147868A1 2023 Aug 10.

  Patent. WO2023147868A1
  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

Protocol (for reference only)

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.

Chemical Information

Molecular Weight	493.6
Formula	C29H31N7O
CAS Number	152459-95-5
Solubility (25°C)	DMSO 10 mg/mL
Storage	Powder          -20°C   3 years ;  4°C   2 years In solvent       -80°C   6 months ;  -20°C   1 month

References

[1] Philip Cohen, et al. Kinase drug discovery 20 years after imatinib: progress and future directions

[2] Simone Claudiani, et al. The argument for using imatinib in CML

[3] Cornelius F Waller. Imatinib Mesylate