Masitinib (AB1010) is a tyrosine kinase inhibitor targeting stem cell factor receptor (c-kit) and platelet-derived growth factor (PDGF) receptor. It can enhance the antiproliferative effects of gemcitabine (GEM) in human pancreatic cancer cells. It potently inhibited human and murine KIT with activating mutations in the juxtamembrane domain. In vivo, masitinib (AB1010) blocked tumour growth in mice with subcutaneous grafts of Ba/F3 cells expressing a juxtamembrane KIT mutant. Masitinib, a c-kit and PDGF-receptor tyrosine kinase inhibitor, may represent an innovative avenue of treatment in corticosteroid-dependent asthma.
|Cell lines||Ba/F3 cell|
|Preparation method||For the assay of Ba/F3 cell proliferation, microtitre plates were seeded with a total of 104 cells/well in 100 µl of RPMI 1640 medium with 10% foetal bovine serum at 37°C. These were supplemented, or not, with either 0.1% conditioned medium from X63-IL-3 cells or 250 ng/ml murine SCF. The murine SCF, which activates KIT, was purified from the conditioned medium of SCF-producing CHO cells (gift of S. Lyman, Immunex). Cells were grown for 48 hours at 37°C and then incubated with 10 µl/well of WST-1 reagent (Roche Applied Science, France) for 3 hours at 37°C. The amount of formazan dye formed was quantified by its absorbance at 450 nm using a scanning multiwell spectrophotometer (MultiSkan MS, Thermo-LabSystems, France). A blank well without cells was used as a background control for the spectrophotometer and all assays were performed in triplicate.|
|Incubation time||48 h|
|Animal models||Ba/F3 Δ27 tumour model in Female MBRI Nu/Nu mice|
|Dosages||10, 30, or 45 mg/kg twice daily for 10 days|
|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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO ≥100 mg/mL|
Transcriptome and proteome analysis of tyrosine Kinase inhibitor treated canine mast cell tumour cells identifies potentially kit signaling-dependent genes.
Klopfleisch et al. BMC Vet Res. 2012 Jun 29;8(1):96. PMID: 22747577.
In vitro effects of the tyrosine kinase inhibitor, masitinib mesylate, on canine hemangiosarcoma cell lines.
Lyles et al. Vet Comp Oncol. 2012 Sep;10(3):223-35. PMID: 22594682.
The tyrosine kinase inhibitor masitinib blunts airway inflammation and improves associated lung mechanics in a feline model of chronic allergic asthma.
Lee-Fowler et al. Int Arch Allergy Immunol. 2012;158(4):369-74. PMID: 22487554.
Mast cell leukemia: identification of a new c-Kit mutation, dup(501-502), and response to masitinib, a c-Kit tyrosine kinase inhibitor.
Georgin-Lavialle et al. Eur J Haematol. 2012 Jul;89(1):47-52. PMID: 22324351.
Masitinib demonstrates anti-proliferative and pro-apoptotic activity in primary and metastatic feline injection-site sarcoma cells.
Lawrence et al. Vet Comp Oncol. 2012 Jun;10(2):143-54. PMID: 22236016.
Masitinib (AB1010), a potent and selective tyrosine kinase inhibitor targeting KIT.
Dubreuil P, et al. PLoS One. 2009 Sep 30;4(9):e7258. PMID: 19789626.
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