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Masitinib

Cat. No. M1838
Masitinib Structure
Synonym:

AB1010

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 31.5  USD35 In stock
10mg USD 45  USD50 In stock
25mg USD 72  USD80 In stock
50mg USD 121.5  USD135 In stock
100mg USD 180  USD200 In stock
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Quality Control
Biological Activity

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.

Product Citations
Customer Product Validations & Biological Datas
Source Blood (2018). Figure 5. Masitinib (Abmole Bioscience)
Method BCR signaling repre
Cell Lines 923 cells lines
Concentrations 2.5 μM, 5 μM or 10 μM
Incubation Time 72 h
Results We observed a consistent reduction of the tumor mass in animals treated with masitinib
Source Res Vet Sci (2014). Figure 2. Masitinib
Method Clonogenic assays
Cell Lines JB, KH and Hamilton ISS cells
Concentrations 6 μM
Incubation Time 24 h
Results There were no differences in radiosensitivity between control cells (0 lM masitinib) and those treated with 1 μM masitinib regardless of radiation dose (JB p = 0.56; KH p = 0.7; Hamilton p = 0.11); due to these comparable findings, the assay was performed only once
Source Res Vet Sci (2014). Figure 1. Masitinib
Method Clonogenic assays
Cell Lines JB, KH and Hamilton ISS cells
Concentrations 6 μM
Incubation Time 24 h
Results For each cell line, there were no significant differences in ISS radiosensitivity between control cells (0 μM masitinib) and those treated with 6 μM masitinib at any radiation dose (JB p = 0.11; KH p = 0.07; Hamilton p = 0.8)
Protocol
Cell Experiment
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.
Concentrations 0~10 μM
Incubation time 48 h
Animal Experiment
Animal models Ba/F3 Δ27 tumour model in Female MBRI Nu/Nu mice
Formulation placebo
Dosages 10, 30, or 45 mg/kg twice daily for 10 days
Administration orally
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 498.64
Formula C28H30N6OS
CAS Number 790299-79-5
Purity 99.87%
Solubility DMSO ≥100 mg/mL
Storage at -20°C
References

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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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Masitinib, AB1010 supplier, VEGFR/PDGFR, inhibitors

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