All AbMole products are for research use only, cannot be used for human consumption.
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.
bioRxiv. 2021 May 23;445261.
Non-coding NFKBIZ 3′ UTR mutations promote cell growth and resistance to targeted therapeutics in diffuse large B-cell lymphoma
Masitinib purchased from AbMole
Blood. 2018 May 24;131(21):2345-2356.
Pan-SRC kinase inhibition blocks B-cell receptor oncogenic signaling in non-Hodgkin lymphoma.
Masitinib purchased from AbMole
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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 |
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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) |
| 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 |
| Molecular Weight | 498.64 |
| Formula | C28H30N6OS |
| CAS Number | 790299-79-5 |
| Solubility (25°C) | DMSO ≥100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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