Free shipping on all orders over $ 500

Masitinib

Cat. No. M1838
Masitinib Structure
Synonym:

AB1010

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 30  USD30 In stock
10mg USD 40  USD40 In stock
25mg USD 80  USD80 In stock
50mg USD 115  USD115 In stock
100mg USD 175  USD175 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

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

[1] Klopfleisch et al. BMC Vet Res. Transcriptome and proteome analysis of tyrosine Kinase inhibitor treated canine mast cell tumour cells identifies potentially kit signaling-dependent genes.

[2] Lyles et al. Vet Comp Oncol. In vitro effects of the tyrosine kinase inhibitor, masitinib mesylate, on canine hemangiosarcoma cell lines.

[3] Lee-Fowler et al. Int Arch Allergy Immunol. The tyrosine kinase inhibitor masitinib blunts airway inflammation and improves associated lung mechanics in a feline model of chronic allergic asthma.

[4] Georgin-Lavialle et al. Eur J Haematol. Mast cell leukemia: identification of a new c-Kit mutation, dup(501-502), and response to masitinib, a c-Kit tyrosine kinase inhibitor.

[5] Lawrence et al. Vet Comp Oncol. Masitinib demonstrates anti-proliferative and pro-apoptotic activity in primary and metastatic feline injection-site sarcoma cells.

[6] Dubreuil P, et al. PLoS One. Masitinib (AB1010), a potent and selective tyrosine kinase inhibitor targeting KIT.

Related VEGFR/PDGFR Products
Pamufetinib

Pamufetinib (TAS-115) is a highly potent inhibitor of both C-MET and VEGFR, with IC50 of 30 nM and 32 nM against recombinant VEGFR2 and VEGFR, respectively.

Chiauranib

Chiauranib (CS2164) is a multi-target inhibitor with oral activity against tumor angiogenesis. Chiauranib effectively inhibits angiogenesis-associated kinases (VEGFR1, VEGFR2, VEGFR3, PDGFRα and c-Kit), mitosis-associated kinase Aurora B, and chronic inflammation-associated kinase CSF-1R,IC50 The value is 1-9 nM. Chiauranib has a strong anti-cancer effect.

TAS-115 mesylate

TAS-115 (Pamufetinib) mesylate inhibited the kinase activity of both VEGFR2 and MET and their signal-dependent cell growth as strongly as other known VEGFR or MET inhibitors.

Ningetinib

Ningetinib is a potent, orally bioavailable tyrosine kinase inhibitor for Axl, VEGFR2 and c-Met with IC50 values of <1.0, 1.9 and 6.7 nM, respectively.

Tanshinone IIA

Tanshinone IIA suppresses angiogenesis by targeting the protein kinase domains of VEGF/VEGFR2. *The compound is unstable in solutions, freshly prepared is recommended.

  Catalog
Abmole Inhibitor Catalog 2017




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

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.