High Quality AB1010 Masitinib 98% CAS 790299-79-5

Payment Type: L/C,T/T,Paypal
Incoterm: FOB,CIF
Min. Order: 10 Gram
Delivery Time: 3 Days

Basic Info

Model No.: CAS 790299-79-5

Additional Info

Packaging: 10g 100g 1kg

Productivity: 100 kg/month

Brand: cy

Transportation: Ocean,Land,Air

Place of Origin: China

Supply Ability: 50kg

Certificate: ISO 9001, GMP

Port: QINGDAO,SHANGHAI

Product Description

Masitinib, also known as AB1010, is an orally bioavailable and multi-targeted protein tyrosine kinase inhibitor with potential antineoplastic activity. Masitinib selectively binds to and inhibits both the wild-type and mutated forms of the stem cell factor receptor (c-Kit; SCFR); platelet-derived growth factor receptor (PDGFR); fibroblast growth factor receptor 3 (FGFR3); and, to a lesser extent, focal adhesion kinase (FAK). As a consequence, tumor cell proliferation may be inhibited in cancer cell types that overexpress these receptor tyrosine kinases (RTKs). Masitinib was approved for veterinary use.


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Properties:
Density: 1.281 g/cm3
Melting Point: 90-95ºC
Refractive Index: 1.682
Storage Condition: Refrigerator

Function and Applition 

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Masitinib is a competitive inhibitor against ATP at concentrations ≤500 nM. Masitinib also potently inhibits recombinant PDGFR and the intracellular kinase Lyn, and to a lesser extent, fibroblast growth factor receptor 3. In contrast, Masitinib demonstrates weak inhibition of Abl and c-Fms. Masitinib more strongly inhibits degranulation, cytokine production, and bone marrow mast cell migration than imatinib. In Ba/F3 cells expressing human wild-type Kit, Masitinib inhibits SCF (stem cell factor)-induced cell proliferation with an IC50 of 150 nM, while the IC50 for inhibition of IL-3-stimulated proliferation is at approximately >10 µM. In Ba/F3 cells expressing PDGFRα, Masitinib inhibits PDGF-BB-stimulated proliferation and PDGFRα tyrosine phosphorylation with IC50 of 300 nM. Masitinib also causes inhibition of SCF-stimulated tyrosine phosphorylation of human Kit in mastocytoma cell-lines and BMMC. Masitinib inhibits Kit gain-of-function mutants, including V559D mutant and Δ27 mouse mutant with IC50 of 3 and 5 nM in Ba/F3 cells. Masitinib inhibits the cell proliferation of mastocytoma cell lines including HMC-1α155 and FMA3 with IC50 of 10 and 30 nM, respectively. Masitinib inhibits cell growth and PDGFR phosphorylation in two novel ISS cell lines, which suggest that Masitinib displays activity against both primary and metastatic ISS cell line and may aid in the clinical management of ISS.

Contact Information

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Contact Person: Jerry

Phone:86-0531-18560179988

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Address: No.215 Beiyuan Main street,tianqiao District,Jinan,Shandong

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