|Place of Origin:||CHINA|
|Certification:||GMP , ISO 9001:2008|
|Minimum Order Quantity:||10g|
|Packaging Details:||Disguised Package|
|Delivery Time:||2 Working Days|
|Payment Terms:||Bank Transfer - Bitcoin - Western Union - MoneyGram|
|Supply Ability:||100 KG/Month|
|Appearance:||White Powder||Usage:||Nootropics Drug|
|Shipping Method:||EMS, HKEMS, FEDEX, DHL, UPS, Aramex, ETC||Synonym:||AB 1010|
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|Product Description||Masitinib also known as Masivet, AB1010 is a tyrosine kinase, c-Kit, PDGFR, FGFR3, the FAK pathway inhibitor with IC50 of 15080, 20040 nM.|
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 M. In Ba/F3 cells expressing PDGFR, Masitinib inhibits PDGF-BB-stimulated proliferation and PDGFR 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 27 mouse mutant with IC50 of 3 and 5 nM in Ba/F3 cells. Masitinib inhibits the cell proliferation of mastocytoma cell lines including HMC-1155 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.
Masitinib aims to slow progression of ALS by reducing inflammation. A kinase inhibitor, masitinib blocks mast cell-mediated degranulation, the release of cytotoxic substances that might further damage the motor nerves. Marketed by AB Science under the name Kinavet, masitinib is currently being used to treat certain cancers in dogs. It is important to note that the company is also exploring the use of its kinase inhibitor in many other diseases, such as multiple sclerosis, Alzheimer’s and different types of cancer, among others.
Masitinib is a potent and selective tyrosine kinase inhibitor targeting KIT that is active, orally bioavailable in vivo, and has low toxicity. Phase II clinical trials demonstrate that Masitinib appears to be effective as a first-line treatment of advanced GIST with comparable results to imatinib in terms of safety and response. PFS and in particular OS data show promise that masitinib may provide sustainable benefits.
Masitinib, also known as methotrexate masitinib, is studied and developed by the AB Science, a platelet-derived growth factor alpha/beta receptor tyrosine kinase inhibitor for the treatment of multiple myeloma, gastrointestinal stromal tumors and prostate cancer. The drug had respectively, been entitled by FDA for the treatment of pancreatic cancer and ALS orphans disease in 2009 and 2015. On August 8, 2016, it has qualified as EMA orphan drug.
Masitinib is a novel kind of oral administrated tyrosine kinase inhibitors that could be targeted to immunizing important cellular mast cells and macrophages by inhibiting a certain amount of kinase. Based on its unique mechanism of action, masitinib can be developed for application in tumors, inflammatory diseases and certain central nervous system diseases. In the oncology, due to its immunotherapy effect, Masitinib may affect the survival period of cancer patients (single administration or in combination with chemotherapy).
By acting on mast cells and microglia, and further inhibiting the activation of the inflammatory process, Masitinib is effective against certain inflammatory, central nervous system disorders as well as symptoms associated with degeneration of these diseases.
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