Masitinib (AB1010) 790299-79-5
Product Description
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Molecular Weight:
498.64 Masitinib is a novel inhibitor for Kit and PDGFRα/β with IC50 of 200 nM and 540 nM/800 nM, weak inhibition to ABL and c-Fms. Phase 3.
Biological Activity
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.
Masitinib inhibits tumour growth and increases the median survival time
in Δ27-expressing Ba/F3 tumor models at 30 mg/kg, without cardiotoxicity
or genotoxicity. Masitinib (12.5 mg/kg/d PO) increases overall TTP (time-to-tumor progression) compared with placebo in dogs. The combination of masitinib/gemcitabine shows synergy in vitro on
proliferation of gemcitabine-refractory cell lines Mia Paca2 and Panc1,
and to a lesser extent on Mia Paca-2 pancreatic tumours in Nog CID mice.
Contact us if you need more details on 790299-79-5. We are ready to answer your questions on packaging, logistics, certification or any other aspects about Masitinib 790299-79-5、AB1010 790299-79-5. If these products fail to match your need, please contact us and we would like to provide relevant information.
Molecular Weight:
498.64 Masitinib is a novel inhibitor for Kit and PDGFRα/β with IC50 of 200 nM and 540 nM/800 nM, weak inhibition to ABL and c-Fms. Phase 3.
Biological Activity
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.
Masitinib inhibits tumour growth and increases the median survival time
in Δ27-expressing Ba/F3 tumor models at 30 mg/kg, without cardiotoxicity
or genotoxicity. Masitinib (12.5 mg/kg/d PO) increases overall TTP (time-to-tumor progression) compared with placebo in dogs. The combination of masitinib/gemcitabine shows synergy in vitro on
proliferation of gemcitabine-refractory cell lines Mia Paca2 and Panc1,
and to a lesser extent on Mia Paca-2 pancreatic tumours in Nog CID mice.
Contact us if you need more details on 790299-79-5. We are ready to answer your questions on packaging, logistics, certification or any other aspects about Masitinib 790299-79-5、AB1010 790299-79-5. If these products fail to match your need, please contact us and we would like to provide relevant information.
Product Categories : Protein Tyrosine Kinase > c-Kit Inhibitor
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