Masitinib

  Cat. No.:  DC7460   Featured
Masitinib
Chemical Structure
790299-79-5
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More than 5000 active chemicals with high quality for research!
Field of application
Masitinib is a broad coronavirus 3CL inhibitor that effectively blocks replication of SARS-CoV-2. Science 20 Jul 2021: eabg5827 DOI: 10.1126/science.abg5827
Cas No.: 790299-79-5
Chemical Name: N-(4-methyl-3-(4-(pyridin-3-yl)thiazol-2-ylamino)phenyl)-4-((4-methylpiperazin-1-yl)methyl)benzamide
Synonyms: AB1010; AB-1010; AB 1010
SMILES: CC1=C(C=C(C=C1)NC(=O)C2=CC=C(C=C2)CN3CCN(CC3)C)NC4=NC(=CS4)C5=CN=CC=C5
Formula: C28H30N6Os
M.Wt: 498.64
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: Masitinib is a broad coronavirus 3CL inhibitor that effectively blocks replication of SARS-CoV-2. Science 20 Jul 2021: eabg5827 DOI: 10.1126/science.abg5827
Description: 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璖CID mice. For the detailed information of Mastinib, the solubility of Mastinib in water, the solubility of Mastinib in DMSO, the solubility of Mastinib in PBS buffer, the animal experiment (test) of Mastinib, the cell expriment (test) of Mastinib, the in vivo, in vitro and clinical trial test of Mastinib, the EC50, IC50,and Affinity of Mastinib, Please contact DC Chemicals.
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MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC7460 Masitinib Masitinib is a broad coronavirus 3CL inhibitor that effectively blocks replication of SARS-CoV-2. Science 20 Jul 2021: eabg5827 DOI: 10.1126/science.abg5827