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MedChemExpress - Model Linifanib -796967-16-3
Linifanib (ABT-869) is a potent and orally active multi-target inhibitor of VEGFR and PDGFR family with IC50s of 4, 3, 66, and 4 nM for KDR, FLT1, PDGFRβ, and FLT3, respectively. Linifanib shows prominent antitumor activity. Linifanib has much less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases. Linifanib is a specific miR-10b inhibitor that blocks miR-10b biogenesis[1][2].MCE products for research use only. We do not sell to patients.
Linifanib
MCE China：Linifanib
Brand：MedChemExpress (MCE)
Cat. No.HY-50751
CAS：796967-16-3
Synonyms：ABT-869; AL-39324
Purity：99.05%
Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Shipping：Room temperature in continental US; may vary elsewhere.
Description：Linifanib (ABT-869) is a potent and orally active multi-target inhibitor of VEGFR and PDGFR family with IC50s of 4, 3, 66, and 4 nM for KDR, FLT1, PDGFRβ, and FLT3, respectively. Linifanib shows prominent antitumor activity. Linifanib has much less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases. Linifanib is a specific miR-10b inhibitor that blocks miR-10b biogenesis.
In Vitro：Linifanib (0-10000 nM; 72 hours) inhibits in vitro the cell proliferation of 8305C and 8505C cell lines in a concentration-dependent manner[3]. Linifanib significantly decreased the levels of phospho-CSF-1R after 24 h and 72 h in both 8505C and 8305C cells[3].
In Vivo：The synergistic ATC antitumor activity of linifanib (10 mg/kg; p.o.; daily for 33 days)/Irinotecan combination significantly increases the survival of ATC affected mice and induces some complete responses[3].
IC50 & Target：Flt-1 3 nM (IC50) KDR 4 nM (IC50) PDGFRβ 66 nM (IC50) FLT3 4 nM (IC50) CSF-1R 3 nM (IC50) Kit 14 nM (IC50)
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References：
[1]. Albert DH, et al. Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor. Mol Cancer Ther, 2006, 5(4), 995-1006. [Content Brief]
[2]. Monroig-Bosque PDC, et al. OncomiR-10b hijacks the small molecule inhibitor linifanib in human cancers. Sci Rep. 2018;8(1):13106. Published 2018 Aug 30. [Content Brief]
[3]. Banchi M, et al. Synergistic activity of linifanib and irinotecan increases the survival of mice bearing orthotopically implanted human anaplastic thyroid cancer. Am J Cancer Res. 2020;10(7):2120-2127. Published 2020 Jul 1. [Content Brief]
Brand introduction:
• MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
• More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
• The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects；
• Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services；
• It has a professional experimental center and strict quality control and verification system；
• Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products；
• The biological activity of the products has been verified by the experiments of customers in various countries；
• A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers；
• Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world；
• It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。