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MedChemExpress - Model SAR125844 -1116743-46-4
SAR125844 is a potent, selective, and ATP-competitive MET kinase inhibitor with the value of IC50 is 4.2 nM and Ki is 2.8 nM. SAR125844 has antitumor activity and can be used for the research of cancer[1][2][3].MCE products for research use only. We do not sell to patients.
SAR125844
MCE China：SAR125844
Brand：MedChemExpress (MCE)
Cat. No.HY-16446
CAS：1116743-46-4
Purity：98.17%
Storage：Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Shipping：Room temperature in continental US; may vary elsewhere.
Description：SAR125844 is a potent, selective, and ATP-competitive MET kinase inhibitor with the value of IC50 is 4.2 nM and Ki is 2.8 nM. SAR125844 has antitumor activity and can be used for the research of cancer.
In Vitro：SAR125844 (1-10000 nM, 96 h) inhibits proliferation in H-460 cells, HCT116 cells, H1993 cells, EBC-1 cells, SNU-5 cells, OE33 cells, Hs 746T cells and MKN-45 cells[1]. SAR125844 (1-300 nM, 24 72 h) promotes apoptosis in SNU-5 cells[1]. SAR125844 (3-1000 nM, 20 h) inhibits HGF-mediated tumor cell migration in PC-3 cells[1].
In Vivo：SAR125844 (45 mg/kg, Intravenous injection, single dose) results in tumor regression in SNU-5 and Hs 746T tumor-bearing mice[1]. SAR125844 (20 mg/kg, Intravenous injection, o single dose) nanoformulation results in long duration pharmacodynamic impact and tumor regression in MET-amplified gastric tumor models[1]. SAR125844 (20 mg/kg, Intravenous injection, single dose) shows MET kinase inhibition was complete at 4 h (96%), significant at 24 h (80%), and partial at 48 h (61%) in mice bearing xenograft tumor of the MET-amplified Hs 746T human gastric tumor cell line[3].
IC50 & Target：c-Met
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References：
[1]. Egile C, et al. The selective intravenous inhibitor of the MET tyrosine kinase SAR125844 inhibits tumor growth in MET-amplified cancer [J]. Molecular cancer therapeutics, 2015, 14(2): 384-394. [Content Brief]
[2]. Angevin E, et al. A first-in-human phase I study of SAR125844, a selective MET tyrosine kinase inhibitor, in patients with advanced solid tumours with MET amplification [J]. European Journal of Cancer, 2017, 87: 131-139. [Content Brief]
[3]. Ugolini A, et al. Discovery and pharmacokinetic and pharmacological properties of the potent and selective MET kinase inhibitor 1-{6-[6-(4-fluorophenyl)-[1, 2, 4] triazolo [4, 3-b] pyridazin-3-ylsulfanyl] benzothiazol-2-yl}-3-(2-morpholin-4-ylethyl) urea (SAR125844) [J]. 2016. [Content Brief]
[4]. Egile C, et al. The selective intravenous inhibitor of the MET tyrosine kinase SAR125844 inhibits tumor growth in MET-amplified cancer. Mol Cancer Ther. 2015 Feb;14(2):384-94. [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。