| Name | S49076 |
| Description | S49076 is a novel and potent inhibitor of MET, AXL/MER, and FGFR1/2/3, effectively blocking cellular phosphorylation of MET, AXL, and FGFRs. |
| Cell Research | For GTL-16 and SNU-16 viability assays, cells are seeded in 96-well microplates at the appropriate density in media containing 10% FCS and supplemented 48 hours later with serial dilutions of S49076 in a final volume of 150 μL per well. After 96 hours (GTL-16) or 120 hours (SNU-16) incubation, 15 μL of a solution of 5 mg/mL MTT is added to each well and the plates are incubated for 4 hours at 37℃. The formazan metabolite is solubilized in SDS for SNU-16 and, following removal of the MTT solution, in DMSO for GTL-16. Global cell viability is estimated by measurement of optical density at 540 nm. (Only for Reference) |
| In vitro | S49076 potently blocks cellular phosphorylation of MET, AXL, and FGFRs, inhibiting downstream signaling both in vitro and in vivo. In cell models, S49076 inhibits proliferation of MET- and FGFR2-dependent gastric cancer cells, blocks MET-driven lung carcinoma cell migration, and inhibits colony formation of hepatocarcinoma cells expressing FGFR1/2 and AXL. S49076 also inhibits viability, motility, and three-dimensional colony formation of cancer cells expressing MET, AXL, or FGFRs[1]. |
| In vivo | S49076 shows marked antitumor activity in MET- and FGFR-dependent tumor xenografts at well-tolerated doses. S49076 has high distribution to tumors, in which the half-life for the dose of 3.125 mg/kg is approximately 7 hours versus less than 2 hours in the blood. At doses of 6.25 mg/kg and higher, more than 50% inhibition of MET phosphorylation is retained at 16 hours. S49076 is also active in a bevacizumab-resistant model and totally inhibits the growth of colon carcinoma xenografts in association with bevacizumab[1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 81 mg/mL (184.72 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (7.53 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
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| Keywords | TAMReceptor | TAM Receptor | S-49076 | S49076 | S 49076 | Met | Mer | Inhibitor | inhibit | HGFR | Fibroblast growth factor receptor | FGFR3 | FGFR2 | FGFR | c-Met/HGFR | cMet/HGFR | c-Met | cMet | AXL |
| Inhibitors Related | Bemcentinib | Gilteritinib | Amlexanox | Regorafenib monohydrate | Ferulic Acid | Crizotinib | Nintedanib esylate | Regorafenib | Afatinib | Formononetin | Lenvatinib | Pazopanib |
| Related Compound Libraries | Osteogenesis Compound Library | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
United States
