S49076

SKU: orb1304357

Description

S49076

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1265965-22-7
• MW: 438.5
• Purity: 95.35%
• Formula: C₂₂H₂₂N₄O₄S
• SMILES: O=C1CSC(=O)N1Cc1ccc2NC(=O)\C(=C/c3cc(CN4CCOCC4)c[nH]3)c2c1
• Target: TAM Receptor,FGFR,c-Met/HGFR
• Solubility: DMSO:81 mg/mL (184.72 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (7.53 mM)

Bioactivity

• Target IC50:
  MET:1 nM|FGFR2:17 nM|Axl:7 nM|Mer:2 nM|FGFR2 (N549H):19 nM|FGFR1:18 nM|FGFR3:15 nM|FGFR1 V561M: 23 nM
• 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 whic the half-life fo the dose of 3.12 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 inhibit the growth of colon carcinoma xenografts in association with bevacizuma.
• 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 FGFR.
• Cell Research:
  For GTL-16 and SNU-16 viability assays, cells are seeded in 96-well microplates a 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 an the plates are incubated for 4 hours at 37℃he formazan metabolite is solubilized in SDS for SNU-16 and following removal o the MTT solution, in DMSO for GTL-16. Global cell viability is estimated by measurement of optical density at 540 nM. (Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

inhibit, Mer, Met, Fibroblast growth factor receptor, FGFR, FGFR3, FGFR2, Inhibitor, HGFR, c-Met/HGFR, c-Met, cMet/HGFR, cMet, AXL, S49076, S-49076, S 49076, TAMReceptor, TAM Receptor

Compound Identifiers

PubChem CID

49870909