Home Protein Tyrosine Kinase c-Met inhibitor - FGFR inhibitor - Axl inhibitor - Mertk inhibitor S49076 For research use only.

S49076

S49076 is a novel, potent inhibitor of Met (c-Met), AXL/MER, and FGFR1/2/3 with IC50 values below 20 nmol/L.

S49076 Chemical Structure

S49076 Chemical Structure

CAS: 1265965-22-7

Selleck's S49076 has been cited by 1 publication

Purity & Quality Control

Batch: S840401 DMSO] 87 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.73%
99.73

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Signaling Pathway

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c-Met Signaling Pathway

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Biological Activity

Description S49076 is a novel, potent inhibitor of Met (c-Met), AXL/MER, and FGFR1/2/3 with IC50 values below 20 nmol/L.
Targets
Met [1]
(Cell-free assay)		 Mer [1]
(Cell-free assay)		 Axl [1]
(Cell-free assay)		 FGFR3 [1]
(Cell-free assay)		 FGFR2 [1]
(Cell-free assay)		 Click to View More Targets
1 nM 2 nM 7 nM 15 nM 17 nM
In vitro
In vitro S49076 potently blocks cellular phosphorylation of MET, AXL, and FGFRs and inhibits downstream signaling in vitro and in vivo. In cell models, S49076 inhibits the proliferation of MET- and FGFR2-dependent gastric cancer cells, blocks MET-driven migration of lung carcinoma cells, and inhibits colony formation of hepatocarcinoma cells expressing FGFR1/2 and AXL. S49076 inhibits viability, motility, and three-dimensional colony formation of cancer cells expressing MET, AXL, or FGFRs[1].
Cell Research Cell lines GTL-16 and SNU-16 cell lines
Concentrations --
Incubation Time 96 h or 120 h
Method

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.
In Vivo
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].
Animal Research Animal Models Female balb/c and swiss nu/nu mice
Dosages 50 or 100 mg/kg
Administration oral administration

Chemical Information & Solubility

Molecular Weight 438.50 Formula

C22H22N4O4S
CAS No. 1265965-22-7 SDF Download S49076 SDF
Smiles C1COCCN1CC2=CNC(=C2)C=C3C4=C(C=CC(=C4)CN5C(=O)CSC5=O)NC3=O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 87 mg/mL ( (198.4 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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