Home Protein Tyrosine Kinase c-Met inhibitor S49076

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S49076 c-Met inhibitor

Cat.No.S8404

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

Chemical Structure

Molecular Weight: 438.50

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 87 mg/mL (198.4 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 438.50 Formula

C22H22N4O4S

 Storage (From the date of receipt)
CAS No. 1265965-22-7 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1COCCN1CC2=CNC(=C2)C=C3C4=C(C=CC(=C4)CN5C(=O)CSC5=O)NC3=O

Mechanism of Action

Targets/IC50/Ki
Met
(Cell-free assay)
1 nM
Mer
(Cell-free assay)
2 nM
Axl
(Cell-free assay)
7 nM
FGFR3
(Cell-free assay)
15 nM
FGFR2
(Cell-free assay)
17 nM
FGFR1
(Cell-free assay)
18 nM
In vitro
S49076 potently blocks cellular phosphorylation of MET, AXL, and FGFRs and inhibits downstream signaling in vitro and in vivo. In cell models, this compound 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. It inhibits viability, motility, and three-dimensional colony formation of cancer cells expressing MET, AXL, or FGFRs.
In vivo
S49076 shows marked antitumor activity in MET- and FGFR-dependent tumor xenografts at well-tolerated doses. This compound 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. It is also active in a bevacizumab-resistant model and totally inhibits the growth of colon carcinoma xenografts in association with bevacizumab.
References

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