S-49076
This product is for research use only, not for human use. We do not sell to patients.
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Size | Price | Stock |
---|---|---|
250mg | $1350 | Check With Us |
500mg | $1950 | Check With Us |
1g | $2925 | Check With Us |
Cat #: V2150 CAS #: 1265965-22-7 Purity ≥ 98%
Description: S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3.
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Molecular Weight (MW) | 438.50 |
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Molecular Formula | C22H22N4O4S |
CAS No. | 1265965-22-7 |
SMILES Code | O=C(N1CC2=CC3=C(NC(/C3=CC4=CC(CN5CCOCC5)=CN4)=O)C=C2)SCC1=O |
Synonyms | S-49076; S49076; S 49076. |
Protocol | In Vitro | S49076 potently blocks cellular phosphorylation of MET, AXL, and FGFRs and inhibits downstream signaling. 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. Total inhibition of MET phosphorylation is seen after 2 hours of incubation with 10 nM S49076 and an with an IC50 of 2 nM. S49076 inhibits MET phosphorylation on this site in GTL-16 gastric carcinoma cells with an IC50 value of 3 nM. The IC50 for AXL inhibition by S49076 is 56 nM. S49076 inhibits AXL signaling via AKT with an IC50 of 33 nM. |
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In Vivo | In tumor xenograft models, a good pharmacokinetic/pharmacodynamic relationship for MET and FGFR2 inhibition following oral administration of S49076 is established and correlated well with impact on tumor growth. MET, AXL, and the FGFRs have all been implicated in resistance to VEGF/VEGFR inhibitors such as bevacizumab. Combination of S49076 with bevacizumab in colon carcinoma xenograft models leads to near total inhibition of tumor growth. S49076 alone caused tumor growth arrest in bevacizumab-resistant tumors. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
Solvent volume to be added | Mass (the weight of a compound) | |||
---|---|---|---|---|
Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 2.2805 mL | 11.4025 mL | 22.8050 mL | 45.6100 mL |
5mM | 0.4561 mL | 2.2805 mL | 4.5610 mL | 9.1220 mL |
10mM | 0.2281 mL | 1.1403 mL | 2.2805 mL | 4.5610 mL |
20mM | 0.1140 mL | 0.5701 mL | 1.1403 mL | 2.2805 mL |
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Step Two: Enter the in vivo formulation
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Method for preparing in vivo formulation:
Take
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PEG300, mix and clarify, next add
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Tween 80,mix and clarify, next add
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ddH2O,mix and clarify.
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