Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C22H22N4O4S |
| Molecular Weight | 438.499 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 1 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
O=C1CSC(=O)N1CC2=CC=C3NC(=O)\C(=C/C4=CC(CN5CCOCC5)=CN4)C3=C2
InChI
InChIKey=AREYWCZYVPSHGS-NVMNQCDNSA-N
InChI=1S/C22H22N4O4S/c27-20-13-31-22(29)26(20)12-14-1-2-19-17(8-14)18(21(28)24-19)9-16-7-15(10-23-16)11-25-3-5-30-6-4-25/h1-2,7-10,23H,3-6,11-13H2,(H,24,28)/b18-9-
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: P08581 Gene ID: 4233.0 Gene Symbol: MET Target Organism: Homo sapiens (Human) |
1.0 nM [IC50] | ||
Target ID: P30530 Gene ID: 558.0 Gene Symbol: AXL Target Organism: Homo sapiens (Human) |
7.0 nM [IC50] | ||
Target ID: Q12866 Gene ID: 10461.0 Gene Symbol: MERTK Target Organism: Homo sapiens (Human) |
2.0 nM [IC50] | ||
Target ID: CHEMBL2095217 |
|||
Target ID: CHEMBL4895 |
7.0 nM [IC50] | ||
| 1.0 nM [IC50] | |||
| 18.0 nM [IC50] | |||
Target ID: CHEMBL4142 |
17.0 nM [IC50] | ||
Target ID: CHEMBL2742 |
15.0 nM [IC50] |
PubMed
| Title | Date | PubMed |
|---|---|---|
| The MET/AXL/FGFR Inhibitor S49076 Impairs Aurora B Activity and Improves the Antitumor Efficacy of Radiotherapy. | 2017-10 |
|
| First-in-human phase I study of oral S49076, a unique MET/AXL/FGFR inhibitor, in advanced solid tumours. | 2017-08 |
|
| S49076 is a novel kinase inhibitor of MET, AXL, and FGFR with strong preclinical activity alone and in association with bevacizumab. | 2013-09 |
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| Code System | Code | Type | Description | ||
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S-49076(FREE BASE)
Created by
admin on Tue Apr 01 16:51:12 GMT 2025 , Edited by admin on Tue Apr 01 16:51:12 GMT 2025
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PRIMARY | MedKoo CAT NO: 206484, CAS NO: 1265965-22-7Description: S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3. S49076 potently blocked cellular phosphorylation of MET, AXL, and FGFRs and inhibited downstream signaling in vitro and in vivo. In cell models, S49076 inhibited the proliferation of MET- and FGFR2-dependent gastric cancer cells, blocked MET-driven migration of lung carcinoma cells, and inhibited colony formation of hepatocarcinoma cells expressing FGFR1/2 and AXL. In tumor xenograft models, a good pharmacokinetic/pharmacodynamic relationship for MET and FGFR2 inhibition following oral administration of S49076 was 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. A phase I study with S-49076 is currently underway in patients with advanced solid tumors. | ||
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1265965-22-7
Created by
admin on Tue Apr 01 16:51:12 GMT 2025 , Edited by admin on Tue Apr 01 16:51:12 GMT 2025
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65ZUU7MATU
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300000042471
Created by
admin on Tue Apr 01 16:51:12 GMT 2025 , Edited by admin on Tue Apr 01 16:51:12 GMT 2025
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49870909
Created by
admin on Tue Apr 01 16:51:12 GMT 2025 , Edited by admin on Tue Apr 01 16:51:12 GMT 2025
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ACTIVE MOIETY
SALT/SOLVATE (PARENT)
