regorafenib
Regorafenib is a small molecule inhibitor of multiple membrane-bound and intracellular kinases involved in normal cellular functions and in pathologic processes such as oncogenesis, tumor angiogenesis, metastasis and tumor immunity. In in vitro biochemical or cellular assays, regorafenib or its major human active metabolites M-2 and M-5 inhibited the activity of RET, VEGFR1, VEGFR2, VEGFR3, KIT, PDGFR-alpha, PDGFR-beta, FGFR1, FGFR2, TIE2, DDR2, TrkA, Eph2A, RAF-1, BRAF, BRAF V600E, SAPK2, PTK5, Abl and CSF1R at concentrations of regorafenib that have been achieved clinically. In in vivo models, regorafenib demonstrated anti-angiogenic activity in a rat tumor model and inhibition of tumor growth in several mouse xenograft models including some for human colorectal carcinoma, gastrointestinal stromal and hepatocellular carcinoma. Regorafenib also demonstrated anti-metastatic activity in a mouse xenograft model and two mouse orthotopic models of human colorectal carcinoma.
Ligand Summary
UNII: 24T2A1DOYB
PubChem: 11167602
Guide to Pharmacology: 5891
ChEMBL: CHEMBL1946170
DrugCentral: 4654
LyCHI: 3HJ7GSS5ADN3
Target Activities
BRAF
Serine/threonine-protein kinase B-raf
5 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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IC50 | 7.55 | |||||
IC50 | 8.82 | Eur J Med Chem, (2019) 179:None:707 | ||||
IC50 | 7.72 | Bioorg. Med. Chem. Lett., (2012) 22:2:789 | ||||
IC50 | 7.55 | Bioorg. Med. Chem. Lett., (2012) 22:2:789 | ||||
IC50 | 7.55 | INHIBITOR | ||||
KDR
Vascular endothelial growth factor receptor 2
5 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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IC50 | 7.9 | |||||
IC50 | 8.38 | Eur J Med Chem, (2019) 179:None:916 | ||||
IC50 | 8.38 | Eur J Med Chem, (2019) 168:None:315 | ||||
IC50 | 8.3 | Eur J Med Chem, (2019) 179:None:707 | ||||
IC50 | 7.9 | INHIBITOR | ||||
EPHX2
Bifunctional epoxide hydrolase 2
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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IC50 | 9.3 | Bioorg. Med. Chem. Lett., (2013) 23:13:3732 | ||||
IC50 | 9.3 | INHIBITOR | ||||
FLT1
Vascular endothelial growth factor receptor 1
2 Activities
RAF1
RAF proto-oncogene serine/threonine-protein kinase
1 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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IC50 | 8.82 | Eur J Med Chem, (2019) 179:None:707 | ||||
PDGFRB
Platelet-derived growth factor receptor beta
1 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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IC50 | 8.82 | Eur J Med Chem, (2019) 179:None:707 | ||||
KIT
Mast/stem cell growth factor receptor Kit
1 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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IC50 | 8.21 | J Med Chem, (2017) 60:21:8801 | ||||
FGFR1
Fibroblast growth factor receptor 1
1 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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IC50 | 8.82 | Eur J Med Chem, (2019) 179:None:707 | ||||
BCR
Breakpoint cluster region protein
1 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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Kd | 6.13 | Science, (2017) 358:6367:None | ||||
GLRA1
Glycine receptor subunit alpha-1
1 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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EC50 | 5.75 | J. Med. Chem., (2015) 58:7:2958 | ||||
TEK
Angiopoietin-1 receptor
1 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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IC50 | 8.82 | Eur J Med Chem, (2019) 179:None:707 | ||||
EPHA1
Ephrin type-A receptor 1
1 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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Kd | 8.15 | Science, (2017) 358:6367:None | ||||