crizotinib
Crizotinib is an inhibitor of receptor tyrosine kinases including ALK, Hepatocyte Growth Factor Receptor (HGFR, c-Met), ROS1 (c-ros), and Recepteur d'Origine Nantais (RON). Translocations can affect the ALK gene resulting in the expression of oncogenic fusion proteins. The formation of ALK fusion proteins results in activation and dysregulation of the gene's expression and signaling which can contribute to increased cell proliferation and survival in tumors expressing these proteins. Crizotinib demonstrated concentration-dependent inhibition of ALK, ROS1, and c-Met phosphorylation in cell-based assays using tumor cell lines and demonstrated antitumor activity in mice bearing tumor xenografts that expressed echinoderm microtubule-associated protein-like 4 (EML4)- or nucleophosmin (NPM)-ALK fusion proteins or c-Met.
Ligand Summary
UNII: 53AH36668S
PubChem: 11626560
Guide to Pharmacology: 4903
ChEMBL: CHEMBL601719
DrugCentral: 4187
LyCHI: C52GL3ADX4W8
Target Activities
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10
1 – 10 of 13
MET
Hepatocyte growth factor receptor
26 Activities
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1 – 10 of 26
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.7 | ACS Med. Chem. Lett., (2013) 4:8:806 | ||||
IC50 | 7.7 | ACS Med. Chem. Lett., (2013) 4:8:806 | ||||
IC50 | 7.8 | Eur. J. Med. Chem., (2016) 108:None:495 | ||||
IC50 | 7.96 | Eur. J. Med. Chem., (2015) 90:None:195 | ||||
IC50 | 8.1 | Bioorg. Med. Chem. Lett., (2010) 20:4:1405 | ||||
IC50 | 8.1 | J. Med. Chem., (2011) 54:18:6342 | ||||
IC50 | 8.1 | Proc. Natl. Acad. Sci. U.S.A., (2007) 104:50:19936 | ||||
IC50 | 8.1 | ACS Med. Chem. Lett., (2015) 6:5:507 | ||||
IC50 | 8.15 | Eur. J. Med. Chem., (2015) 95:None:302 | ||||
IC50 | 8.4 | Eur. J. Med. Chem., (2011) 46:9:3675 | ||||
ALK
ALK tyrosine kinase receptor
19 Activities
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1 – 10 of 19
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.55 | ACS Med. Chem. Lett., (2014) 5:4:304 | ||||
IC50 | 7.6 | Eur J Med Chem, (2016) 123:None:80 | ||||
IC50 | 7.62 | Eur. J. Med. Chem., (2015) 90:None:195 | ||||
IC50 | 7.7 | J. Med. Chem., (2011) 54:18:6342 | ||||
IC50 | 7.7 | Proc. Natl. Acad. Sci. U.S.A., (2007) 104:50:19936 | ||||
IC50 | 7.86 | J. Med. Chem., (2015) 58:1:197 | ||||
Ki | 8.09 | J. Med. Chem., (2014) 57:4:1170 | ||||
Ki | 8.09 | J. Med. Chem., (2014) 57:11:4720 | ||||
IC50 | 8.13 | None, (2016) None:None:None | ||||
IC50 | 8.3 | J. Med. Chem., (2013) 56:17:6991 | ||||
ROS1
Proto-oncogene tyrosine-protein kinase ROS
3 Activities
ABL1
Tyrosine-protein kinase ABL1
3 Activities
AXL
Tyrosine-protein kinase receptor UFO
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 8.11 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 8.11 | |||||
EPHB6
Ephrin type-B receptor 6
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 8.22 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 8.22 | |||||
MST1R
Macrophage-stimulating protein receptor
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.6 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.6 | |||||
SLK
STE20-like serine/threonine-protein kinase
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.75 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.74 | |||||
MERTK
Tyrosine-protein kinase Mer
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 8.44 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 8.44 | |||||
LTK
Leukocyte tyrosine kinase receptor
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.92 | Nat. Biotechnol., (2011) 29:11:1046 | ||||