midostaurin
Midostaurin is a small molecule that inhibits multiple receptor tyrosine kinases. In vitro biochemical or cellular assays have shown that midostaurin or its major human active metabolites CGP62221 and CGP52421 inhibit the activity of wild type FLT3, FLT3 mutant kinases (ITD and TKD), KIT (wild type and D816V mutant), PDGFR-alfa/beta, VEGFR2, as well as members of the serine/threonine kinase PKC (protein kinase C) family. Midostaurin demonstrated the ability to inhibit FLT3 receptor signaling and cell proliferation, and it induced apoptosis in leukemic cells expressing ITD and TKD mutant FLT3 receptors or overexpressing wild type FLT3 and PDGF receptors. Midostaurin also demonstrated the ability to inhibit KIT signaling, cell proliferation and histamine release and induce apoptosis in mast cells.
Ligand Summary
UNII: ID912S5VON
PubChem: 9829523
Guide to Pharmacology: 5702
ChEMBL: CHEMBL608533
DrugCentral: 5231
LyCHI: GKJ653JJL4Q5
Target Activities
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1 – 10 of 18
FLT3
Receptor-type tyrosine-protein kinase FLT3
20 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.82 | Blood, (2009) 114:14:2984 | ||||
Kd | 7.82 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.82 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
IC50 | 7.89 | Blood, (2009) 114:14:2984 | ||||
Kd | 7.92 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.96 | Blood, (2009) 114:14:2984 | ||||
Kd | 7.96 | Blood, (2009) 114:14:2984 | ||||
Kd | 7.96 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.96 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.96 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
MARK3
MAP/microtubule affinity-regulating kinase 3
4 Activities
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1 – 4 of 4
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.68 | Blood, (2009) 114:14:2984 | ||||
Kd | 7.68 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.68 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.68 | |||||
PKN1
Serine/threonine-protein kinase N1
4 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 8.03 | Blood, (2009) 114:14:2984 | ||||
Kd | 8.03 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 8.03 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 8.03 | |||||
PKN2
Serine/threonine-protein kinase N2
4 Activities
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1 – 4 of 4
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.82 | Blood, (2009) 114:14:2984 | ||||
Kd | 7.82 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.82 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.82 | |||||
MAP3K9
Mitogen-activated protein kinase kinase kinase 9
4 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.82 | Blood, (2009) 114:14:2984 | ||||
Kd | 7.82 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.82 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.82 | |||||
CAMK2A
Calcium/calmodulin-dependent protein kinase type II subunit alpha
4 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.7 | Blood, (2009) 114:14:2984 | ||||
Kd | 7.7 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.7 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.7 | |||||
MAP3K11
Mitogen-activated protein kinase kinase kinase 11
4 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.77 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.77 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.77 | J. Med. Chem., (2013) 56:20:8032 | ||||
Kd | 7.77 | |||||
KIT
Mast/stem cell growth factor receptor Kit
4 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.8 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 8.11 | Eur. J. Med. Chem., (2011) 46:6:2043 | ||||
Kd | 8.11 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 8.11 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
TBK1
Serine/threonine-protein kinase TBK1
3 Activities
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1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 8.03 | Blood, (2009) 114:14:2984 | ||||
Kd | 8.03 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 8.03 | |||||
MAP3K19
Mitogen-activated protein kinase kinase kinase 19
3 Activities
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1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.82 | Blood, (2009) 114:14:2984 | ||||
Kd | 7.82 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.82 | |||||