| Drug General Information |
| Drug ID |
D0N8RV
|
| Former ID |
DCL000352
|
| Drug Name |
OSI-930
|
| Synonyms |
OSI 930; OSI930; OSI-930 is a multi-targeted tyrosine kinase inhibitor; 3-(quinolin-4-ylmethylamino)-N-[4-(trifluoromethoxy)phenyl]thiophene-2-carboxamide
|
| Drug Type |
Small molecular drug
|
| Indication |
Solid tumours [ICD9: 140-199, 210-229; ICD10:C00-D48]
|
Phase 1 |
[1],
[2]
|
|---|
| Therapeutic Class |
Anticancer Agents
|
| Company |
OSI Pharmaceuticals
|
| Structure |
|
Download
2D MOL
3D MOL
|
| Formula |
C22H16F3N3O2S
|
| Canonical SMILES |
C1=CC=C2C(=C1)C(=CC=N2)CNC3=C(SC=C3)C(=O)NC4=CC=C(C=C4)<br />OC(F)(F)F
|
| InChI |
1S/C22H16F3N3O2S/c23-22(24,25)30-16-7-5-15(6-8-16)28-21(29)20-19(10-12-31-20)27-13-14-9-11-26-18-4-2-1-3-17(14)18/h1-12,27H,13H2,(H,28,29)
|
| InChIKey |
FGTCROZDHDSNIO-UHFFFAOYSA-N
|
| PubChem Compound ID |
|
| PubChem Substance ID |
14832924, 24159478, 45290301, 50086917, 76827455, 99437032, 124757092, 125163896, 126671661, 131480731, 134339004, 135261678, 136367364, 136920358, 136933680, 136960901, 137276003, 142845297, 144116325, 152258120, 160646959, 162011684, 162037502, 162202664, 174530503, 177748914, 180386841, 186007038, 188899584, 198968760, 223679984, 223704833, 226933716, 242059898, 248747184, 251971154, 252160242, 252215971, 252451811
|
| Target and Pathway |
| Target(s) |
Vascular endothelial growth factor receptor 2 |
Target Info |
Modulator |
[1],
[2]
|
|---|
| Mast/stem cell growth factor receptor |
Target Info |
Modulator |
[1],
[2]
|
|
KEGG Pathway
|
Ras signaling pathway
|
|
Rap1 signaling pathway
|
|
Cytokine-cytokine receptor interaction
|
|
Endocytosis
|
|
PI3K-Akt signaling pathway
|
|
VEGF signaling pathway
|
|
Focal adhesion
|
|
Proteoglycans in cancerhsa04014:Ras signaling pathway
|
|
Hematopoietic cell lineage
|
|
Melanogenesis
|
|
Pathways in cancer
|
|
Acute myeloid leukemia
|
|
Central carbon metabolism in cancer
|
|
NetPath Pathway
|
IL2 Signaling PathwayNetPath_15:IL3 Signaling Pathway
|
|
IL4 Signaling Pathway
|
|
KitReceptor Signaling Pathway
|
|
PANTHER Pathway
|
Angiogenesis
|
|
VEGF signaling pathway
|
|
Pathway Interaction Database
|
HIF-2-alpha transcription factor network
|
|
Beta3 integrin cell surface interactions
|
|
Signaling events mediated by TCPTP
|
|
SHP2 signaling
|
|
S1P1 pathway
|
|
VEGF and VEGFR signaling network
|
|
Integrins in angiogenesis
|
|
Signaling events mediated by VEGFR1 and VEGFR2
|
|
Notch-mediated HES/HEY networkcmyb_pathway:C-MYB transcription factor network
|
|
Signaling events mediated by Stem cell factor receptor (c-Kit)
|
|
Reactome
|
Neurophilin interactions with VEGF and VEGFR
|
|
VEGF binds to VEGFR leading to receptor dimerization
|
|
Integrin cell surface interactions
|
|
EPHA-mediated growth cone collapse
|
|
VEGFA-VEGFR2 Pathway
|
|
VEGFR2 mediated cell proliferationR-HSA-1257604:PIP3 activates AKT signaling
|
|
Regulation of KIT signaling
|
|
Constitutive Signaling by Aberrant PI3K in Cancer
|
|
RAF/MAP kinase cascade
|
|
WikiPathways
|
Focal Adhesion
|
|
Nifedipine Activity
|
|
Cardiac Progenitor Differentiation
|
|
Signaling by VEGF
|
|
AngiogenesisWP304:Kit receptor signaling pathway
|
|
Differentiation Pathway
|
|
Signaling by SCF-KIT
|
|
PIP3 activates AKT signaling
|
|
miR-targeted genes in muscle cell - TarBase
|
|
miR-targeted genes in lymphocytes - TarBase
|
|
miR-targeted genes in epithelium - TarBase
|
| References |
| REF 1 | Inhibition of c-Kit, VEGFR-2 (KDR), and ABCG2 by analogues of OSI-930. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6495-9. |
|---|
| REF 2 | OSI-930 analogues as novel reversal agents for ABCG2-mediated multidrug resistance. Biochem Pharmacol. 2012 Sep 15;84(6):766-74. |
|---|
