Drug Information

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 [531624], [531955]
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
9868037
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 [531624], [531955]
Mast/stem cell growth factor receptor Target Info Modulator [531624], [531955]
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 531624Inhibition 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 531955OSI-930 analogues as novel reversal agents for ABCG2-mediated multidrug resistance. Biochem Pharmacol. 2012 Sep 15;84(6):766-74.
Ref 531624Inhibition 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 531955OSI-930 analogues as novel reversal agents for ABCG2-mediated multidrug resistance. Biochem Pharmacol. 2012 Sep 15;84(6):766-74.

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