Drug Information

Drug General Information
Drug ID
D0N7AJ
Former ID
DIB018904
Drug Name
AST-487
Synonyms
AST 487; NVP-AST 487; NVP-AST487
Drug Type
Small molecular drug
Indication Discovery agent Investigative [529722]
Formula
C26H30F3N7O2
InChI
InChI=1S/C26H30F3N7O2/c1-3-35-10-12-36(13-11-35)16-18-4-5-20(14-22(18)26(27,28)29)34-25(37)33-19-6-8-21(9-7-19)38-24-15-23(30-2)31-17-32-24/h4-9,14-15,17H,3,10-13,16H2,1-2H3,(H,30,31,32)(H2,33,34,37)
InChIKey
ODPGGGTTYSGTGO-UHFFFAOYSA-N
PubChem Compound ID
11409972
PubChem Substance ID
16505659, 23558201, 42489108, 50100088, 77948236, 103694306, 103905682, 134964216, 152258619, 160647454, 162011980, 172650221, 174530108, 178102289, 180387178, 185975426, 198941880, 227869652, 246030715, 251962970, 252477710, 252543480, 252615335
Target and Pathway
Target(s) FL cytokine receptor Target Info Inhibitor [531679]
Proto-oncogene tyrosine-protein kinase receptor ret Target Info Inhibitor [528954]
Vascular endothelial growth factor receptor 2 Target Info Inhibitor [528954]
Mast/stem cell growth factor receptor Target Info Inhibitor [528954]
KEGG Pathway Cytokine-cytokine receptor interaction
Hematopoietic cell lineage
Pathways in cancer
Transcriptional misregulation in cancer
Acute myeloid leukemia
Central carbon metabolism in cancerhsa04144:Endocytosis
Thyroid cancer
Central carbon metabolism in cancerhsa04014:Ras signaling pathway
Rap1 signaling pathway
Endocytosis
PI3K-Akt signaling pathway
VEGF signaling pathway
Focal adhesion
Proteoglycans in cancerhsa04014:Ras signaling pathway
Melanogenesis
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 Signaling events regulated by Ret tyrosine kinase
Posttranslational regulation of adherens junction stability and dissassemblyhif2pathway: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 SIDS Susceptibility Pathways
Dopaminergic NeurogenesisWP306: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 529722Antileukemic effects of the novel, mutant FLT3 inhibitor NVP-AST487: effects on PKC412-sensitive and -resistant FLT3-expressing cells. Blood. 2008 Dec 15;112(13):5161-70.
Ref 528954The RET kinase inhibitor NVP-AST487 blocks growth and calcitonin gene expression through distinct mechanisms in medullary thyroid cancer cells. Cancer Res. 2007 Jul 15;67(14):6956-64.
Ref 531679Comprehensive analysis of kinase inhibitor selectivity. Nat Biotechnol. 2011 Oct 30;29(11):1046-51.

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