Drug Information

Drug General Information
Drug ID
D07OZR
Former ID
DCL000248
Drug Name
TKI258
Synonyms
Chir 258; CHIR-258; TKI-258; TKI-258, Dovitinib, CHIR258, TKI258; 4-Amino-5-fluoro-3-(5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl)quinolin-2(1H)-one
Drug Type
Small molecular drug
Indication Advanced or metastatic renal cell cancer [ICD9: 189; ICD10:C64] Phase 1/2 [536674], [541242]
Therapeutic Class
Anticancer Agents
Company
Novartis & Chiron Corp
Structure
Download
2D MOL

3D MOL
Formula
C21H21FN6O
InChI
InChI=1S/C21H21FN6O/c1-27-7-9-28(10-8-27)12-5-6-14-16(11-12)25-20(24-14)18-19(23)17-13(22)3-2-4-15(17)26-21(18)29/h2-6,11,24-25H,7-10,23H2,1H3/b20-18-
InChIKey
KCOYQXZDFIIGCY-ZZEZOPTASA-N
CAS Number
CAS 804551-71-1
PubChem Compound ID
9886808
PubChem Substance ID
14854259, 16526641, 16823163, 39896483, 45633748, 50100092, 56374260, 74418884, 109693511, 121280185, 135261170, 136367994, 141243978, 141243980, 141913081, 141913174, 144115820, 152258853, 152344214, 160647703, 162205181, 164044350, 174529303, 177748727, 178102585, 180190845, 188899516, 196378498, 198975799, 223397268, 226534136, 235322191, 249565565, 249565566, 249565567, 249582865, 251856461, 252215131, 252543299
Target and Pathway
Target(s) FGF-3 receptor Target Info Inhibitor [536474]
Platelet-derived growth factor receptor Target Info Inhibitor [536474]
KEGG Pathway MAPK signaling pathway
Ras signaling pathway
Rap1 signaling pathway
Endocytosis
PI3K-Akt signaling pathway
Signaling pathways regulating pluripotency of stem cells
Regulation of actin cytoskeleton
Pathways in cancer
MicroRNAs in cancer
Bladder cancer
Central carbon metabolism in cancer
PANTHER Pathway FGF signaling pathway
Reactome FGFR3 mutant receptor activation
WikiPathways Regulation of Actin Cytoskeleton
Endochondral Ossification
Bladder Cancer
Neural Crest Differentiation
Signaling by FGFR
References
Ref 536674A phase I pharmacokinetic and pharmacodynamic study of TKI258, an oral, multitargeted receptor tyrosine kinase inhibitor in patients with advanced solid tumors. Clin Cancer Res. 2008 Apr 1;14(7):2075-81.
Ref 541242(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5962).
Ref 536474A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.

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