CHEBI:90623 - vatalanib succinate

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ChEBI Name vatalanib succinate
ChEBI ID CHEBI:90623
Definition A succinate salt obtained by combining vatalanib with one molar equivalent of succinic acid. It is a multi-targeted tyrosine kinase inhibitor for all isoforms of VEGFR, PDGFR and c-Kit.
Stars This entity has been manually annotated by the ChEBI Team.
Supplier Information ChemicalBook:CB62624136, ZINC000077024213
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Vatalanib (INN, codenamed PTK787 or PTK/ZK) is a small molecule protein kinase inhibitor that inhibits angiogenesis. It is being studied as a possible treatment for several types of cancer, particularly cancer that is at an advanced stage or has not responded to chemotherapy. Vatalanib is orally active, which is to say it is effective when taken by mouth. Vatalanib is being developed by Bayer Schering and Novartis. It inhibits all known VEGF receptors, as well as platelet-derived growth factor receptor-beta and c-kit, but is most selective for VEGFR-2.
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Formula C24H21ClN4O4
Net Charge 0
Average Mass 464.902
Monoisotopic Mass 464.12513
InChI InChI=1S/C20H15ClN4.C4H6O4/c21-15-5-7-16(8-6-15)23-20-18-4-2-1-3-17(18)19(24-25-20)13-14-9-11-22-12-10-14;5-3(6)1-2-4(7)8/h1-12H,13H2,(H,23,25);1-2H2,(H,5,6)(H,7,8)
InChIKey LLDWLPRYLVPDTG-UHFFFAOYSA-N
SMILES C(CC(O)=O)C(O)=O.N1=NC(=C2C(=C1CC=3C=CN=CC3)C=CC=C2)NC4=CC=C(C=C4)Cl
Roles Classification
Biological Role(s): EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor
An EC 2.7.10.* (protein-tyrosine kinase) inhibitor that interferes with the action of receptor protein-tyrosine kinase (EC 2.7.10.1).
vascular endothelial growth factor receptor antagonist
An antagonist at the vascular endothelial growth factor receptor.
Application(s): angiogenesis inhibitor
An agent and endogenous substances that antagonize or inhibit the development of new blood vessels.
antineoplastic agent
A substance that inhibits or prevents the proliferation of neoplasms.
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ChEBI Ontology
Outgoing vatalanib succinate (CHEBI:90623) has part vatalanib (CHEBI:90620)
vatalanib succinate (CHEBI:90623) has role angiogenesis inhibitor (CHEBI:48422)
vatalanib succinate (CHEBI:90623) has role antineoplastic agent (CHEBI:35610)
vatalanib succinate (CHEBI:90623) has role EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor (CHEBI:62434)
vatalanib succinate (CHEBI:90623) has role vascular endothelial growth factor receptor antagonist (CHEBI:65207)
vatalanib succinate (CHEBI:90623) is a succinate salt (CHEBI:51381)
Synonyms Sources
CGP 79787D ChemIDplus
PTK 787 ChemIDplus
PTK 787/ZK 222584 ChemIDplus
PTK-787 ChemIDplus
PTK787/ZK222584 ChemIDplus
vatalanib monosuccinate ChEBI
ZK 222584 ChemIDplus
Manual Xref Database
Vatalanib Wikipedia
View more database links
Registry Numbers Types Sources
212142-18-2 CAS Registry Number ChemIDplus
8664962 Reaxys Registry Number Reaxys
Citations
Dragovich T, Laheru D, Dayyani F, Bolejack V, Smith L, Seng J, Burris H, Rosen P, Hidalgo M, Ritch P, Baker AF, Raghunand N, Crowley J, Von Hoff DD (2014)
Phase II trial of vatalanib in patients with advanced or metastatic pancreatic adenocarcinoma after first-line gemcitabine therapy (PCRT O4-001).
Cancer chemotherapy and pharmacology 74, 379-387 [PubMed:24939212]
[show Abstract]
Raizer JJ, Grimm SA, Rademaker A, Chandler JP, Muro K, Helenowski I, Rice L, McCarthy K, Johnston SK, Mrugala MM, Chamberlain M (2014)
A phase II trial of PTK787/ZK 222584 in recurrent or progressive radiation and surgery refractory meningiomas.
Journal of neuro-oncology 117, 93-101 [PubMed:24449400]
[show Abstract]
Langenberg MH, Witteveen PO, Lankheet NA, Roodhart JM, Rosing H, van den Heuvel IJ, Beijnen JH, Voest EE (2010)
Phase 1 study of combination treatment with PTK 787/ZK 222584 and cetuximab for patients with advanced solid tumors: safety, pharmacokinetics, pharmacodynamics analysis.
Neoplasia (New York, N.Y.) 12, 206-213 [PubMed:20126478]
[show Abstract]
Hess-Stumpp H, Haberey M, Thierauch KH (2005)
PTK 787/ZK 222584, a tyrosine kinase inhibitor of all known VEGF receptors, represses tumor growth with high efficacy.
Chembiochem : a European journal of chemical biology 6, 550-557 [PubMed:15742376]
[show Abstract]
Solorzano CC, Baker CH, Bruns CJ, Killion JJ, Ellis LM, Wood J, Fidler IJ (2001)
Inhibition of growth and metastasis of human pancreatic cancer growing in nude mice by PTK 787/ZK222584, an inhibitor of the vascular endothelial growth factor receptor tyrosine kinases.
Cancer biotherapy & radiopharmaceuticals 16, 359-370 [PubMed:11776753]
[show Abstract]
Wood JM, Bold G, Buchdunger E, Cozens R, Ferrari S, Frei J, Hofmann F, Mestan J, Mett H, O'Reilly T, Persohn E, Rösel J, Schnell C, Stover D, Theuer A, Towbin H, Wenger F, Woods-Cook K, Menrad A, Siemeister G, Schirner M, Thierauch KH, Schneider MR, Drevs J, Martiny-Baron G, Totzke F (2000)
PTK787/ZK 222584, a novel and potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, impairs vascular endothelial growth factor-induced responses and tumor growth after oral administration.
Cancer research 60, 2178-2189 [PubMed:10786682]
[show Abstract]
Last Modified
03 December 2015