WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 206321
Description: Orantinib, also known as TSU-68；SU6668, is an orally bioavailable receptor tyrosine kinase inhibitor. Orantinib binds to and inhibits the autophosphorylation of vascular endothelial growth factor receptor 2 (VEGFR2), platelet-derived growth factor receptor (PDGFR), and fibroblast growth factor receptor (FGFR), thereby inhibiting angiogenesis and cell proliferation. Orantinib also inhibits the phosphorylation of the stem cell factor receptor tyrosine kinase c-kit, often expressed in acute myelogenous leukemia cells. Check for active clinical trials or closed clinical trials using this agent.
MedKoo Cat#: 206321
Chemical Formula: C28H26N4O4
Exact Mass: 482.19541
Molecular Weight: 482.53
Elemental Analysis: C, 69.70; H, 5.43; N, 11.61; O, 13.26
Synonym: TSU68; TSU 68; TSU-68; SU6668; SU 6668; SU-6668; NSC 702827; Orantinib.
IUPAC/Chemical Name: (Z)-3-(2,4-dimethyl-5-((2-oxoindolin-3-ylidene)methyl)-1H-pyrrol-3-yl)propanoic acid
InChi Key: NHFDRBXTEDBWCZ-ZROIWOOFSA-N
InChi Code: InChI=1S/C18H18N2O3/c1-10-12(7-8-17(21)22)11(2)19-16(10)9-14-13-5-3-4-6-15(13)20-18(14)23/h3-6,9,19H,7-8H2,1-2H3,(H,20,23)(H,21,22)/b14-9-
SMILES Code: O=C(O)CCC1=C(C)NC(/C=C2C(NC3=C\2C=CC=C3)=O)=C1C
TSU68 is an inhibitor of vascular endothelial growth factor receptor 2, platelet-derived growth factor receptor beta, and fibroblast growth factor receptor 1 (FGFR1).
TSU-68 (SU-6668) was developed as an inhibitor of RTKs involved in VEGF, bFGF and PDGF signaling, which then inhibits endothelial cell proliferation. In a in vivo trial, TSU-68 was administered orally at a dose of 200 mg/kg twice daily. Mice bearing human colon carcinoma, HT-29, or WiDr xenografts were treated for 16 days. As TSU-68 significantly inhibited tumor growth and liver metastasis formation of human colon cancer xenografts, probably through anti-angiogenic activity, this agent may be useful for the treatment of colon cancer. see. http://www.ncbi.nlm.nih.gov/pubmed/16077974.