TSU-68 (SU6668,Orantinib)

Short Summary : PDGFR/Flk-1/FGFR1 inhibitor,potent and competitive

Category : Tyrosine Kinase|VEGFR

Purity : 0.98

CAS Number : 252916-29-3

Formula : C18H18N2O3

Molecular Weight : 310.35

SMILE : CC1=C(NC(=C1CCC(=O)O)C)C=C2C3=CC=CC=C3NC2=O

Solubility : >15.5mg/mL in DMSO

Storage : Store at -20°C

Description : Ki: Flk-1trans-phosphorylation (2.1 mM), FGFR1 trans-phosphorylation (1.2 mM), and PDGFR autophosphorylation (0.008 mM).Vascular endothelial growth factor, fibroblast growth factor (FGF), and platelet-derived growth factor (PDGF) and their cognate receptor tyrosine kinases are strongly implicated in angiogenesis associated with solid tumors. TSU-68 is a novel inhibitor of these receptors.In vitro: Biochemical kinetic studies using isolated Flk-1, FGF receptor 1, and PDGF receptor kinases revealed that TSU-68 has competitive inhibitory properties with respect to ATP. In cellular systems, TSU-68 inhibited receptor tyrosine phosphorylation and mitogenesis after stimulation of cells by appropriate ligands [1]. In vivo: Oral or i.p. administration of TSU-68 in athymic mice resulted in significant growth inhibition of a diverse panel of human tumor xenografts of glioma, melanoma, lung, colon, ovarian, and epidermoid origin [1]. Clinical trial: Phase I clinical study indicated that TSU-68 can be safely combined with standard doses of carboplatin-paclitaxel, with the combination manifesting promising antitumor activity [2].References:[1] Laird AD, Vajkoczy P, Shawver LK et al. SU6668 is a potent antiangiogenic and antitumor agent that induces regression of established tumors. Cancer Res. 2000 Aug 1;60(15):4152-60.[2] Okamoto I, Yoshioka H, Takeda K et al. Phase I clinical study of the angiogenesis inhibitor TSU-68 combined with carboplatin and paclitaxel in chemotherapy-naive patients with advanced non-small cell lung cancer. J Thorac Oncol. 2012 Feb;7(2):427-33.

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