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TSU-68 (SU6668,Orantinib)
PDGFR/Flk-1/FGFR1 inhibitor,potent and competitive

TSU-68 (SU6668,Orantinib)

Catalog No. A5331
Size Price Stock Qty
10mM (in 1mL DMSO) $63.00 In stock
5mg $50.00 In stock
10mg $89.00 In stock
50mg $350.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

TSU-68 (SU6668)

Biological Activity

Description TSU-68 (SU6668, Orantinib) is a potent inhibitor of PDGFR with a Ki value of 8 nM.
Targets PDGFRβ FGFR1 Flk1      
IC50 8 nM (Ki) 1.2 μM(Ki) 2.1 μM(Ki)      

TSU-68 (SU6668,Orantinib) Dilution Calculator

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Chemical Properties

Cas No. 252916-29-3 SDF Download SDF
Chemical Name 3-[2,4-dimethyl-5-[(Z)-(2-oxo-1H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid
Canonical SMILES CC1=C(NC(=C1CCC(=O)O)C)C=C2C3=CC=CC=C3NC2=O
Formula C18H18N2O3 M.Wt 310.35
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

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 β 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.