TSU-68 (SU6668, Orantinib)
TSU-68 (SU6668, Orantinib)
CAS: 252916-29-3
Molecular Formula: C18H18N2O3
TSU-68 (SU6668, Orantinib) - Names and Identifiers
TSU-68 (SU6668, Orantinib) - Physico-chemical Properties
| Molecular Formula | C18H18N2O3 |
| Molar Mass | 310.35 |
| Density | 1.328±0.06 g/cm3(Predicted) |
| Melting Point | 252-254 °C |
| Boling Point | 590.5±50.0 °C(Predicted) |
| Solubility | DMSO (Slightly), Methanol (Slightly) |
| Appearance | Solid |
| Color | Orange to Brown |
| pKa | 4?+-.0.10(Predicted) |
| Storage Condition | Store at RT |
| In vitro study | TSU-68 is a competitive inhibitor of ATP and acts on Flk-1/KDR phosphate transfer, FGFR1 phosphate transfer, and PDGFRβ kinase with K I of 2.1 μm, 1.2 μm, and 8 nM, respectively. 0.03-10 μm TSU-68 inhibits KDR tyrosine phosphorylation by acting on VEGF-stimulated HUVECs. TSU-68, at a minimum concentration of 0.03-0.1 μm, also inhibited PDGF-stimulated PDGFRβ tyrosine phosphorylation by NIH-3T3 cells overexpressing PDGFRβ. 10 μm and higher concentrations inhibited FGF acid-induced phosphorylation of FGFR1 substrate 2 by TSU-68. However, up to 100 μm TSU-68 action on NIH-3T3 cells overexpressing EGFR did not inhibit EGF-stimulated EGFR tyrosine phosphorylation. TSU-68 inhibited the division of VEGF-driven and FGF-driven HUVECs with a mean IC50 of 0.34 and 9.6 μm, respectively. TSU-68, it acts on human myeloid leukemia MO7E cells to inhibit tyrosine autophosphorylation of hepatocyte factor (SCF) receptor c-kit with IC50 of 0.1-1 μm, and also inhibits ERK1/2 phosphorylation. TSU-68 also inhibited SCF-stimulated MO7E cell proliferation with an IC50 of 0.29 μm and induced apoptosis. |
| In vivo study | TSU-68 inhibited cell growth at a dose of 75-200 mg/kg in athymic mice bearing a variety of xenografts, including A375,Colo205,H460,Calu-6,C6,SF763T, and SKOV3TP5 cells. TSU-68 at a dose of 75 mg/kg on the C6 glial cell transplantation tumor, also blocked tumor angiogenesis. TSU-68 at a dose of 200 mg/kg in the HT29 human colon cancer tumor model, the mean vascular permeability of the tumor edge and the mean plasma volume fraction of the tumor center were reduced. TSU-68 promote the formation of abnormal matrix around the tumor. In TSU-68, 200 mg/kg dose was applied to the rabbit VX2 liver tumor model to increase the effect of injection chemotherapy. |
TSU-68 (SU6668, Orantinib) - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.222 ml | 16.111 ml | 32.222 ml |
| 5 mM | 0.644 ml | 3.222 ml | 6.444 ml |
| 10 mM | 0.322 ml | 1.611 ml | 3.222 ml |
| 5 mM | 0.064 ml | 0.322 ml | 0.644 ml |
Last Update：2024-01-02 23:10:35
TSU-68 (SU6668, Orantinib) - Reference Information
| molecular targeted drug | Orantinib (SU6668; TSU-68) is a multi-target receptor tyrosine kinase inhibitor with Ki values of 2.1 μM,8 nM and 1.2 μM for Flt-1,PDGFRβ and FGFR1 respectively. Orantinib orantinib (TSU‐ 68) has been shown to inhibit VEGFR2, PDGFRβ and FGFR1. Clinical studies have shown that orantinib has the activity to stabilize the disease progression after chemoembolization of advanced liver cancer. A phase I/II study shows that orantinib is a molecular targeted drug that can inhibit vascular endothelial growth factor (VEGF), vascular endothelial growth factor (PDGF) and fibroblast growth factor receptor in patients with advanced liver cancer, with good efficacy and safety. Based on promising results, a phase II study was conducted to evaluate the efficacy of combined treatment with TACE and orantinib. The results show that the primary endpoint of the study has improved progression-free survival (PFS), indicating that the combined application of orantinib and TACE has an additive effect. Therefore, Phase III (ORIENTAL) studies were conducted in Japan, South Korea and Taiwan. |
| biological activity | Orantinib (TSU-68, SU6668) effectively acts on PDGFR autophosphorylation, Ki is 8 nM in cell-free test, and also strongly inhibits Flk-1 and FGFR1 transphosphorylation, with little inhibitory activity on IGF-1R,Met, Src,Lck,Zap70,Abl and CDK2; there was no inhibitory effect on EGFR. Phase 3. |
| target | TargetValue PDGFRβ (Cell-free say) 8 nM(Ki) |
| Target | Value |
| PDGFRβ (Cell-free assay) | 8 nM(Ki) |
| in vitro study | TSU-68 are ATP competitive inhibitors. when acting on Flk-1/KDR phosphate transfer, FGFR1 phosphate transfer, and PDGFRβ kinase, K I is 2.1 μM and 1.2 μM respectively, and 8 nM. 0.03-10 μM TSU-68 acts on VEGF-stimulated HUVECs and inhibits KDR tyrosine phosphorylation. TSU-68 with a minimum concentration of 0.03-0.1 μM acts on NIH-3T3 cells overexpressing PDGFRβ and also inhibits PDGFRβ tyrosine phosphorylation stimulated by PDGF. 10 μM and higher concentrations TSU-68 inhibit FGF acid-induced phosphorylation of FGFR1 substrate 2. However, up to 100 μM TSU-68 act on NIH-3T3 cells overexpressing EGFR and do not inhibit EGFR tyrosine phosphorylation stimulated by EGF. TSU-68 inhibit VEGF-driven and FGF-driven HUVECs division with an average IC50 of 0.34 and 9.6 μM, respectively. TSU-68 acts on human myeloid leukemia MO7E cells, inhibits tyrosine autophosphorylation of hepatocyte factor (SCF) receptor c-kit, IC50 is 0.1-1 μM, and also inhibits ERK1/2 phosphorylation. TSU-68 also inhibited SCF-stimulated MO7E cell proliferation with IC50 of 0.29 μM and induced apoptosis. |
| in vivo study | TSU-68 acts on athymic mice carrying various transplanted tumors at doses of 75-200 mg/kg, including A375,Colo205,H460,Calu-6,C6,SF763T, and SKOV3TP5 cells, inhibiting cell growth. The TSU-68 acts on C6 neuroglial cell transplanted tumor at a dose of 75 mg/kg, which also blocks tumor angiogenesis. TSU-68 acted on HT29 human colon cancer tumor model at a dose of 200 mg/kg to reduce the average vascular permeability at the tumor edge and the average plasma volume fraction at the tumor center. TSU-68 promote the formation of abnormal matrix around the tumor. TSU-68 200 mg/kg dose was applied to rabbit VX2 liver tumor model to increase the effect of injection chemotherapy. |
Last Update：2024-04-10 22:29:15
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Product Name: TSU-68 (SU6668, Orantinib) Visit Supplier Webpage Request for quotation
CAS: 252916-29-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 252916-29-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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