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Products are for research use only. Not for human use. We do not sell to patients.
(SU 6668; TSU68; TSU 68; SU6668)
TSU-68 Chemical Structure
|Product name: TSU-68|
|Cat. No.: HY-10517|
TSU-68 (SU6668; Orantinib) is a novel multiple receptor tyrosine kinase inhibitor with IC50 of 2.1 μM, 8 nM and 1.2 μM for VEGF-R1, PDGF-Rβ and FGF-R1, respectively; has greatest potency against PDGFR autophosphorylation.
IC50 value: 8 nM (Ki) 
in vitro: TSU-68 is a competitive inhibitor, with regard to ATP, to Flk-1/KDR trans-phosphorylation, FGFR1 trans-phosphorylation, and PDGFRβ kinases autophosphorylation. TSU-68 (0.03-10 μM) inhibits tyrosine phosphorylation of KDR in VEGF stimulated HUVECs. TSU-68 also inhibits PDGF-stimulated PDGFRβ tyrosine phosphorylation in NIH-3T3 cells overexpressing PDGFRβ at a minimum concentration of 0.03-0.1 μM. TSU-68 inhibits acidic FGF-induced phosphorylation of the FGFR1 substrate 2 at 10 μM and higher. However, TSU-68 (up to 100 μM) has no effect on EGF-stimulated EGFR tyrosine phosphorylation in NIH-3T3 cells overexpressing EGFR. TSU-68 inhibits VEGF-driven and FGF-driven mitogenesis of HUVECs with mean IC50 of 0.34 μM and 9.6 μM, respectively . In human myeloid leukemia MO7E cells, TSU-68 inhibits the tyrosine autophosphorylation of stem cell factor (SCF) receptor, c-kit, with IC50 of 0.1-1 μM, as well as ERK1/2 phosphorylation, a signaling event downstream of c-kit activation. TSU-68 also inhibits SCF-induced proliferation of MO7E cells with IC50 of 0.29 μM, and induces apoptosis .
in vivo: TSU-68 (75-200 mg/kg) induces tumor growth inhibition against a broad range of tumor types in xenograft models in athymic mice, including A375, Colo205, H460, Calu-6, C6, SF763T, and SKOV3TP5 cells. TSU-68 (75 mg/kg) also suppresses tumor angiogenesis of C6 glioma xenografts . In a tumor model of HT29 human colon carcinoma, TSU-68 (200 mg/kg) decreases the average vessel permeability and average fractional plasma volume in the tumor rim and core. TSU-68 promotes abnormal stromal development at the periphery of carcinomas .
|M.Wt||310.35||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
DMSO ≥60mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL
|1 mg||5 mg||10 mg|
|1 mM||3.2222 mL||16.1108 mL||32.2217 mL|
|5 mM||0.6444 mL||3.2222 mL||6.4443 mL|
|10 mM||0.3222 mL||1.6111 mL||3.2222 mL|
|Product Name||Sponsor Only||Condition||Start Date||End Date||Phase||Last Change Date|
|TSU-68||Jonsson Comprehensive Cancer Center||Advanced solid tumor||13-SEP-01||Phase 1||17-NOV-11|
|Solid tumor||31-JUL-01||01-JUL-03||Phase 1||25-OCT-13|
|Taiho Pharmaceutical Co Ltd||Hepatocellular carcinoma||31-DEC-10||31-MAY-17||Phase 3||06-AUG-13|
|Taiho Pharmaceutical Co Ltd||Hepatocellular carcinoma||30-SEP-03||01-MAR-12||Phase 2||14-SEP-13|
. Smolich BD, et al. The antiangiogenic protein kinase inhibitors SU5416 and SU6668 inhibit the SCF receptor (c-kit) in a human myeloid leukemia cell line and in acute myeloid leukemia blasts. Blood, 2001, 97(5), 1413-1421.
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