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Signaling Pathway

TSU-68

HY-10517

(SU 6668; TSU68; TSU 68; SU6668)

TSU-68

TSU-68 Chemical Structure

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.

Size Price Stock Quantity
10 mM * 1 mL in DMSO $99 In-stock
10 mg $90 In-stock
50 mg $360 In-stock
100 mg $630 In-stock
200 mg Get quote
500 mg Get quote
Size Price Stock Quantity
10 mM * 1 mL in DMSO €97 In-stock
10 mg €88 In-stock
50 mg €353 In-stock
100 mg €617 In-stock
200 mg Get quote
500 mg Get quote

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Product name: TSU-68
Cat. No.: HY-10517

TSU-68 Data Sheet

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    Purity: 99.21%

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Biological Activity of TSU-68

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) [1]
Target: PDGF-Rβ
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 [1]. 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 [2].
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 [1]. 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 [3].

Protocol (Extracted from published papers and Only for reference)

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Chemical Information

M.Wt 310.35 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C18H18N2O3
CAS No 252916-29-3
Solvent & Solubility

DMSO: ≥ 28 mg/mL

Preparing Stock Solutions

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

Clinical Information of TSU-68

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

References on TSU-68

Inhibitor Kit

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