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TSU-68

Cat. No. M2153
TSU-68 Structure
Synonym:

SU6668

Size Price Availability Quantity
10mg USD 90 In stock
50mg USD 370 In stock
100mg USD 650 In stock
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Quality Control
Biological Activity

TSU-68 (SU6668) is an oral tyrosine kinase inhibitor of VEGFR-2, PDGFR and FGFR. TSU-68 inhibits SCF-induced proliferation of MO7E cells with IC50 of 0.29 μM, and induces apoptosis. TSU-68 (SU6668) also inhibits Aurora kinases B and C (IC50 = 35 and 210 nM respectively). TSU68 suppresses tumor growth, blocks angiogenesis in tumors, and induces apoptosis of tumor vasculature and regression of established tumors. 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.

Protocol
Cell Experiment
Cell lines HUVECs cells
Preparation method HUVECs (seeded at 2 × 106 cells/10-cm plate) were grown to confluence in endothelial cell growth media [containing 12 μg/ml bovine brain extract, 10 μg/ml human epidermal growth factor, 1 μg/ml hydrocortisone, 2% (v/v) FBS, 50 μg/ml gentamicin, and 50 mg/ml amphotericin B in modified MCDB 131 (Clonetics Corp., Walkersville, MD)] and then quiesced in endothelial cell basal media (modified MCDB 131; Clonetics) containing 0.5% FBS for 24 h before drug treatment. All cell lines were incubated with the indicated concentrations of SU6668 for 60 min before ligand stimulation (100 ng/ml) for 10 min. Preparation of cell lysates, separation of cellular proteins (30 μg from NIH-3T3 engineered cells, 100 μg from HUVECs), and immunoblotting with antiphosphotyrosine antibody were performed as described previously.
Concentrations 0~50 μM
Incubation time 60 min
Animal Experiment
Animal models A375, Calu-6, A431, C6, and SF763T tumor cells xenograft in athymic mice
Formulation DMSO
Dosages 75 or 100 mg/kg
Administration i.p. by bolus injection
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 310.35
Formula C18H18N2O3
CAS Number 252916-29-3
Purity 100.00%
Solubility DMSO 60 mg/mL
Storage at -20°C
References

TSU68 prevents liver metastasis of colon cancer xenografts by modulating the premetastatic niche.
Yamamoto M, et al. Cancer Res. 2008 Dec 1;68(23):9754-62. PMID: 19047154.

In vivo assessment of antiangiogenic activity of SU6668 in an experimental colon carcinoma model.
Marzola P, et al. Clin Cancer Res. 2004 Jan 15;10(2):739-50. PMID: 14760097.

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.
Smolich BD, et al. Blood. 2001 Mar 1;97(5):1413-21. PMID: 11222388.

SU6668 is a potent antiangiogenic and antitumor agent that induces regression of established tumors.
Laird AD, et al. Cancer Res. 2000 Aug 1;60(15):4152-60. PMID: 10945623.

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Keywords: TSU-68, SU6668 supplier, VEGFR/PDGFR, inhibitors

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