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SU5416

Cat. No. M2031

SU5416 Structure

Synonym: Semaxanib

Size Price Availability Quantity
10mg USD 80 In stock
100mg USD 200 In stock
50mg USD 300 In stock
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Quality Control
Biological Activity

SU5416 (Semaxanib) is a potent and selective vascular endothelial growth factor (VEGF) receptor protein tyrosine kinase 1/2 inhibitor that also inhibits other tyrosine kinases KIT, MET, FLT3 and RET. SU5416 inhibited cell migration of human vascular endothelial cells expressing both Flt-1 and KDR in response to VEGF and also inhibited the cell migration in response to placenta growth factor (PIGF), a specific ligand for Flt-1. Chemotaxis of monocytes expressing only Flt-1 was also inhibited by SU5416 in a dose-dependent manner. Moreover, SU5416 was found to inhibit tyrosine kinase of Flt-1 in response to PIGF in vitro. SU5416 efficiently inhibited Kit activity in vivo when administered on a twice-weekly schedule.

Protocol
Cell Experiment
Cell lines C6, Calu 6, A375, A431, and SF767T
Preparation method Tumor Cell Lines and Growth Assays. The EPH4-VEGF cell line is a murine epithelial cell line engineered to overexpress murine VEGF. EPH4-VEGF cells were cultured in DMEM/F-12; C6 cells were cultured in Ham’s F-10 and A375, A431, and LNCAP cells in DMEM. All of these cultures were supplemented with 10% FBS and 2 mM L-glutamine. Calu 6 and SF767T cells were cultured in MEM supplemented with 10% FBS, 2 mM L-glutamine, 1 mM sodium pyruvate, and 0.1 mM MEM nonessential amino acids solution. C6, Calu 6, A375, A431, and SF767T were plated in their respective growth medium at 2 × 103 cells/100 μl/well in 96-well, flat-bottomed plates. SU5416 was serially diluted in media containing DMSO (<0.5%) and added to cultures of tumor cells 1 day after the initiation of culture. Cell growth was measured after 96 h using the sulforhodamine B method. IC50s were calculated by curve fitting using four-parameter analysis.
Concentrations 0, 0.05, 0.5, 5, 50 µm
Incubation time 96 h
Animal Experiment
Animal models Female BALB/c nu/nu mice Intracolonic Xenograft Model
Formulation DMSO
Dosages 25 mg/kg/day 50µl for 39 days
Administration i.p. 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 238.28
Formula C15H14N2O
CAS Number 204005-46-9
Purity >99%
Solubility DMSO
Storage at -20°C
References

A Phase I study of the angiogenesis inhibitor SU5416 (semaxanib) in solid tumours, incorporating dynamic contrast MR pharmacodynamic end points.
O'Donnell A, et al. Br J Cancer. 2005 Oct 17;93(8):876-83. PMID: 16222321.

Antiangiogenic effect by SU5416 is partly attributable to inhibition of Flt-1 receptor signaling.
Itokawa T, et al. Mol Cancer Ther. 2002 Mar;1(5):295-302. PMID: 12489845.

The angiogenesis inhibitor SU5416 has long-lasting effects on vascular endothelial growth factor receptor phosphorylation and function.
Mendel DB, et al. Clin Cancer Res. 2000 Dec;6(12):4848-58. PMID: 11156244.

SU5416 is a potent and selective inhibitor of the vascular endothelial growth factor receptor (Flk-1/KDR) that inhibits tyrosine kinase catalysis, tumor vascularization, and growth of multiple tumor types.
Fong TA, et al. Cancer Res. 1999 Jan 1;59(1):99-106. PMID: 9892193.

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Keywords: SU5416, Semaxanib supplier, VEGFR/PDGFR, inhibitors

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