SU 5416 Chemical Properties

Melting point:

226-228 °C

Boiling point:

481.4±45.0 °C(Predicted)

Density 

1.256±0.06 g/cm3(Predicted)

storage temp. 

-20°C

solubility 

H₂O: insoluble

form 

Yellow orange solid

pka

12.59±0.20(Predicted)

color 

yellow to yellow orange

Safety Information

Hazard Codes 

Xi

Risk Statements 

36/37/38

Safety Statements 

26-36

WGK Germany 

3

HS Code 

29339900

SU 5416 Usage And Synthesis

Uses

SU 5416 is a vascular endothelial growth factor receptor blocker that may induce severe pulmonary hypertension if combined with chronic hypoxia. Angiogenesis inhibitor used for deep penetration into tumor tissues.

Uses

SU 516 was used to study the mechanism of development of cerebral vasculature in zebrafish hindbrain.³ It was used to study the pulmonary vascular remodeling in response to hypoxia in mouse model of pulmonary arterial hypertension.⁴

Definition

ChEBI: Semaxanib is an oxindole that is 3-methyleneoxindole in which one of the hydrogens of the methylene group is replaced by a 3,5-dimethylpyrrol-2-yl group. It has a role as an antineoplastic agent, a vascular endothelial growth factor receptor antagonist, an EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor and an angiogenesis modulating agent. It is a member of pyrroles, a member of oxindoles and an olefinic compound. It is functionally related to a 3-methyleneoxindole.

Biological Activity

Inhibitor of vascular endothelial growth factor receptor (VEGFR) that also inhibits other tyrosine kinases KIT, MET, FLT3 and RET. Displays no activity against EGFR, HER2, IGF1R and PDGFR. Inhibits tumor vascularization and growth of multiple tumor types.

Biochem/physiol Actions

SU 516 inhibits the activity of neuronal nitric oxide synthase and protects the neuronal cells from nitric oxide-mediated neurotoxicity.1 It also acts an agonist of aryl hydrocarbon receptor and is an effective clinical agent for treating autoimmune diseases and transplant rejection.2

storage

Desiccate at -20°C

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