Semaxanib (SU5416) - 99%, high purity , Vascular endothelial growth factor receptor inhibitor, CAS No.194413-58-6, Vascular endothelial growth factor receptor inhibitor

Item Number

S412802

• Synonyms: (Z)-Semaxinib | BRN 0844684 | CAS-204005-46-9 | NCGC00094381-01 | SCHEMBL194769 | SCHEMBL19571 | SU005416 | Lopac0_001110 | (Z)-SU 5416 | NCGC00094381-19 | Sugen 5416 | HMS3648O12 | HY-10374 | MLS001304019 | TSU 16 | WUWDLXZGHZSWQZ-WQLSENKSSA-N | ES-0010
• Specifications & Purity: Moligand™, ≥99%
• Biochemical and Physiological Mechanisms: Semaxanib (SU5416) is a potent and selective VEGFR(Flk-1/KDR) inhibitor with IC50 of 1.23 μM, 20-fold more selective for VEGFR than PDGFRβ, lack of activity against EGFR, InsR and FGFR. Phase 3.
• Storage Temp: Store at -20°C
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™
• Action Type: INHIBITOR
• Mechanism of action: Vascular endothelial growth factor receptor inhibitor

Product Description

Information

Semaxanib (SU5416) is a potent and selectiveVEGFR(Flk-1/KDR) inhibitor withIC50of 1.23 μM, 20-fold more selective for VEGFR than PDGFRβ, lack of activity against EGFR, InsR and FGFR. Phase 3.

Targets

VEGFR2/Flk1 (Cell-free assay) 1.23 μM

In vitro

Semaxanib inhibits VEGF-dependent phosphorylation of the Flk-1 receptor in Flk-1-overexpressing NIH 3T3 cells with IC50 of 1.04 μM. Semaxanib inhibits PDGF-dependent autophosphorylation in NIH 3T3 cells with IC50 of 20.3 μM. Semaxanib inhibits VEGF- and FGF-driven mitogenesis in a dose-dependent manner with IC50 of 0.04 and 50 μM, respectively. Semaxanib treatment has no effect on the in vitro growth of C6 glioma, Calu 6 lung carcinoma, A375 melanoma, A431 epidermoid carcinoma, and SF767T glioma cells (all IC50s > 20 μM).

In vivo

Semaxanib dose-related inhibits growth of A375 tumor in vivo. A >85% inhibition of subcutaneous tumor growth is observed with daily i.p. administration of SU5416 in DMSO at Semaxanib, without measurable toxicity. Semaxanib shows broad spectrum antitumor activity. SU5416 significantly inhibits the subcutaneous growth of 8 of 10 tumor lines tested (A431, Calu-6, C6, LNCAP, EPH4-VEGF, 3T3HER2, 488G2M2 and SF763T cells) with an average mortality rate of 2.5%. Semaxanib (25 mg/kg/day) displays potent antiangiogenic activity, resulting in a significant reduction of both the total and functional vascular density of the tumor microvasculature.

Cell Research(from reference)

Cell lines：HUVECs 

Concentrations：~100 μM 

Incubation Time：2 days