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Products are for research use only. Not for human use. We do not sell to patients.
(Semaxinib; SU-5416; SU 5416)
SU5416 Chemical Structure
|Product name: SU5416|
|Cat. No.: HY-10374|
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.
IC50 value: 1.23 uM 
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 .
|M.Wt||238.28||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
DMSO: ≥ 22.5 mg/mL
|1 mg||5 mg||10 mg|
|1 mM||4.1967 mL||20.9837 mL||41.9674 mL|
|5 mM||0.8393 mL||4.1967 mL||8.3935 mL|
|10 mM||0.4197 mL||2.0984 mL||4.1967 mL|
|Product Name||Sponsor Only||Condition||Start Date||End Date||Phase||Last Change Date|
|SU5416||Renal tumor||31-DEC-00||Phase 2||30-JAN-13|
|University of Chicago||Hormone refractory prostate cancer||30-JUN-00||01-JAN-06||Phase 2||30-SEP-13|
|City of Hope Medical Center||Metastatic renal cancer||30-NOV-00||28-FEB-07||Phase 2||03-OCT-13|
|Stage IV melanoma||31-MAR-01||01-SEP-03||Phase 2||20-SEP-13|
|Pfizer Inc||Metastatic colorectal cancer||30-NOV-99||01-SEP-07||Phase 3||13-SEP-13|
. Fong TA, et al. 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. Cancer Res, 1999, 59(1), 99-106.
. Vajkoczy P, et al. Inhibition of tumor growth, angiogenesis, and microcirculation by the novel Flk-1 inhibitor SU5416 as assessed by intravital multi-fluorescence videomicroscopy. Neoplasia, 1999, 1(1), 31-41.
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