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Signaling Pathway

SU5416

HY-10374

(Semaxinib; SU-5416; SU 5416)

SU5416

SU5416 Chemical Structure

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.

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10 mM * 1 mL in DMSO $77 In-stock
10 mg $70 In-stock
50 mg $190 In-stock
100 mg $250 In-stock
200 mg Get quote
500 mg Get quote
Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO €75 In-stock
10 mg €69 In-stock
50 mg €186 In-stock
100 mg €245 In-stock
200 mg Get quote
500 mg Get quote

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Product name: SU5416
Cat. No.: HY-10374

SU5416 Data Sheet

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    Purity: 99.93%

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    DataSheet

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    NMR

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Biological Activity of SU5416

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 [1]
Target: VEGFR
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) [1].
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% [1]. 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 [2].

Protocol (Extracted from published papers and Only for reference)

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Chemical Information

M.Wt 238.28 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C15H14N2O
CAS No 204005-46-9
Solvent & Solubility

DMSO: ≥ 22.5 mg/mL

Preparing Stock Solutions

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

Clinical Information of SU5416

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

References on SU5416

Inhibitor Kit

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