SU5402

For research use only.

Catalog No.S7667

5 publications

SU5402 Chemical Structure

CAS No. 215543-92-3

SU5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGF-Rβ, respectively.

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Selleck's SU5402 has been cited by 5 publications

2 Customer Reviews

  • Four FGFR inhibitors, namely PD-173074 (PD-74), PD-166866 (PD-66), SU5402 (SU54) and NVP-BGJ398 (BG-98), inhibit A673, SKNMC, POE, RDES and SKES Ewing cell growth in vitro in a dose-dependent manner, whereas normal cells (IMR90 fibroblasts) remained unaffected. PD-74 proved to be most effective in four out of five Ewing sarcoma cell lines tested. Cells were grown in 10% FBS conditions and cell proliferation was measured after 72 h using a Resazurin assay.

    Oncogene, 2017, 36(6):766-776. SU5402 purchased from Selleck.

    HUVEC spheroids embedded in fibrin gel were incubated with a pool of PDR vitreous fluid samples (1:4 dilution) in the absence or in the presence of different extracellular (a) pathway inhibitors. Formation of radially growing sprouts was evaluated after 24 h of incubation. Data are the mean ± S.E.M. of 30 spheroids per experimental point. *p<0.05, **p<0.01 versus PDR vitreous.

    Angiogenesis, 2017, 20(4):629-640. SU5402 purchased from Selleck.

Purity & Quality Control

Choose Selective VEGFR Inhibitors

Biological Activity

Description SU5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGF-Rβ, respectively.
Targets
VEGFR2 [1]
(Cell-free assay)		 FGFR1 [1]
(Cell-free assay)		 PDGFRβ [1]
(Cell-free assay)
20 nM 30 nM 510 nM
In vitro

SU5402 inhibits VEGF-, FGF-, PDGF- dependent cell proliferation with IC50 of 0.05 μM, 2.80μM, 28.4 μM, respectively. [1] In HUVECs, SU5416 selectively inhibits VEGF-driven mitogenesis in a dose-dependent manner with IC50 of 0.04 μM. [2] In nasopharyngeal epithelial cells, SU5402 attenuates LMP1-mediated aerobic glycolysis, cellular transformation, cell migration, and invasion. [3] In mouse C3H10T1/2 cells, SU 5402 diminishes the effect of FGF23 on cell differentiation. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
mouse NIH/3T3 cell Ml;DSpVv[3Srb36gZZN{[Xl? MWLJcohq[mm2aX;uJI9nKGGlaXTpZ{BHT0Zvc4TpcZVt[XSnZDDGS2ZTOSC2eYLvd4lv\SCjdYTvdIhwe3Cqb4L5cIF1cW:wIHnuJI1wfXOnIF7JTE8{XDNiY3XscJMh[nliaX3teY5w[myxdITpcoduNCCLQ{WwQVExKM7:TR?= NIjjbFU6OTN7Nk[w
mouse NIHIR cells MXfGeY5kfGmxbjDhd5NigQ>? MknDTY5pcWKrdHnvckBw\iCrboP1cIlvNXO2aX31cIF1\WRiaX7zeYxqdiC{ZXPldJRweiCkZYThJJN2[nWwaYSgZZV1d3Cqb4PwbI9zgWyjdHnvckBqdiCvb4Xz[UBPUUiLUjDj[Yxtew>? NWjoUGNUQTF|OU[2NC=>
mouse HER14 cells MX\GeY5kfGmxbjDhd5NigQ>? NULEd|B3UW6qaXLpeIlwdiCxZjDFS2ZTKGmwIH3veZNmKEiHUkG0JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiRVfGMZN1cW23bHH0[YQhW2ilIIDoc5NxcG:{eXzheIlwdiCkeTDpcY12dm:kbH;0eIlv\w>? M4XMS|kyOzl4NkC=

... Click to View More Cell Line Experimental Data
In vivo In mice, SU5416 (25 mg/kg, i.p.) inhibits subcutaneous growth of a panel of tumor cell lines by inhibiting the angiogenic process associated with tumor growth. [2]

Protocol

Kinase Assay:[1]
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FGF-R1 and Flk-1/KDR kinase assays.:

The catalytic portion of FGF-R1 and Flk-1/KDR are expressed as GST fusion proteins following infection of Spodoptera frugiperda (sf9) cells with engineered baculoviruses. GST-FGFR1 and GST-Flk1 are purified to homogeneity from infected sf9 cell lysates by glutathione sepharose chromatography. The assays are performed in 96-well microtiter plates that had been coated overnight with 2.0 μg of a polyGlu-Tyr peptide (4:1) in 0.1 mL of PBS per well. The purified kinases are diluted in kinase assay buffer (100 mM Hepes pH 7.5, 100 mM NaCl, and 0.1 mM sodium orthovanadate) and added to all test wells at 5 ng of GST fusion protein per 0.05 mL volume buffer. Test compounds are diluted in 4% DMSO and added to test wells (0.025 mL/well). The kinase reaction is initiated by the addition of 0.025 mL of 40 μM ATP/40 mM MnCl2, and plates are shaken for 10 min before stopping the reactions with the addition of 0.025 mL of 0.5 M EDTA. The final ATP concentration was 10 μM, which is twice the experimentally determined Km value for ATP. Negative control wells receive MnCl2 alone without ATP. The plates are washed three times with 10 mM Tris pH 7.4, 150 mM NaCl, and 0.05% Tween-20 (TBST). Rabbit polyclonal anti-phosphotyrosine antiserum is added to the wells at a 1:10000 dilution in TBST for 1 h. The plates are then washed three times with TBST. Goat anti-rabbit antiserum conjugated with horseradish peroxidase was then added to all wells for 1 h. The plates are washed three times with TBST, and the peroxidase reaction is detected with the addition of 2,2‘-azinobis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS). The color readout of the assay is allowed to develop for 20−30 min and read on a Dynatech MR5000 ELISA plate reader using a 410 nM test filter.
Cell Research:[2]
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  • Cell lines: SF767T, SF763, EPH4-VEGF, C6, A375, A431, LNCAP, Calu-6, 3T3Her2 and 488G2M2 cells
  • Concentrations: ~50 μM
  • Incubation Time: 96 hours
  • Method: Tumor cell lines used in the in vitro growth are cultured in media at 37°C in 5–10% CO2. SU5416 is serially diluted in media containing DMSO (<0.5%) and added to cultures of tumor cells 1 day after the initiation of culture. Cell growth is measured after 96 h using the sulforhodamine B method. IC50s are calculated by curve fitting using four-parameter analysis.
    (Only for Reference)
Animal Research:[2]
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  • Animal Models: Mice bearing SF767T, SF763, EPH4-VEGF, C6, A375, A431, LNCAP, Calu-6, 3T3Her2 or 488G2M2 tumors
  • Dosages: 25 mg/kg/d
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 59 mg/mL (199.1 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 296.32
Formula

C17H16N2O3
CAS No. 215543-92-3
Storage powder
in solvent
Synonyms N/A
Smiles CC1=CNC(=C1CCC(=O)O)C=C2C3=CC=CC=C3NC2=O

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID