SU5402

Catalog No.S7667

For research use only.

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.

SU5402 Chemical Structure

CAS No. 215543-92-3

Selleck's SU5402 has been cited by 12 Publications

2 Customer Reviews

Purity & Quality Control

Choose Selective VEGFR Inhibitors

Other VEGFR Products

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
HUVEC or NIH3T3 M4PDV2Z2dmO2aX;uJIF{e2G7 NYTrcXY{TX[jbIXheIVlKG[xcjD0bIUhcW6qaXLpeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gbY5lfWOnZDDifUBXTUeIIHnuJGhWXkWFIH;yJG5KUDOWMzDj[YxteyxiSVO1NF0xNjB3zszN NIXuRZM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMEi5N|MxOyd-MUC4PVM{ODN:L3G+
HUVEC or NIH3T3 Ml;3SpVv[3Srb36gZZN{[Xl? MmTmSZZidHWjdHXkJIZweiC2aHWgbY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25iaX7keYNm\CCkeTDGS2YhcW5iSGXWSWMhd3JiTlnIN3Q{KGOnbHzzMEBKSzVyPUKuPO69VQ>? MojNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTB6OUOzNFMoRjFyOEmzN|A{RC:jPh?=
NIH/3T3 MlLtSpVv[3Srb36gZZN{[Xl? M{PlZWlvcGmkaYTpc44hd2ZiYXPp[IlkKE[JRj3zeIlufWyjdHXkJGZITlJzIIT5do9{cW6nIHH1eI9xcG:|cHjvdplt[XSrb36gbY4hdW:3c3WgUmlJNzOWMzDj[YxteyCkeTDpcY12dm:kbH;0eIlv\yxiSVO1NF0yOM7:TR?= MkPqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwQTF|OU[2NEc,QTF|OU[2NFww[T5?
NIH 3T3 M4TnbGZ2dmO2aX;uJIF{e2G7 MYG1JI1qdnN? MnHaTY5pcWKrdHnvckBw\iCIR1[gbY5lfWOnZDDGS2ZTOSCjdYTvdIhwe3Cqb4L5cIF1cW:wIHnuJI1wfXOnIF7JTEA{XDNiY3XscJMheHKnaX7jeYJifGWmIH\vdkA2KG2rboOg[o9tdG:5ZXSgZpkhTkeILYP0bY12dGG2aX;uJIZweiB3IH3pcpMhcW5icILld4Vv[2Vib3[gX4didW2jLUOyVH1CXFBiYomgV2RUNVCDR1WgZoF{\WRiYYX0c5Ji\GmxZ4LhdIh6NCCLQ{WwQVEx|ryP NXrCVmhlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke5NVQ{PjJpPkK3PVE1OzZ{PD;hQi=>
HUVEC or NIH3T3 MlKySpVv[3Srb36gZZN{[Xl? NYrzVXFpTX[jbIXheIVlKG[xcjD0bIUhcW6qaXLpeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gbY5lfWOnZDDifUBRTEeIIHnuJGhWXkWFIH;yJG5KUDOWMzDj[YxteyxiSVO1NF0zQC52zszN MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yODh7M{OwN{c,OTB6OUOzNFM9N2F-
NIH/3T3 MmS3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmX3S5Jwf3SqIHnubIljcXSrb36gc4YhdW:3c3WgUmlJNzOWMzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGGlaXTpZ{BHT0Zvc4TpcZVt[XSnZDDbN2hefGi7bXnkbY5mKGmwY3;ydI9z[XSrb36= M3\PeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzlzM{m2OlAoRjlzM{m2OlA9N2F-
NIH/3T3 NYr4eWZJTnWwY4Tpc44h[XO|YYm= MkTGTY5pcWKrdHnvckBw\iCIR1\SNUBqdiCvb4Xz[UBPUUhxM2SzJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiYV\HSk1{fGmvdXzheIVlKHCyOUCgdIhwe3Cqb4Dyc5RmcW5icHjvd5Bpd3K7bHH0bY9vKGK7IHntcZVvd2Kub4T0bY5o NYrLPHR6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxOUGzPVY3OCd-OUGzPVY3ODxxYU6=
NIH/3T3 MmKwSpVv[3Srb36gZZN{[Xl? Ml;RTY5pcWKrdHnvckBw\iCIR1\SNUBqdiCvb4Xz[UBPUUhxM2SzJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiYXPp[IlkKE[JRj3zeIlufWyjdHXkJGVTUzFicHjvd5Bpd3K7bHH0bY9vKGK7IHntcZVvd2Kub4T0bY5o NWDTTnZlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxOUGzPVY3OCd-OUGzPVY3ODxxYU6=
NIH/3T3 NXXJUIs5TnWwY4Tpc44h[XO|YYm= NXzIfHZOUW6qaXLpeIlwdiCxZjDGS2ZTOSCrbjDtc5V{\SCQSVivN3Q{KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gZYNq\GmlIF\HSk1{fGmvdXzheIVlKEWUS{KgdIhwe3Cqb4L5cIF1cW:wIHL5JIludXWwb3Lsc5R1cW6p MnXrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwQTF|OU[2NEc,QTF|OU[2NFww[T5?
NIHIR NEe4cHFHfW6ldHnvckBie3OjeR?= MnjHTY5pcWKrdHnvckBw\iCrboP1cIlvNXO2aX31cIF1\WRiaX7zeYxqdiC{ZXPldJRweiCkZYThJJN2[nWwaYSgZZV1d3Cqb4PwbI9zgWyjdHnvckBqdiCvb4Xz[UBPUUiLUjDj[Yxtew>? NVuyXVNXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxOUGzPVY3OCd-OUGzPVY3ODxxYU6=
HER14 MWXGeY5kfGmxbjDhd5NigQ>? MVXJcohq[mm2aX;uJI9nKEWJRj3zeIlufWyjdHXkJGVITlJicHjvd5Bpd3K7bHH0bY9vKGmwIH3veZNmKEiHUkG0JINmdGy|IHL5JIludXWwb3Lsc5R1cW6p MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek86OTN7Nk[wK|46OTN7Nk[wQE9iRg>?
HER14 NGHIV3hHfW6ldHnvckBie3OjeR?= NVXJVYc4UW6qaXLpeIlwdiCxZjDFS2ZTKGmwIH3veZNmKEiHUkG0JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiRVfGMZN1cW23bHH0[YQhW2ilIIDoc5NxcG:{eXzheIlwdiCkeTDpcY12dm:kbH;0eIlv\w>? Moj3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwQTF|OU[2NEc,QTF|OU[2NFww[T5?
HER14 M4rENmZ2dmO2aX;uJIF{e2G7 NWTJdnV5UW6qaXLpeIlwdiCxZjDFS2ZTKGmwIH3veZNmKEiHUkG0JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiRVfGMZN1cW23bHH0[YQhTVKNMjDhZ5RqfmG2aX;uJIJ6KGmvbYXuc4Jtd3S2aX7n NU\XZ|lVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxOUGzPVY3OCd-OUGzPVY3ODxxYU6=
NIHIR NYDDXJVUTnWwY4Tpc44h[XO|YYm= M2XFe2lvcGmkaYTpc44hd2ZiaX7zeYxqdiC{ZXPldJRweiCrbjDtc5V{\SCQSVjJVkBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHnud5VtcW5vc4TpcZVt[XSnZDDJVnMyKHCqb4PwbI9zgWyjdHnvci=> NFnQeVE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi97MUO5OlYxLz57MUO5OlYxRC:jPh?=
NIH/3T3 MWnGeY5kfGmxbjDhd5NigQ>? M3:wNmlvcGmkaYTpc44hd2ZiUFTHSnIhcW5ibX;1d4UhVkmKL{PUN{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIGDES2Yue3SrbYXsZZRm\CC2eYLvd4lv\SCjdYTvdIhwe3Cqb4L5cIF1cW:wIHL5JIludXWwb3Lsc5R1cW6p MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek86OTN7Nk[wK|46OTN7Nk[wQE9iRg>?
NIH/3T3 MnfKSpVv[3Srb36gZZN{[Xl? NIPSXY1KdmirYnn0bY9vKG:oIGDES2ZTKGmwIH3veZNmKE6LSD:zWFMh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDQSGdHNXO2aX31cIF1\WRicHjvd5Bpd2yrcHHz[UBEKGejbX3hJJBpd3OyaH;yfYxifGmxbjDifUBqdW23bn;icI91fGmwZx?= Ml;MQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwQTF|OU[2NEc,QTF|OU[2NFww[T5?
NIH/3T3 NH3pfHJHfW6ldHnvckBie3OjeR?= MVzJcohq[mm2aX;uJI9nKFCGR1\SJIlvKG2xdYPlJG5KUC9|VEOgZ4VtdHNiYYPz[ZN{\WRiYYOgVGRITi2|dHnteYxifGWmIFXyb|Ih[WO2aY\heIlwdiCkeTDpcY12dm:kbH;0eIlv\w>? NIP0cmo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi97MUO5OlYxLz57MUO5OlYxRC:jPh?=
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 (from reference)

Kinase Assay:[1]
  • 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]
  • 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.
Animal Research:[2]
  • 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.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 296.32
Formula

C17H16N2O3

CAS No. 215543-92-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CNC(=C1CCC(=O)O)C=C2C3=CC=CC=C3NC2=O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy SU5402 | SU5402 supplier | purchase SU5402 | SU5402 cost | SU5402 manufacturer | order SU5402 | SU5402 distributor