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SU5402

Name: SU5402
Brand: Selleck Chemicals
SKU: S7667
Rating: 5 (11 reviews)

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.

CAS No. 215543-92-3

Selleck's SU5402 has been cited by 11 Publications

2 Customer Reviews

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VEGFR Signaling Pathway Map

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	NWD0[Y9DTnWwY4Tpc44h[XO\|YYm=		NGLlVnhGfmGudXH0[YQh\m:{IITo[UBqdmirYnn0bY9vKG:oIHPlcIwheHKxbHnm[ZJifGmxbjDpcoR2[2WmIHL5JHZGT0ZiaX6gTHVXTUNib4KgUmlJO1R\|IHPlcIx{NCCLQ{WwQVAvODYQvF2=	MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yODh7M{OwN{c,OTB6OUOzNFM9N2F-
HUVEC or NIH3T3	M4HWdWZ2dmO2aX;uJIF{e2G7		NFfPSIlGfmGudXH0[YQh\m:{IITo[UBqdmirYnn0bY9vKG:oIHPlcIwheHKxbHnm[ZJifGmxbjDpcoR2[2WmIHL5JGZITiCrbjDIWXZGSyCxcjDOTWg{XDNiY3XscJMtKEmFNUC9Nk45\|ryP	MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yODh7M{OwN{c,OTB6OUOzNFM9N2F-
NIH/3T3	NH7RbppHfW6ldHnvckBie3OjeR?=		NUDmcWZEUW6qaXLpeIlwdiCxZjDhZ4llcWNiRlfGMZN1cW23bHH0[YQhTkeIUkGgeJlzd3OrbnWgZZV1d3Cqb4PwbI9zgWyjdHnvckBqdiCvb4Xz[UBPUUhxM2SzJINmdGy\|IHL5JIludXWwb3Lsc5R1cW6pLDDJR\|UxRTFyzszN	MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek86OTN7Nk[wK\|46OTN7Nk[wQE9iRg>?
NIH 3T3	NHzsVItHfW6ldHnvckBie3OjeR?=	NEW0PFk2KG2rboO=	MkfXTY5pcWKrdHnvckBw\iCIR1[gbY5lfWOnZDDGS2ZTOSCjdYTvdIhwe3Cqb4L5cIF1cW:wIHnuJI1wfXOnIF7JTEA{XDNiY3XscJMheHKnaX7jeYJifGWmIH\vdkA2KG2rboOg[o9tdG:5ZXSgZpkhTkeILYP0bY12dGG2aX;uJIZweiB3IH3pcpMhcW5icILld4Vv[2Vib3[gX4didW2jLUOyVH1CXFBiYomgV2RUNVCDR1WgZoF{\WRiYYX0c5Ji\GmxZ4LhdIh6NCCLQ{WwQVEx\|ryP	MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzlzNEO2Nkc,Ojd7MUSzOlI9N2F-
HUVEC or NIH3T3	NUnndoFCTnWwY4Tpc44h[XO\|YYm=		MoLuSZZidHWjdHXkJIZweiC2aHWgbY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25iaX7keYNm\CCkeTDQSGdHKGmwIFjVWmVEKG:{IF7JTFNVOyClZXzsd{whUUN3ME2yPE41\|ryP	NU\ZWWp4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUC4PVM{ODNpPkGwPFk{OzB\|PD;hQi=>
NIH/3T3	NFi3WZdIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		MnHDS5Jwf3SqIHnubIljcXSrb36gc4YhdW:3c3WgUmlJNzOWMzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGGlaXTpZ{BHT0Zvc4TpcZVt[XSnZDDbN2hefGi7bXnkbY5mKGmwY3;ydI9z[XSrb36=	MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek86OTN7Nk[wK\|46OTN7Nk[wQE9iRg>?
NIH/3T3	NVe3dY1jTnWwY4Tpc44h[XO\|YYm=		NFnVW4VKdmirYnn0bY9vKG:oIF\HSnIyKGmwIH3veZNmKE6LSD:zWFMh[2WubIOgZZN{\XO\|ZXSgZZMhcW6qaXLpeIlwdiCxZjDhSmdHNXO2aX31cIF1\WRicIC5NEBxcG:\|cHjvdJJwfGWrbjDwbI9{eGixconsZZRqd25iYomgbY1ufW6xYnzveJRqdmd?	M3rJUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzlzM{m2OlAoRjlzM{m2OlA9N2F-
NIH/3T3	MVXGeY5kfGmxbjDhd5NigQ>?		NEHvdpJKdmirYnn0bY9vKG:oIF\HSnIyKGmwIH3veZNmKE6LSD:zWFMh[2WubIOgZZN{\XO\|ZXSgZZMhcW6qaXLpeIlwdiCxZjDhZ4llcWNiRlfGMZN1cW23bHH0[YQhTVKNMTDwbI9{eGixconsZZRqd25iYomgbY1ufW6xYnzveJRqdmd?	MmS0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwQTF\|OU[2NEc,QTF\|OU[2NFww[T5?
NIH/3T3	MYTGeY5kfGmxbjDhd5NigQ>?		MWrJcohq[mm2aX;uJI9nKE[JRmKxJIlvKG2xdYPlJG5KUC9\|VEOgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCjY3nkbYMhTkeILYP0bY12dGG2ZXSgSXJMOiCyaH;zdIhwenmuYYTpc44h[nliaX3teY5w[myxdITpcoc>	M4iyOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzlzM{m2OlAoRjlzM{m2OlA9N2F-
NIHIR	M37XcGZ2dmO2aX;uJIF{e2G7		NF;3U2VKdmirYnn0bY9vKG:oIHnud5VtcW5vc4TpcZVt[XSnZDDpcpN2dGmwIILlZ4VxfG:{IHLleIEhe3WkdX7peEBifXSxcHjvd5Bpd3K7bHH0bY9vKGmwIH3veZNmKE6LSFnSJINmdGy\|	M2fwOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzlzM{m2OlAoRjlzM{m2OlA9N2F-
HER14	MkK1SpVv[3Srb36gZZN{[Xl?		M{nFRmlvcGmkaYTpc44hd2ZiRVfGMZN1cW23bHH0[YQhTUeIUjDwbI9{eGixconsZZRqd25iaX6gcY92e2ViSFXSNVQh[2WubIOgZpkhcW2vdX7vZoxwfHSrbne=	NXToZYZURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxOUGzPVY3OCd-OUGzPVY3ODxxYU6=
HER14	NIfDN\|dHfW6ldHnvckBie3OjeR?=		M{\IN2lvcGmkaYTpc44hd2ZiRVfGVkBqdiCvb4Xz[UBJTVJzNDDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKEWJRj3zeIlufWyjdHXkJHNp[yCyaH;zdIhwenmuYYTpc44h[nliaX3teY5w[myxdITpcoc>	M37KbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzlzM{m2OlAoRjlzM{m2OlA9N2F-
HER14	NWOzc5pbTnWwY4Tpc44h[XO\|YYm=		MlPPTY5pcWKrdHnvckBw\iCHR1\SJIlvKG2xdYPlJGhGWjF2IHPlcIx{KGG\|c3Xzd4VlKGG\|IHnubIljcXSrb36gc4YhTUeILYP0bY12dGG2ZXSgSXJMOiCjY4TpeoF1cW:wIHL5JIludXWwb3Lsc5R1cW6p	NXXPT3J2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxOUGzPVY3OCd-OUGzPVY3ODxxYU6=
NIHIR	NF3UcY5HfW6ldHnvckBie3OjeR?=		MYfJcohq[mm2aX;uJI9nKGmwc4XsbY4hemWlZYD0c5IhcW5ibX;1d4UhVkmKSWKgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCrboP1cIlvNXO2aX31cIF1\WRiSWLTNUBxcG:\|cHjvdplt[XSrb36=	NFu4d5I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi97MUO5OlYxLz57MUO5OlYxRC:jPh?=
NIH/3T3	NIW4fHJHfW6ldHnvckBie3OjeR?=		NGPFflJKdmirYnn0bY9vKG:oIGDES2ZTKGmwIH3veZNmKE6LSD:zWFMh[2WubIOgZZN{\XO\|ZXSgZZMhcW6qaXLpeIlwdiCxZjDQSGdHNXO2aX31cIF1\WRidInyc5NqdmViYYX0c5Bpd3OyaH;yfYxifGmxbjDifUBqdW23bn;icI91fGmwZx?=	NI\XT\|E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi97MUO5OlYxLz57MUO5OlYxRC:jPh?=
NIH/3T3	M{f2RWZ2dmO2aX;uJIF{e2G7		MV;Jcohq[mm2aX;uJI9nKFCGR1\SJIlvKG2xdYPlJG5KUC9\|VEOgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCSRFfGMZN1cW23bHH0[YQheGixc4Doc4xqeGG\|ZTDDJIdidW2jIIDoc5NxcG:{eXzheIlwdiCkeTDpcY12dm:kbH;0eIlv\w>?	Mk\kQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwQTF\|OU[2NEc,QTF\|OU[2NFww[T5?
NIH/3T3	Mlv2SpVv[3Srb36gZZN{[Xl?		MlX2TY5pcWKrdHnvckBw\iCSRFfGVkBqdiCvb4Xz[UBPUUhxM2SzJINmdGy\|IHHzd4V{e2WmIHHzJHBFT0Zvc4TpcZVt[XSnZDDFdoszKGGldHn2ZZRqd25iYomgbY1ufW6xYnzveJRqdmd?	NXfzXVVtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxOUGzPVY3OCd-OUGzPVY3ODxxYU6=

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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.

References

[4] Li Y, et al. Calcif Tissue Int. 2013, 93(6), 556-5 64.

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Solubility (25°C)

In vitro

Chemical Information

Molecular Weight	296.32
Formula	C₁₇H₁₆N₂O₃
CAS No.	215543-92-3
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CC1=CNC(=C1CCC(=O)O)C=C2C3=CC=CC=C3NC2=O

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