Sunitinib Malate

For research use only.

Licensed by Pfizer Catalog No.S1042

66 publications

Sunitinib Malate Chemical Structure

CAS No. 341031-54-7

Sunitinib Malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit. Sunitinib Malate effectively inhibits autophosphorylation of Ire1α. Sunitinib Malate increases both death receptor and mitochondrial-dependent apoptosis.

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Selleck's Sunitinib Malate has been cited by 66 publications

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Choose Selective PDGFR Inhibitors

Biological Activity

Description Sunitinib Malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit. Sunitinib Malate effectively inhibits autophosphorylation of Ire1α. Sunitinib Malate increases both death receptor and mitochondrial-dependent apoptosis.
Targets
Kit [1]
(Cell-free assay)
FLT3 [1]
(Cell-free assay)
PDGFRβ [1]
(Cell-free assay)
VEGFR2 [1]
(Cell-free assay)
2 nM 80 nM
In vitro

Sunitinib also potently inhibits Kit and FLT-3. [1] Sunitinib is a potent ATP-competitive inhibitor of VEGFR2 (Flk1) and PDGFRβ with Ki of 9 nM and 8 nM, respectively, displaying >10-fold higher selectivity for VEGFR2 and PDGFR than FGFR-1, EGFR, Cdk2, Met, IGFR-1, Abl, and src. In serum-starved NIH-3T3 cells expressing VEGFR2 or PDGFRβ, Sunitinib inhibits VEGF-dependent VEGFR2 phosphorylation and PDGF-dependent PDGFRβ phosphorylation with IC50 of 10 nM and 10 nM, respectively. Sunitinib inhibits VEGF-induced proliferation of serum-starved HUVECs with IC50 of 40 nM, and inhibits PDGF-induced proliferation of NIH-3T3 cells overexpressing PDGFRβ or PDGFRα with IC50 of 39 nM and 69 nM, respectively. [2] Sunitinib inhibits phosphorylation of wild-type FLT3, FLT3-ITD, and FLT3-Asp835 with IC50 of 250 nM, 50 nM, and 30 nM, respectively. Sunitinib inhibits the proliferation of MV4;11 and OC1-AML5 cells with IC50 of 8 nM and 14 nM, respectively, and induces apoptosis in a dose-dependent manner. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
3T3 NVG0NmV[U2mwYYPlJGF{e2G7 NWDWbId2UW6qaXLpeIlwdiCxZjDQSGdHNWmwZIXj[YQhSnKmVTDpcoNwenCxcnH0bY9vKHerdHigTWM2OCCxZjCwMlAxPyEQvF2= NUi0V49[OTJ4NE[wNVk>
3T3 NHrXU2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLa[2xVUW6qaXLpeIlwdiCxZjDQcIF1\WyndD3k[ZJqfmWmIHfyc5d1cCCoYXP0c5IhcW6mdXPl[EA{XDNiY3XscEBxem:uaX\ldoF1cW:wIIfpeIghUUN3MDDv[kAxNjBzIN88US=> MorZNVI3PDZyMUm=
3T3 M4X0U2Z2dmO2aX;uJGF{e2G7 M3q4fGlvcGmkaYTpc44hd2ZiVnHzZ5Vt[XJiZX7kc5Rp\WyrYXyg[5Jwf3SqIH\hZ5RweiC{ZXPldJRweiC5aYToJGlEPTBib3[gNE4xPSEQvF2= NIS4T40yOjZ2NkCxPS=>
3T3 M{fmT2tqdmG|ZTDBd5NigQ>? MYeyNEBucW5? NIHqdWhFVVOR MUHD[YxtfWyjcjDpcohq[mm2aX;uJI9nKF[HR1[gbY5lfWOnZDDoeY1idiCNRGKgdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAxNjB{MjFOwG0> NHHhd5oyPjF4MkCwPC=>
NIH3T3 M1n4U2tqdmG|ZTDBd5NigQ>? M2njTlIxKG2rbh?= MoXCSG1UVw>? NEnoOGpqdmirYnn0JIh2dWGwIFvEVkBscW6jc3Wg[ZhxemW|c3XkJJdqfGhiSVO1NEBw\iByLkCxPEDPxE1? MV6xOlE3OjByOB?=
A549 MlrQSpVv[3Srb36gRZN{[Xl? NGD6fXJFVVOR Ml\yTY5pcWKrdHnvckBw\iClLV3leEBl\XCnbnTlcpQhUEeILXnu[JVk\WRiaIXtZY4hSTV2OTDj[YxtKG2rZ4LheIlwdiC5aYToJGlEPTBib3[gNkDPxE1? MkPTNVg1OzRzNEW=
DU145 M4\R[2Z2dmO2aX;uJGF{e2G7 NGnncZhFVVOR M2DP[mlvcGmkaYTpc44hd2ZiYz3N[ZQh\GWyZX7k[Y51KEiJRj3pcoR2[2WmIHj1cYFvKESXMUS1JINmdGxic3PheJRmemmwZzD3bZRpKEmFNUCgc4YhOTBizszN MoTKNVg1OzRzNEW=
KB3-1 M2O0Z2N6fG:2b4jpZ{BCe3OjeR?= NEPJNWc4OiCq NXroW4VETE2VTx?= M1LpSWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHAu\3BvbnXnZZRqfmViS1KtN{0yKGOnbHzzJJdqfGhiSVO1NEBw\iB{LkOg{txO M16yXlE6Ozl5M{Ky
KBV1 M320U2N6fG:2b4jpZ{BCe3OjeR?= MUe3NkBp M{jQW2ROW09? NITXWIREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRNWeueXPvdJJwfGWrbj3lfJBz\XO|aX7nJGtDXjFiY3XscJMhf2m2aDDJR|UxKG:oIESuNUDPxE1? M1iwclE6Ozl5M{Ky
A375 MVfDfZRwfG:6aXOgRZN{[Xl? MmfyO|IhcA>? M{\xU2ROW09? MlLCTWM2OD13LkSg{txO NVXRcGt7OTl4NUS0NFg>
RS4-11 MUPGeY5kfGmxbjDBd5NigQ>? NIO1SIgzKGh? NUD6bW9QUW6qaXLpeIlwdiCxZjDGUHQ{KGG3dH;wbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFAvODB7OTFOwG0> NEPJWG4yQTZ3NESwPC=>
RS4-11 MUDGeY5kfGmxbjDBd5NigQ>? NU\K[5ZyOiCq MoHTTY5pcWKrdHnvckBw\iCITGSzJGlVTCCvdYThcpQh[XW2b4Doc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gNE4xOzRizszN NHHEWGsyQTZ3NESwPC=>
Sf9 MnXGT4lv[XOnIFHzd4F6 MoXQN|AhdWmw Mn75TY5pcWKrdHnvckBw\iCJU2SteIFo\2WmIG\FS2ZTKGW6cILld5Nm\CC5aYToJGlEPTBib3[gNE4yQDVizszN NE\VdWcyQTh3NEC1NS=>
Ba/F3 NHe3dHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXGO|IhcA>? NWnCOIVrUUN3ME2xMlIh|ryP MViyNFEyPzByNB?=
BaPTC2 M3zPNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDDO3E4OiCq MlXDTWM2OD1yLkKyJO69VQ>? MoPENlAyOTdyMES=
Sf9 MXnGeY5kfGmxbjDBd5NigQ>? M1PXRVEhcA>? MYHEUXNQ NITLfmJKdmirYnn0bY9vKG:oIHj1cYFvKHKnY3;tZolv[W62IFjpd{11[WepZXSgVmVVKGW6cILld5Nm\CC5aYToJGlEPTBib3[gNU4{KM7:TR?= MmrBNlAyOTdyMES=
H4 NEntTZREgXSxdH;4bYMhSXO|YYm= MXOxNEDPxE1? MmDLWI95cWOrdImgbY4hcHWvYX6gTFQh[2WubIO= NYPLSG5lOjB|NUC4NFY>
SF-539 NX\ucHp[U2mwYYPlJGF{e2G7 NX;aSVJwOzN|IN88US=> NGnjS3g3OCCvaX6= MX3EUXNQ NXi3RlBOUW6qaXLpeIlwdiCxZjDQSGdHWmKndHGgdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAyOi5{IN88US=> M1yzelIxPDB|N{Cw
U251 Mn;iT4lv[XOnIFHzd4F6 MYizN|Mh|ryP MkXJOlAhdWmw MkjRSG1UVw>? MYnJcohq[mm2aX;uJI9nKF[HR1\SNkBxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDF6Lkmg{txO M1raNlIxPDB|N{Cw
A431 NGfLXIZMcW6jc3WgRZN{[Xl? Mn;STY5pcWKrdHnvckBw\iCSRFfGVoJmfGFiZYjwdoV{e2WmIIfpeIghUUN3MDDv[kAyOi5{IN88US=> NXnncVBoOjB3NUiwO|I>
A431 NF3XXWFMcW6jc3WgRZN{[Xl? MYTJcohq[mm2aX;uJI9nKF[HR1\SNkBmgHC{ZYPz[YQhf2m2aDDJR|UxKG:oIEG4Mlkh|ryP MVqyNFU2QDB5Mh?=
HepG2 Mlj5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHCO|IhcA>? MnSxTWM2OD1|LkixJO69VQ>? MnjiNlA2PzB3Mk[=
Kasumi-1 M1XkWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPCSlFVPzJiaB?= MXjJR|UxRTBwMEG2JO69VQ>? NXrZelBiOjB3N{C1NlY>
RS4-11 NYnGNnZxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{m1bVczKGh? NWm4cFZsUUN3ME2xJO69VQ>? NGTaXWQzODV5MEWyOi=>
THP1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVm3NkBp MkX6TWM2OD1yLkWg{txO NGfiZ2czODV5MEWyOi=>
Kasumi-1 MnLJSpVv[3Srb36gRZN{[Xl? Mlf2TY5pcWKrdHnvckBw\iClLVvpeEBifXSxcHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCwMlAyPSEQvF2= NYLqdotZOjB6M{OwN|k>
A549 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWqxOkBp NI\rbFFCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzz Ml\qNlE1PTB2NkO=
HL60 M4X5TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH20dJoyPiCq NYTIUoVtSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gTGw3OCClZXzsdy=> NIX1ZpUzOTR3MES2Ny=>
HUVEC MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXpUopSOTZiaB?= NVjsR5NWUW6qaXLpeIlwdiCxZjDWSWdHNWmwZIXj[YQh[2WubDDwdo9tcW[ncnH0bY9vKHerdHigTWM2OCCxZjCyMlc2KM7:TR?= NXLPZ4ZpOjF2NUC0OlM>
HUVEC MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnEOHYzOTZiaB?= NFTsd29KdmirYnn0bY9vKG:oIHLGS2YucW6mdXPl[EBk\WyuIIDyc4xq\mW{YYTpc44hf2m2aDDJR|UxKG:oIESuNFQh|ryP Ml;xNlE1PTB2NkO=
IM9 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVexOkBp MkPiRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSV25JINmdGy| MWeyNVQ2ODR4Mx?=
K562 NVTiR25{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4K3bVE3KGh? NGLnWWZCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzz MWKyNVQ2ODR4Mx?=
MDA-MB-231 NFvp[4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3mzR|E3KGh? MoCyRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTJ|MTDj[Yxtew>? NGPLO4UzOTR3MES2Ny=>
H460 NGjhTo1EgXSxdH;4bYMhSXO|YYm= Mn\GO|IhcA>? MlXHTWM2OD1{Lkeg{txO MWqyNVYzOTh6MB?=
SMMC7721 NImxdIREgXSxdH;4bYMhSXO|YYm= NInIfos4OiCq NVfaT281UUN3ME22MlQ4KM7:TR?= NF23SJUzOTZ{MUi4NC=>
WI38 MXTDfZRwfG:6aXOgRZN{[Xl? MXG3NkBp NUm5eI9bUUN3ME24MlU3KM7:TR?= NUTGXHdjOjF4MkG4PFA>
HEK293 MXfLbY5ie2ViQYPzZZk> MlS2NVAxKG6P NV\xS4VWOSCq NFLkPJRld2W|IH7veEBqdmirYnn0JHZGT0ZvaX7keYNm\CCjdYTvdIhwe3Cqb4L5cIF1cW:wIH;mJJR6em:|aX7lJFEyPzVicnXzbYR2\SCxbjDWSWdHWjJiZYjwdoV{e2WmIHnuJGhGUzJ7MzDj[Yxtew>? MVmyNVg5PTJ6Nx?=
HUVEC MWDGeY5kfGmxbjDBd5NigQ>? NGSzbocyKM7:TR?= MX2yOEBp NH[wRlZCdnSrYX7nbY9o\W6rYzDhZ5Rqfmm2eTDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCYRVfGMYlv\HWlZXSgZ4VtdCCvaXfyZZRqd25? NFTKUXQzOTl4M{OwOS=>
HUVEC MVHGeY5kfGmxbjDBd5NigQ>? MVWxJO69VQ>? NFH6S|IyKGh? NFrvfWZKdmirYnn0bY9vKG:oIFXST{BxcG:|cHjvdplt[XSrb36gZZQhXGi{MkCyM3R6ejJyNDDpckBXTUeILYP0bY12dGG2ZXSgTHVXTUN? NH;ZXXozOTl4M{OwOS=>
HUVEC M33VUGZ2dmO2aX;uJGF{e2G7 NEfHOmUyKM7:TR?= MlLVNUBp NUfWVW9PUW6qaXLpeIlwdiCxZjDlUm9UKHCqb4PwbI9zgWyjdHnvckBifCCVZYKtNVE4OiCrbjDWSWdHNXO2aX31cIF1\WRiSGXWSWM> M2P4XlIyQTZ|M{C1
HUVEC MX7LbY5ie2ViQYPzZZk> NH\DeWoyKM7:TR?= MVWxJIg> NXTVVml5UW6qaXLpeIlwdiCxZjDWSWdHWjJicHjvd5Bpd3K7bHH0bY9vKGG2IIT5dk0yOTd3IHnuJHZGT0Zvc4TpcZVt[XSnZDDIWXZGSw>? NUPzcVR6OjF7NkOzNFU>
HUVEC NUHYNI14TnWwY4Tpc44hSXO|YYm= M4rVVFEh|ryP M3WwRlEhcA>? NIHNN4Zld2W|IH7veEBqdmirYnn0JGFMXCCyaH;zdIhwenmuYYTpc44h[XRiU3XyMVQ4OyCrbjDWSWdHNXO2aX31cIF1\WRiSGXWSWM> MnjKNlE6PjN|MEW=
HL60 MXnDfZRwfG:6aXOgRZN{[Xl? NIDiNIc2OCEQvF2= NWO4W4NnPDhiaB?= NFLOSXJFVVOR M2r4ZmlEPTB;MUWuOUDPxE1? NEPBO2MzOjBzOUG4PC=>
K562 NVPkUmlKS3m2b4TvfIlkKEG|c3H5 NWftSHJPPTBizszN M13JPVQ5KGh? NETIXohFVVOR NIXwU4VKSzVyPUKxMlkh|ryP Mn;rNlIxOTlzOEi=
PC3 M3HHSGN6fG:2b4jpZ{BCe3OjeR?= NH7VVXM2OCEQvF2= MUS0PEBp MWPEUXNQ NWH3XmFmUUN3ME2yOU4yKM7:TR?= NH\qeWwzOjBzOUG4PC=>
SF-539 NXHyRnZoU2mwYYPlJGF{e2G7 NGjKN5M{OzNizszN M4raVlYxKG2rbh?= MVXJcohq[mm2aX;uJI9nKFCGR1\SZoV1[SC2eYLvd4lv\SCtaX7hd4Uh[WO2aY\peJkhcW5iUFTHSk1DSi2|dHnteYxifGWmIHj1cYFvKFOILUWzPUBk\WyuczD3bZRpKEmFNUCgc4YhOTJwMjFOwG0> M3jpUlIzOjB2N{Sx
HAEC MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LrOlExOCEQvF2= Mn;CO|IhcA>? Mk\WRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQVXDJINmdGy|IHX4dJJme3OrbnegWmVITlJid3n0bEBKSzVyIH;mJFAvOSEQvF2= NYPYOY1JOjJ2NES2O|k>
HT-29 M1\S[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVGxNFAh|ryP MVi3NkBp M3TqeWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSGStNlkh[2WubIOg[ZhxemW|c3nu[{BXTUeIUjD3bZRpKEmFNUCgc4YhOC5|MzFOwG0> Mn7FNlI1PDR4N{m=
MV4-11 M{npemN6fG:2b4jpZ{BCe3OjeR?= NXnWbJRCPzJiaB?= M3GxXmlEPTB;MD6wNFMh|ryP MkntNlI1PTJ3MUi=
HepG2 NXy0b2hqS3m2b4TvfIlkKEG|c3H5 NX;6U5Z7PDhiaB?= NV7CTo96UUN3ME2xN{4zPCEQvF2= M3z5XFIzPDh|NkC4
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MCF7 MoCyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHu[5E{OTByIN88US=> MljVOFghcA>? NHLCbGpFVVOR MlrFS2k2OT1{IN88US=> MVmyNlU3ODZ{Nx?=
MDA-MB-435 NGfONpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nablExOCEQvF2= NWrCSG9vPDhiaB?= M33JV2ROW09? NHr3RmxIUTV{PUKg{txO M1zEZVIzPTZyNkK3
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SNB19 NVvDOXJNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXmxNFAh|ryP MmXXOFghcA>? MUfEUXNQ MnSzS2k2PD1zMDFOwG0> MoHKNlI2PjB4Mke=
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ACHN NIHUTGdEgXSxdH;4bYMhSXO|YYm= Mon6OkBl NV;ufnNVUUN3ME2yMlUh|ryP MkLDNlM{PjBzMES=
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HUVEC MlfaT4lv[XOnIFHzd4F6 NITycYIzODBizszN NWH5dW9YTE2VTx?= MX;Jcohq[mm2aX;uJI9nKF[HR1\SNkBxcG:|cHjvdplt[XSrb36gbY4h\3Kxd4ToJIZi[3Sxcj3zeIlufWyjdHXkJGhWXkWF NFe0bowzOzV6M{mxNS=>
HUVEC MlL3T4lv[XOnIFHzd4F6 MmPMNlAxKM7:TR?= M{fFZmROW09? NFvTNJBKdmirYnn0bY9vKG:oIG\FS2ZTOSCyaH;zdIhwenmuYYTpc44hcW5iZ4Lve5RpKG[jY4Tvdk1{fGmvdXzheIVlKEiXVlXD NETacI4zOzV6M{mxNS=>
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HCT116 M3;Tb2N6fG:2b4jpZ{BCe3OjeR?= M{DF[FczKGh? M1m2cWROW09? MnS0TWM2OD12LkexJO69VQ>? MVOyN|YxOjR2MR?=
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BGC MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTQSXE4OiCq NGrNVHFFVVOR M1v0PGlEPTB;ND63PEDPxE1? NIHL[nAzOzl7OUC0NC=>
BxPC3 M2e4Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHFSlNFPzJiaB?= MVnEUXNQ NVLQ[3psUUN3ME2zMlY{KM7:TR?= NWi1c5hwOjN7OUmwOFA>
HT-29 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXm0Om0zPzJiaB?= MV;EUXNQ M3LT[2lEPTB;MT60O{DPxE1? NFu1XIQzOzl7OUC0NC=>
T24 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVm3NkBp MnzrSG1UVw>? MXHJR|UxRTJwNESg{txO M3G5N|I{QTl7MESw
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MCF7 MVTDfZRwfG:6aXOgRZN{[Xl? NV7HdGlSPzJiaB?= NGHHdHRFVVOR M{jBR2lEPTB;MD6wNlcyKM7:TR?= NILBXJgzPDh7ME[1Ni=>
MCF7 NGOwOVNEgXSxdH;4bYMhSXO|YYm= NHv0S5Q4OiCq NH7jbGVFVVOR NF\0fGlKSzVyPUCuNFI6OyEQvF2= MYmyOFg6ODZ3Mh?=
MDA-MB-231 NVTmTYVXS3m2b4TvfIlkKEG|c3H5 NV\ucXpZPzJiaB?= M4LFOWROW09? NHnqUJZKSzVyPUCuNFIzOyEQvF2= NYXBTWpUOjR6OUC2OVI>
MDA-MB-435 M4\veWN6fG:2b4jpZ{BCe3OjeR?= NXLFNYxmPzJiaB?= Ml3nSG1UVw>? NH7y[XlKSzVyPUCuNFA6PyEQvF2= MWOyOFg6ODZ3Mh?=
MDA-MB-468 NWn4OGNvS3m2b4TvfIlkKEG|c3H5 M1nISVczKGh? NXnSUnpOTE2VTx?= NULLN3pTUUN3ME2wMlAxPjFizszN MofpNlQ5QTB4NUK=
A431 NUPqSFNUU2mwYYPlJGF{e2G7 NFTMfoQyOCEQvF2= NV\qSWo{OSCq NYfGPJpjTE2VTx?= NIqzUWFKdmirYnn0bY9vKG:oIFXHSnIhf2m2aDDJR|UxKG:oIECuNVczOSEQvF2= NIHYOYozPDh7ME[1Ni=>
SH-SY5Y MWTLbY5ie2ViQYPzZZk> MY[xNEDPxE1? MmrPNUBp Mn3JSG1UVw>? NXPReoFUUW6qaXLpeIlwdiCxZjDQSGdHWmKndHGge4l1cCCLQ{WwJI9nKDBwMEizNUDPxE1? M4LT[lI1QDlyNkWy
U251 M{HaeGtqdmG|ZTDBd5NigQ>? MXSxNEDPxE1? MVexJIg> NXXhdnVETE2VTx?= M3HDVGlvcGmkaYTpc44hd2ZiVlXHSnIzKHerdHigTWM2OCCxZjCwMlAyQDlizszN MoHoNlQ5QTB4NUK=
Bel7402 MkPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnSxO|IhcA>? M2XSZmROW09? MoDKTWM2OD1{Lk[3JO69VQ>? NFvaRlYzPDlyNEm2NS=>
HK2 NHXwXW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDoV3U4OiCq M4LsZWROW09? M4nwU2lEPTB;NT64OUDPxE1? MoPDNlQ6ODR7NkG=
LO2 NVXBW3JoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLyU4U4OiCq NEO2dlJFVVOR MonsTWM2OD1zOT65N{DPxE1? MoKxNlQ6ODR7NkG=
MV4-11 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLLOFghcA>? NGSxXVRFVVOR M3vaOmlEPTB;MD6wNFMh|ryP M1jTVVI1QTB2OU[x
NCI-H3122 M4jqW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jDRVczKGh? MULEUXNQ NWXyTG8xUUN3ME2wMlg{KM7:TR?= M3O4S|I1QTB2OU[x
NCI-H460 MlGwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLzOpRvPzJiaB?= NFLtd5dFVVOR NXnVdXBVUUN3ME20MlMyKM7:TR?= NF\GXm8zPDlyNEm2NS=>
NCI-H526 M1rLemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEO0XHg4OiCq MkXwSG1UVw>? NYnVeY5xUUN3ME2xMlAyKM7:TR?= Mm\KNlQ6ODR7NkG=
TT Mn7aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zDZVczKGh? MXXEUXNQ MWXJR|UxRTBwMESg{txO MmnLNlQ6ODR7NkG=
EoL-1-cell M{TFe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4iyTmlEPTB;MT62OEBxVQ>? M1HWSHNCVkeHUh?=
MV-4-11 MlHxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{T1TWlEPTB;MkeyJJBO MVPTRW5ITVJ?
NOS-1 NHzUW5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\qeWxKSzVyPUG1MlMhdk1? MVLTRW5ITVJ?
CGTH-W-1 NH\TXFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTNyLkm0JI5O MoXNV2FPT0WU
MONO-MAC-6 NF3RSWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYrmc3kyUUN3ME2zN{45KG6P NET1UnlUSU6JRWK=
ALL-PO MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTd7Lki5JI5O NFvIeHVUSU6JRWK=
NKM-1 NGXRSnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTl6LkWyJI5O NILDfXRUSU6JRWK=
KM12 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfsWVhKSzVyPUO1NE4yPCCwTR?= NWHRe41jW0GQR1XS
TE-15 M3TUeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnmSYZtUUN3ME21NFcvPjFibl2= NXTpXJI4W0GQR1XS
697 NEPFS3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TsOWlEPTB;NkG0MlI2KG6P M1i0VXNCVkeHUh?=
MOLT-16 NITsfnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIi5d2FKSzVyPU[zNU4{OiCwTR?= MVHTRW5ITVJ?
GB-1 M3HzXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTdzMD6yN{BvVQ>? NYS1UopEW0GQR1XS
TE-12 M{jK[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPhTWM2OD16MESuOVUhdk1? NEXnSFFUSU6JRWK=
ES6 M1v0OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTl6MT6wOkBvVQ>? NIDXPIRUSU6JRWK=
LC-2-ad NF3aUVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\iTWM2OD1zLkGxOFA4KM7:TR?= M4SxW3NCVkeHUh?=
BL-70 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrBeppKSzVyPUGuNVE5PDZizszN M3vxOnNCVkeHUh?=
ETK-1 NHTjeW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LCN2lEPTB;MT6yPFU5KM7:TR?= NV3OcmRtW0GQR1XS
A4-Fuk MkXMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzBb21KSzVyPUGuN|QyPDFizszN MYrTRW5ITVJ?
OCI-AML2 MnrRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\5e|hpUUN3ME2xMlM3QDVzIN88US=> NVXV[2Z7W0GQR1XS
SIG-M5 MknwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TJcmlEPTB;MT6zO|AxQSEQvF2= M{DkSnNCVkeHUh?=
NCI-SNU-16 MmO5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTFwNE[0PFYh|ryP MoHrV2FPT0WU
PSN1 NU\o[5NwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\jOGY2UUN3ME2xMlUxPjd4IN88US=> M4HoT3NCVkeHUh?=
SR Mn3TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vQdmlEPTB;MT61OFU4OiEQvF2= M2DtOHNCVkeHUh?=
A3-KAW NF\j[FRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrYdGNKSzVyPUGuOlI2PDZizszN NIPCbJVUSU6JRWK=
KS-1 NFnzTYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXHTWM2OD1zLk[5NlQ4KM7:TR?= M3jiNHNCVkeHUh?=
CTV-1 NFvRSIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4rId2lEPTB;MT63Nlc2OSEQvF2= Mn\6V2FPT0WU
LB1047-RCC M1y3eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmKxTWM2OD1zLkixOlI1KM7:TR?= M2\a[3NCVkeHUh?=
EMG-01 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDFWItKSzVyPUGuPFM2PjNizszN NY\LUnlMW0GQR1XS
TE-11 MoTKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrmUo9KSzVyPUGuPFM6QDVizszN NX7rcItDW0GQR1XS
CMK NVXHRY9kT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPyTWM2OD1zLkm1OVE4KM7:TR?= MUjTRW5ITVJ?
NB1 NX\YW3BOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\UVGJCUUN3ME2xMlk3OTF5IN88US=> NYLqNmU4W0GQR1XS
HAL-01 NFnBPHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTJwMEW5OFYh|ryP NVLmc2xYW0GQR1XS
DEL MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTJwMEi0PFIh|ryP NE\kdoZUSU6JRWK=
RL95-2 NFXEbHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTJwMUGxN|ch|ryP NVjiXY01W0GQR1XS
KARPAS-299 NVfzV5FET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NID5VXpKSzVyPUKuNVE{OTNizszN MV3TRW5ITVJ?
EW-16 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{C3PWlEPTB;Mj6xN|UxQCEQvF2= NVTEcpJHW0GQR1XS
RS4-11 NWjPcppmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHG3WXBKSzVyPUKuNVc6OjRizszN M3zFe3NCVkeHUh?=
BB30-HNC NUTme21nT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTJwMkKzO|Uh|ryP NF[wSFBUSU6JRWK=
DOHH-2 NEXORllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzITWM2OD1{LkOzOFMyKM7:TR?= Ml\xV2FPT0WU
RPMI-8402 Ml30S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTJwM{O2NVgh|ryP NFTNRYdUSU6JRWK=
BV-173 NGCxcY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\sZWlEPTB;Mj6zN|Y3KM7:TR?= MWTTRW5ITVJ?
TE-10 M17M[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzzeFJnUUN3ME2yMlM1Ozh2IN88US=> MXPTRW5ITVJ?
TE-8 M3zZW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmq2TWM2OD1{LkO3NFM5KM7:TR?= MlnUV2FPT0WU
K052 NI\qT|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTJwNECyNFIh|ryP MlXQV2FPT0WU
KARPAS-45 M4W4VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TxZmlEPTB;Mj60PVQ1PiEQvF2= MVjTRW5ITVJ?
SK-NEP-1 NFLQbYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnsVFBJUUN3ME2yMlYxOjN5IN88US=> NFnlN4tUSU6JRWK=
KGN NGG4fZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWqzeHNsUUN3ME2yMlYxOzN7IN88US=> Mm\EV2FPT0WU
ML-2 MkPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33TVGlEPTB;Mj62N|UyOiEQvF2= MW\TRW5ITVJ?
LAMA-84 NGLucVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTJwNkm1OFUh|ryP M3fOdnNCVkeHUh?=
LXF-289 M3HHfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHPTWM2OD1{LkeyPVg6KM7:TR?= MlLiV2FPT0WU
A101D NX3qRVBZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGG3WotKSzVyPUKuO|g{ODRizszN M1:4SHNCVkeHUh?=
KY821 MnPLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX62N2pmUUN3ME2yMlc6PzV6IN88US=> NWL0[FU2W0GQR1XS
ES4 M17iOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTJwOEC2Nlgh|ryP M3LsVnNCVkeHUh?=
SCC-3 NF\ReGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPpTWM2OD1{LkiyPFkyKM7:TR?= Mn;hV2FPT0WU
NALM-6 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HXOGlEPTB;Mj65NFQ4OyEQvF2= MnHKV2FPT0WU
BL-41 M1jY[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjEVmJKSzVyPUKuPVEzOjJizszN NFnuSXVUSU6JRWK=
OPM-2 NV7VeYlrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXX[GJjUUN3ME2zMlA2QTV2IN88US=> Mo\pV2FPT0WU
SF126 MlS4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTNwME[xPVgh|ryP MVrTRW5ITVJ?
BE-13 Ml\LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVq2[WFRUUN3ME2zMlI{OTFzIN88US=> Ml\rV2FPT0WU
SF268 NWT0ZXFXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;W[mR[UUN3ME2zMlMzQDZ7IN88US=> MmHaV2FPT0WU
MOLT-4 MlG3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnP1TWM2OD1|LkO5PFM5KM7:TR?= MYTTRW5ITVJ?
PF-382 NIXQN4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHFOIhmUUN3ME2zMlQ1PTdizszN M1n0ZXNCVkeHUh?=
HEL MlfyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk[2TWM2OD1|LkS4NFA2KM7:TR?= M3fKRXNCVkeHUh?=
RPMI-6666 NHT0TVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2i2SGlEPTB;Mz61OFE4OSEQvF2= NFK1WJNUSU6JRWK=
QIMR-WIL NYTiR4J{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTNwNkOzPVEh|ryP M{P2d3NCVkeHUh?=
ATN-1 M3\Kcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTNwNkexNVQh|ryP MV;TRW5ITVJ?
BB49-HNC MkTKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTNwN{C1NFgh|ryP MUHTRW5ITVJ?
HCE-4 MmWwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTNwN{i2OFIh|ryP NEjHZnJUSU6JRWK=
SK-LMS-1 NUC5cGV6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHhTWM2OD1|LkizN|M5KM7:TR?= NEjFU|FUSU6JRWK=
MS-1 M1;IfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXflfFNKUUN3ME2zMlg{Pzd6IN88US=> M{PDVHNCVkeHUh?=
JAR MkXTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELld4tKSzVyPUOuPVg5OzJizszN Mlv4V2FPT0WU
KE-37 NYfQRVA2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTRwME[xOVgh|ryP NUnCUm9SW0GQR1XS
LB996-RCC MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfBVnVmUUN3ME20MlEzOTZ6IN88US=> M33vfXNCVkeHUh?=
HH NF\YTo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLuTWM2OD12LkKwPVE1KM7:TR?= M3i5Z3NCVkeHUh?=
HL-60 M3rzRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfxWVVTUUN3ME20MlIyODZ3IN88US=> NIHvSIVUSU6JRWK=
HOP-62 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LmbWlEPTB;ND6zN|UzKM7:TR?= Ml\KV2FPT0WU
NOMO-1 NHHRO5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTRwM{O2PVkh|ryP Mn32V2FPT0WU
DU-4475 M2fxXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTRwM{[3Nlkh|ryP NXfHNlVFW0GQR1XS
LC4-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrWTWM2OD12LkO4NFch|ryP MXnTRW5ITVJ?
MC116 M4LPT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3:5dGlEPTB;ND60N|A5OSEQvF2= Mm[yV2FPT0WU
SW982 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rMPGlEPTB;ND61OVMxPyEQvF2= NIHD[ZlUSU6JRWK=
SK-N-DZ NYDveWdGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTRwNkewPVkh|ryP MlryV2FPT0WU
EW-1 NFrZXIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nlS2lEPTB;ND62O|kyOSEQvF2= NFnwTWhUSU6JRWK=
SU-DHL-1 Mn;lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDkUY9iUUN3ME20MlgxOTd2IN88US=> NEDCcnRUSU6JRWK=
L-363 NX;mNWN[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvzcpI3UUN3ME20MlgxPjJzIN88US=> MW\TRW5ITVJ?
OS-RC-2 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTRwOEezNUDPxE1? MWrTRW5ITVJ?
HD-MY-Z M1P1S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PCUmlEPTB;NT6xO|MxOSEQvF2= NHjldVNUSU6JRWK=
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SCH NFrINWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zK[WlEPTB;M{KuPFQ5PSEQvF2= NFrIR2lUSU6JRWK=
EHEB MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfZTWM2OD1|ND6xNVk{KM7:TR?= NXToRZU3W0GQR1XS
U-266 MkO0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknrTWM2OD1|ND6yO|gyKM7:TR?= MYPTRW5ITVJ?
EW-11 NYT2XIdtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTN2LkS3NlUh|ryP NY\xNJVIW0GQR1XS
TE-9 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTN5LkC0NFEh|ryP NVXoeWI5W0GQR1XS
ES3 NX7hZoQ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTN5LkWwNFQh|ryP MYjTRW5ITVJ?
NCI-H2141 Ml;hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDue2VKSzVyPUO4MlA5PDNizszN Ml7OV2FPT0WU
MPP-89 NHy5dnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTR{LkC1PFYh|ryP NX6xfW1HW0GQR1XS
SK-MEL-2 NE\JeGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7XTmc5UUN3ME20Nk43PDB3IN88US=> MX\TRW5ITVJ?
LC-1F NHqyNGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjUZYZiUUN3ME20N{4{Pjh{IN88US=> NX3uRYRsW0GQR1XS
NH-12 NFvtdIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXRTWM2OD12Mz65N|U6KM7:TR?= NVz1ZlVlW0GQR1XS
RKO MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfTRXNSUUN3ME20OE4yOjV{IN88US=> M4PUSnNCVkeHUh?=
KM-H2 NV7qd4RoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTR2Lkm1O|ch|ryP MUXTRW5ITVJ?
SK-UT-1 Mof3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7YPVNKSzVyPUS5Mlg5OjVizszN M{L3UHNCVkeHUh?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-AKT / AKT / p-ERK / ERK; 

PubMed: 24759734     


Effect of 72 h treatment with sunitinib on SH-SY5Y, SK N BE(2), SK-N-AS and IMR-32 NB cell lines analyzed by Western blot with pSer473Akt, Akt, pThr202/Thr204 Erk1/2 and Erk1/2 antibodies. β-actin was used as a loading control.

p-GSK3β / GSK3β / MYCN ; 

PubMed: 24759734     


Effect of sunitinib on GSK3β phosphorylation and on MYCN total protein in MYCN amplified NB cell lines.

p-STAT3 / STAT3 / p-Src / Src / p-AKT / AKT / p-ERK / ERK ; 

PubMed: 19244102     


Sunitinib reduced Stat3 and Src activity, with no dramatic reduction of AKT, MAPK and JAK signaling in 786-O cells. Tumor cells were treated with sunitinib at indicated concentrations for 2 h (left panels) or 24 h (right panels). Total cell lysates were prepared and western blots were performed using relevant antibodies to detect total protein levels, with β-actin used as the loading control.

24759734 19244102
Growth inhibition assay
Cell viability; 

PubMed: 24369536     


Isolated effects of sunitinib malate on urinary bladder-cancer cell lines viability, assessed by using the MTT assay. The data shown and bars represent the mean values ± SD (SD: standard deviation). *P < 0.05 versus untreated cells.

24369536
In vivo Consistent with the substantial and selective inhibition of VEGFR2 or PDGFR phosphorylation and signaling in vivo, Sunitinib (20-80 mg/kg/day) exhibits broad and potent dose-dependent anti-tumor activity against a variety of tumor xenograft models including HT-29, A431, Colo205, H-460, SF763T, C6, A375, or MDA-MB-435. Sunitinib dosing at 80 mg/kg/day for 21 days leads to complete tumor regression in six of eight mice, without tumor re-growing during a 110-day observation period after the end of treatment. Second round of treatment with Sunitinib remains efficacious against tumors that are not fully regressed during the first round of treatment. Sunitinib treatment results in significant decrease in tumor MVD, with ~40% reduction in SF763T glioma tumors. SU11248 treatment results in a complete inhibition of additional tumor growth of luciferase-expressing PC-3M xenografts, despite no reduction in tumor size. [2] Sunitinib treatment (20 mg/kg/day) dramatically suppresses the growth subcutaneous MV4;11 (FLT3-ITD) xenografts and prolongs survival in the FLT3-ITD bone marrow engraftment model. [3]

Protocol

Kinase Assay:[1]
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Biochemical Tyrosine Kinase Assays:

IC50 values for Sunitinib against VEGFR2 (Flk-1) and PDGFRβ are determined using glutathione S-transferasefusion proteins containing the complete cytoplasmic domain of the RTK. Biochemical tyrosine kinase assays to quantitate the trans-phosphorylation activity of VEGFR2 (Flk-1) and PDGFRβ are performed in 96-well microtiter plates precoated (20 μg/well in PBS; incubated overnight at 4 °C) with the peptide substrate poly-Glu,Tyr (4:1). Excess protein binding sites are blocked with the addition of 1-5% (w/v) BSA in PBS. Purified GST-fusion proteins are produced in baculovirus-infected insect cells. GST-VEGFR2 and GST-PDGFRβ are then added to the microtiter wells in 2 × concentration kinase dilution buffer consisting of 100 mM HEPES, 50 mM NaCl, 40 μM NaVO4, and 0.02% (w/v) BSA. The final enzyme concentration for GST-VEGFR2 or GST-PDGFRβ is 50 ng/mL. Twenty-five μL of diluted Sunitinib are subsequently added to each reaction well to produce a range of inhibitor concentrations appropriate for each enzyme. The kinase reaction is initiated by the addition of different concentrations of ATP in a solution of MnCl2 so that the final ATP concentrations spanned the Km for the enzyme, and the final concentration of MnCl2 is 10 mM. The plates are incubated for 5-15 minutes at room temperature before stopping the reaction with the addition of EDTA. The plates are then washed three times with TBST. Rabbit polyclonal antiphosphotyrosine antisera are added to the wells at a 1:10,000 dilution in TBST containing 0.5% (w/v) BSA, 0.025% (w/v) nonfat dry milk, and 100 μM NaVO4 and incubated for 1 hour at 37 °C. The plates are then washed three times with TBST, followed by the addition of goat antirabbit antisera conjugated with horseradish peroxidase (1:10,000 dilution in TBST). The plates are incubated for 1 hour at 37 °C and then washed three times with TBST. The amount of phosphotyrosine in each well is quantitated after the addition of 2,2′-azino-di-[3-ethylbenzthiazoline sulfonate] as substrate.
Cell Research:[3]
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  • Cell lines: RS4;11, MV4;11, and OC1-AML5
  • Concentrations: Dissolved in DMSO, final concentrations ~10 μM
  • Incubation Time: 24 and 48 hours
  • Method: Cells are starved overnight in medium containing 0.1% FBS prior to addition of Sunitinib and FL (50 ng/mL; FLT3-WT cells only). Proliferation is measured after 48 hours of culture using the Alamar Blue assay or trypan blue cell viability assays. Apoptosis is measured 24 hours after Sunitinib addition by Western blotting to detect cleavage of poly (ADP-ribose) polymerase (PARP) or levels of caspase-3.
    (Only for Reference)
Animal Research:[2]
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  • Animal Models: Female nu/nu mice implanted s.c. with HT-29, A431, Colo205, H-460, SF763T, C6, A375, or MDA-MB-435, and male nu/nu mice bearing luciferase-expressing PC-3M tumors
  • Dosages: ~80 mg/kg
  • Administration: Orally once daily
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 15 mg/mL (28.16 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
4% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.
2mg/mL

* 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 532.56
Formula

C22H27FN4O2.C4H6O5

CAS No. 341031-54-7
Storage powder
in solvent
Synonyms N/A
Smiles CCN(CC)CCNC(=O)C1=C(NC(=C1C)C=C2C3=C(C=CC(=C3)F)NC2=O)C.C(C(C(=O)O)O)C(=O)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03916458 Recruiting -- Carcinoma Renal Cell Pfizer January 21 2020 --
NCT04115189 Active not recruiting Drug: Sunitinib Metastatic Renal Cell Carcinoma ( mRCC) Pfizer December 13 2019 --
NCT04033991 Active not recruiting Drug: Sunitinib|Drug: Axitinib Carcinoma|Renal Cell Pfizer September 27 2019 --
NCT03900793 Recruiting Drug: Losartan|Drug: Sunitinib Osteosarcoma University of Colorado Denver|National Cancer Institute (NCI) August 22 2019 Phase 1
NCT03846128 Not yet recruiting Biological: blood sample Metastatic Kidney Cancer University Hospital Rouen August 2019 --
NCT03905889 Recruiting Drug: Abemaciclib|Drug: Sunitinib Renal Cell Carcinoma Metastatic Milton S. Hershey Medical Center|Eli Lilly and Company June 5 2019 Phase 1

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.

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Frequently Asked Questions

  • Question 1:

    I was wondering that the compound is in its cis or trans form?

  • Answer:

    S1042 Sunitinib Malate is Z form.

  • Question 2:

    What is the difference between Sunitinib Malate(S1042) and Sunitinib(S7781)?

  • Answer:

    S1042 is the Malate salt form of Sunitinib. The biological activities of these two compounds are the same but the solubility of these two compounds in aqueous solvent are different.

PDGFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID