Sunitinib Malate

For research use only.

Licensed by Pfizer Catalog No.S1042

90 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 90 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
IRE1α [7]
()
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 MmPLT4lv[XOnIFHzd4F6 MVrJcohq[mm2aX;uJI9nKFCGR1[tbY5lfWOnZDDCdoRWKGmwY3;ydI9z[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEC3JO69VQ>? M3TsPVEzPjR4MEG5
3T3 M{[zOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYj4dWlyUW6qaXLpeIlwdiCxZjDQcIF1\WyndD3k[ZJqfmWmIHfyc5d1cCCoYXP0c5IhcW6mdXPl[EA{XDNiY3XscEBxem:uaX\ldoF1cW:wIIfpeIghUUN3MDDv[kAxNjBzIN88US=> M{HV[FEzPjR4MEG5
3T3 MVrGeY5kfGmxbjDBd5NigQ>? MXfJcohq[mm2aX;uJI9nKF[jc3P1cIFzKGWwZH;0bIVtcWGuIHfyc5d1cCCoYXP0c5IhemWlZYD0c5Ihf2m2aDDJR|UxKG:oIECuNFUh|ryP MoLkNVI3PDZyMUm=
3T3 MXXLbY5ie2ViQYPzZZk> NITwV28zOCCvaX6= MY\EUXNQ NWXFcHZjS2WubIXsZZIhcW6qaXLpeIlwdiCxZjDWSWdHKGmwZIXj[YQhcHWvYX6gT2RTKHCqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMD6wNlIh|ryP NVvpdIVoOTZzNkKwNFg>
NIH3T3 M{T1c2tqdmG|ZTDBd5NigQ>? M1:1cFIxKG2rbh?= NWe0fm41TE2VTx?= MnvDbY5pcWKrdDDoeY1idiCNRGKgb4lv[XOnIHX4dJJme3OnZDD3bZRpKEmFNUCgc4YhOC5yMUig{txO M{X6blE3OTZ{MEC4
A549 NF;YNZNHfW6ldHnvckBCe3OjeR?= M1y1VWROW09? NYPMfIpmUW6qaXLpeIlwdiCxZjDjMW1mfCCmZYDlcoRmdnRiSFfGMYlv\HWlZXSgbJVu[W5iQUW0PUBk\WyuIH3p[5JifGmxbjD3bZRpKEmFNUCgc4YhOiEQvF2= NH2xVZgyQDR|NEG0OS=>
DU145 MWLGeY5kfGmxbjDBd5NigQ>? NYP6cFVCTE2VTx?= NGC3[Y9KdmirYnn0bY9vKG:oIHOtUYV1KGSncHXu[IVvfCCKR1[tbY5lfWOnZDDoeY1idiCGVUG0OUBk\WyuIIPjZZR1\XKrbnege4l1cCCLQ{WwJI9nKDFyIN88US=> M1m0SFE5PDN2MUS1
KB3-1 NH[zT|FEgXSxdH;4bYMhSXO|YYm= M{HCTlczKGh? NGHJT3VFVVOR M13YV2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHAu\3BvbnXnZZRqfmViS1KtN{0yKGOnbHzzJJdqfGhiSVO1NEBw\iB{LkOg{txO M3jlRVE6Ozl5M{Ky
KBV1 M3rTb2N6fG:2b4jpZ{BCe3OjeR?= MmGxO|IhcA>? MUDEUXNQ M3TXTmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHAu\2y7Y3;wdo91\WmwLXX4dJJme3OrbnegT2JXOSClZXzsd{B4cXSqIFnDOVAhd2ZiND6xJO69VQ>? MVWxPVM6PzN{Mh?=
A375 MWfDfZRwfG:6aXOgRZN{[Xl? M2r1VVczKGh? MVLEUXNQ NXjDPIp{UUN3ME21MlQh|ryP NEK2RpgyQTZ3NESwPC=>
RS4-11 NXy2dJU{TnWwY4Tpc44hSXO|YYm= MoPVNkBp MknlTY5pcWKrdHnvckBw\iCITGSzJIF2fG:yaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIECuNFA6QSEQvF2= MXSxPVY2PDRyOB?=
RS4-11 MkLMSpVv[3Srb36gRZN{[Xl? MXeyJIg> MlK1TY5pcWKrdHnvckBw\iCITGSzJGlVTCCvdYThcpQh[XW2b4Doc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gNE4xOzRizszN Mnj5NVk3PTR2MEi=
Sf9 MX3LbY5ie2ViQYPzZZk> MoPLN|AhdWmw M3HYU2lvcGmkaYTpc44hd2ZiR2PUMZRi\2enZDDWSWdHWiCneIDy[ZN{\WRid3n0bEBKSzVyIH;mJFAvOTh3IN88US=> NXzHUGsyOTl6NUSwOVE>
Ba/F3 MkHIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUm3NkBp M{SzZWlEPTB;MT6yJO69VQ>? NGfuWW8zODFzN{CwOC=>
BaPTC2 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\pZ5U4OiCq MVHJR|UxRTBwMkKg{txO MlrlNlAyOTdyMES=
Sf9 NHSxSldHfW6ldHnvckBCe3OjeR?= MUSxJIg> NEXkR3pFVVOR MnK1TY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCKaYOteIFo\2WmIGLFWEBmgHC{ZYPz[YQhf2m2aDDJR|UxKG:oIEGuN{DPxE1? MVeyNFEyPzByNB?=
H4 NIn4e2VEgXSxdH;4bYMhSXO|YYm= MX:xNEDPxE1? NX;lZnRxXG:6aXPpeJkhcW5iaIXtZY4hUDRiY3XscJM> NHLad3AzODN3MEiwOi=>
SF-539 NFzDdo5McW6jc3WgRZN{[Xl? M{XEd|M{OyEQvF2= M17qNlYxKG2rbh?= M{OwbGROW09? MWjJcohq[mm2aX;uJI9nKFCGR1\SZoV1[SCyaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIEGyMlIh|ryP MmjBNlA1ODN5MEC=
U251 M1fQTWtqdmG|ZTDBd5NigQ>? NGjvcWQ{OzNizszN M{P5N|YxKG2rbh?= MUjEUXNQ NVS1UGJMUW6qaXLpeIlwdiCxZjDWSWdHWjJicHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCxPE46KM7:TR?= NY\5fmlZOjB2MEO3NFA>
A431 NUjTblJ2U2mwYYPlJGF{e2G7 M4G4WmlvcGmkaYTpc44hd2ZiUFTHSnJj\XSjIHX4dJJme3OnZDD3bZRpKEmFNUCgc4YhOTJwMjFOwG0> NUmwZnZuOjB3NUiwO|I>
A431 MX3LbY5ie2ViQYPzZZk> NHnqVZlKdmirYnn0bY9vKG:oIG\FS2ZTOiCneIDy[ZN{\WRid3n0bEBKSzVyIH;mJFE5NjlizszN M{T2bVIxPTV6MEey
HepG2 Mn7pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfqOlh3PzJiaB?= MoC3TWM2OD1|LkixJO69VQ>? M1fXV|IxPTdyNUK2
Kasumi-1 M1zFRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rxVlczKGh? NGf3fVBKSzVyPUCuNFE3KM7:TR?= NGnDXI0zODV5MEWyOi=>
RS4-11 NG[1Z5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVv0WFMyPzJiaB?= NUO1fFdVUUN3ME2xJO69VQ>? MYGyNFU4ODV{Nh?=
THP1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUi3NkBp MYnJR|UxRTBwNTFOwG0> MnrrNlA2PzB3Mk[=
Kasumi-1 NFTZTG5HfW6ldHnvckBCe3OjeR?= M3nwSmlvcGmkaYTpc44hd2ZiYz3LbZQh[XW2b4Doc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gNE4xOTVizszN MYKyNFg{OzB|OR?=
A549 NV7IVFY6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLMNVYhcA>? M33lcmFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG1OFkh[2WubIO= MYKyNVQ2ODR4Mx?=
HL60 MoTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTxRmluOTZiaB?= MmjpRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFy2NEBk\Wyucx?= M4rZVFIyPDVyNE[z
HUVEC M2jBW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXexOkBp MljNTY5pcWKrdHnvckBw\iCYRVfGMYlv\HWlZXSgZ4VtdCCycn;sbYZmemG2aX;uJJdqfGhiSVO1NEBw\iB{Lke1JO69VQ>? MlHNNlE1PTB2NkO=
HUVEC NIHxTFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfF[oFTOTZiaB?= NV3NUGl{UW6qaXLpeIlwdiCxZjDiSmdHNWmwZIXj[YQh[2WubDDwdo9tcW[ncnH0bY9vKHerdHigTWM2OCCxZjC0MlA1KM7:TR?= M1vTcFIyPDVyNE[z
IM9 NIf6WotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3ruPVE3KGh? NV\kPHlOSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gTW06KGOnbHzz MknCNlE1PTB2NkO=
K562 MljDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHENVYhcA>? MmDMRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS{W2NkBk\Wyucx?= NYTWXVRHOjF2NUC0OlM>
MDA-MB-231 NWHWU|NKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3qx[VE3KGh? M3vvfGFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHN? M1vhflIyPDVyNE[z
H460 M37lU2N6fG:2b4jpZ{BCe3OjeR?= NGHTfm84OiCq M37ydWlEPTB;Mj63JO69VQ>? M{TjUlIyPjJzOEiw
SMMC7721 MW\DfZRwfG:6aXOgRZN{[Xl? MlPVO|IhcA>? M3jiXmlEPTB;Nj60O{DPxE1? Mk\MNlE3OjF6OEC=
WI38 NUjYVYJnS3m2b4TvfIlkKEG|c3H5 MYO3NkBp NETyb4pKSzVyPUiuOVYh|ryP NHP4b3EzOTZ{MUi4NC=>
HEK293 NV\NOZl[U2mwYYPlJGF{e2G7 MlPGNVAxKG6P NXfXbYhVOSCq MYfkc4V{KG6xdDDpcohq[mm2IG\FS2YucW6mdXPl[EBifXSxcHjvd5Bpd3K7bHH0bY9vKG:oIIT5do9{cW6nIEGxO|UhemW|aXT1[UBwdiCYRVfGVlIh\XiycnXzd4VlKGmwIFjFT|I6OyClZXzsdy=> MlHZNlE5QDV{OEe=
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HUVEC MV\GeY5kfGmxbjDBd5NigQ>? Ml64NUDPxE1? NV7l[VhmOSCq NGDXRYFKdmirYnn0bY9vKG:oIFXST{BxcG:|cHjvdplt[XSrb36gZZQhXGi{MkCyM3R6ejJyNDDpckBXTUeILYP0bY12dGG2ZXSgTHVXTUN? M2fLSVIyQTZ|M{C1
HUVEC M2DMS2Z2dmO2aX;uJGF{e2G7 NFHRbIoyKM7:TR?= MoGxNUBp M1:4d2lvcGmkaYTpc44hd2ZiZV7PV{BxcG:|cHjvdplt[XSrb36gZZQhW2W{LUGxO|IhcW5iVlXHSk1{fGmvdXzheIVlKEiXVlXD NGLPOWUzOTl4M{OwOS=>
HUVEC M1jJR2tqdmG|ZTDBd5NigQ>? MlvENUDPxE1? MUmxJIg> MVjJcohq[mm2aX;uJI9nKF[HR1\SNkBxcG:|cHjvdplt[XSrb36gZZQhfHm{LUGxO|UhcW5iVlXHSk1{fGmvdXzheIVlKEiXVlXD NWDIN|M5OjF7NkOzNFU>
HUVEC M37uZ2Z2dmO2aX;uJGF{e2G7 MYOxJO69VQ>? NITKTmYyKGh? MYLkc4V{KG6xdDDpcohq[mm2IFHLWEBxcG:|cHjvdplt[XSrb36gZZQhW2W{LUS3N{BqdiCYRVfGMZN1cW23bHH0[YQhUFWYRVO= MkfwNlE6PjN|MEW=
HL60 NFjzZlJEgXSxdH;4bYMhSXO|YYm= NYr2XIhSPTBizszN NYrpZYxiPDhiaB?= MnvNSG1UVw>? M2LmZ2lEPTB;MUWuOUDPxE1? M4nUeVIzODF7MUi4
K562 NIXV[4NEgXSxdH;4bYMhSXO|YYm= NHnmSHo2OCEQvF2= NWLocVR{PDhiaB?= NULxfFZZTE2VTx?= MofFTWM2OD1{MT65JO69VQ>? NUH3XHV{OjJyMUmxPFg>
PC3 M4K0cmN6fG:2b4jpZ{BCe3OjeR?= NVnTU4Y1PTBizszN M3LlPVQ5KGh? NIHjb|lFVVOR M325ZmlEPTB;MkWuNUDPxE1? M3f1VFIzODF7MUi4
SF-539 MYXLbY5ie2ViQYPzZZk> MWizN|Mh|ryP MVO2NEBucW5? MkTtTY5pcWKrdHnvckBw\iCSRFfGVoJmfGFidInyc5NqdmVia3nuZZNmKGGldHn2bZR6KGmwIGDES2YuSkJvc4TpcZVt[XSnZDDoeY1idiCVRj21N|kh[2WubIOge4l1cCCLQ{WwJI9nKDF{LkKg{txO Mn;wNlIzODR5NEG=
HAEC NGL2W4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIW3TIEyODBizszN MonYO|IhcA>? M1nvbGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFHFR{Bk\WyuczDlfJBz\XO|aX7nJHZGT0[UIIfpeIghUUN3MDDv[kAxNjFizszN NGXYVlEzOjR2NE[3PS=>
HT-29 NFTFVIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fsd|ExOCEQvF2= NFLPXIU4OiCq MnTQRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKVD2yPUBk\WyuczDlfJBz\XO|aX7nJHZGT0[UIIfpeIghUUN3MDDv[kAxNjN|IN88US=> MXeyNlQ1PDZ5OR?=
MV4-11 Mn75R5l1d3SxeHnjJGF{e2G7 MVm3NkBp Mn3TTWM2OD1yLkCwN{DPxE1? NIXET3YzOjR3MkWxPC=>
HepG2 NYLXR3EzS3m2b4TvfIlkKEG|c3H5 Mo\MOFghcA>? Mm\ITWM2OD1zMz6yOEDPxE1? MXGyNlQ5OzZyOB?=
PC9 MofuR5l1d3SxeHnjJGF{e2G7 NFvZU2Y1QCCq Mn;0TWM2OD1zMD65O{DPxE1? M4DKblIzPDh|NkC4
CAKI-1 MnLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUOxNFAh|ryP Mn3KOFghcA>? MkXjSG1UVw>? M3;ITmdKPTB;MD62N{DPxE1? NUXLXmVuOjJ3NkC2Nlc>
EKVX NXHGZnVLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\NNVAxKM7:TR?= Mn\zOFghcA>? M1PiRWROW09? MX7HTVUxRTdwOTFOwG0> NYjWSm9nOjJ3NkC2Nlc>
MCF7 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\3XYNqOTByIN88US=> M4\OeFQ5KGh? NGnodW9FVVOR NXvKeod[T0l3MU2yJO69VQ>? MnzWNlI2PjB4Mke=
MDA-MB-435 NGKy[ppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3L4OlExOCEQvF2= MmryOFghcA>? MnrxSG1UVw>? M2[wU2dKPTJ;MjFOwG0> M2\aelIzPTZyNkK3
OVCAR3 NHfiTXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYOwbFBzOTByIN88US=> M13NcVQ5KGh? M2T1SmROW09? NIjaN|BIUTV|PUOuNkDPxE1? NFy4OlMzOjV4ME[yOy=>
SNB19 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInaUnMyODBizszN MoLtOFghcA>? MX7EUXNQ M{TDS2dKPTR;MUCg{txO NXHoeGhEOjJ3NkC2Nlc>
SW620 NUXvR3BYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXizbXBMOTByIN88US=> MUe0PEBp MmjySG1UVw>? M4XpdmdKPTV;MT6zJO69VQ>? NGDBN4ozOjV4ME[yOy=>
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UACC257 NWD1Xo1UT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnX2NVAxKM7:TR?= NVnNfog3PDhiaB?= MkPsSG1UVw>? MX3HTVU4RTRizszN MnP3NlI2PjB4Mke=
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HT-29 NIjpcVlEgXSxdH;4bYMhSXO|YYm= MkPrNVAxKM7:TR?= NGryTHM4OiCq M1TFWWROW09? NYnOd5VES3m2b4TvfIlkcXS7IHHnZYlve3RiVlXHSnIh\XiycnXzd4lv\yCqdX3hckBJXC1{OTDj[YxteyC5aYToJGlEPTBib3[gNE4{OyEQvF2= M3zGRVI{OTNzNUSx
HCT116 M{XrbGZ2dmO2aX;uJGF{e2G7 NWnsXZhyOjRiaB?= NYDuXXpQTE2VTx?= MlHpRY51cW2rZ4LheI9zgSCjY4Tpeol1gSCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHygcYloemG2aX;u NHnzR|UzOzF3M{KwNC=>
HUVEC Mlu3SpVv[3Srb36gRZN{[Xl? NWS2XnV4OiEQvF2= NUPNTWhSOThiaB?= NH60PIZFVVOR MWrBcpRq[W6paX;n[Y5q[yCjY4Tpeol1gSCrbjDIWXZGS3NidX7k[ZIhcHmyb4jpZ{Bkd26maYTpc44h[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kB1fWKnIH\vdo1ifGmxbh?= Mn7WNlMyPTN{MEC=
ACHN M1\obmN6fG:2b4jpZ{BCe3OjeR?= NXXlN|J7PiCm M3T1cGlEPTB;Mj61JO69VQ>? MV6yN|M3ODFyNB?=
A498 M4e0TGN6fG:2b4jpZ{BCe3OjeR?= Mn3SNVAxKM7:TR?= M3K0bVczKGh? MVvEUXNQ MWTJR|UxRTRwMzFOwG0> NV7mc2lIOjN2OEm2NlY>
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MDA-MB-231 MmHrR5l1d3SxeHnjJGF{e2G7 MUm3NkBp M4q0ZWROW09? MmS1TWM2OD1yLkCyNlMh|ryP NHqy[IQzPDh7ME[1Ni=>
MDA-MB-435 NH3EZXBEgXSxdH;4bYMhSXO|YYm= MljZO|IhcA>? NV3CfHdrTE2VTx?= MVTJR|UxRTBwMEC5O{DPxE1? M4TUcVI1QDlyNkWy
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SH-SY5Y M2n1N2tqdmG|ZTDBd5NigQ>? NVuzT5lQOTBizszN M2jXRVEhcA>? M1vhN2ROW09? MYLJcohq[mm2aX;uJI9nKFCGR1\SZoV1[SC5aYToJGlEPTBib3[gNE4xQDNzIN88US=> NYWxPI1OOjR6OUC2OVI>
U251 NH[z[llMcW6jc3WgRZN{[Xl? MWixNEDPxE1? NHLsWXYyKGh? NV\y[HhJTE2VTx?= MWTJcohq[mm2aX;uJI9nKF[HR1\SNkB4cXSqIFnDOVAhd2ZiMD6wNVg6KM7:TR?= Ml;sNlQ5QTB4NUK=
Bel7402 NUDhdmVGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XoWVczKGh? NF;McnlFVVOR MXzJR|UxRTJwNkeg{txO MWmyOFkxPDl4MR?=
HK2 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfvWZpmPzJiaB?= NWHv[3dYTE2VTx?= M{LXeWlEPTB;NT64OUDPxE1? NEnIOI4zPDlyNEm2NS=>
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MV4-11 M1mz[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUf3dWd7PDhiaB?= NXjpXng6TE2VTx?= M2fIemlEPTB;MD6wNFMh|ryP MlTlNlQ6ODR7NkG=
NCI-H3122 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHxO|IhcA>? MlTBSG1UVw>? MVnJR|UxRTBwOEOg{txO NHzmZ3EzPDlyNEm2NS=>
NCI-H460 M2jhd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TvZlczKGh? NWXie41kTE2VTx?= NU\I[GZkUUN3ME20MlMyKM7:TR?= M13MWFI1QTB2OU[x
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TT M4HFcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3Hz[VczKGh? M4P4VGROW09? MXfJR|UxRTBwMESg{txO MkHRNlQ6ODR7NkG=
EoL-1-cell M2Dr[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUL6TWVMUUN3ME2xMlY1KHCP M2ftcHNCVkeHUh?=
MV-4-11 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;aTWM2OD1{N{KgdG0> MnT3V2FPT0WU
NOS-1 M2OxXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvuPZhKSzVyPUG1MlMhdk1? M1LpfnNCVkeHUh?=
CGTH-W-1 NVjJNFdDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTNyLkm0JI5O NEf5[49USU6JRWK=
MONO-MAC-6 M3z5bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LnbWlEPTB;M{OuPEBvVQ>? NXLaXoltW0GQR1XS
ALL-PO M{KxbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTd7Lki5JI5O MX;TRW5ITVJ?
NKM-1 M2\ySWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfYOWNKSzVyPUm4MlUzKG6P MojyV2FPT0WU
KM12 NV;SOZdFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nLSGlEPTB;M{WwMlE1KG6P NUnjR3FRW0GQR1XS
TE-15 M33hcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEToPYxKSzVyPUWwO{43OSCwTR?= NV\MNoVtW0GQR1XS
697 M{XEcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLhTWM2OD14MUSuNlUhdk1? M2\mPXNCVkeHUh?=
MOLT-16 NXz5eVQ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnhTWM2OD14M{GuN|Ihdk1? NV3yTZlvW0GQR1XS
GB-1 NH;hR25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIix[4NKSzVyPUexNE4zOyCwTR?= NHjPdW9USU6JRWK=
TE-12 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRThyND61OUBvVQ>? NHLkfJpUSU6JRWK=
ES6 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTl6MT6wOkBvVQ>? MWfTRW5ITVJ?
LC-2-ad NXXkbmo4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHCTWM2OD1zLkGxOFA4KM7:TR?= NFjMTHlUSU6JRWK=
BL-70 NX3JfZJPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;KdmxKSzVyPUGuNVE5PDZizszN NHvTb|lUSU6JRWK=
ETK-1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7jS5M2UUN3ME2xMlI5PThizszN MUfTRW5ITVJ?
A4-Fuk MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{P1bGlEPTB;MT6zOFE1OSEQvF2= NHzYSohUSU6JRWK=
OCI-AML2 MmfES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mke2TWM2OD1zLkO2PFUyKM7:TR?= Moi3V2FPT0WU
SIG-M5 NWnYT3pLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7WTWM2OD1zLkO3NFA6KM7:TR?= MVzTRW5ITVJ?
NCI-SNU-16 NVrUe|RbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF20WpdKSzVyPUGuOFY1QDZizszN M1;xNnNCVkeHUh?=
PSN1 M4XWRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGT2RYhKSzVyPUGuOVA3PzZizszN NInWdmpUSU6JRWK=
SR NHPDeJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlX6TWM2OD1zLkW0OVczKM7:TR?= NYi1V4hJW0GQR1XS
A3-KAW MnX6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rTRmlEPTB;MT62NlU1PiEQvF2= NH;uVW1USU6JRWK=
KS-1 MmfxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\IbVVrUUN3ME2xMlY6OjR5IN88US=> MnzPV2FPT0WU
CTV-1 NEfjTGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPlO3BGUUN3ME2xMlczPzVzIN88US=> M125cnNCVkeHUh?=
LB1047-RCC NEfDZZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTFwOEG2NlQh|ryP MoP2V2FPT0WU
EMG-01 NVnQboxCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fNU2lEPTB;MT64N|U3OyEQvF2= NWT4dXRGW0GQR1XS
TE-11 NH\uXmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3K3dGlEPTB;MT64N|k5PSEQvF2= M3TTenNCVkeHUh?=
CMK NXHrbJNbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzydWVqUUN3ME2xMlk2PTF5IN88US=> NEXjcHpUSU6JRWK=
NB1 MmLlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TQTWlEPTB;MT65OlEyPyEQvF2= M1mx[XNCVkeHUh?=
HAL-01 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkW1TWM2OD1{LkC1PVQ3KM7:TR?= NIm5UGZUSU6JRWK=
DEL NIjvOWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTJwMEi0PFIh|ryP NHjaS|FUSU6JRWK=
RL95-2 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjCb4NKSzVyPUKuNVEyOzdizszN NYXmfGhOW0GQR1XS
KARPAS-299 M4nROGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmSzTWM2OD1{LkGxN|E{KM7:TR?= MUXTRW5ITVJ?
EW-16 NUPRNWltT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LVOGlEPTB;Mj6xN|UxQCEQvF2= NGTSR4JUSU6JRWK=
RS4-11 M{T2OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTJwMUe5NlQh|ryP M3jzNnNCVkeHUh?=
BB30-HNC M3TWdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37INGlEPTB;Mj6yNlM4PSEQvF2= Mo\yV2FPT0WU
DOHH-2 NGDLXJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTJwM{O0N|Eh|ryP M2fGNHNCVkeHUh?=
RPMI-8402 MnHyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjRfpRGUUN3ME2yMlM{PjF6IN88US=> MX7TRW5ITVJ?
BV-173 MkL5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTJwM{O2OkDPxE1? MlzjV2FPT0WU
TE-10 MlryS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LWWWlEPTB;Mj6zOFM5PCEQvF2= NF21N5RUSU6JRWK=
TE-8 NXjxSGg1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYT2VlZ{UUN3ME2yMlM4ODN6IN88US=> MXTTRW5ITVJ?
K052 NIHsSVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4SzfWlEPTB;Mj60NFIxOiEQvF2= MWnTRW5ITVJ?
KARPAS-45 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HhT2lEPTB;Mj60PVQ1PiEQvF2= MnPxV2FPT0WU
SK-NEP-1 NFjTcmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3uRXlKSzVyPUKuOlAzOzdizszN NUCwOIxlW0GQR1XS
KGN NEWySnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfMOWdKSzVyPUKuOlA{OzlizszN MkiyV2FPT0WU
ML-2 M4KxZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HKd2lEPTB;Mj62N|UyOiEQvF2= NIPZcnpUSU6JRWK=
LAMA-84 NEHRRnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXryVnJQUUN3ME2yMlY6PTR3IN88US=> MoD0V2FPT0WU
LXF-289 M3Li[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HPXWlEPTB;Mj63Nlk5QSEQvF2= M4\qb3NCVkeHUh?=
A101D MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYSzd2dwUUN3ME2yMlc5OzB2IN88US=> NUTKfJZ7W0GQR1XS
KY821 NYDmRo9XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEm2d3NKSzVyPUKuO|k4PThizszN M3vEfXNCVkeHUh?=
ES4 NULJc5QyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWWye2dlUUN3ME2yMlgxPjJ6IN88US=> M3jHZXNCVkeHUh?=
SCC-3 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjORXVbUUN3ME2yMlgzQDlzIN88US=> NYTqfJBPW0GQR1XS
NALM-6 NFnWfZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LnNmlEPTB;Mj65NFQ4OyEQvF2= NWnnXmRsW0GQR1XS
BL-41 M1yyPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnMOmlKSzVyPUKuPVEzOjJizszN M3roPXNCVkeHUh?=
OPM-2 NHLXSGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGj5ZlNKSzVyPUOuNFU6PTRizszN M3nQb3NCVkeHUh?=
SF126 NGDhcopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XORmlEPTB;Mz6wOlE6QCEQvF2= Mln3V2FPT0WU
BE-13 M{\nUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDHTGFKSzVyPUOuNlMyOTFizszN MlvOV2FPT0WU
SF268 NX\ob|BQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\XWGZKSzVyPUOuN|I5PjlizszN NEnnPJpUSU6JRWK=
MOLT-4 MnfTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTNwM{m4N|gh|ryP MXrTRW5ITVJ?
PF-382 MnrWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTMWHM4UUN3ME2zMlQ1PTdizszN NYO4WVd4W0GQR1XS
HEL NEDHU5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTNwNEiwNFUh|ryP MnL1V2FPT0WU
RPMI-6666 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fnN2lEPTB;Mz61OFE4OSEQvF2= NGXobJBUSU6JRWK=
QIMR-WIL M17LTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIToZ|JKSzVyPUOuOlM{QTFizszN MnPQV2FPT0WU
ATN-1 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvRT3JZUUN3ME2zMlY4OTF2IN88US=> Mn;2V2FPT0WU
BB49-HNC MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\OTWM2OD1|LkewOVA5KM7:TR?= NFnmWm9USU6JRWK=
HCE-4 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTNwN{i2OFIh|ryP MYHTRW5ITVJ?
SK-LMS-1 M3jicWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTNwOEOzN|gh|ryP NF;DN29USU6JRWK=
MS-1 NEfJcpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TkcGlEPTB;Mz64N|c4QCEQvF2= NVy3fWRSW0GQR1XS
JAR NInnTHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTNwOUi4N|Ih|ryP MojmV2FPT0WU
KE-37 NHz0UFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXiTWM2OD12LkC2NVU5KM7:TR?= NX3YUoxwW0GQR1XS
LB996-RCC M1O0cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVKxO4VOUUN3ME20MlEzOTZ6IN88US=> M{TUenNCVkeHUh?=
HH NFP5RVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjkTWM2OD12LkKwPVE1KM7:TR?= M3HrSnNCVkeHUh?=
HL-60 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTpTmw4UUN3ME20MlIyODZ3IN88US=> MWfTRW5ITVJ?
HOP-62 NV;SNZBkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnre4ExUUN3ME20MlM{PTJizszN NWG1U2VFW0GQR1XS
NOMO-1 NEOyWHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HPNWlEPTB;ND6zN|Y6QSEQvF2= MnzLV2FPT0WU
DU-4475 NWnFfVJmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUj4fo55UUN3ME20MlM3PzJ7IN88US=> M3PWe3NCVkeHUh?=
LC4-1 MlP2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXr2Rm5FUUN3ME20MlM5ODdizszN M3O0dnNCVkeHUh?=
MC116 MmHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTRwNEOwPFEh|ryP MojMV2FPT0WU
SW982 NFzMeohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDCW29KSzVyPUSuOVU{ODdizszN NVG2TXN5W0GQR1XS
SK-N-DZ MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGr2UVlKSzVyPUSuOlcxQTlizszN NGHW[FFUSU6JRWK=
EW-1 NYXFNWdzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPDZoRKSzVyPUSuOlc6OTFizszN MkDuV2FPT0WU
SU-DHL-1 NU\pNIhET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjVTWM2OD12LkiwNVc1KM7:TR?= M1LPVHNCVkeHUh?=
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LB831-BLC Mnj6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjEV4ZKSzVyPUOyMlM5PDNizszN MVzTRW5ITVJ?
SCH M4HaSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfWTWM2OD1|Mj64OFg2KM7:TR?= MWTTRW5ITVJ?
EHEB MkHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2X2N2lEPTB;M{SuNVE6OyEQvF2= M1Xlc3NCVkeHUh?=
U-266 MnrCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTN2LkK3PFEh|ryP MnzTV2FPT0WU
EW-11 Ml\ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYG2endbUUN3ME2zOE41PzJ3IN88US=> NFT0d2JUSU6JRWK=
TE-9 NFO0TXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHvU|VKSzVyPUO3MlA1ODFizszN M{TBd3NCVkeHUh?=
ES3 NXzLRVlpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmX2TWM2OD1|Nz61NFA1KM7:TR?= MXXTRW5ITVJ?
NCI-H2141 MkDMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXU[HRKSzVyPUO4MlA5PDNizszN NV7Dcnc6W0GQR1XS
MPP-89 NF73dFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTR{LkC1PFYh|ryP MkLwV2FPT0WU
SK-MEL-2 M3zRVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fzW2lEPTB;NEKuOlQxPSEQvF2= MV3TRW5ITVJ?
LC-1F NFXNOItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTR|LkO2PFIh|ryP NEK5VlRUSU6JRWK=
NH-12 M1LmNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDCTWM2OD12Mz65N|U6KM7:TR?= Mni5V2FPT0WU
RKO NGrMR3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXDTWM2OD12ND6xNlUzKM7:TR?= MV;TRW5ITVJ?
KM-H2 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7sVotKSzVyPUS0Mlk2PzdizszN MkThV2FPT0WU
SK-UT-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPzeFRKSzVyPUS5Mlg5OjVizszN MnHyV2FPT0WU

... 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
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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
NCT04669366 Not yet recruiting Drug: sunitinib|Drug: axitinib Kidney Neoplasms Pfizer December 15 2020 --
NCT04633122 Recruiting Drug: Ripretinib|Drug: Sunitinib Gastrointestinal Stromal Tumor(GIST) Zai Lab (Shanghai) Co. Ltd. November 25 2020 Phase 2
NCT04115189 Active not recruiting Drug: Sunitinib Metastatic Renal Cell Carcinoma ( mRCC) Pfizer December 13 2019 --
NCT03916458 Completed -- Carcinoma Renal Cell Pfizer December 17 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

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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID