Sunitinib Malate

For research use only.

Licensed by Pfizer Catalog No.S1042 Synonyms: SU 11248 Malate

99 publications

Sunitinib Malate Chemical Structure

CAS No. 341031-54-7

Sunitinib Malate (SU 11248) 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 99 publications

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Choose Selective PDGFR Inhibitors

Biological Activity

Description Sunitinib Malate (SU 11248) 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
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3T3 Mk\nT4lv[XOnIFHzd4F6 NUX0OlFkOjBibXnu NHzTRYtFVVOR MV7D[YxtfWyjcjDpcohq[mm2aX;uJI9nKF[HR1[gbY5lfWOnZDDoeY1idiCNRGKgdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAxNjB{MjFOwG0> NXfhO5loRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[xOlIxODhpPkG2NVYzODB6PD;hQi=>
NIH3T3 NED1cXVMcW6jc3WgRZN{[Xl? MlvpNlAhdWmw NWXZeFgzTE2VTx?= M{\a[olvcGmkaYSgbJVu[W5iS1TSJItqdmG|ZTDlfJBz\XO|ZXSge4l1cCCLQ{WwJI9nKDBwMEG4JO69VQ>? NHv2Zow9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNkG2NlAxQCd-MU[xOlIxODh:L3G+
A549 MWjGeY5kfGmxbjDBd5NigQ>? MkXKSG1UVw>? M1XZOmlvcGmkaYTpc44hd2ZiYz3N[ZQh\GWyZX7k[Y51KEiJRj3pcoR2[2WmIHj1cYFvKEF3NEmgZ4VtdCCvaXfyZZRqd25id3n0bEBKSzVyIH;mJFIh|ryP MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDR|NEG0OUc,OTh2M{SxOFU9N2F-
DU145 NHrJb3hHfW6ldHnvckBCe3OjeR?= MnHJSG1UVw>? MW\Jcohq[mm2aX;uJI9nKGNvTXX0JIRmeGWwZHXueEBJT0ZvaX7keYNm\CCqdX3hckBFXTF2NTDj[YxtKHOlYYT0[ZJqdmdid3n0bEBKSzVyIH;mJFExKM7:TR?= M33vNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6NEO0NVQ2Lz5zOESzOFE1PTxxYU6=
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A431 NUi2[m1OU2mwYYPlJGF{e2G7 MkntTY5pcWKrdHnvckBw\iCSRFfGVoJmfGFiZYjwdoV{e2WmIIfpeIghUUN3MDDv[kAyOi5{IN88US=> MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODV3OEC3Nkc,OjB3NUiwO|I9N2F-
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Kasumi-1 MnzQSpVv[3Srb36gRZN{[Xl? NWDlWG82UW6qaXLpeIlwdiCxZjDjMWtqfCCjdYTvdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAxNjBzNTFOwG0> NWHrdHVTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4N|MxOzlpPkKwPFM{ODN7PD;hQi=>
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U251 NFHnUplMcW6jc3WgRZN{[Xl? NXjMW2s5OTBizszN MUCxJIg> MoHtSG1UVw>? MVrJcohq[mm2aX;uJI9nKF[HR1\SNkB4cXSqIFnDOVAhd2ZiMD6wNVg6KM7:TR?= MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh7ME[1Nkc,OjR6OUC2OVI9N2F-
Bel7402 MkizS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPxO|IhcA>? NIDR[YJFVVOR MULJR|UxRTJwNkeg{txO M334VFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUC0PVYyLz5{NEmwOFk3OTxxYU6=
HK2 NFPwN2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVS3NkBp MVrEUXNQ MoXoTWM2OD13Lki1JO69VQ>? M4e1eFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUC0PVYyLz5{NEmwOFk3OTxxYU6=
LO2 M1fq[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;NUWM4OiCq M3S5dGROW09? M2HYTGlEPTB;MUmuPVMh|ryP MlzLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MES5OlEoRjJ2OUC0PVYyRC:jPh?=
MV4-11 NVPw[opMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmG0OFghcA>? NFnoVmxFVVOR MmTGTWM2OD1yLkCwN{DPxE1? MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyNEm2NUc,OjR7MES5OlE9N2F-
NCI-H3122 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoT0O|IhcA>? NUPGW5FsTE2VTx?= MoD6TWM2OD1yLkizJO69VQ>? MnvTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MES5OlEoRjJ2OUC0PVYyRC:jPh?=
NCI-H460 MnLjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\uZWRPPzJiaB?= M33tV2ROW09? MnvjTWM2OD12LkOxJO69VQ>? NEO2R409[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwOFk3OSd-MkS5NFQ6PjF:L3G+
NCI-H526 NUXNOndrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXW3NkBp Mnj1SG1UVw>? Mon1TWM2OD1zLkCxJO69VQ>? NFf6V2Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwOFk3OSd-MkS5NFQ6PjF:L3G+
TT MmPjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUGz[IxUPzJiaB?= MWPEUXNQ MoToTWM2OD1yLkC0JO69VQ>? M2XmSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUC0PVYyLz5{NEmwOFk3OTxxYU6=
3T3 NGPj[4xCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M4q1SVczKGi{cx?= NGj0PGhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIEPUN{Bk\WyuczDlfJBz\XO|aX7nJIh2dWGwIFPTSlFTKGGodHXyJFczKGi{czDifUBE\WyudHn0[ZIh[XO|YYmsJGFkfGm4aYT5JF0hOC5yOTFOwG0v NGDlb2c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOE[5OFY1OSd-MUi2PVQ3PDF:L3G+
MV4-11 NHHlSGtCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M3rmbFczKGi{cx?= Mni1RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPVkStNVEh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IHPlcIwhfGm2ZYKtZox2\SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OCB;IECuNFA1OyEQvF2u NFjqTWE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUe1OFE6QSd-MUm3OVQyQTl:L3G+
HEK293 M{e4OGZ2dmO2aX;uJIF{e2G7 NUjSc41qSmmwZHnu[{Bi\m[rbnn0fUB1dyCITGSzJINifGGueYTpZ{Bld22jaX6g[ZhxemW|c3XkJIlvKEiHS{K5N{Bk\WyuczDifUBkd22yZYTpeIl3\SCkaX7kbY5oKGG|c3H5MEBM\CB;IECuNFAxPDdizszNMi=> NX3KWXJlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm3OVQyQTlpPkG5O|U1OTl7PD;hQi=>
FDC-P1 M4Tkd2Z2dmO2aX;uJIF{e2G7 M3\NRVQ5KGi{cx?= MlG0TY5pcWKrdHnvckBw\iCqdX3hckBHVVNiZYjwdoV{e2WmIHnuJIdzd3e2aDDmZYN1d3JiZHXw[Y5l\W62IH3veZNmKE[GQz3QNUBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIF\NV{1u\WSrYYTl[EBk\WyuIIDyc4xq\mW{YYTpc44hcW5icILld4Vv[2ViaIXtZY4hS1OIMTDh[pRmeiB2ODDodpMh[nlicnXzZZp2emmwIHT5[UBz\WS3Y4Tpc44h[XO|YYmsJGlEPTBiPTCwMlE2PSEQvF2u NVX6flFLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCxOVY3QDlpPkKwNVU3Pjh7PD;hQi=>
primary leukemia cells MkDDR5l1d3SxeHnjbZR6KGG|c3H5 M4\pV|czKGi{cx?= M2rUXmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJJBzcW2jcomgcIV2c2WvaXGgZ4VtdHNiaYPvcIF1\WRiZoLvcUBi[3W2ZTDtfYVtd2mmIHzleYtmdWmjIIDheIlmdnRiZYjwdoV{e2mwZzDGUHQ{NUmWRDDteZRifGmxbjDhd5Nme3OnZDDhd{Bk\WyuII\pZYJqdGm2eTDh[pRmeiB5MjDodpMh[nlibIXjbYZmemG|ZTDhd5NigSxiSVO1NEA:KDBwMEOg{txONg>? NHPmZnI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkKyNVIxOSd-MkKyNlEzODF:L3G+
primary leukemia cells MWPDfZRwfG:6aXPpeJkh[XO|YYm= NGr1Nng4OiCqcoO= M{fQRWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJJBzcW2jcomgcIV2c2WvaXGgZ4VtdHNiaYPvcIF1\WRiZoLvcUBi[3W2ZTDtfYVtd2mmIHzleYtmdWmjIIDheIlmdnRiZYjwdoV{e2mwZzD3bYxlKHS7cHWgSmxVOyCjc4Pld5Nm\CCjczDj[YxtKH[rYXLpcIl1gSCjZoTldkA4OiCqcoOgZpkhdHWlaX\ldoF{\SCjc4PhfUwhUUN3MDC9JFAvODNizszNMi=> NFvOSXE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkKyNVIxOSd-MkKyNlEzODF:L3G+
primary leukemia cells NGrDVY9EgXSxdH;4bYNqfHliYYPzZZk> NHvENpg4OiCqcoO= MV;DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDwdolu[XK7IHzleYtmdWmjIHPlcIx{KGm|b3zheIVlKG[{b32gZYN2fGVibYnlcI9q\CCuZYXr[Y1q[SCyYYTp[Y51KGW6cILld5NqdmdiRlzUN{1FQDN3WTDteZRifGmxbjDhd5Nme3OnZDDhd{Bk\WyuII\pZYJqdGm2eTDh[pRmeiB5MjDodpMh[nlibIXjbYZmemG|ZTDhd5NigSxiSVO1NEA:KDFwMTFOwG0v NHW3UHY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkKyNVIxOSd-MkKyNlEzODF:L3G+
endothelial precursor cells NH2zO2VHfW6ldHnvckBie3OjeR?= M1HSSWlvcGmkaYTpc44hd2ZiZX7kc5Rp\WyrYXygZ49z\CCjcnXhJIZwem2jdHnvckBqdiCnbnTveIhmdGmjbDDwdoVkfXK|b4KgZ4VtdHNiYomgR2Q{OSClb4LkJIFz\WFiZHX0[YN1cW:wIHLhd4VlKHCqZX7veJlxcWNiZIL1[{BlcXOlb4\ldpkh[mG|ZXSgZZN{[XluIFnDOVAhRSByLkCwPVYh|ryPLh?= MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjRyOU[2Okc,OjJ2MEm2OlY9N2F-
endothelial precursor cells MnXaSpVv[3Srb36gZZN{[Xl? MoDaTY5pcWKrdHnvckBw\iClZXzsJI1q\3KjdHnvckBqdiCnbnTveIhmdGmjbDDwdoVkfXK|b4KgZ4VtdHNiYomgU5JqeyClZXzsJI1q\3KjdHnvckBscXRiYnHz[YQheGinbn;0fZBq[yCmcoXnJIRqe2OxdnXyfUBj[XOnZDDhd5NigSxiSVO1NEA:KDF|Lk[g{txONg>? MmLVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ2MEm2OlYoRjJ{NEC5OlY3RC:jPh?=
U251 NVPjblg{TnWwY4Tpc44h[XO|YYm= M3O3[FYxKG2rboO= NEnIZXNKdmirYnn0bY9vKG:oIG\FS2ZTOiCrbjDoeY1idiCXMkWxJINmdGy|IIDy[ZRz\WG2ZXSg[o9zKDZyIH3pcpMhdWWjc4Xy[YQh[W[2ZYKgNUBpeiCkeTDFUGlUSSxiSVO1NEA:KDF6Lkmg{txONg>? NGnoc3Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkezPVA6OCd-MkK3N|kxQTB:L3G+
U251 MWjGeY5kfGmxbjDhd5NigQ>? M2HH[FYxKG2rboO= NGrXU5BKdmirYnn0bY9vKG:oIG\FS2YucW6mdXPl[EBXTUeIUkKgdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIGWyOVEh[2WubIOgc5ZmemW6cILld5NqdmdiRnzrMVEheHKndILlZZRm\CCob4KgOlAhdWmwczDwdolweiC2bzDWSWdHKGGmZHn0bY9vKG2nYYP1doVlKGGodHXyJFExKG2rboOgZpkheGixc4Doc5R6em:|aX7lJGVNUVODIHP5eI9jdG:2IHHuZYx6e2m|LDDJR|UxKD1iMUiuPUDPxE1w M4LMdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{e1NFkxLz5{M{O3OVA6ODxxYU6=
U251 M{CydGZ2dmO2aX;uJIF{e2G7 Ml;POlAhdWmwcx?= MUfJcohq[mm2aX;uJI9nKF[HR1\SNkBqdiCqdX3hckBWOjVzIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhXkWJRj3pcoR2[2WmIIT5do9{cW6nIIDoc5NxcG:{eXzheIlwdiCrbnP1ZoF1\WRiZn;yJFYxKG2rboOgdJJqd3JidH:gWmVITi2jY4TpeoF1cW:wIH3lZZN2emWmIEGwJI1qdnNiYomgSWxKW0FuIFnDOVAhRSBzOD65JO69VS5? M1n3blxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NEO0NVM6Lz5{M{SzOFE{QTxxYU6=
CHO NIfvbYdHfW6ldHnvckBie3OjeR?= MmPLTY5pcWKrdHnvckBw\iCFYY[xMlIh[3W{cnXueEBu\WG|dYLl[EB2e2mwZzDRVIF1[2hiYYX0c41ifGmlIIDheIgh[2yjbYCgd5l{fGWvIHnuJGNJVyClZXzsd{BmgHC{ZYPzbY5oKEOjdkGuNkwh[mW2YT2yJIFv\CCjbIDoZU0zN2SnbIThMVEhe3WkdX7peJMtKEmFNUCgQUA{Oy52IN88UU4> MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzhzMkWwN{c,OjN6MUK1NFM9N2F-
U251 MkHESpVv[3Srb36gZZN{[Xl? MXnJcohq[mm2aX;uJI9nKF[HR1\SNkBqdiCqdX3hckBWOjVzIHPlcIx{KGK7IIDoc5NxcG:2eYLvd4lv\SCHTFnTRUwhUUN3MDC9JFAvODF6OTFOwG0v NHzJNlc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwNFg3PSd-MkS5NFA5PjV:L3G+
MCF7 NX;6eFJSSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NFnUZ|Q1QCCqcoO= MVHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkegZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NEA:KDFyLkWg{txONg>? MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB4NEO0O{c,OjVyNkSzOFc9N2F-
HepG2 NW\CPYxvSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M1f1W|Q5KGi{cx?= NWXZb4hGSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDI[ZBIOiClZXzsd{Bi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gNVMvPiEQvF2u MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB4NEO0O{c,OjVyNkSzOFc9N2F-
CHO MXrGeY5kfGmxbjDhd5NigQ>? NIHmZodKdmirYnn0bY9vKG:oIILhdIllKGSnbHH5[YQhcW65YYLkJJJm[3SrZonpcocheG:2YYPzbZVuKGO3coLlcpQhMEmNcjmgbY4hS2irbnXz[UBp[W2|dHXyJI93[XK7IDjDTG8qKGOnbHzzJJN1[WKuZTDlfJBz\XO|aX7nJIhGWkdibXXhd5Vz\WRidYPpcochUW:wV3;yb5MhSmG{cnHjeYRiKGG3dH;tZZRm\CCyYYTjbEBkdGGvcDDwcIF1\m:{bTygTWM2OCB;IEeuPVQ{OjhizszNMi=> Ml7yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyOEe3OVMoRjJ3MEi3O|U{RC:jPh?=
CHO K1 NVHFVo1vTnWwY4Tpc44h[XO|YYm= M{\LTWlvcGmkaYTpc44hd2ZicnHwbYQh\GWuYYnl[EBqdnejcnSgdoVkfGmoeXnu[{Bxd3Sjc4PpeY0h[3W{cnXueEApUUu{KTDpckBEcGmwZYPlJIhidXO2ZYKgc5ZienliKFPIU{khUzFiY3XscJMhe3SjYnz5JIV5eHKnc4PpcochcEWURzDt[YF{fXKnZDD1d4lv\yCLb37Xc5JseyCTdXH0eJJwKGG3dH;tZZRm\CCyYYTjbEBkdGGvcDDwcIF1\m:{bTygTWM2OCB;IEGwJO69VS5? MlH5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyOEe3OVMoRjJ3MEi3O|U{RC:jPh?=
CHO K1 M{Hs[2Z2dmO2aX;uJIF{e2G7 NVLKVW97UW6qaXLpeIlwdiCxZjDmZZN1KHOxZHn1cUBkfXK{ZX70JEhKVmFrIHnuJGNpcW6nc3WgTIFue3SncjDPeoFzgSBqQ1jPLUBMOSClZXzsd{B1emGwc3\lZ5Rm\CC5aYToJIh2dWGwIF7helEvPSCvZXHzeZJm\CC3c3nu[{BKd26Zb4Lrd{BSfWG2dILvJIF2fG:vYYTl[EBx[XSlaDDjcIFueCCybHH0[o9zdSxiSVO1NEA:KDF3Lki0PFkh|ryPLh?= NV3WSG9sRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwPFc4PTNpPkK1NFg4PzV|PD;hQi=>
HEK293 NUfyS|BuTnWwY4Tpc44h[XO|YYm= MnriTY5pcWKrdHnvckBw\iCoYYP0JJNw\Gm3bTDjeZJz\W62IDjJUoEqKGmwIFjFT|I6OyClZXzsd{B1emGwc3\lZ5Rm\CC5aYToJIh2dWGwIF7helEvPSCvZXHzeZJm\CC3c3nu[{BKd26Zb4Lrd{BSfWG2dILvJIF2fG:vYYTl[EBx[XSlaDDjcIFueCCybHH0[o9zdSxiSVO1NEA:KDN7LkixNFch|ryPLh?= NIjMcpI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC4O|c2Oyd-MkWwPFc4PTN:L3G+
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... 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 SU 11248 Malate
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)
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Step 2: Enter the in vivo formulation ()
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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)

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*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 )

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* 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

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Molecular Weight Calculator

Molecular Weight Calculator

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Total Molecular Weight: g/mol

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Molarity Calculator

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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

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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