Sunitinib

For research use only.

Catalog No.S7781 Synonyms: SU11248

146 publications

Sunitinib Chemical Structure

CAS No. 557795-19-4

Sunitinib (SU11248) is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. Sunitinib is also a dose-dependent inhibitor of the autophosphorylation activity of IRE1α. Sunitinib induces autophagy and apoptosis.

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Selleck's Sunitinib has been cited by 146 publications

Purity & Quality Control

Choose Selective PDGFR Inhibitors

Biological Activity

Description Sunitinib (SU11248) is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. Sunitinib is also a dose-dependent inhibitor of the autophosphorylation activity of IRE1α. Sunitinib induces autophagy and apoptosis.
Targets
FLT3 [1]
(Cell-free assay)
c-Kit [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
human SW756 cell MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVvJcohq[mm2aX;uJI9nKGi3bXHuJHNYPzV4IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUmuNVM2OSEQvF2= NXjaRVI5W0GQR1XS
human EoL-1-cell cell M2XmTWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NH;2fG1KdmirYnn0bY9vKG:oIHj1cYFvKEWxTD2xMYNmdGxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLk[0[U0xPg>? MnLLV2FPT0WU
human MV-4-11 cell M3LiT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlzYTY5pcWKrdHnvckBw\iCqdX3hckBOXi12LUGxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zPzJibl2= MnLlV2FPT0WU
human MV411 cells M1Tv[nBzd2yrZnXyZZRqd25iYYPzZZk> MY[0PEBp Ml\QRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPVkSxNUBk\WyuczDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDpZ|UxRTNibl2= Mn7tNlQ6ODR7NkG=
3T3 cells MlXsSpVv[3Srb36gZZN{[Xl? MljRTY5pcWKrdHnvckBw\iCSRFfGMYlv\HWlZXSgRpJlXSCrbnPvdpBwemG2aX;uJIlvKDOWMzDj[YxteyC5aYToJFAvOSViYn;2bY5mKHOncoXtJIFt[nWvaX6sJGlEPTB;NzDuUS=> M33rO|EzPjR4MEG5
HEK293 cells NXXoT3FnTnWwY4Tpc44h[XO|YYm= MmjKRolv\GmwZzDh[oZqdmm2eTD0c{BHVFR|IHPheIFtgXSrYzDkc41icW5iZYjwdoV{e2WmIHnuJGhGUzJ7MzDj[YxteyCkeTDjc41x\XSrdHn2[UBjcW6maX7nJIF{e2G7LDDL[F0xNjR5IH7N MoPxNVk4PTRzOUm=
human MDA-MB-435 cells Mo\nR5l1d3SxeHnjxsBie3OjeR?= M3;rZlIhcA>? MnzFR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUSzOUBk\WyuczygTWM2OD17Lkegcm0> MY[yOFg6ODZ3Mh?=
human RS4-11 cells MkP2SpVv[3Srb36gZZN{[Xl? M33Fd2lvcGmkaYTpc44hd2ZiRlzUN{BifXSxcHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKFKVND2xNUBk\WyuczDh[pRmeiB{IHjyd{BjgSCnbHXjeJJw[2inbXnseY1qdmW|Y3XuZ4Uh[XO|YYmsJGlEPTB;OT65JI5O M3qzeVE6PjV2NEC4
HUVEC MYrDfZRwfG:6aXRCpIF{e2G7 MY\DfZRwfG:6aXPpeJkh[WejaX7zeEBJXV[HQzygTWM2OD1zMT64JI5O NXfvOoVmOjR6OUC2OVI>
human Kasumi-1 cells NUP3XlFSTnWwY4Tpc44h[XO|YYm= M1eyc2lvcGmkaYTpc44hd2ZiYz3LbZQh[XW2b4Doc5NxcG:{eXzheIlwdiCrbjDoeY1idiCNYYP1cYkuOSClZXzsd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYOsJGlEPTB;MUWgcm0> NWDLeIpGOjB6M{OwN|k>
human NOS-1 cell NHvVW3pIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUTJcohq[mm2aX;uJI9nKGi3bXHuJG5QWy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUWuN{BvVQ>? NWrERopKW0GQR1XS
mouse triple negative 4T1 cells Mkf6R5l1d3SxeHnjxsBie3OjeR?= NY\H[HRiS3m2b4TvfIlkcXS7IHHnZYlve3RibX;1d4UhfHKrcHzlJI5m\2G2aY\lJFRVOSClZXzsd{whUUN3ME2xOkBvVQ>? NITJ[oczPDh7ME[1Ni=>
human RS4-11 cells M2riVWZ2dmO2aX;uJIF{e2G7 M1rIUWlvcGmkaYTpc44hd2ZiRlzUN{BifXSxcHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKFKVND2xNUBk\WyuczDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXNuIFnDOVA:OTZibl2= NYiwUXN6OjB6M{OwN|k>
human MOLM13 cells MYfDfZRwfG:6aXRCpIF{e2G7 NX\uTIV[S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVU:OTUGzJINmdGy|IHHzd4V{e2WmIHHzJINmdGxidnnhZoltcXS7IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OTdwNzDuUS=> NGO0cVQzPTB6OUixNC=>
human U251 cells M{PuTWZ2dmO2aX;uJIF{e2G7 M1nZPWlvcGmkaYTpc44hd2ZiVlXHSnIzKGmwIHj1cYFvKFV{NUGgZ4VtdHNiYomgdIhwe3Cqb4T5do9{cW6nIFXMTXNCNCCLQ{WwQVE5Njlibl2= M17NblI1QTByOE[1
NIH3T3 cells NXzhbW17TnWwY4Tpc44h[XO|YYm= Mnu5NUBp NUTzVXg4UW6qaXLpeI9zgSClb37j[Y51emG2aX;uJIFo[Wmwc4SgbJVu[W5iS1TSJItqdmG|ZTDlfJBz\XO|ZXSgbY4hVkmKM2SzJINmdGy|IIfpeIghPCC3TTDCbY91cW5vQXj4MWFGTUW\Rl\MSmEu[W2rZHWgZZQh[W2kaXXueEB1\W2yZYLheJVz\SCob4KgNUBpeg>? M{\D[|E3OTZ{MEC4
MDA-MB-231 cells Mm\hR5l1d3SxeHnjxsBie3OjeR?= MlnWR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6geJJqeGynIH7l[4F1cX[nIF3ERU1OSi1{M{GgZ4VtdHNuIFnDOVA:OjJwMzDuUS=> NEDGWZYzPDh7ME[1Ni=>
MCF7 cells MmfpR5l1d3SxeHnjxsBie3OjeR?= M3n6NGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGVTNXCxc3n0bZZmKE2FRkegZ4VtdHNuIFnDOVA:OjdwMTDuUS=> MYmyOFg6ODZ3Mh?=
human CGTH-W-1 cell NX;sSoZ[T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MofLTY5pcWKrdHnvckBw\iCqdX3hckBET1SKLWetNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMxNjl2IH7N Mn[5V2FPT0WU
human MONO-MAC-6 cell NXq1enI4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnfUTY5pcWKrdHnvckBw\iCqdX3hckBOV06RLV3BR{03KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzNwODDuUS=> NILPd2JUSU6JRWK=
human HL60 cells M1u2T2N6fG:2b4jpZ:Kh[XO|YYm= NYridFB3PDhiaB?= NUnkdlRXS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEx4MDDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKH[rYXLpcIl1gSCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVM3Njhibl2= NGS4WFkzPTB6OUixNC=>
human TT cells MWfQdo9tcW[ncnH0bY9vKGG|c3H5 M3f5XlczKGh? Mm[3RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCWVDDj[YxteyCycnX0doVifGWmIH\vdkA4OiCqcoOg[o9tdG:5ZXSgZpkh[2:vcH;1coQuf2G|aH;1eEBu\WG|dYLl[EBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUSwJI5O NWjFSIdHOjR7MES5OlE>
human THP1 cells MWHDfZRwfG:6aXRCpIF{e2G7 MU[0PEBp NU\RTI55S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hXEiSMTDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKH[rYXLpcIl1gSCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVQ2Njdibl2= M3r6b|I2ODh7OEGw
3T3 cells MmfmSpVv[3Srb36gZZN{[Xl? NU\XVGdXUW6qaXLpeIlwdiCxZjDWZZNkfWyjcjDlcoRwfGinbHnhcEBoem:5dHig[oFkfG:{IILlZ4VxfG:{IHnuJFNVOyClZXzsd{whUUN3ME21NEBvVQ>? NWPiV5JIOTJ4NE[wNVk>
human ALL-PO cell M4fPT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFvpOnFKdmirYnn0bY9vKG:oIHj1cYFvKEGOTD3QU{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVc6Njh7IH7N M1POc3NCVkeHUh?=
human SH-SY5Y cells MUHGeY5kfGmxbjDhd5NigQ>? Ml\MTY5pcWKrdHnvckBw\iCSRFfGVoJmfGFiaX6gbJVu[W5iU1itV3k2YSClZXzsd{BjgSCyaH;zdIhwfHm{b4PpcoUhTUyLU1GgZZN{[XluIFnDOVA:QDNwMTDuUS=> NILJOpozPDh7ME[1Ni=>
human U251 cells NX\zVIR1TnWwY4Tpc44h[XO|YYm= Mn;QOlAhdWmwcx?= M4Hoe2lvcGmkaYTpc44hd2ZiUFTHSnIu[mW2YTDpckBpfW2jbjDVNlUyKGOnbHzzJINwdXCxdX7kJJBz\XS{ZXH0[YQh\m:{IE[wJI1qdiCkZX\vdoUhWESJRj3CRkB{fGmvdXzheIlwdiCob4KgNVAhdWmwczDifUBxcG:|cHjveJlzd3OrbnWgSWxKW0FiY4n0c4Jtd3RibXX0bI9lNCCLQ{WwQVg{NjFibl2= NVnlWJA6OjV6OEK1NVk>
human NKM-1 cell M1zvSWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVTJRY5JUW6qaXLpeIlwdiCxZjDoeY1idiCQS12tNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVk5NjV{IH7N MoqxV2FPT0WU
human HAEC cells NHX5WmtRem:uaX\ldoF1cW:wIHHzd4F6 NHTxTXg4OiCq NEW0TlJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjBSWMh[2WubIOg[ZhxemW|c3nu[{BXTUeIUjDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTBwMTFOwG0> M3ftcVIzPDR2Nke5
HUVEC cell M{nD[2Z2dmO2aX;uJIF{e2G7 MW[yOEBp MorQTY5pcWKrdHnvckBw\iCYRVfGMWEhcW6mdXPl[EBJXV[HQzDj[YxtKHOycn;1eIlv\yCjZoTldkAzPCCqcoOgZpkh[W6paX;n[Y5me2m|IHHzd4F6NCCLQ{WwQVAvOTJizszN M1zZcFIyPzRzMkS5
human A431 cells MlzxSpVv[3Srb36gZZN{[Xl? M4D0[VYxKG2rboO= NUj1dVg6UW6qaXLpeIlwdiCxZjDFS2ZTKGmwIHj1cYFvKEF2M{GgZ4VtdHNiY3;tdI92dmRicILleJJm[XSnZDDmc5IhPjBibXnuJIJm\m:{ZTDFS2Yhe3SrbYXsZZRqd25iZn;yJFExKG2rboOgZpkheGixc4Doc5R6em:|aX7lJGVNUVODIHP5eI9jdG:2IH3leIhw\CxiSVO1NF0yPzJwMTDuUS=> MV[yOVg5OjVzOR?=
Sf9 cells NIjaOpZHfW6ldHnvckBie3OjeR?= MkLYTY5pcWKrdHnvckBw\iCJU2SteIFo\2WmIG\FS2ZTKGW6cILld5Nm\CCrbjDT[lkh[2WubIOsJGlEPTB;MD6xPFUh|ryP NY\OVIxSOTl6NUSwOVE>
human HT-29 cells Mn\OVJJwdGmoZYLheIlwdiCjc4PhfS=> MXe3NkBp MW\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiWLUK5JINmdGy|IHX4dJJme3OrbnegWmVITlJiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5Nige,:jDDJR|UxRTBwM{Og{txO MoLxNlI1PDR4N{m=
human KM12 cell Mn7ES5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NX;TNnpYUW6qaXLpeIlwdiCxZjDoeY1idiCNTUGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{PTBzNDFOwG0> MkDCV2FPT0WU
human TE-15 cell NHLld5FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWnETok2UW6qaXLpeIlwdiCxZjDoeY1idiCWRT2xOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPTB5NkGg{txO MkOzV2FPT0WU
human 697 cell NYrZeohST3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUjJcohq[mm2aX;uJI9nKGi3bXHuJFY6PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwNkG0NlUh|ryP MVzTRW5ITVJ?
human CAKI-1 cells M{HhS3Bzd2yrZnXyZZRqd25iYYPzZZk> MVzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEODS1mtNUBk\WyuczDh[pRmeiB2ODDodpMh[nliU2LCJIF{e2G7LDDHTVUxRTBwNkOg{txO NX;ISIVEOjJ3NkC2Nlc>
human MOLT-16 cell MWfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVPJcohq[mm2aX;uJI9nKGi3bXHuJG1QVFRvMU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlY{OTN{IN88US=> M3XY[nNCVkeHUh?=
human GB-1 cell NHrjR5VIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3\HTWlvcGmkaYTpc44hd2ZiaIXtZY4hT0JvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuO|ExOjNizszN MX\TRW5ITVJ?
human TE-12 cell NHXXbpdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEG0OlBKdmirYnn0bY9vKG:oIHj1cYFvKFSHLUGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE45ODR3NTFOwG0> NH3FeJlUSU6JRWK=
human NCI-H3122 cells M3X0T3Bzd2yrZnXyZZRqd25iYYPzZZk> NVfrc3ZOPzJiaB?= M1rWNWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWg{OTJ{IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9NE45OyEQvF2= MmKyNlQ6ODR7NkG=
human ES6 cell M4n4UGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2DKSmlvcGmkaYTpc44hd2ZiaIXtZY4hTVN4IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD65PFExPiEQvF2= NV;PdFNXW0GQR1XS
human NCI-H526 cells MlPZVJJwdGmoZYLheIlwdiCjc4PhfS=> MlTnO|IhcA>? NFHYOZNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU1JPTJ4IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9NU4xOSEQvF2= MWWyOFkxPDl4MR?=
human LC-2-ad cell NH70WplIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFHyeWJKdmirYnn0bY9vKG:oIHj1cYFvKEyFLUKtZYQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjFzNEC3JO69VQ>? NYH0dpd3W0GQR1XS
human BL-70 cell M2H5dGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIPZPJpKdmirYnn0bY9vKG:oIHj1cYFvKEKOLUewJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4yOTh2NjFOwG0> MoL2V2FPT0WU
human ETK-1 cell MYPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWXkcJpZUW6qaXLpeIlwdiCxZjDoeY1idiCHVFutNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvOjh3ODFOwG0> NWnqdldZW0GQR1XS
human SW620 cells NHzwZW1Rem:uaX\ldoF1cW:wIHHzd4F6 NGLUcpc1QCCq NX\sWZQxSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTW|YzOCClZXzsd{Bi\nSncjC0PEBpenNiYomgV3JDKGG|c3H5MEBIUTVyPUGuN{DPxE1? MoPpNlI2PjB4Mke=
IM9 cells NVLMOW06S3m2b4TvfIlkyqCjc4PhfS=> NWLmb2tuS3m2b4TvfIlkcXS7IHHnZYlve3RiSH;tc{B{[XCrZX7zJEhpfW2jbjmgTW06KGOnbHzzJIF{e2W|c3XkJIF{KGe{b4f0bEBqdmirYnn0bY9vKGK7IF3UWEBie3OjeTygTWM2OD1zLkO1JO69VQ>? MXnTRW5ITVJ?
human A4-Fuk cell M3rGOGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWLJcohq[mm2aX;uJI9nKGi3bXHuJGE1NU[3azDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H589yNKEmFNUC9NU4{PDF2MTFOwG0> NH3Rc5hUSU6JRWK=
human SR cell M3;5fGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmS4TY5pcWKrdHnvckBw\iCqdX3hckBUWiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwNUS1O|Ih|ryP MXHTRW5ITVJ?
human A3-KAW cell Mn7iS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIHqNFRKdmirYnn0bY9vKG:oIHj1cYFvKEF|LVvBW{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCrY{WwQVEvPjJ3NE[g{txO MkPBV2FPT0WU
human KS-1 cell M1nsTmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3Ht[GlvcGmkaYTpc44hd2ZiaIXtZY4hU1NvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOlkzPDdizszN NIrOV2ZUSU6JRWK=
human CTV-1 cell MoPTS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MX\Jcohq[mm2aX;uJI9nKGi3bXHuJGNVXi1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT63Nlc2OSEQvF2= NX7wT45kW0GQR1XS
human LB1047-RCC cell MmftS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFHNU4dKdmirYnn0bY9vKG:oIHj1cYFvKEyEMUC0O{1TS0NiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkixOlI1KM7:TR?= NXTFcnlqW0GQR1XS
human MEG-01 cell Mnr2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYfJcohq[mm2aX;uJI9nKGi3bXHuJG1GTy1yMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuPFM2PjNizszN M3XyeHNCVkeHUh?=
human TE-11 cell M1zBZWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYW1[XhKUW6qaXLpeIlwdiCxZjDoeY1idiCWRT2xNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvQDN7OEWg{txO M{H2dHNCVkeHUh?=
human CMK cell NX70WI5jT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXiySIE5UW6qaXLpeIlwdiCxZjDoeY1idiCFTVugZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlk2PTF5IN88US=> M4WySXNCVkeHUh?=
human NB1 cell MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NETuTmpKdmirYnn0bY9vKG:oIHj1cYFvKE6EMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuPVYyOTdizszN MVjTRW5ITVJ?
human MDA-MB-435 cells NV3ISVB7WHKxbHnm[ZJifGmxbjDhd5NigQ>? MWS0PEBp MnLpRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuPDN3IHPlcIx{KGGodHXyJFQ5KGi{czDifUBUWkJiYYPzZZktKEeLPUKg{txO MV:yNlU3ODZ{Nx?=
human MCF7 cells NEjGbJRRem:uaX\ldoF1cW:wIHHzd4F6 NGjLNGY1QCCq MXTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkegZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KFOUQjDhd5NigSxiR1m1NF0zKM7:TR?= MUOyNlU3ODZ{Nx?=
human A549 cells MUXDfZRwfG:6aXRCpIF{e2G7 MXO3NkBp MYfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIF{e2W|c3XkJIF{KGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9Nk41PCEQvF2= MnPPNlM3ODJ2NEG=

... 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 pSer(473)Akt, 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-transferase fusion 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 25 mg/mL warmed (62.73 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+corn oil
For best results, use promptly after mixing.
0.875mg/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 398.47
Formula

C22H27FN4O2

CAS No. 557795-19-4
Storage powder
in solvent
Synonyms SU11248
Smiles CCN(CC)CCNC(=O)C1=C(NC(=C1C)C=C2C3=C(C=CC(=C3)F)NC2=O)C

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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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

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID