Sunitinib Malate

Licensed by Pfizer Catalog No.S1042

Sunitinib Malate Chemical Structure

Molecular Weight(MW): 532.56

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.

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Cited by 43 Publications

12 Customer Reviews

  • PDGF-AA induces Ezh2 expression and proliferation in juvenile islets but not in adult islets. Western immunoblots of indicated islet proteins from 3 week or 9 month-old WT islets 2 days after exposure to PDGF-AA alone, or PDGF-AA plus RTK inhibitors Sunitinib.

    Nature 2011 478(7369):349-55. Sunitinib Malate purchased from Selleck.

    Assessment of effects on human juvenile or adult islets after exposure to PDGF-AA (50 ng/ml) for 2 days, with or without Sunitinib (2 uM) or U0126 (10 uM)co-treatment. Average percentage of BrdU+ insulin+ cells was morphometry from sectioned islets immunostained for insulin (green), glucagon (white) and BrdU (red). n = 3-6 independent experiments.

    Nature 2011 478(7369):349-55. Sunitinib Malate purchased from Selleck.

  • Combinational treatment of kinase inhibitors induces the similar phenotype produced by PP1. All images are lateral view with dorsal to the top and anterior to the left. The combinational treatment of Dasatinib (D) or U0126 (U) with Sunitinib (SU),PTK787 (PTK), or ZM323881 (Z) resulted in the shrinkage of dorsal aorta.

    Cell Res 2011 21, 1080-1087. Sunitinib Malate purchased from Selleck.

    A, Tumor growth curves from the initial sunitinib drug trials, with endpoint set at 1,300 mm3 (mean ± SEM). Measurements began one week after tumor inoculation and on the day sunitinib treatment began. Subsequent experimental endpoints were set on the basis of these growth curves and their intersections with this data are shown. B, Histogram plot showing the distribution of tumor sizes at day 8 of treatment. Sunitinib-treated tumors exceeding 250 mm3 in size were identified as falling into the nonresponsive cohort. Sunitinib treatment significantly retards growth of responsive tumors.

    Cancer Res, 2017, 77(4):1008-1020 . Sunitinib Malate purchased from Selleck.

  • Sunitinib decreases FLT-3 and RET phosphor ylation but increases ERK phosphorylation in a time-dependent manner. H295R and SW13 cells were treated with sunitinib (10 nM) for various time points as indi-cated. Cell lysates were prepared and phospho-FLT-3, RET, and ERK levels were monitored by Western Blot-ting. Re-probing against FLT-3, RET, and ERK was done to ensure equal protein loading.

    Surgery 2012 152, 1045-50. Sunitinib Malate purchased from Selleck.

    Sunitinib or PD98059 decreases cell proliferation in a dose-dependent manner. H295R and SW13 cells were treated with various concentration of sunitinib or PD98059 for 48 hours as indicated. Treated cells were subjected to the MTS proliferation assay. Similar experiments were repeated 3 times. Histograms represent relative % of OD490 nm absorbance (* P < .05). All data are relative multiples of expression compared with untreated cells. The data are representative of three experiments and are expressed as the mean ?SE.

    Surgery 2012 152, 1045-50. Sunitinib Malate purchased from Selleck.

  • Autophagic activation in sunitinib- and sorafenib- but not AZD6244-treated cells. Medullary thyroid cancer-1.1 (MTC-1.1; A) and TT ( B) cells were treated with dimethyl sulfoxide (DMSO), sunitinib (50 nM), sorafenib (10 nM), AZD6244 (30 nM), or everolimus (20 nM) for 48 hours. Cell lysates were prepared, and light chain 3 (LC3)-I and -II cleaved caspase-3 protein levels were monitored by Western blotting. Reprobing against actin was per formed to ensure equal protein loading. ( C ) MTC-1.1 and TT cells were transiently transfected with autophagy protein 5 (Atg-5) small inter fering RNA. Transfection with scrambled small inter fering RNA was used as a control. After transfection, cells with and without Atg-5 knockdown were exposed to DMSO or 20 nM of everolimus for 48 hours. Cell lysates were pre- pared and LC3-I and -II protein expression levels were monitored by Western blotting. Reprobing against Atg-5 was per formed to monitor Atg-5 knockdown efficiency. Reprobing against actin was per formed to ensure equal protein.

    Surgery 2012 152, 1142-9. Sunitinib Malate purchased from Selleck.

    Autophagy inhibition blocks the antiproliferative effects of sunitinib and sorafenib but not AZD6244. Medullary thyroid cancer–1.1 (MTC-1.1) and TT cells were transfected transiently with scrambled or autophagy protein 5 (Atg-5) small inter fering RNA. After transfection, cells with and without Atg-5 knockdown were exposed to sunitinib (50 nM), sorafenib (10 nM), and AZD6244 (30 nM) for 48 hours. Treated cells were subjected to a 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium proliferation assay. Similar experiments were repeated 3 times. Histograms represent the relative percent of OD490 nM absorbance. The asterisk indicates significance versus scrambled small inter fering RNA–treated control ( P < .05). All data are relative multiples of expression compared to untreated cells. The data are representative of 3 experiments and are expressed as the mean ± the standard error.

    Surgery 2012 152, 1142-9. Sunitinib Malate purchased from Selleck.

  • Sunitinib limits the colonial growth of HT-29 by downregulating HIF-1a. (A) The number and size of colonies formed in soft agar. The numbers of small colonies (<50 μm diameter) were not different among conditions of a serial concentration of sunitinib. On the contrary, large colonies (>50 μm diameter) disappeared after incubation with sunitinib. Each point represents the mean and SD from four separate experiments. (B) HIF-1a expression and hypoxia within HT-29 colony. After colonies grew for 4 weeks, HIF-1a and hypoxia were visualized by immunofluoroscence staining. Bar = 20 μm.

    Biochem Bioph Res Co 2010 398, 205–211. Sunitinib Malate purchased from Selleck.

    2. Sunitinib downregulates HIF-1a. (A) Dose-dependent repression of HIF-1a protein level by sunitinib in HT-29. HT-29 cells were incubated under normoxic (N) or hypoxic (H) conditions in the presence of sunitinib for 24 h. HIF-1a and ARNT proteins in total cell lysates were analyzed by Western blotting. (B) Sunitinib attenuates the hypoxic induction of HIF-1 target genes. RNAs were isolated from HT-29 cells subjected to normoxia (N) or hypoxia (H) in the presence of sunitinib for 16 h. The mRNAs of HIF-1a and its target genes were analyzed by RT-PCR and autoradiography. PGK1 indicates phosphoglycerate kinase 1; PDK1, pyruvate dyhydrogenase kinase 1; CAIX, carbonic anhydrase IX. (C) Sunitinib-induced HIF-1 inhibition. Epo-enhancer and b- galactosidase reporter plasmids were co-transfected into HEK293 cells. After 16 h incubation, luciferase and b-galactosidase activities were measured. *P < .05 versus the hypoxic control.

     

     

    Biochem Bioph Res Co 2010 398, 205–211. Sunitinib Malate purchased from Selleck.

  • Sunitinib inhibits 50-UTR-dependent translation of HIF-1a. (A) 50 cap-dependent translational activity of HIF-1a. The luciferase reporter plasmid contains the HIF-1a 50-UTR segment between the tk promoter and the luciferase gene. HT-29 cells were co-transfected with the reporter plasmid (8 lg per 100-mm dish) and the b-gal plasmid (4 μg). After 16 h incubation under normoxic or hypoxic conditions with sunitinib, cells were lysed and subjected to luciferase assay. *P < .05 versus the hypoxic control. (B) IRES-dependent translational activity of HIF-1a. The luciferase reporter plasmid contains the HIF-1a 50-UTR segment between the GFP gene and the luciferase gene. HT-29 cells were co-transfected with the reporter plasmid (8 μg) and the b-gal plasmid (4 μg). *P < .05 versus the hypoxic control. (C) Sunitinib inhibits phosphorylation of Akt. After 8 h incubation under hypoxic condition with sunitinib, HT-29 cells were lysed and subjected to Western blotting. (D) Sunitinib suppresses HIF-1a in VHL-null RCC4 cells. VHL (-/-) RCC4 cells were incubated under normoxic conditions sunitinib for 8 h, and HIF-1a in total cell lysates was analyzed by Western blotting.

     

     

    Biochem Bioph Res Co 2010 398, 205–211. Sunitinib Malate purchased from Selleck.

    Experimental layout for VEGF signaling blocking and LCMV infection in WT mice. Mice received two injections on day 0 and 3 p.i. of Abs as described in Material and Methods, or daily gavage of the VEGFR/PDGFR-inhibitor sunitinib. Inguinal LN volume on day 0 (D0) or day 8 (D8) p.i. after treatment of mice with control Ig or anti-VEGFR2, anti-VEGF-A Abs or sunitinib. Pooled from 1-2 independent experiments with 3-5 mice per treatment. D. Total HEV length on day 0 (D0) or day 8 (D8) p.i. as in C. No significant difference was found in C and D between day 8 control Ig and Ab- or inhibitor-treated values (One-way ANOVA).

    AACR Sunitinib Malate purchased from Selleck.

Purity & Quality Control

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.
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 MkDQT4lv[XOnIFHzd4F6 NY\3WYg3UW6qaXLpeIlwdiCxZjDQSGdHNWmwZIXj[YQhSnKmVTDpcoNwenCxcnH0bY9vKHerdHigTWM2OCCxZjCwMlAxPyEQvF2= MmXoNVI3PDZyMUm=
3T3 NEHCNGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEH1SpFKdmirYnn0bY9vKG:oIGDsZZRmdGW2LXTldol3\WRiZ4Lve5RpKG[jY4TvdkBqdmS3Y3XkJFNVOyClZXzsJJBzd2yrZnXyZZRqd25id3n0bEBKSzVyIH;mJFAvODFizszN MnLtNVI3PDZyMUm=
3T3 NVfmdVdbTnWwY4Tpc44hSXO|YYm= NF7oUGxKdmirYnn0bY9vKG:oIG\hd4N2dGG{IHXu[I91cGWuaXHsJIdzd3e2aDDmZYN1d3JicnXj[ZB1d3Jid3n0bEBKSzVyIH;mJFAvODVizszN NVKxTmlkOTJ4NE[wNVk>
3T3 NVzod3BoU2mwYYPlJGF{e2G7 M4rPfFIxKG2rbh?= MlP4SG1UVw>? NF3IcJZE\WyudXzhdkBqdmirYnn0bY9vKG:oIG\FS2YhcW6mdXPl[EBpfW2jbjDLSHIheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCyNkDPxE1? M2XQUFE3OTZ{MEC4
NIH3T3 NH23c|NMcW6jc3WgRZN{[Xl? NEDyc4EzOCCvaX6= MYHEUXNQ NF3IO4RqdmirYnn0JIh2dWGwIFvEVkBscW6jc3Wg[ZhxemW|c3XkJJdqfGhiSVO1NEBw\iByLkCxPEDPxE1? M2q1TlE3OTZ{MEC4
A549 MYnGeY5kfGmxbjDBd5NigQ>? NUTK[3NHTE2VTx?= NGPEbGlKdmirYnn0bY9vKG:oIHOtUYV1KGSncHXu[IVvfCCKR1[tbY5lfWOnZDDoeY1idiCDNUS5JINmdGxibXnndoF1cW:wIIfpeIghUUN3MDDv[kAzKM7:TR?= Mn;xNVg1OzRzNEW=
DU145 MVrGeY5kfGmxbjDBd5NigQ>? NHnnUZFFVVOR MXHJcohq[mm2aX;uJI9nKGNvTXX0JIRmeGWwZHXueEBJT0ZvaX7keYNm\CCqdX3hckBFXTF2NTDj[YxtKHOlYYT0[ZJqdmdid3n0bEBKSzVyIH;mJFExKM7:TR?= MYKxPFQ{PDF2NR?=
KB3-1 NVP6NWdES3m2b4TvfIlkKEG|c3H5 MkW2O|IhcA>? NWrkWopQTE2VTx?= MVTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQMYdxNW6nZ3H0bZZmKEuELUOtNUBk\WyuczD3bZRpKEmFNUCgc4YhOi5|IN88US=> NF7BNZgyQTN7N{OyNi=>
KBV1 M1\KfGN6fG:2b4jpZ{BCe3OjeR?= NETVVGU4OiCq MYTEUXNQ MXHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQMYdtgWOxcILveIVqdi2neIDy[ZN{cW6pIFvCWlEh[2WubIOge4l1cCCLQ{WwJI9nKDRwMTFOwG0> NFvScGoyQTN7N{OyNi=>
A375 Mo\jR5l1d3SxeHnjJGF{e2G7 MYC3NkBp NXnhU2doTE2VTx?= M3e3Z2lEPTB;NT60JO69VQ>? NF3sSWUyQTZ3NESwPC=>
RS4-11 MnnkSpVv[3Srb36gRZN{[Xl? NFfBbXczKGh? M{TqZWlvcGmkaYTpc44hd2ZiRlzUN{BifXSxcHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCwMlAxQTlizszN MUSxPVY2PDRyOB?=
RS4-11 NX;INohYTnWwY4Tpc44hSXO|YYm= M4P5W|IhcA>? MWPJcohq[mm2aX;uJI9nKE[OVEOgTXRFKG23dHHueEBifXSxcHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCwMlA{PCEQvF2= MkPuNVk3PTR2MEi=
Sf9 NUjab21[U2mwYYPlJGF{e2G7 MUGzNEBucW5? MnXvTY5pcWKrdHnvckBw\iCJU2SteIFo\2WmIG\FS2ZTKGW6cILld5Nm\CC5aYToJGlEPTBib3[gNE4yQDVizszN M4j2XVE6QDV2MEWx
Ba/F3 MnXDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjEZWs4OiCq MYnJR|UxRTFwMjFOwG0> MYOyNFEyPzByNB?=
BaPTC2 NUD2TnYxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jyNlczKGh? NEnNenRKSzVyPUCuNlIh|ryP MWKyNFEyPzByNB?=
Sf9 M2L0eGZ2dmO2aX;uJGF{e2G7 M3jpdFEhcA>? M1jYNmROW09? NUPDRWNRUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDIbZMufGGpZ3XkJHJGXCCneIDy[ZN{\WRid3n0bEBKSzVyIH;mJFEvOyEQvF2= MWSyNFEyPzByNB?=
H4 NUjHd3ZwS3m2b4TvfIlkKEG|c3H5 MoHsNVAh|ryP NFnC[o1Vd3irY3n0fUBqdiCqdX3hckBJPCClZXzsdy=> MXGyNFM2ODhyNh?=
SF-539 NG[2fHFMcW6jc3WgRZN{[Xl? MXWzN|Mh|ryP MlWxOlAhdWmw MULEUXNQ MkHzTY5pcWKrdHnvckBw\iCSRFfGVoJmfGFicHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCxNk4zKM7:TR?= NE\XNlEzODRyM{ewNC=>
U251 M4C3eWtqdmG|ZTDBd5NigQ>? NITpR20{OzNizszN MmjSOlAhdWmw NWjQfoIzTE2VTx?= NHjze5FKdmirYnn0bY9vKG:oIG\FS2ZTOiCyaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIEG4Mlkh|ryP NYHjVpRXOjB2MEO3NFA>
A431 NGnTW4hMcW6jc3WgRZN{[Xl? MkTrTY5pcWKrdHnvckBw\iCSRFfGVoJmfGFiZYjwdoV{e2WmIIfpeIghUUN3MDDv[kAyOi5{IN88US=> MXWyNFU2QDB5Mh?=
A431 NWTJfFJ7U2mwYYPlJGF{e2G7 NXTic2VZUW6qaXLpeIlwdiCxZjDWSWdHWjJiZYjwdoV{e2WmIIfpeIghUUN3MDDv[kAyQC57IN88US=> MU[yNFU2QDB5Mh?=
HepG2 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTvdYhLPzJiaB?= NVLlVFBKUUN3ME2zMlgyKM7:TR?= NWjx[nhqOjB3N{C1NlY>
Kasumi-1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLEO|IhcA>? M2foS2lEPTB;MD6wNVYh|ryP MkLnNlA2PzB3Mk[=
RS4-11 M1;mfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHiSnI4OiCq MnjjTWM2OD1zIN88US=> MX2yNFU4ODV{Nh?=
THP1 M3;ae2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfWO|IhcA>? NHzhNoFKSzVyPUCuOUDPxE1? M17od|IxPTdyNUK2
Kasumi-1 MVrGeY5kfGmxbjDBd5NigQ>? NV;Pbm1LUW6qaXLpeIlwdiCxZjDjMWtqfCCjdYTvdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAxNjBzNTFOwG0> MnP2NlA5OzNyM{m=
A549 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYSxOkBp M{\veWFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG1OFkh[2WubIO= M3nVelIyPDVyNE[z
HL60 MkfFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW[xOkBp MYHBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKTE[wJINmdGy| Mor2NlE1PTB2NkO=
HUVEC MoexS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYr2W|Y2OTZiaB?= NVLZcJh2UW6qaXLpeIlwdiCxZjDWSWdHNWmwZIXj[YQh[2WubDDwdo9tcW[ncnH0bY9vKHerdHigTWM2OCCxZjCyMlc2KM7:TR?= MViyNVQ2ODR4Mx?=
HUVEC M{HYc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XyeVE3KGh? MWfJcohq[mm2aX;uJI9nKGKIR1[tbY5lfWOnZDDj[YxtKHC{b3zp[oVz[XSrb36ge4l1cCCLQ{WwJI9nKDRwMESg{txO NWLUTlFZOjF2NUC0OlM>
IM9 NEfoT41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3v2c|E3KGh? MlzyRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSV25JINmdGy| MUeyNVQ2ODR4Mx?=
K562 M2nydWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnqxNVYhcA>? NW\DVYg1SW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gT|U3OiClZXzsdy=> MYKyNVQ2ODR4Mx?=
MDA-MB-231 MnXBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfYNnoyPiCq MVTBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuOjNzIHPlcIx{ MYiyNVQ2ODR4Mx?=
H460 NH[xPINEgXSxdH;4bYMhSXO|YYm= NFnmbYI4OiCq MXXJR|UxRTJwNzFOwG0> NUjVdlV2OjF4MkG4PFA>
SMMC7721 NYjqWHM{S3m2b4TvfIlkKEG|c3H5 Ml3ZO|IhcA>? MWnJR|UxRTZwNEeg{txO MX:yNVYzOTh6MB?=
WI38 NUDLXlVZS3m2b4TvfIlkKEG|c3H5 NEf2doo4OiCq MWLJR|UxRThwNU[g{txO M360T|IyPjJzOEiw
HEK293 MoTOT4lv[XOnIFHzd4F6 MYWxNFAhdk1? NE\pUooyKGh? M1\ReIRw\XNibn;0JIlvcGmkaYSgWmVITi2rbnT1Z4VlKGG3dH;wbI9{eGixconsZZRqd25ib3[geJlzd3OrbnWgNVE4PSC{ZYPp[JVmKG:wIG\FS2ZTOiCneIDy[ZN{\WRiaX6gTGVMOjl|IHPlcIx{ MnjWNlE5QDV{OEe=
HUVEC NXf6O|hvTnWwY4Tpc44hSXO|YYm= M4WyflEh|ryP NVXDTmprOjRiaB?= NV3p[5RoSW62aXHu[4lw\2WwaXOgZYN1cX[rdImgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5iVlXHSk1qdmS3Y3XkJINmdGxibXnndoF1cW:w MkfYNlE6PjN|MEW=
HUVEC Mn3QSpVv[3Srb36gRZN{[Xl? NWq5bYkyOSEQvF2= NX7lRZRjOSCq MnLBTY5pcWKrdHnvckBw\iCHUlugdIhwe3Cqb4L5cIF1cW:wIHH0JHRpejJyMj;UfZIzODRiaX6gWmVITi2|dHnteYxifGWmIFjVWmVE M{HKU|IyQTZ|M{C1
HUVEC NXzuRVNUTnWwY4Tpc44hSXO|YYm= NUXhfG9nOSEQvF2= Moe0NUBp NEnqd3pKdmirYnn0bY9vKG:oIHXOU3MheGixc4Doc5J6dGG2aX;uJIF1KFOncj2xNVczKGmwIG\FS2Yue3SrbYXsZZRm\CCKVW\FRy=> M4r6ZlIyQTZ|M{C1
HUVEC NFHi[WhMcW6jc3WgRZN{[Xl? MUSxJO69VQ>? NVHjO3dkOSCq MUnJcohq[mm2aX;uJI9nKF[HR1\SNkBxcG:|cHjvdplt[XSrb36gZZQhfHm{LUGxO|UhcW5iVlXHSk1{fGmvdXzheIVlKEiXVlXD NEK3Um0zOTl4M{OwOS=>
HUVEC NXK2RVR6TnWwY4Tpc44hSXO|YYm= MoO3NUDPxE1? MVixJIg> MnH3[I9meyCwb4SgbY5pcWKrdDDBT3QheGixc4Doc5J6dGG2aX;uJIF1KFOncj20O|MhcW5iVlXHSk1{fGmvdXzheIVlKEiXVlXD NYLENlJNOjF7NkOzNFU>
HL60 NHGz[nNEgXSxdH;4bYMhSXO|YYm= MkTxOVAh|ryP MojjOFghcA>? Ml7XSG1UVw>? M1fTUGlEPTB;MUWuOUDPxE1? Mn;jNlIxOTlzOEi=
K562 MXLDfZRwfG:6aXOgRZN{[Xl? NHrjVFE2OCEQvF2= M3XyeVQ5KGh? NIPub3dFVVOR NEPXfWlKSzVyPUKxMlkh|ryP MkH5NlIxOTlzOEi=
PC3 Ml7RR5l1d3SxeHnjJGF{e2G7 MnjLOVAh|ryP NVz4UJBxPDhiaB?= MV3EUXNQ MXvJR|UxRTJ3LkGg{txO NGPwSoozOjBzOUG4PC=>
SF-539 Mk\2T4lv[XOnIFHzd4F6 MVGzN|Mh|ryP NUW5[WlIPjBibXnu MVzJcohq[mm2aX;uJI9nKFCGR1\SZoV1[SC2eYLvd4lv\SCtaX7hd4Uh[WO2aY\peJkhcW5iUFTHSk1DSi2|dHnteYxifGWmIHj1cYFvKFOILUWzPUBk\WyuczD3bZRpKEmFNUCgc4YhOTJwMjFOwG0> NHLjN4gzOjJyNEe0NS=>
HAEC MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjUcVBsOTByIN88US=> M2j0bVczKGh? M1fMUWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFHFR{Bk\WyuczDlfJBz\XO|aX7nJHZGT0[UIIfpeIghUUN3MDDv[kAxNjFizszN MnnuNlI1PDR4N{m=
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MDA-MB-435 MkC0R5l1d3SxeHnjJGF{e2G7 NHqwZnM4OiCq NHTJVlhFVVOR MXXJR|UxRTBwMEC5O{DPxE1? MnPkNlQ5QTB4NUK=
MDA-MB-468 MXLDfZRwfG:6aXOgRZN{[Xl? NXzWbo01PzJiaB?= M121RmROW09? MnuyTWM2OD1yLkCwOlEh|ryP NFjMZoUzPDh7ME[1Ni=>
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Bel7402 Mk[5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnG2O|IhcA>? NUDD[ZdvTE2VTx?= NVrZ[2JuUUN3ME2yMlY4KM7:TR?= Mn;DNlQ6ODR7NkG=
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NCI-H3122 NETFWWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWq3NkBp MlroSG1UVw>? NFrIeXhKSzVyPUCuPFMh|ryP MVGyOFkxPDl4MR?=
NCI-H460 NV:3bW5IT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYj5SJlPPzJiaB?= NWrOSGFwTE2VTx?= M{jtN2lEPTB;ND6zNUDPxE1? MXKyOFkxPDl4MR?=
NCI-H526 NGnUS5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DUNVczKGh? NHvGWoRFVVOR M4rmdGlEPTB;MT6wNUDPxE1? NGi1TIYzPDlyNEm2NS=>
TT M{XrdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1u2T|czKGh? NGLufGRFVVOR M3T4UGlEPTB;MD6wOEDPxE1? M{W2R|I1QTB2OU[x
EoL-1-cell NFnCTVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4m5cmlEPTB;MT62OEBxVQ>? M2\MeHNCVkeHUh?=
MV-4-11 M1\ReWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LMNWlEPTB;MkeyJJBO MVXTRW5ITVJ?
NOS-1 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF[1cXFKSzVyPUG1MlMhdk1? M{jE[HNCVkeHUh?=
CGTH-W-1 Mly2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPYVWNKSzVyPUOwMlk1KG6P NXz3d|M5W0GQR1XS
MONO-MAC-6 MmjmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTN|Lkigcm0> M2\yc3NCVkeHUh?=
ALL-PO MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\NfWlEPTB;N{muPFkhdk1? NHrwU3ZUSU6JRWK=
NKM-1 M{XOfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DZTWlEPTB;OUiuOVIhdk1? NGnjOppUSU6JRWK=
KM12 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3kZnNKSzVyPUO1NE4yPCCwTR?= MnfKV2FPT0WU
TE-15 Ml[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TST2lEPTB;NUC3MlYyKG6P MnfRV2FPT0WU
697 M1r1[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHztWFJKSzVyPU[xOE4zPSCwTR?= M4jWe3NCVkeHUh?=
MOLT-16 MlHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXVTWM2OD14M{GuN|Ihdk1? M{SwdXNCVkeHUh?=
GB-1 M{fCdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXzeZlKSzVyPUexNE4zOyCwTR?= NVy0eGJGW0GQR1XS
TE-12 MkfpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PGZ2lEPTB;OEC0MlU2KG6P NIHhVFVUSU6JRWK=
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BL-70 MnW4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\GTWM2OD1zLkGxPFQ3KM7:TR?= NYfpdGE1W0GQR1XS
ETK-1 MmjaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlH4TWM2OD1zLkK4OVgh|ryP MlHrV2FPT0WU
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SIG-M5 NIHKbnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;FZ2lEPTB;MT6zO|AxQSEQvF2= MXnTRW5ITVJ?
NCI-SNU-16 NFLEZ5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXmTWM2OD1zLkS2OFg3KM7:TR?= MoX6V2FPT0WU
PSN1 NF7T[4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTFwNUC2O|Yh|ryP MUDTRW5ITVJ?
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KS-1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVOzfGk5UUN3ME2xMlY6OjR5IN88US=> MVrTRW5ITVJ?
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LB1047-RCC M33PfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTFwOEG2NlQh|ryP M4TB[nNCVkeHUh?=
EMG-01 NUPhNXRST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTFwOEO1OlMh|ryP MYHTRW5ITVJ?
TE-11 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnT[nV5UUN3ME2xMlg{QTh3IN88US=> MmjVV2FPT0WU
CMK M3TZeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjyZ2dQUUN3ME2xMlk2PTF5IN88US=> NFzFe5pUSU6JRWK=
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HAL-01 NUO4OlA4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DVUGlEPTB;Mj6wOVk1PiEQvF2= M2rWdnNCVkeHUh?=
DEL M1XnSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTFbolKSzVyPUKuNFg1QDJizszN M1TBNnNCVkeHUh?=
RL95-2 NFntN3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTJwMUGxN|ch|ryP Mmr3V2FPT0WU
KARPAS-299 NGLGSIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4[3T2lEPTB;Mj6xNVMyOyEQvF2= MXfTRW5ITVJ?
EW-16 NYTneIN7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1n6SWlEPTB;Mj6xN|UxQCEQvF2= NXG0OIdMW0GQR1XS
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BB30-HNC NFnrS2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PYeGlEPTB;Mj6yNlM4PSEQvF2= NGXDUJBUSU6JRWK=
DOHH-2 NGOzXZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{K3S2lEPTB;Mj6zN|Q{OSEQvF2= MVLTRW5ITVJ?
RPMI-8402 NWLXWYRQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDtO|h4UUN3ME2yMlM{PjF6IN88US=> NGrCWo9USU6JRWK=
BV-173 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTJwM{O2OkDPxE1? M3Xl[HNCVkeHUh?=
TE-10 MnTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXjTWM2OD1{LkO0N|g1KM7:TR?= MkmxV2FPT0WU
TE-8 NXS2XpA2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVv6SlMxUUN3ME2yMlM4ODN6IN88US=> NHvPVm9USU6JRWK=
K052 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYX1UVl2UUN3ME2yMlQxOjB{IN88US=> NIjRZnRUSU6JRWK=
KARPAS-45 MlXHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTJwNEm0OFYh|ryP MmfzV2FPT0WU
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ML-2 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoS1TWM2OD1{Lk[zOVEzKM7:TR?= NGDa[o5USU6JRWK=
LAMA-84 MmmzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUC2c2V6UUN3ME2yMlY6PTR3IN88US=> NEXVcnBUSU6JRWK=
LXF-289 NF3QNmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEi1WllKSzVyPUKuO|I6QDlizszN M4\rU3NCVkeHUh?=
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NCI-H1882 NGj5Z2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TiS2lEPTB;MUeuPVg{PCEQvF2= NUTvXJVoW0GQR1XS
A704 M3XpRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nIV2lEPTB;MUeuPVkxPCEQvF2= NGXMNWtUSU6JRWK=
L-428 NF[2T4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHH1colKSzVyPUG4MlAyPTFizszN NEjm[ohUSU6JRWK=
HCC1187 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVP3c5c6UUN3ME2xPE4xOTh5IN88US=> NEHPcmNUSU6JRWK=
NCI-H1581 M335[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jBSWlEPTB;MUiuNFg3PiEQvF2= MULTRW5ITVJ?
BB65-RCC MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fObmlEPTB;MUiuOFE3OiEQvF2= M13IT3NCVkeHUh?=
EM-2 M{Ptcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDJRm5KSzVyPUG4MlU3PzJizszN NUn1XGsxW0GQR1XS
Raji Mme4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlm5TWM2OD1zOT65OVY2KM7:TR?= NXfTZpFFW0GQR1XS
TE-1 M4TSTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXwcoRKSzVyPUKwMlQyODRizszN NEewb3hUSU6JRWK=
SW962 MoTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTJyLkSyPVMh|ryP NEPBTWxUSU6JRWK=
MHH-NB-11 NFjxeVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTJyLkW1NlEh|ryP NWnDcHJPW0GQR1XS
no-10 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTJzLkCyOlQh|ryP M{f6dHNCVkeHUh?=
GDM-1 M3zxO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXhTIVKSzVyPUKxMlk1OTRizszN M1;kV3NCVkeHUh?=
KMS-12-PE MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7NU|FKSzVyPUKyMlI4PCEQvF2= NEXHPIhUSU6JRWK=
NCI-H510A MlTxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlq4TWM2OD1{ND6xNlc5KM7:TR?= MXPTRW5ITVJ?
ES5 NIXBfIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTJ2LkezOFkh|ryP M3nRfnNCVkeHUh?=
JiyoyeP-2003 NWTneXNMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\hcnJKSzVyPUK2MlI4PDJizszN NFTHU2NUSU6JRWK=
NMC-G1 NVTv[3hCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\Ie49KSzVyPUK3MlE5OjJizszN NE\4Z5NUSU6JRWK=
NCI-H446 M4jtfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDRR2tKSzVyPUK3MlQ6PDZizszN M1Gz[3NCVkeHUh?=
NB7 MoLmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{Xw[GlEPTB;MkeuPVIzQSEQvF2= NH7KUoZUSU6JRWK=
A388 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHsN2E5UUN3ME2yPE4xODd2IN88US=> M4nO[3NCVkeHUh?=
JVM-2 M2Pnd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fM[2lEPTB;MkiuNlg6QCEQvF2= MXzTRW5ITVJ?
HT-144 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnLZ3pKSzVyPUK4MlY6KM7:TR?= Mn;rV2FPT0WU
NCI-H747 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTJ6LkmxPVUh|ryP NIqyT5RUSU6JRWK=
NCI-H1650 NFfxNZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGn0S21KSzVyPUK5MlAyPzZizszN MYTTRW5ITVJ?
EB-3 MmDDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnyyTWM2OD1{OT61N|A6KM7:TR?= MWnTRW5ITVJ?
KLE NGfFUldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWH6PI17UUN3ME2yPU43OTlizszN MkDBV2FPT0WU
TK10 NXTNbVlGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHW2XpRKSzVyPUOwMlEzPiEQvF2= Ml7xV2FPT0WU
COLO-668 NWHybIFCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvjNI1{UUN3ME2zNE44QTJizszN MlfSV2FPT0WU
NCI-H23 Mke3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTNzLkGwOlMh|ryP NI\6emJUSU6JRWK=
GOTO MnTiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTNzLk[wPFUh|ryP NF6zcFlUSU6JRWK=
MSTO-211H NFPyVHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvpUYN1UUN3ME2zNU45Pjd6IN88US=> NXfzN4M3W0GQR1XS
LB831-BLC MlvxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVixRppMUUN3ME2zNk4{QDR|IN88US=> NGrKZ|BUSU6JRWK=
SCH NUfIb4tHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{O5[2lEPTB;M{KuPFQ5PSEQvF2= NGPERmJUSU6JRWK=
EHEB Mk\QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfwVm9RUUN3ME2zOE4yOTl|IN88US=> NGL5dnhUSU6JRWK=
U-266 NIjJR5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDVTWM2OD1|ND6yO|gyKM7:TR?= MnzaV2FPT0WU
EW-11 NUG5O4R4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkWwTWM2OD1|ND60O|I2KM7:TR?= MmTnV2FPT0WU
TE-9 NVrVVVVzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLFSY5KSzVyPUO3MlA1ODFizszN NEPvUYtUSU6JRWK=
ES3 NVXCcWRuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn76TWM2OD1|Nz61NFA1KM7:TR?= NGrOXJdUSU6JRWK=
NCI-H2141 M1XGUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3PVJdKSzVyPUO4MlA5PDNizszN NFLJbYZUSU6JRWK=
MPP-89 M4jjVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXoTWM2OD12Mj6wOVg3KM7:TR?= M{XrS3NCVkeHUh?=
SK-MEL-2 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1P2ZmlEPTB;NEKuOlQxPSEQvF2= MoTKV2FPT0WU
LC-1F NHPBWo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTR|LkO2PFIh|ryP NEH0e4VUSU6JRWK=
NH-12 MoH5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTR|LkmzOVkh|ryP Moi2V2FPT0WU
RKO NH3ZVlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\zVotDUUN3ME20OE4yOjV{IN88US=> NGHhfVNUSU6JRWK=
KM-H2 NV\6ZXdTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHnXdHNKSzVyPUS0Mlk2PzdizszN NIHTRm9USU6JRWK=
SK-UT-1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2q0WWlEPTB;NEmuPFgzPSEQvF2= M1KzcnNCVkeHUh?=

... Click to View More Cell Line Experimental Data

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]
+ Expand

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]
+ Expand
  • 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]
+ Expand
  • 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
  • Formulation: Formulated as a carboxymethyl cellulose suspension or as a citrate buffered (pH 3.5) solution
  • 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

Bio Calculators

Molarity Calculator

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

Mass (g) = Concentration (mol/L) × Volume (L) × 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).

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Dilution Calculator

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

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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03463460 Suspended Thymic Carcinoma Dwight Owen|National Cancer Institute (NCI)|Ohio State University Comprehensive Cancer Center June 19 2018 Phase 2
NCT03463460 Suspended Thymic Carcinoma Dwight Owen|National Cancer Institute (NCI)|Ohio State University Comprehensive Cancer Center June 19 2018 Phase 2
NCT02761057 Recruiting Stage III Renal Cell Cancer AJCC v7|Stage IV Renal Cell Cancer AJCC v7|Type 1 Papillary Renal Cell Carcinoma|Type 2 Papillary Renal Cell Carcinoma|Unresectable Renal Cell Carcinoma National Cancer Institute (NCI)|Canadian Cancer Trials Group April 5 2016 Phase 2
NCT02761057 Recruiting Stage III Renal Cell Cancer AJCC v7|Stage IV Renal Cell Cancer AJCC v7|Type 1 Papillary Renal Cell Carcinoma|Type 2 Papillary Renal Cell Carcinoma|Unresectable Renal Cell Carcinoma National Cancer Institute (NCI)|Canadian Cancer Trials Group April 5 2016 Phase 2
NCT02779283 Recruiting Acute Lymphoblastic Leukemia|Acute Myeloid Leukemia OHSU Knight Cancer Institute|National Cancer Institute (NCI) January 13 2016 Phase 1
NCT02779283 Recruiting Acute Lymphoblastic Leukemia|Acute Myeloid Leukemia OHSU Knight Cancer Institute|National Cancer Institute (NCI) January 13 2016 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