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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In DMSO USD 191 In stock
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USD 147 In stock
USD 447 In stock
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Cited by 42 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 MoOwT4lv[XOnIFHzd4F6 NYnMXWE1UW6qaXLpeIlwdiCxZjDQSGdHNWmwZIXj[YQhSnKmVTDpcoNwenCxcnH0bY9vKHerdHigTWM2OCCxZjCwMlAxPyEQvF2= MVyxNlY1PjBzOR?=
3T3 NVXzNG9tT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFn2WYFKdmirYnn0bY9vKG:oIGDsZZRmdGW2LXTldol3\WRiZ4Lve5RpKG[jY4TvdkBqdmS3Y3XkJFNVOyClZXzsJJBzd2yrZnXyZZRqd25id3n0bEBKSzVyIH;mJFAvODFizszN MlvLNVI3PDZyMUm=
3T3 Mn[zSpVv[3Srb36gRZN{[Xl? NV;k[2xJUW6qaXLpeIlwdiCxZjDWZZNkfWyjcjDlcoRwfGinbHnhcEBoem:5dHig[oFkfG:{IILlZ4VxfG:{IIfpeIghUUN3MDDv[kAxNjB3IN88US=> M1fUZVEzPjR4MEG5
3T3 MnLQT4lv[XOnIFHzd4F6 M1vGUVIxKG2rbh?= NYDnS4N6TE2VTx?= MXjD[YxtfWyjcjDpcohq[mm2aX;uJI9nKF[HR1[gbY5lfWOnZDDoeY1idiCNRGKgdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAxNjB{MjFOwG0> MnrFNVYyPjJyMEi=
NIH3T3 NWnKZZVjU2mwYYPlJGF{e2G7 NETKdWMzOCCvaX6= NYThc5p1TE2VTx?= MXfpcohq[mm2IHj1cYFvKEuGUjDrbY5ie2ViZYjwdoV{e2WmIIfpeIghUUN3MDDv[kAxNjBzODFOwG0> MkLuNVYyPjJyMEi=
A549 NY\uNVNiTnWwY4Tpc44hSXO|YYm= M2fJb2ROW09? NHHDWYZKdmirYnn0bY9vKG:oIHOtUYV1KGSncHXu[IVvfCCKR1[tbY5lfWOnZDDoeY1idiCDNUS5JINmdGxibXnndoF1cW:wIIfpeIghUUN3MDDv[kAzKM7:TR?= MVKxPFQ{PDF2NR?=
DU145 M{XqTmZ2dmO2aX;uJGF{e2G7 MWTEUXNQ MlnnTY5pcWKrdHnvckBw\iClLV3leEBl\XCnbnTlcpQhUEeILXnu[JVk\WRiaIXtZY4hTFVzNEWgZ4VtdCC|Y3H0eIVzcW6pIIfpeIghUUN3MDDv[kAyOCEQvF2= NYXvUoNGOTh2M{SxOFU>
KB3-1 Mm\PR5l1d3SxeHnjJGF{e2G7 MXW3NkBp MoP1SG1UVw>? NWf0eHQ3S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWC2pcD3u[YdifGm4ZTDLRk0{NTFiY3XscJMhf2m2aDDJR|UxKG:oIEKuN{DPxE1? MoHNNVk{QTd|MkK=
KBV1 M4TlfGN6fG:2b4jpZ{BCe3OjeR?= NYjhe3FRPzJiaB?= NV\RfY1lTE2VTx?= MWrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQMYdtgWOxcILveIVqdi2neIDy[ZN{cW6pIFvCWlEh[2WubIOge4l1cCCLQ{WwJI9nKDRwMTFOwG0> NYDBfW9xOTl|OUezNlI>
A375 MkGyR5l1d3SxeHnjJGF{e2G7 NEPucFc4OiCq NYTOPYNwTE2VTx?= NWP5eWZLUUN3ME21MlQh|ryP M1HBNFE6PjV2NEC4
RS4-11 Mk\6SpVv[3Srb36gRZN{[Xl? NXXa[ZZZOiCq NIPHVpBKdmirYnn0bY9vKG:oIF\MWFMh[XW2b4Doc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gNE4xODl7IN88US=> MmHNNVk3PTR2MEi=
RS4-11 NVXLdodkTnWwY4Tpc44hSXO|YYm= M165[VIhcA>? MXfJcohq[mm2aX;uJI9nKE[OVEOgTXRFKG23dHHueEBifXSxcHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCwMlA{PCEQvF2= NUn6[3EzOTl4NUS0NFg>
Sf9 MnfRT4lv[XOnIFHzd4F6 Mn76N|AhdWmw NWrQd3RxUW6qaXLpeIlwdiCxZjDHV3QufGGpZ3XkJHZGT0[UIHX4dJJme3OnZDD3bZRpKEmFNUCgc4YhOC5zOEWg{txO NED4OoEyQTh3NEC1NS=>
Ba/F3 Mn\JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\4cJE4OiCq NV\5U3IyUUN3ME2xMlIh|ryP MWGyNFEyPzByNB?=
BaPTC2 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\IO|IhcA>? NX7PV4JYUUN3ME2wMlIzKM7:TR?= MmHsNlAyOTdyMES=
Sf9 MojsSpVv[3Srb36gRZN{[Xl? MkjpNUBp M4\md2ROW09? M4rLZmlvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiSHnzMZRi\2enZDDSSXQh\XiycnXzd4VlKHerdHigTWM2OCCxZjCxMlMh|ryP M3fVVFIxOTF5MEC0
H4 MmXLR5l1d3SxeHnjJGF{e2G7 MVSxNEDPxE1? M{\0[HRwgGmlaYT5JIlvKGi3bXHuJGg1KGOnbHzz M4TrR|IxOzVyOEC2
SF-539 NF;CS4hMcW6jc3WgRZN{[Xl? NIDXSFI{OzNizszN MUm2NEBucW5? MoriSG1UVw>? MkHPTY5pcWKrdHnvckBw\iCSRFfGVoJmfGFicHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCxNk4zKM7:TR?= NV3K[2R6OjB2MEO3NFA>
U251 NFHyc3BMcW6jc3WgRZN{[Xl? MWWzN|Mh|ryP NESwXHg3OCCvaX6= NYrzPG41TE2VTx?= MV;Jcohq[mm2aX;uJI9nKF[HR1\SNkBxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDF6Lkmg{txO MVOyNFQxOzdyMB?=
A431 MXXLbY5ie2ViQYPzZZk> M13GRmlvcGmkaYTpc44hd2ZiUFTHSnJj\XSjIHX4dJJme3OnZDD3bZRpKEmFNUCgc4YhOTJwMjFOwG0> NWrrNHB4OjB3NUiwO|I>
A431 MXfLbY5ie2ViQYPzZZk> NGrPb4dKdmirYnn0bY9vKG:oIG\FS2ZTOiCneIDy[ZN{\WRid3n0bEBKSzVyIH;mJFE5NjlizszN NEnLcoozODV3OEC3Ni=>
HepG2 MnfLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHXO|IhcA>? M3G5d2lEPTB;Mz64NUDPxE1? NH\i[W8zODV5MEWyOi=>
Kasumi-1 NXjmepJ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXi3NkBp M1fUbGlEPTB;MD6wNVYh|ryP M4fwNlIxPTdyNUK2
RS4-11 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\EfJBKPzJiaB?= NFWzbphKSzVyPUGg{txO MYCyNFU4ODV{Nh?=
THP1 NH[yTHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnKeYY4OiCq MnLuTWM2OD1yLkWg{txO NF;DRYgzODV5MEWyOi=>
Kasumi-1 NY\CbmJjTnWwY4Tpc44hSXO|YYm= M4\XTmlvcGmkaYTpc44hd2ZiYz3LbZQh[XW2b4Doc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gNE4xOTVizszN Mo\XNlA5OzNyM{m=
A549 Mn3US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHK3WVAyPiCq NGDxZlNCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzz MUmyNVQ2ODR4Mx?=
HL60 NIKwPIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjURndKOTZiaB?= NY[1ToF6SW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gTGw3OCClZXzsdy=> MX2yNVQ2ODR4Mx?=
HUVEC NUPUSItTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojWNVYhcA>? MYnJcohq[mm2aX;uJI9nKF[HR1[tbY5lfWOnZDDj[YxtKHC{b3zp[oVz[XSrb36ge4l1cCCLQ{WwJI9nKDJwN{Wg{txO NUT2VW5QOjF2NUC0OlM>
HUVEC MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3f3SFE3KGh? Mn72TY5pcWKrdHnvckBw\iCkRlfGMYlv\HWlZXSgZ4VtdCCycn;sbYZmemG2aX;uJJdqfGhiSVO1NEBw\iB2LkC0JO69VQ>? NFjsZYEzOTR3MES2Ny=>
IM9 NWX6cI5VT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWqxOkBp M3e1TGFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFnNPUBk\Wyucx?= MYCyNVQ2ODR4Mx?=
K562 MnS5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUWxOkBp NEDaVZRCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzz M2X2W|IyPDVyNE[z
MDA-MB-231 M2HGdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGexdnoyPiCq M4jlRWFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHN? MmjTNlE1PTB2NkO=
H460 NFO3U|REgXSxdH;4bYMhSXO|YYm= MXi3NkBp M3Hzc2lEPTB;Mj63JO69VQ>? NVjzeIZwOjF4MkG4PFA>
SMMC7721 MYjDfZRwfG:6aXOgRZN{[Xl? Mme0O|IhcA>? M17PSGlEPTB;Nj60O{DPxE1? MkPyNlE3OjF6OEC=
WI38 MlO2R5l1d3SxeHnjJGF{e2G7 NWf3WGhxPzJiaB?= NXTTOG5GUUN3ME24MlU3KM7:TR?= MV6yNVYzOTh6MB?=
HEK293 NXrIPJh5U2mwYYPlJGF{e2G7 NELq[WIyODBibl2= NVjBWZpvOSCq NVT5UlJM\G:nczDuc5QhcW6qaXLpeEBXTUeILXnu[JVk\WRiYYX0c5Bpd3OyaH;yfYxifGmxbjDv[kB1gXKxc3nu[UAyOTd3IILld4llfWVib36gWmVITlJ{IHX4dJJme3OnZDDpckBJTUt{OUOgZ4VtdHN? MV[yNVg5PTJ6Nx?=
HUVEC NXK5ZlE6TnWwY4Tpc44hSXO|YYm= Mm\PNUDPxE1? NGHLdVAzPCCq NG\ic3dCdnSrYX7nbY9o\W6rYzDhZ5Rqfmm2eTDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCYRVfGMYlv\HWlZXSgZ4VtdCCvaXfyZZRqd25? Mof0NlE6PjN|MEW=
HUVEC NUixTWt[TnWwY4Tpc44hSXO|YYm= NUDqbXBMOSEQvF2= NVjlVpJDOSCq NHrxUG1KdmirYnn0bY9vKG:oIFXST{BxcG:|cHjvdplt[XSrb36gZZQhXGi{MkCyM3R6ejJyNDDpckBXTUeILYP0bY12dGG2ZXSgTHVXTUN? M3jqVFIyQTZ|M{C1
HUVEC NXnMR3kxTnWwY4Tpc44hSXO|YYm= NUDPWIhlOSEQvF2= M1fqelEhcA>? M1rOTGlvcGmkaYTpc44hd2ZiZV7PV{BxcG:|cHjvdplt[XSrb36gZZQhW2W{LUGxO|IhcW5iVlXHSk1{fGmvdXzheIVlKEiXVlXD MojyNlE6PjN|MEW=
HUVEC NX3xR4tjU2mwYYPlJGF{e2G7 NYWxW|MyOSEQvF2= MmLKNUBp MmG5TY5pcWKrdHnvckBw\iCYRVfGVlIheGixc4Doc5J6dGG2aX;uJIF1KHS7cj2xNVc2KGmwIG\FS2Yue3SrbYXsZZRm\CCKVW\FRy=> MVOyNVk3OzNyNR?=
HUVEC NHXyZVJHfW6ldHnvckBCe3OjeR?= NFrUUlUyKM7:TR?= NVTZR2dFOSCq M4LwU4Rw\XNibn;0JIlvcGmkaYSgRWtVKHCqb4PwbI9zgWyjdHnvckBifCCVZYKtOFc{KGmwIG\FS2Yue3SrbYXsZZRm\CCKVW\FRy=> M2PsSVIyQTZ|M{C1
HL60 NInEXHNEgXSxdH;4bYMhSXO|YYm= NH3OdnI2OCEQvF2= NELO[Vg1QCCq M{LJe2ROW09? MYHJR|UxRTF3LkWg{txO M3PLSFIzODF7MUi4
K562 MVHDfZRwfG:6aXOgRZN{[Xl? Moe0OVAh|ryP NGXzWmY1QCCq MUDEUXNQ M2LkS2lEPTB;MkGuPUDPxE1? MlPyNlIxOTlzOEi=
PC3 NXLUVlBES3m2b4TvfIlkKEG|c3H5 M{fXN|UxKM7:TR?= M4TrRVQ5KGh? M{PhbGROW09? M2TlWWlEPTB;MkWuNUDPxE1? NXLDeFJYOjJyMUmxPFg>
SF-539 M2[3c2tqdmG|ZTDBd5NigQ>? MV2zN|Mh|ryP NFfRc4o3OCCvaX6= NGD3cW9KdmirYnn0bY9vKG:oIGDES2ZT[mW2YTD0fZJwe2mwZTDrbY5ie2ViYXP0bZZqfHliaX6gVGRITi2EQj3zeIlufWyjdHXkJIh2dWGwIGPGMVU{QSClZXzsd{B4cXSqIFnDOVAhd2ZiMUKuNkDPxE1? MoD1NlIzODR5NEG=
HAEC NHvkNFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXuxNFAh|ryP MnX3O|IhcA>? NFvzXoJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjBSWMh[2WubIOg[ZhxemW|c3nu[{BXTUeIUjD3bZRpKEmFNUCgc4YhOC5zIN88US=> NWLWfFB3OjJ2NES2O|k>
HT-29 MkP6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHZNVAxKM7:TR?= NXzpS2RuPzJiaB?= MYPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiWLUK5JINmdGy|IHX4dJJme3OrbnegWmVITlJid3n0bEBKSzVyIH;mJFAvOzNizszN NFLOOHYzOjR2NE[3PS=>
MV4-11 NGHjV2tEgXSxdH;4bYMhSXO|YYm= NHPXS|A4OiCq MXPJR|UxRTBwMECzJO69VQ>? MmDZNlI1PTJ3MUi=
HepG2 M4DlOmN6fG:2b4jpZ{BCe3OjeR?= NVq3S5FvPDhiaB?= NGTjOXpKSzVyPUGzMlI1KM7:TR?= NGTI[owzOjR6M{[wPC=>
PC9 MnTyR5l1d3SxeHnjJGF{e2G7 M{DRPFQ5KGh? M2rxd2lEPTB;MUCuPVch|ryP NGj3U3YzOjR6M{[wPC=>
CAKI-1 NWfzVWRUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPaTll1OTByIN88US=> MkDCOFghcA>? MkjoSG1UVw>? M2\DNWdKPTB;MD62N{DPxE1? NWroTWlTOjJ3NkC2Nlc>
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MDA-MB-435 M4jUPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHMOWMyODBizszN M4L6XVQ5KGh? MXjEUXNQ MYXHTVUzRTJizszN M3[z[FIzPTZyNkK3
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TK10 M1PRUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXEO49QOTByIN88US=> MWW0PEBp M{HKcmROW09? Ml3ZS2k2Pj14LkOg{txO M{nsXVIzPTZyNkK3
UACC257 NHHX[ZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXqxNFAh|ryP NEDMc3c1QCCq MkL0SG1UVw>? NUK0b3ZwT0l3N{20JO69VQ>? M3\mT|IzPTZyNkK3
HAEC NF3pVIFEgXSxdH;4bYMhSXO|YYm= NIPVTpMyODBizszN NFS0O|g4OiCq MV;EUXNQ NWLkSFZqS3m2b4TvfIlkcXS7IHHnZYlve3RiVlXHSnIh\XiycnXzd4lv\yCKQVXDJJdqfGhiSVO1NEBw\iByLkGg{txO M4PBO|I{OTNzNUSx
HT-29 MknwR5l1d3SxeHnjJGF{e2G7 MXixNFAh|ryP MUS3NkBp NXz3flZITE2VTx?= NHTsZ29EgXSxdH;4bYNqfHliYXfhbY5{fCCYRVfGVkBmgHC{ZYPzbY5oKGi3bXHuJGhVNTJ7IHPlcIx{KHerdHigTWM2OCCxZjCwMlM{KM7:TR?= M3fvRVI{OTNzNUSx
HCT116 M1PXdmZ2dmO2aX;uJGF{e2G7 NIXwOYgzPCCq M1rRd2ROW09? MYrBcpRqdWmpcnH0c5J6KGGldHn2bZR6KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh[2WubDDtbYdz[XSrb36= NGH6fVczOzF3M{KwNC=>
HUVEC NVj6T4o6TnWwY4Tpc44hSXO|YYm= MoHZNkDPxE1? MXuxPEBp NFvwOG5FVVOR MnzNRY51cWGwZ3nv[4VvcWNiYXP0bZZqfHliaX6gTHVXTUO|IIXu[IVzKGi7cH;4bYMh[2:wZHn0bY9vKGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhfHWkZTDmc5Ju[XSrb36= MVGyN|E2OzJyMB?=
ACHN MlfJR5l1d3SxeHnjJGF{e2G7 NUS4NolFPiCm NV3Xcpp3UUN3ME2yMlUh|ryP Ml\QNlM{PjBzMES=
A498 MUPDfZRwfG:6aXOgRZN{[Xl? M{i4WFExOCEQvF2= MWK3NkBp NXvu[GsyTE2VTx?= MUHJR|UxRTRwMzFOwG0> M3W4clI{PDh7NkK2
HUVEC MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlP4N{DPxE1? NUn0VZBvOjRiaB?= NV7LNJlSTE2VTx?= MmnvRY51cWGwZ3nv[4VvcWNiYXP0bZZqfHliYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCYRVfGMYlv\HWlZXSgeJVj\SCob4LtZZRqd25id3n0bEBGSzVyIH;mJFAvPjR3IN88US=> MWGyN|U5OzlzMR?=
HUVEC NWTHXZNrU2mwYYPlJGF{e2G7 MnroNlAxKM7:TR?= M4rucGROW09? MVLJcohq[mm2aX;uJI9nKF[HR1\SNkBxcG:|cHjvdplt[XSrb36gbY4h\3Kxd4ToJIZi[3Sxcj3zeIlufWyjdHXkJGhWXkWF NFKwR44zOzV6M{mxNS=>
HUVEC MVTLbY5ie2ViQYPzZZk> MmrLNlAxKM7:TR?= MlT2SG1UVw>? NInFdHVKdmirYnn0bY9vKG:oIG\FS2ZTOSCyaH;zdIhwenmuYYTpc44hcW5iZ4Lve5RpKG[jY4Tvdk1{fGmvdXzheIVlKEiXVlXD NXXPRXo5OjN3OEO5NVE>
A549 NVzQR|lYS3m2b4TvfIlkKEG|c3H5 NELVPWo4OiCq NVWwbJN4TE2VTx?= NI\JU4VKSzVyPUKuOFQh|ryP M4PCdVI{PjB{NESx
HCT116 MnrSR5l1d3SxeHnjJGF{e2G7 Mo\EO|IhcA>? NIrPSnhFVVOR MVLJR|UxRTRwN{Gg{txO MV2yN|YxOjR2MR?=
MCF7 NYizcZRwS3m2b4TvfIlkKEG|c3H5 MXm3NkBp NYj1RnE4TE2VTx?= M2TtR2lEPTB;Nj6yPUDPxE1? M{nrTVI{PjB{NESx
BGC Mn7vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEH3XVk4OiCq NUPpSmNCTE2VTx?= NVu3c5RxUUN3ME20Mlc5KM7:TR?= M{PkZlI{QTl7MESw
BxPC3 M{nIZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvzNIh[PzJiaB?= NUT4O3lRTE2VTx?= M4j0OGlEPTB;Mz62N{DPxE1? NGTp[o8zOzl7OUC0NC=>
HT-29 M{jUcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWW3NkBp M4HFSmROW09? NE\iNm1KSzVyPUGuOFch|ryP NWLlVFJmOjN7OUmwOFA>
T24 NFnYfmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;qWGE4OiCq MUjEUXNQ M13YSGlEPTB;Mj60OEDPxE1? MlzhNlM6QTlyNEC=
4T1 MWfDfZRwfG:6aXOgRZN{[Xl? M2\OWVczKGh? M4rNTmROW09? MYnJR|UxRTBwMEG2JO69VQ>? MlT1NlQ5QTB4NUK=
MCF7 MmPPR5l1d3SxeHnjJGF{e2G7 NX3XPFFGPzJiaB?= MnXOSG1UVw>? MYnJR|UxRTBwMEK3NUDPxE1? MkHlNlQ5QTB4NUK=
MCF7 MWjDfZRwfG:6aXOgRZN{[Xl? MUC3NkBp MXTEUXNQ MV;JR|UxRTBwMEK5N{DPxE1? MYCyOFg6ODZ3Mh?=
MDA-MB-231 NEKzSFVEgXSxdH;4bYMhSXO|YYm= MXG3NkBp NGHVZWNFVVOR MVjJR|UxRTBwMEKyN{DPxE1? NFTTdoczPDh7ME[1Ni=>
MDA-MB-435 MoixR5l1d3SxeHnjJGF{e2G7 NIrLbXY4OiCq NWm2RmZPTE2VTx?= MXXJR|UxRTBwMEC5O{DPxE1? MYqyOFg6ODZ3Mh?=
MDA-MB-468 M1\5[mN6fG:2b4jpZ{BCe3OjeR?= NHf2c5k4OiCq NFHZNVBFVVOR M{PtSmlEPTB;MD6wNFYyKM7:TR?= M3fTU|I1QDlyNkWy
A431 NV3wWGpJU2mwYYPlJGF{e2G7 NULrO5dZOTBizszN NY\neG1{OSCq MofJSG1UVw>? M1rSdWlvcGmkaYTpc44hd2ZiRVfGVkB4cXSqIFnDOVAhd2ZiMD6xO|IyKM7:TR?= NIS0cIMzPDh7ME[1Ni=>
SH-SY5Y MoKwT4lv[XOnIFHzd4F6 NX6yUm92OTBizszN NX7tT4lWOSCq M3qyb2ROW09? MnXlTY5pcWKrdHnvckBw\iCSRFfGVoJmfGFid3n0bEBKSzVyIH;mJFAvODh|MTFOwG0> MX:yOFg6ODZ3Mh?=
U251 MUDLbY5ie2ViQYPzZZk> M17RNlExKM7:TR?= NX\Ud4MyOSCq NYLUSYJTTE2VTx?= MoP1TY5pcWKrdHnvckBw\iCYRVfGVlIhf2m2aDDJR|UxKG:oIECuNFE5QSEQvF2= MUOyOFg6ODZ3Mh?=
Bel7402 MkPYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nHS|czKGh? MkT0SG1UVw>? NVf2e20zUUN3ME2yMlY4KM7:TR?= MUKyOFkxPDl4MR?=
HK2 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILNVZA4OiCq MUnEUXNQ M33XTWlEPTB;NT64OUDPxE1? MnLJNlQ6ODR7NkG=
LO2 NILr[Y5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVO3NkBp NVTVO2ZCTE2VTx?= NGP5d5RKSzVyPUG5Mlk{KM7:TR?= MVGyOFkxPDl4MR?=
MV4-11 MlzkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jzZlQ5KGh? MXTEUXNQ NWPpRZBKUUN3ME2wMlAxOyEQvF2= MWiyOFkxPDl4MR?=
NCI-H3122 MoTtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjVO41NPzJiaB?= NWTMcWN5TE2VTx?= MYTJR|UxRTBwOEOg{txO NIXxWWUzPDlyNEm2NS=>
NCI-H460 NUjufVJnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HKe|czKGh? NXr4OphDTE2VTx?= NYPsTpJrUUN3ME20MlMyKM7:TR?= NEnPPHAzPDlyNEm2NS=>
NCI-H526 M33CXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWi3NkBp M33INWROW09? NHK5c4VKSzVyPUGuNFEh|ryP NHfmTogzPDlyNEm2NS=>
TT NGHk[nhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjzUFByPzJiaB?= MV3EUXNQ Ml74TWM2OD1yLkC0JO69VQ>? NFzKU5gzPDlyNEm2NS=>
EoL-1-cell NUPXcXI4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV23[oN4UUN3ME2xMlY1KHCP NEDSZY5USU6JRWK=
MV-4-11 M4\uUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfVTWM2OD1{N{KgdG0> MWPTRW5ITVJ?
NOS-1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rhbmlEPTB;MUWuN{BvVQ>? NW\XfWhyW0GQR1XS
CGTH-W-1 NYj3TY9jT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTNyLkm0JI5O NX7uU4prW0GQR1XS
MONO-MAC-6 MoexS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLxcYtEUUN3ME2zN{45KG6P MWPTRW5ITVJ?
ALL-PO MnXWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTd7Lki5JI5O Ml:3V2FPT0WU
NKM-1 NHPa[25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnpdVBKSzVyPUm4MlUzKG6P NU[1RmVoW0GQR1XS
KM12 NGLwU5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHNTWM2OD1|NUCuNVQhdk1? M{jXcnNCVkeHUh?=
TE-15 NGDQW5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYH6NpZMUUN3ME21NFcvPjFibl2= MV3TRW5ITVJ?
697 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUjJR|UxRTZzND6yOUBvVQ>? MYXTRW5ITVJ?
MOLT-16 MnHQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHK2fGZKSzVyPU[zNU4{OiCwTR?= M3vidnNCVkeHUh?=
GB-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17LdWlEPTB;N{GwMlI{KG6P MmXpV2FPT0WU
TE-12 MlPES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPCeYF5UUN3ME24NFQvPTVibl2= NEnNR2dUSU6JRWK=
ES6 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX[4OIVmUUN3ME25PFEvODZibl2= NVnQUo5PW0GQR1XS
LC-2-ad MoruS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3THSmlEPTB;MT6xNVQxPyEQvF2= NEezbHdUSU6JRWK=
BL-70 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTrTWM2OD1zLkGxPFQ3KM7:TR?= MUHTRW5ITVJ?
ETK-1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\Yd2xnUUN3ME2xMlI5PThizszN M2\4OXNCVkeHUh?=
A4-Fuk NWexd5hLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTFwM{SxOFEh|ryP NVfDdFh1W0GQR1XS
OCI-AML2 MnLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HxNmlEPTB;MT6zOlg2OSEQvF2= NWj4RZBmW0GQR1XS
SIG-M5 NYO5O5R[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTFwM{ewNFkh|ryP MoTOV2FPT0WU
NCI-SNU-16 NIfV[mpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF2zd4VKSzVyPUGuOFY1QDZizszN NW\GdVJKW0GQR1XS
PSN1 MnvWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnITWM2OD1zLkWwOlc3KM7:TR?= M371XHNCVkeHUh?=
SR MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TSTGlEPTB;MT61OFU4OiEQvF2= NXTZ[VFJW0GQR1XS
A3-KAW M334U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnCTWM2OD1zLk[yOVQ3KM7:TR?= MVzTRW5ITVJ?
KS-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;XTWM2OD1zLk[5NlQ4KM7:TR?= NIPsTndUSU6JRWK=
CTV-1 M1HsSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPxc5dKSzVyPUGuO|I4PTFizszN M{jI[XNCVkeHUh?=
LB1047-RCC NGDDZWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTFwOEG2NlQh|ryP MXLTRW5ITVJ?
EMG-01 NGjZdGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTiTmk4UUN3ME2xMlg{PTZ|IN88US=> MYDTRW5ITVJ?
TE-11 M2rKcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTFwOEO5PFUh|ryP NYfzOXRyW0GQR1XS
CMK NEfxdI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTFwOUW1NVch|ryP NFLyeGZUSU6JRWK=
NB1 NGO3ZpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;3b2lEPTB;MT65OlEyPyEQvF2= MWTTRW5ITVJ?
HAL-01 NVK0OoNGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PQR2lEPTB;Mj6wOVk1PiEQvF2= M{TyXnNCVkeHUh?=
DEL MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfLWZIxUUN3ME2yMlA5PDh{IN88US=> NV:x[IxCW0GQR1XS
RL95-2 M{fucWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTJwMUGxN|ch|ryP NIHuO4VUSU6JRWK=
KARPAS-299 M3nsemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjxSXdKSzVyPUKuNVE{OTNizszN M{nZb3NCVkeHUh?=
EW-16 M2\3S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\i[WlEPTB;Mj6xN|UxQCEQvF2= M1jBfXNCVkeHUh?=
RS4-11 M4LSdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{GzdWlEPTB;Mj6xO|kzPCEQvF2= Mn;JV2FPT0WU
BB30-HNC MnvzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTJwMkKzO|Uh|ryP M{LWUXNCVkeHUh?=
DOHH-2 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHzTWM2OD1{LkOzOFMyKM7:TR?= MlHmV2FPT0WU
RPMI-8402 MnTkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnYXIU1UUN3ME2yMlM{PjF6IN88US=> NV7jSpVuW0GQR1XS
BV-173 MoHjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zBcmlEPTB;Mj6zN|Y3KM7:TR?= NX;BOVVsW0GQR1XS
TE-10 MkPLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXrTWM2OD1{LkO0N|g1KM7:TR?= M2nufHNCVkeHUh?=
TE-8 NXHSPVFIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LybGlEPTB;Mj6zO|A{QCEQvF2= NUHNNYFZW0GQR1XS
K052 NFn6TnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXu1dYMzUUN3ME2yMlQxOjB{IN88US=> NV2wSXF1W0GQR1XS
KARPAS-45 NGP4cWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHZTWM2OD1{LkS5OFQ3KM7:TR?= M{\rSHNCVkeHUh?=
SK-NEP-1 M4XPNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rRUGlEPTB;Mj62NFI{PyEQvF2= NIfXRmpUSU6JRWK=
KGN Mk\NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHlTlVDUUN3ME2yMlYxOzN7IN88US=> MlP6V2FPT0WU
ML-2 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzmd3JKSzVyPUKuOlM2OTJizszN NIfCelhUSU6JRWK=
LAMA-84 MnjsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnm4TWM2OD1{Lk[5OVQ2KM7:TR?= MkfLV2FPT0WU
LXF-289 NYTmRWFoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTJwN{K5PFkh|ryP MVLTRW5ITVJ?
A101D NVPnSXRUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUmyNFZIUUN3ME2yMlc5OzB2IN88US=> M2XFPHNCVkeHUh?=
KY821 NH;SRlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrZTWM2OD1{Lke5O|U5KM7:TR?= MlrrV2FPT0WU
ES4 NFH5d4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7aTWM2OD1{LkiwOlI5KM7:TR?= M3\0ZXNCVkeHUh?=
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NCI-H1304 Ml;FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRThwMkC2OlEh|ryP MknOV2FPT0WU
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NTERA-S-cl-D1 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPuSYRnUUN3ME2xO{45PTd{IN88US=> MWDTRW5ITVJ?
NCI-H1882 M4XzVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTF5Lkm4N|Qh|ryP NYW5VGJjW0GQR1XS
A704 NGDIe|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTF5Lkm5NFQh|ryP MofwV2FPT0WU
L-428 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4jKT2lEPTB;MUiuNFE2OSEQvF2= M1;4W3NCVkeHUh?=
HCC1187 NVzS[mxRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrwTWM2OD1zOD6wNVg4KM7:TR?= MWfTRW5ITVJ?
NCI-H1581 M3zGOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTF6LkC4OlYh|ryP NXLFcG5rW0GQR1XS
BB65-RCC NV;UT2d{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3EUZJKSzVyPUG4MlQyPjJizszN NYnhPFZDW0GQR1XS
EM-2 M{PGTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnL0TWM2OD1zOD61OlczKM7:TR?= MkPlV2FPT0WU
Raji NX\BcJh7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfrclVTUUN3ME2xPU46PTZ3IN88US=> NULCWZpkW0GQR1XS
TE-1 NW\DfY1jT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlr1TWM2OD1{MD60NVA1KM7:TR?= NHHDR5dUSU6JRWK=
SW962 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37tTWlEPTB;MkCuOFI6OyEQvF2= MljnV2FPT0WU
MHH-NB-11 NEnYVJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHaVmtYUUN3ME2yNE42PTJzIN88US=> NHnDV4xUSU6JRWK=
no-10 NX7rWHNmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIC4VlNKSzVyPUKxMlAzPjRizszN MVnTRW5ITVJ?
GDM-1 MlvrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPnTYlKSzVyPUKxMlk1OTRizszN NH\ZZpdUSU6JRWK=
KMS-12-PE NInJU3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYm0RnR2UUN3ME2yNk4zPzRizszN MVzTRW5ITVJ?
NCI-H510A M4WxdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\xNXhNUUN3ME2yOE4yOjd6IN88US=> MWrTRW5ITVJ?
ES5 MmT0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHS4VHRKSzVyPUK0Mlc{PDlizszN MWnTRW5ITVJ?
JiyoyeP-2003 Mmf1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTJ4LkK3OFIh|ryP MmroV2FPT0WU
NMC-G1 Mkf2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVv3eG9jUUN3ME2yO{4yQDJ{IN88US=> MmTSV2FPT0WU
NCI-H446 NGPDVolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTJ5LkS5OFYh|ryP M4rNcXNCVkeHUh?=
NB7 NYGwV5diT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPkfHI6UUN3ME2yO{46OjJ7IN88US=> MoH1V2FPT0WU
A388 NV7BXYMyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlz1TWM2OD1{OD6wNFc1KM7:TR?= NYXZbWdJW0GQR1XS
JVM-2 MmrVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTJ6LkK4PVgh|ryP NXnZSnY5W0GQR1XS
HT-144 M1\l[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mli4TWM2OD1{OD62PUDPxE1? Ml;wV2FPT0WU
NCI-H747 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnTbI5RUUN3ME2yPE46OTl3IN88US=> NGP3UJZUSU6JRWK=
NCI-H1650 NYridXR6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojkTWM2OD1{OT6wNVc3KM7:TR?= NXf3VYJUW0GQR1XS
EB-3 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vuVGlEPTB;MkmuOVMxQSEQvF2= M2\pNnNCVkeHUh?=
KLE NGfHNZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTJ7Lk[xPUDPxE1? MnPKV2FPT0WU
TK10 M37jUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjHXXQ1UUN3ME2zNE4yOjZizszN NHLZc21USU6JRWK=
COLO-668 M{X2R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInLdnVKSzVyPUOwMlc6OiEQvF2= MXzTRW5ITVJ?
NCI-H23 NHPYSXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmexTWM2OD1|MT6xNFY{KM7:TR?= NVXZNYtpW0GQR1XS
GOTO M4\YWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4npZmlEPTB;M{GuOlA5PSEQvF2= Ml\sV2FPT0WU
MSTO-211H MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTNzLki2O|gh|ryP NYq0TIVUW0GQR1XS
LB831-BLC NXzYWo9OT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{[2[GlEPTB;M{KuN|g1OyEQvF2= M{HudnNCVkeHUh?=
SCH MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDNTWM2OD1|Mj64OFg2KM7:TR?= NY\pVI51W0GQR1XS
EHEB NEnmRolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2qzO2lEPTB;M{SuNVE6OyEQvF2= M2HvPXNCVkeHUh?=
U-266 MnvrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfQSmdKSzVyPUO0MlI4QDFizszN NGe2SpBUSU6JRWK=
EW-11 MlTVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXG5Soc6UUN3ME2zOE41PzJ3IN88US=> MYXTRW5ITVJ?
TE-9 MlzqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4n6U2lEPTB;M{euNFQxOSEQvF2= Mnz5V2FPT0WU
ES3 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTN5LkWwNFQh|ryP NHzDXGlUSU6JRWK=
NCI-H2141 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDKbmhuUUN3ME2zPE4xQDR|IN88US=> Moq2V2FPT0WU
MPP-89 NVfN[JM1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXITWM2OD12Mj6wOVg3KM7:TR?= M17EV3NCVkeHUh?=
SK-MEL-2 MnvGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTR{Lk[0NFUh|ryP NIPVcY9USU6JRWK=
LC-1F MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3RTWM2OD12Mz6zOlgzKM7:TR?= M3:yV3NCVkeHUh?=
NH-12 NEDjOGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3VTWM2OD12Mz65N|U6KM7:TR?= MUDTRW5ITVJ?
RKO MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTWTWM2OD12ND6xNlUzKM7:TR?= NH7uRVVUSU6JRWK=
KM-H2 MoLWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTR2Lkm1O|ch|ryP NFrrPGpUSU6JRWK=
SK-UT-1 NIHDUoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfP[4x6UUN3ME20PU45QDJ3IN88US=> NY\6SYRzW0GQR1XS

... 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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01835158 Active not recruiting Clear Cell Renal Cell Carcinoma|Metastatic Renal Cell Cancer|Stage III Renal Cell Cancer AJCC v7|Stage IV Renal Cell Cancer AJCC v7 National Cancer Institute (NCI) July 8 2013 Phase 2
NCT00381641 Active not recruiting Recurrent Thyroid Gland Carcinoma|Stage III Thyroid Gland Follicular Carcinoma AJCC v7|Stage III Thyroid Gland Medullary Carcinoma AJCC v7|Stage IV Thyroid Gland Follicular Carcinoma AJCC v7|Stage IV Thyroid Gland Medullary Carcinoma AJCC v7|Stage IV Thyroid Gland Papillary Carcinoma AJCC v7|Stage IVA Thyroid Gland Follicular Carcinoma AJCC v7|Stage IVA Thyroid Gland Medullary Carcinoma AJCC v7|Stage IVA Thyroid Gland Papillary Carcinoma AJCC v7|Stage IVB Thyroid Gland Follicular Carcinoma AJCC v7|Stage IVB Thyroid Gland Medullary Carcinoma AJCC v7|Stage IVB Thyroid Gland Papillary Carcinoma AJCC v7|Stage IVC Thyroid Gland Follicular Carcinoma AJCC v7|Stage IVC Thyroid Gland Medullary Carcinoma AJCC v7|Stage IVC Thyroid Gland Papillary Carcinoma AJCC v7|Thyroid Gland Oncocytic Follicular Carcinoma|Unresectable Thyroid Gland Carcinoma National Cancer Institute (NCI) August 8 2006 Phase 2
NCT01061411 Completed Clear Cell Sarcoma of the Kidney|Recurrent Renal Cell Carcinoma|Stage III Renal Cell Cancer|Stage IV Renal Cell Cancer Roswell Park Cancer Institute|National Cancer Institute (NCI)|Pfizer February 6 2010 Phase 1
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 National Cancer Institute (NCI) April 5 2016 Phase 2
NCT00478426 Active not recruiting Endometrial Adenocarcinoma|Endometrial Endometrioid Adenocarcinoma|Endometrial Serous Adenocarcinoma|Recurrent Uterine Corpus Carcinoma|Stage IVA Uterine Corpus Cancer AJCC v7|Stage IVB Uterine Corpus Cancer AJCC v7|Uterine Carcinosarcoma|Uterine Corpus Carcinosarcoma National Cancer Institute (NCI) April 30 2007 Phase 2
NCT03249740 Recruiting Neovascular Age-Related Macular Degeneration Graybug Vision August 29 2017 Phase 1|Phase 2

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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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