Sunitinib (SU11248) malate

Licensed by Pfizer 製品コード:S1042

For research use only.

Sunitinib (SU11248) malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit. Sunitinib Malate effectively inhibits autophosphorylation of Ire1α. Sunitinib Malate increases both death receptor and mitochondrial-dependent apoptosis.

Sunitinib (SU11248) malate化学構造

CAS No. 341031-54-7

サイズ 価格(税別)
10mM (1mL in DMSO) JPY 29500
JPY 13000
JPY 17400
JPY 26400
JPY 76200

代表番号: 03-5615-9297|電子メール:[email protected]
よく尋ねられる質問

文献中Selleckの製品使用例(142)

製品安全説明書

PDGFR阻害剤の選択性比較

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生物活性

製品説明 Sunitinib (SU11248) malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit. Sunitinib Malate effectively inhibits autophosphorylation of Ire1α. Sunitinib Malate increases both death receptor and mitochondrial-dependent apoptosis.
ターゲット
IRE1α [7] Kit [1]
(Cell-free assay)
FLT3 [1]
(Cell-free assay)
PDGFRβ [1]
(Cell-free assay)
VEGFR2 [1]
(Cell-free assay)
2 nM 80 nM
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
3T3 MYLLbY5ie2ViQYPzZZk> M1zB[mlvcGmkaYTpc44hd2ZiUFTHSk1qdmS3Y3XkJGJz\FViaX7jc5Jxd3KjdHnvckB4cXSqIFnDOVAhd2ZiMD6wNFch|ryP NUO2fFdORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUK2OFYxOTlpPkGyOlQ3ODF7PD;hQi=>
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3T3 M2C0[2Z2dmO2aX;uJGF{e2G7 NYjLOZJmUW6qaXLpeIlwdiCxZjDWZZNkfWyjcjDlcoRwfGinbHnhcEBoem:5dHig[oFkfG:{IILlZ4VxfG:{IIfpeIghUUN3MDDv[kAxNjB3IN88US=> NXT0RnltRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUK2OFYxOTlpPkGyOlQ3ODF7PD;hQi=>
3T3 M{e1R2tqdmG|ZTDBd5NigQ>? M{naOFIxKG2rbh?= M{nzTmROW09? Mo\jR4VtdHWuYYKgbY5pcWKrdHnvckBw\iCYRVfGJIlv\HWlZXSgbJVu[W5iS1TSJJBpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5yMkKg{txO M{XFelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF4MU[yNFA5Lz5zNkG2NlAxQDxxYU6=
NIH3T3 NVzKRVR7U2mwYYPlJGF{e2G7 NYjieWp[OjBibXnu MVHEUXNQ NFPpbXBqdmirYnn0JIh2dWGwIFvEVkBscW6jc3Wg[ZhxemW|c3XkJJdqfGhiSVO1NEBw\iByLkCxPEDPxE1? NVHIcHJHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[xOlIxODhpPkG2NVYzODB6PD;hQi=>
A549 NXjzSIhuTnWwY4Tpc44hSXO|YYm= NFvWSJRFVVOR M3rzfGlvcGmkaYTpc44hd2ZiYz3N[ZQh\GWyZX7k[Y51KEiJRj3pcoR2[2WmIHj1cYFvKEF3NEmgZ4VtdCCvaXfyZZRqd25id3n0bEBKSzVyIH;mJFIh|ryP MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDR|NEG0OUc,OTh2M{SxOFU9N2F-
DU145 NEfO[ZNHfW6ldHnvckBCe3OjeR?= NECwRVhFVVOR MmrDTY5pcWKrdHnvckBw\iClLV3leEBl\XCnbnTlcpQhUEeILXnu[JVk\WRiaIXtZY4hTFVzNEWgZ4VtdCC|Y3H0eIVzcW6pIIfpeIghUUN3MDDv[kAyOCEQvF2= NHfTbos9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOESzOFE1PSd-MUi0N|QyPDV:L3G+
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HepG2 M4TtNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW[zcZZmPzJiaB?= NX7MS4NEUUN3ME2zMlgyKM7:TR?= MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODV5MEWyOkc,OjB3N{C1NlY9N2F-
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U251 MkjET4lv[XOnIFHzd4F6 NIGxeZQyOCEQvF2= MX6xJIg> Mk\2SG1UVw>? MYPJcohq[mm2aX;uJI9nKF[HR1\SNkB4cXSqIFnDOVAhd2ZiMD6wNVg6KM7:TR?= NULGcG02RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4PVA3PTJpPkK0PFkxPjV{PD;hQi=>
Bel7402 NVHoU3dkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfCO|IhcA>? NHn2[ZBFVVOR MWLJR|UxRTJwNkeg{txO MkLmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MES5OlEoRjJ2OUC0PVYyRC:jPh?=
HK2 NWC2TZByT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;uOWg4OiCq MUfEUXNQ NVL1OIU6UUN3ME21Mlg2KM7:TR?= MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyNEm2NUc,OjR7MES5OlE9N2F-
LO2 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWO3NkBp MofPSG1UVw>? NYfXfnJtUUN3ME2xPU46OyEQvF2= MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyNEm2NUc,OjR7MES5OlE9N2F-
MV4-11 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGK1Z2g1QCCq M1O2ZWROW09? NUHo[md6UUN3ME2wMlAxOyEQvF2= M2XaZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUC0PVYyLz5{NEmwOFk3OTxxYU6=
NCI-H3122 NXP2dGpXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUC3NkBp M{Hu[2ROW09? NGLaOoVKSzVyPUCuPFMh|ryP NV\4dWxVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFQ6PjFpPkK0PVA1QTZzPD;hQi=>
NCI-H460 M2HqR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX23NkBp NVXBeXQ2TE2VTx?= MonvTWM2OD12LkOxJO69VQ>? MlPvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MES5OlEoRjJ2OUC0PVYyRC:jPh?=
NCI-H526 NHjDfHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnBO|IhcA>? M4LqfWROW09? MX;JR|UxRTFwMEGg{txO NFL5O2g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwOFk3OSd-MkS5NFQ6PjF:L3G+
TT NUHaZYxFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUC3NkBp MoLjSG1UVw>? MYrJR|UxRTBwMESg{txO M3n5[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUC0PVYyLz5{NEmwOFk3OTxxYU6=
3T3 MkKyRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M2nkflczKGi{cx?= NIXSN3NCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIEPUN{Bk\WyuczDlfJBz\XO|aX7nJIh2dWGwIFPTSlFTKGGodHXyJFczKGi{czDifUBE\WyudHn0[ZIh[XO|YYmsJGFkfGm4aYT5JF0hOC5yOTFOwG0v M2LtblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6Nkm0OlQyLz5zOE[5OFY1OTxxYU6=
MV4-11 MnftRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NXmwfIZGPzJiaILz MlLVRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPVkStNVEh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IHPlcIwhfGm2ZYKtZox2\SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OCB;IECuNFA1OyEQvF2u NUTYNo9TRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm3OVQyQTlpPkG5O|U1OTl7PD;hQi=>
HEK293 NVXnPIlFTnWwY4Tpc44h[XO|YYm= NIHwO4hDcW6maX7nJIFn\mmwaYT5JJRwKE[OVEOgZ4F1[Wy7dHnjJIRwdWGrbjDlfJBz\XO|ZXSgbY4hUEWNMkmzJINmdGy|IHL5JINwdXCndHn0bZZmKGKrbnTpcoch[XO|YYmsJGtlKD1iMD6wNFA1PyEQvF2u NUG0[oxKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm3OVQyQTlpPkG5O|U1OTl7PD;hQi=>
FDC-P1 MU\GeY5kfGmxbjDhd5NigQ>? MVG0PEBpenN? M3jHbWlvcGmkaYTpc44hd2ZiaIXtZY4hTk2VIHX4dJJme3OnZDDpckBoem:5dHig[oFkfG:{IHTldIVv\GWwdDDtc5V{\SCIRFOtVFEh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDGUXMudWWmaXH0[YQh[2WubDDwdo9tcW[ncnH0bY9vKGmwIIDy[ZNmdmOnIHj1cYFvKEOVRkGgZYZ1\XJiNEigbJJ{KGK7IILld4F7fXKrbjDkfYUhemWmdXP0bY9vKGG|c3H5MEBKSzVyIE2gNE4yPTVizszNMi=> NXvRelBWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCxOVY3QDlpPkKwNVU3Pjh7PD;hQi=>
primary leukemia cells NUDPeY5xS3m2b4TvfIlkcXS7IHHzd4F6 NVrqfZFTPzJiaILz NEXrcnZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBxemmvYYL5JIxmfWunbXnhJINmdGy|IHnzc4xifGWmIH\yc40h[WO3dHWgcZlmdG:rZDDs[ZVs\W2rYTDwZZRq\W62IHX4dJJme3OrbnegSmxVOy2LVFSgcZV1[XSrb36gZZN{\XO|ZXSgZZMh[2WubDD2bYFjcWyrdImgZYZ1\XJiN{KgbJJ{KGK7IHz1Z4ln\XKjc3WgZZN{[XluIFnDOVAhRSByLkCzJO69VS5? NVq5fJlkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyNlEzODFpPkKyNlIyOjBzPD;hQi=>
primary leukemia cells M4DSXGN6fG:2b4jpZ4l1gSCjc4PhfS=> MWS3NkBpenN? MXzDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDwdolu[XK7IHzleYtmdWmjIHPlcIx{KGm|b3zheIVlKG[{b32gZYN2fGVibYnlcI9q\CCuZYXr[Y1q[SCyYYTp[Y51KGW6cILld5Nqdmdid3ns[EB1gXCnIF\MWFMh[XO|ZYPz[YQh[XNiY3XscEB3cWGkaXzpeJkh[W[2ZYKgO|IhcHK|IHL5JIx2[2moZYLhd4Uh[XO|YYmsJGlEPTBiPTCwMlA{KM7:TT6= NUTrcIgzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyNlEzODFpPkKyNlIyOjBzPD;hQi=>
primary leukemia cells M{HicWN6fG:2b4jpZ4l1gSCjc4PhfS=> NFrwRo04OiCqcoO= NWrLRYZUS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4heHKrbXHyfUBt\XWtZX3pZUBk\WyuczDpd49t[XSnZDDmdo9uKGGldYTlJI16\WyxaXSgcIV2c2WvaXGgdIF1cWWwdDDlfJBz\XO|aX7nJGZNXDNvREizOXkhdXW2YYTpc44h[XO|ZYPz[YQh[XNiY3XscEB3cWGkaXzpeJkh[W[2ZYKgO|IhcHK|IHL5JIx2[2moZYLhd4Uh[XO|YYmsJGlEPTBiPTCxMlEh|ryPLh?= NGLFXZc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkKyNVIxOSd-MkKyNlEzODF:L3G+
endothelial precursor cells NVHiS3hETnWwY4Tpc44h[XO|YYm= M1;UV2lvcGmkaYTpc44hd2ZiZX7kc5Rp\WyrYXygZ49z\CCjcnXhJIZwem2jdHnvckBqdiCnbnTveIhmdGmjbDDwdoVkfXK|b4KgZ4VtdHNiYomgR2Q{OSClb4LkJIFz\WFiZHX0[YN1cW:wIHLhd4VlKHCqZX7veJlxcWNiZIL1[{BlcXOlb4\ldpkh[mG|ZXSgZZN{[XluIFnDOVAhRSByLkCwPVYh|ryPLh?= NGP5XGw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkSwPVY3Pid-MkK0NFk3PjZ:L3G+
endothelial precursor cells NY[xXY5wTnWwY4Tpc44h[XO|YYm= NWTSOoRMUW6qaXLpeIlwdiCxZjDj[YxtKG2rZ4LheIlwdiCrbjDlcoRwfGinbHnhcEBxemWldYLzc5Ih[2WubIOgZpkhV3KrczDj[YxtKG2rZ4LheIlwdiCtaYSgZoF{\WRicHjlco91gXCrYzDkdpVoKGSrc3PveoVzgSCkYYPl[EBie3OjeTygTWM2OCB;IEGzMlYh|ryPLh?= MkXTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ2MEm2OlYoRjJ{NEC5OlY3RC:jPh?=
U251 M1[xcWZ2dmO2aX;uJIF{e2G7 NIizcHg3OCCvaX7z M4jrWGlvcGmkaYTpc44hd2ZiVlXHSnIzKGmwIHj1cYFvKFV{NUGgZ4VtdHNicILleJJm[XSnZDDmc5IhPjBibXnud{Bu\WG|dYLl[EBi\nSncjCxJIhzKGK7IFXMTXNCNCCLQ{WwJF0hOThwOTFOwG0v MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjd|OUC5NEc,OjJ5M{mwPVA9N2F-
U251 NFrnNHhHfW6ldHnvckBie3OjeR?= NFXjS5U3OCCvaX7z M3L3bmlvcGmkaYTpc44hd2ZiVlXHSk1qdmS3Y3XkJHZGT0[UMjDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iVUK1NUBk\WyuczDveoVz\XiycnXzd4lv\yCIbHutNUBxemW2cnXheIVlKG[xcjC2NEBucW6|IIDybY9zKHSxIG\FS2Yh[WSmaYTpc44hdWWjc4Xy[YQh[W[2ZYKgNVAhdWmwczDifUBxcG:|cHjveJlzd3OrbnWgSWxKW0FiY4n0c4Jtd3RiYX7hcJl{cXNuIFnDOVAhRSBzOD65JO69VS5? MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN5NUC5NEc,OjN|N{WwPVA9N2F-
U251 NFnKUppHfW6ldHnvckBie3OjeR?= MUe2NEBucW6| MmK3TY5pcWKrdHnvckBw\iCYRVfGVlIhcW5iaIXtZY4hXTJ3MTDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKF[HR1[tbY5lfWOnZDD0fZJwe2mwZTDwbI9{eGixconsZZRqd25iaX7jeYJifGWmIH\vdkA3OCCvaX7zJJBzcW:{IITvJHZGT0ZvYXP0bZZifGmxbjDt[YF{fXKnZDCxNEBucW6|IHL5JGVNUVODLDDJR|UxKD1iMUiuPUDPxE1w NIHxb|U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{SzOFE{QSd-MkO0N|QyOzl:L3G+
CHO M4rkPWZ2dmO2aX;uJIF{e2G7 M3L0XWlvcGmkaYTpc44hd2ZiQ3H2NU4zKGO3coLlcpQhdWWjc4Xy[YQhfXOrbnegVXBifGOqIHH1eI9u[XSrYzDwZZRpKGOuYX3wJJN6e3SnbTDpckBEUE9iY3XscJMh\XiycnXzd4lv\yCFYY[xMlItKGKndHGtNkBidmRiYXzwbIEuOi:mZXz0ZU0yKHO3YoXubZR{NCCLQ{WwJF0hOzNwNDFOwG0v MojyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6MUK1NFMoRjJ|OEGyOVA{RC:jPh?=
U251 NVj6PFRMTnWwY4Tpc44h[XO|YYm= M4HP[WlvcGmkaYTpc44hd2ZiVlXHSnIzKGmwIHj1cYFvKFV{NUGgZ4VtdHNiYomgdIhwe3Cqb4T5do9{cW6nIFXMTXNCNCCLQ{WwJF0hOC5yMUi5JO69VS5? M{SwVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUCwPFY2Lz5{NEmwNFg3PTxxYU6=
MCF7 NWnjTlN3SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= Moi1OFghcHK| NF3wdGZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IEGwMlUh|ryPLh?= NXfjXWE2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwOlQ{PDdpPkK1NFY1OzR5PD;hQi=>
HepG2 Mo\ZRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NVLqfYh5PDhiaILz NGrOPYtCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjldGczKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTBiPTCxN{43KM7:TT6= NWjXUWZ4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwOlQ{PDdpPkK1NFY1OzR5PD;hQi=>
CHO NUXqeINOTnWwY4Tpc44h[XO|YYm= NEjPdmhKdmirYnn0bY9vKG:oIILhdIllKGSnbHH5[YQhcW65YYLkJJJm[3SrZonpcocheG:2YYPzbZVuKGO3coLlcpQhMEmNcjmgbY4hS2irbnXz[UBp[W2|dHXyJI93[XK7IDjDTG8qKGOnbHzzJJN1[WKuZTDlfJBz\XO|aX7nJIhGWkdibXXhd5Vz\WRidYPpcochUW:wV3;yb5MhSmG{cnHjeYRiKGG3dH;tZZRm\CCyYYTjbEBkdGGvcDDwcIF1\m:{bTygTWM2OCB;IEeuPVQ{OjhizszNMi=> NEDoUHc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC4O|c2Oyd-MkWwPFc4PTN:L3G+
CHO K1 NF[5O41HfW6ldHnvckBie3OjeR?= NXfONJlMUW6qaXLpeIlwdiCxZjDyZZBq\CCmZXzhfYVlKGmwd3Hy[EBz\WO2aX\5bY5oKHCxdHHzd4l2dSCldYLy[Y51KCiLS4KpJIlvKEOqaX7ld4UhcGGvc4TldkBwfmG{eTCoR2hQMSCNMTDj[YxteyC|dHHicJkh\XiycnXzd4lv\yCqRWLHJI1m[XO3cnXkJJV{cW6pIFnvcndwemu|IGH1ZZR1em9iYYX0c41ifGWmIIDheINpKGOuYX3wJJBt[XSob4LtMEBKSzVyIE2gNVAh|ryPLh?= MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB6N{e1N{c,OjVyOEe3OVM9N2F-
CHO K1 Mo\hSpVv[3Srb36gZZN{[Xl? M1zMUmlvcGmkaYTpc44hd2ZiZnHzeEB{d2SrdX2gZ5VzemWwdDCoTW5iMSCrbjDDbIlv\XOnIFjhcZN1\XJiT4\hdpkhMEOKTzmgT|Eh[2WubIOgeJJidnOoZXP0[YQhf2m2aDDoeY1idiCQYY[xMlUhdWWjc4Xy[YQhfXOrbnegTY9vX2:{a4OgVZVifHS{bzDheZRwdWG2ZXSgdIF1[2hiY3zhcZAheGyjdH\vdo0tKEmFNUCgQUAyPS56NEi5JO69VS5? NWi1[|lYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwPFc4PTNpPkK1NFg4PzV|PD;hQi=>
HEK293 MUPGeY5kfGmxbjDhd5NigQ>? NVjBdppnUW6qaXLpeIlwdiCxZjDmZZN1KHOxZHn1cUBkfXK{ZX70JEhKVmFrIHnuJGhGUzJ7MzDj[YxteyC2cnHud4Zm[3SnZDD3bZRpKGi3bXHuJG5ifjFwNTDt[YF{fXKnZDD1d4lv\yCLb37Xc5JseyCTdXH0eJJwKGG3dH;tZZRm\CCyYYTjbEBkdGGvcDDwcIF1\m:{bTygTWM2OCB;IEO5MlgyODdizszNMi=> MlOwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyOEe3OVMoRjJ3MEi3O|U{RC:jPh?=
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BAF3 M1vCOmZ2dmO2aX;uJIF{e2G7 MmDKO|IhcHK| MkfHTY5pcWKrdHnvckBw\iCWZXyt[pV{\WRiY1vJWEBVPjdyST;WOVU6TCCmb4XicIUhdXW2YX70JEh2dmuwb4fuJI9zcWerbjmgeJJidnOoZXP0[YQhcW5ibX;1d4UhSkGIMzDj[YxteyCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckBk\WyuIIDyc4xq\mW{YYTpc44h[W[2ZYKgO|IhcHK|IHL5JINmdGy2aYTldk1odG9xQ1PLPEBie3OjeTygS2k2OCB;IECuNFU{KM7:TT6= NGHoSpA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{C3O|cxPSd-MkewO|c4ODV:L3G+
BAF3 M1:xRmZ2dmO2aX;uJIF{e2G7 Mn7DO|IhcHK| M2PRemlvcGmkaYTpc44hd2ZiVHXsMYZ2e2WmIHPLTXQhMHWwa37ve44hd3KrZ3nuLUB1emGwc3\lZ5Rm\CCrbjDtc5V{\SCEQV[zJINmdGy|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKGOnbHygdJJwdGmoZYLheIlwdiCjZoTldkA4OiCqcoOgZpkh[2WubITpeIVzNWeubz;DR2s5KGG|c3H5MEBIUTVyIE2gNE4xPzhizszNMi=> NV\RS|BRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewO|c4ODVpPkK3NFc4PzB3PD;hQi=>
GIST882 MXfBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M{DyWlczKGi{cx?= NXfV[|JYSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBkU0mWIHTldIVv\GWwdDDoeY1idiCJSWPUPFgzKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkA4OiCqcoOgZpkh[2WubITpeIVzNWeubz;DR2s5KGG|c3H5MEBIUTVyIE2gNE4yOSEQvF2u NFHOXnE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{C3O|cxPSd-MkewO|c4ODV:L3G+
BAF3 MnjuSpVv[3Srb36gZZN{[Xl? M2f5S|czKGi{cx?= M{L3TmlvcGmkaYTpc44hd2ZiVHXsMYZ2e2WmIHPLTXQhVjh{MlugcZV1[W62IDj1cotvd3ewIH;ybYdqdilidILhcpNn\WO2ZXSgbY4hdW:3c3WgRmFHOyClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDj[YxtKHC{b3zp[oVz[XSrb36gZYZ1\XJiN{KgbJJ{KGK7IHPlcIx1cXSncj3ncI8wS0ONODDhd5NigSxiR1m1NEA:KDBwNUGg{txONg>? NIjOOWc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{C3O|cxPSd-MkewO|c4ODV:L3G+
Rec1 MljBRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M4jpdFczKGi{cx?= MnLpRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCUZXOxJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBi\nSncjC3NkBpenNiYomgZ4VtdHSrdHXyMYdtdy:FQ1u4JIF{e2G7LDDHTVUxKD1iMD64O{DPxE1w MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzB5N{ewOUc,OjdyN{e3NFU9N2F-
K562 Ml3yRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M325flczKGi{cx?= M1zD[GFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgRmNTNUGETDDk[ZBmdmSnboSgbJVu[W5iS{W2NkBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgO|IhcHK|IHL5JINmdGy2aYTldk1odG9xQ1PLPEBie3OjeTygS2k2OCB;IEGg{txONg>? NGTwN5k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{C3O|cxPSd-MkewO|c4ODV:L3G+
KU812 NEKzPYtCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M4jJb|czKGi{cx?= MY\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IFLDVk1CSkxiZHXw[Y5l\W62IHj1cYFvKEuXOEGyJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBi\nSncjC3NkBpenNiYomgZ4VtdHSrdHXyMYdtdy:FQ1u4JIF{e2G7LDDHTVUxKD1iMT6xJO69VS5? NVnRWI1ERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewO|c4ODVpPkK3NFc4PzB3PD;hQi=>
BCR-ABL dependent MEG01 MVXBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MoHRO|IhcHK| Ml\YRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCEQ2KtRWJNKGSncHXu[IVvfCCPRVewNUBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgO|IhcHK|IHL5JINmdGy2aYTldk1odG9xQ1PLPEBie3OjeTygS2k2OCB;IEGuNkDPxE1w NYj2Z4E1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewO|c4ODVpPkK3NFc4PzB3PD;hQi=>
BAF3 NUfFOI1DTnWwY4Tpc44h[XO|YYm= NY[0VWxSPzJiaILz MlnYTY5pcWKrdHnvckBw\iCWZXyt[pV{\WRiY1vJWEBFQDF4VjDteZRidnRiKIXub45wf25ib4Lp[4lvMSC2cnHud4Zm[3SnZDDpckBud3W|ZTDCRWY{KGOnbHzzJIF{e2W|c3XkJIF{KGSnY4LlZZNmKGmwIHPlcIwheHKxbHnm[ZJifGmxbjDh[pRmeiB5MjDodpMh[nliY3XscJRqfGW{LXfsc{9ES0t6IHHzd4F6NCCJSUWwJF0hOS5|ODFOwG0v MnvnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyN{e3NFUoRjJ5MEe3O|A2RC:jPh?=
U937 MmnURY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NGKxUFM4OiCqcoO= NUjUcG1NSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDVPVM4KGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkA4OiCqcoOgZpkh[2WubITpeIVzNWeubz;DR2s5KGG|c3H5MEBIUTVyIE2gNU44KM7:TT6= NWK4bY1XRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewO|c4ODVpPkK3NFc4PzB3PD;hQi=>
GIST48B MnG2RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M{TYblczKGi{cx?= NWO0[HhPSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDHTXNVPDiEIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBk\WyuII\pZYJqdGm2eTDh[pRmeiB5MjDodpMh[nliY3XscJRqfGW{LXfsc{9ES0t6IHHzd4F6NCCJSUWwJF0hOi5yMTFOwG0v NELNNFE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{C3O|cxPSd-MkewO|c4ODV:L3G+
CHO MUDBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M{Dwb|czKGi{cx?= NVK5R41[SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBEUE9iY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJINmdGxidnnhZoltcXS7IHHmeIVzKDd{IHjyd{BjgSClZXzseIl1\XJvZ3zvM2NEUzhiYYPzZZktKEeLNUCgQUAzNjB|IN88UU4> Mnr2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyN{e3NFUoRjJ5MEe3O|A2RC:jPh?=
CHL M1H0WGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 Mo\0O|IhcHK| NYTaOlNjSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBEUExiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJINmdGxidnnhZoltcXS7IHHmeIVzKDd{IHjyd{BjgSClZXzseIl1\XJvZ3zvM2NEUzhiYYPzZZktKEeLNUCgQUAzNjR6IN88UU4> MlP6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyN{e3NFUoRjJ5MEe3O|A2RC:jPh?=
BAF3 M{[xSWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 Mn7hRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDtc5V{\SCEQV[zJINmdGy|LDDHTVUxKD1iMj63PEDPxE1w MlG3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyN{e3NFUoRjJ5MEe3O|A2RC:jPh?=
MDA-MB-231 NF7jZVJEgXSxdH;4bYNqfHliYYPzZZk> MWW0PEBpenN? NEDSbGhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTEFvTVKtNlMyKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTBiPTC3MlQh|ryPLh?= M2faflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MUK4NVc{Lz5{N{GyPFE4OzxxYU6=
BT549 Mn22R5l1d3SxeHnjbZR6KGG|c3H5 M37U[FQ5KGi{cx?= M4\CWWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGJVPTR7IHPlcIx{KGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUAyPS53IN88UU4> MlPrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzMkixO|MoRjJ5MUK4NVc{RC:jPh?=
DU145 MkCzR5l1d3SxeHnjbZR6KGG|c3H5 MX60PEBpenN? MXTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDEWVE1PSClZXzsd{Bi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gNVYvPCEQvF2u NGW0cIU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{GyPFE4Oyd-MkexNlgyPzN:L3G+
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RWPE1 M2mwdWN6fG:2b4jpZ4l1gSCjc4PhfS=> M1rGWlQ5KGi{cx?= NHj2UpNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBTX1CHMTDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOjNizszNMi=> MoCxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzMkixO|MoRjJ5MUK4NVc{RC:jPh?=
MCF7 M1yy[2Z2dmO2aX;uJIF{e2G7 NXTZepB2OSC3TR?= NInEVoszPCCqcoO= M4D5eGlvcGmkaYTpc44hd2ZiVlXHSnIzKHCqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBOS0Z5IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBmgHC{ZYPzbY9vKG:oIIDoc5NxcG:{eXzheIVlKEWUS{GvNkBifCBzIIXNJIlv[3WkYYTl[EBnd3JiMkSgbJJ{KGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=> MnvoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzN{[5OFQoRjJ5MUe2PVQ1RC:jPh?=
MCF7 NY\TXIV4TnWwY4Tpc44h[XO|YYm= M{K4bFEhfU1? Mn71NlQhcHK| M3naOGlvcGmkaYTpc44hd2ZiVlXHSnIzKHCqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBOS0Z5IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBmgHC{ZYPzbY9vKG:oIIDoc5NxcG:{eXzheIVlKFKjZkGgZZQhOSC3TTDpcoN2[mG2ZXSg[o9zKDJ2IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= NE\nOW89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{G3Olk1PCd-MkexO|Y6PDR:L3G+
PA1 NEnwZ4JEgXSxdH;4bYNqfHliYYPzZZk> NW\uTYtJPDhiaILz MXzDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQRVEh[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhUUN3MDC9JFcvQTdizszNMi=> Ml7GQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd{MUC0N|goRjJ5MkGwOFM5RC:jPh?=
LNCAP M1XBNGN6fG:2b4jpZ4l1gSCjc4PhfS=> NHT3Rm81QCCqcoO= MYDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDMUmNCWCClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOTJwNkGg{txONg>? NYjhd2FXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkeyNVA1OzhpPkK3NlExPDN6PD;hQi=>
RWPE1 NU\3U|ZCS3m2b4TvfIlkcXS7IHHzd4F6 NGiwTGU1QCCqcoO= NHrBNnhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBTX1CHMTDj[YxteyCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckBk\WyuII\pZYJqdGm2eTDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iMkOg{txONg>? M{\4TVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MkGwOFM5Lz5{N{KxNFQ{QDxxYU6=
MCF7 MVrDfZRwfG:6aXPpeJkh[XO|YYm= M2jDWVQ5KGi{cx?= MknmR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOjNwN{[g{txONg>? Mn64QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd{MUC0N|goRjJ5MkGwOFM5RC:jPh?=
MDA-MB-231 Mm[0R5l1d3SxeHnjbZR6KGG|c3H5 NETXTmE1QCCqcoO= Mnj2R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhUUN3MDC9JFcvPDRizszNMi=> NYHS[YlURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke0OFg6OTZpPkK3OFQ5QTF4PD;hQi=>
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アッセイ
Methods Test Index PMID
Western blot p-STAT3 / STAT3 / p-Src / Src / p-AKT / AKT / p-ERK / ERK ; p-GSK3β / GSK3β / MYCN ; p-AKT / AKT / p-ERK / ERK 19244102 24759734
Growth inhibition assay Cell viability 24369536
体内試験

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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:

[1]

  • 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.

細胞試験:

[3]

  • 細胞株:RS4;11, MV4;11, and OC1-AML5
  • 濃度: Dissolved in DMSO, final concentrations ~10 μM
  • 反応時間:24 and 48 hours
  • 実験の流れ:

    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.

動物試験:

[2]

  • 動物モデル: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
  • 投薬量:~80 mg/kg
  • 投与方法:Orally once daily

溶解度 (25°C)

体外

体内

左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
4% DMSO+30% PEG 300+ddH2O
混合させたのち直ちに使用することを推奨します。

2mg/mL

化学情報

分子量 532.56
化学式

C22H27FN4O2.C4H6O5

CAS No. 341031-54-7
Storage 3年 -20°C
2年 -80°C in solvent
Smiles CCN(CC)CCNC(=O)C1=C(NC(=C1C)C=C2C3=C(C=CC(=C3)F)NC2=O)C.C(C(C(=O)O)O)C(=O)O

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

便利ツール

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05043090 Recruiting Drug: savolitinib|Drug: durvalumab|Drug: sunitinib Papillary Renal Cell Carcinoma AstraZeneca October 28 2021 Phase 3
NCT04669366 Completed Drug: sunitinib|Drug: axitinib Kidney Neoplasms Pfizer January 20 2021 --
NCT04633122 Recruiting Drug: Ripretinib|Drug: Sunitinib Gastrointestinal Stromal Tumor(GIST) Zai Lab (Shanghai) Co. Ltd.|Zai Lab (Hong Kong) Ltd. November 25 2020 Phase 2
NCT04115189 Completed Drug: Sunitinib Metastatic Renal Cell Carcinoma ( mRCC) Pfizer December 13 2019 --
NCT04175262 Completed Drug: sunitinib Metastatic Renal Cell Carcinoma (mRCC) Pfizer|IMDC group|Analysis Group October 31 2019 --

(data from https://clinicaltrials.gov, updated on 2022-08-01)

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

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よくある質問(FAQ)

質問1:
I was wondering that the compound is in its cis or trans form?

回答
S1042 Sunitinib Malate is Z form.

質問2:
What is the difference between Sunitinib Malate(S1042) and Sunitinib(S7781)?

回答
S1042 is the Malate salt form of Sunitinib. The biological activities of these two compounds are the same but the solubility of these two compounds in aqueous solvent are different.

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