Imatinib (STI571) Mesylate

For research use only. Not for use in humans.

目录号:S1026 别名: Gleevec, Glivec, CGP-57148B 中文名称:甲磺酸伊马替尼

Imatinib (STI571) Mesylate Chemical Structure

CAS No. 220127-57-1

Imatinib Mesylate (STI571, CGP-57148B)是一种口服生物有效的Imatinib甲磺酸盐,是一种多靶点抑制剂,作用于v-Ablc-KitPDGFR,在无细胞和细胞试验中,IC50分别为0.6 μM,0.1 μM 和0.1 μM。Imatinib Mesylate (STI571) 可诱导自噬。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1567.38 现货
RMB 780.01 现货
RMB 1603.82 现货
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客户使用Selleck生产的Imatinib (STI571) Mesylate发表文献159篇:

产品安全说明书

Bcr-Abl抑制剂选择性比较

生物活性

产品描述 Imatinib Mesylate (STI571, CGP-57148B)是一种口服生物有效的Imatinib甲磺酸盐,是一种多靶点抑制剂,作用于v-Ablc-KitPDGFR,在无细胞和细胞试验中,IC50分别为0.6 μM,0.1 μM 和0.1 μM。Imatinib Mesylate (STI571) 可诱导自噬。
靶点
PDGFR [1]
(Cell-free assay)
c-Kit [2]
(M-07e cells)
v-Abl [1]
(Cell-free assay)
100 nM 100 nM 600 nM
体外研究

抑制酪氨酸和丝氨酸/苏氨酸蛋白激酶的体外测定法显示Imatinib有效抑制V-Abl酪氨酸激酶和PDGFR,IC50分别为0.6 μM和0.1 μM。[1] Imatinib抑制SLF-依赖性激活的野生型的c-kit激酶活性,IC 50约为0.1 μM,这类似抑制PDGFR所需的浓度。[2] Imatinib表现出对人支气管类癌细胞系NCI-H727和人胰腺类癌细胞系BON-1的抑制作用,IC50分别为32.4 μM和32.8 μM。 [3] 最近的一项研究显示,Imatinib通过下调hERG1 K(+)通道发挥在慢性粒细胞白血病的抗白血病作用,hERG1 K(+)通道在白血病细胞中高表达并表现有利于白血病出现。[4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
GIST882 Mnn0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUW5OkBp M3LYO2lEPTB;MT63JO69VQ>? MkDKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MECyNVIoRjJ2OUCwNlEzRC:jPh?=
K562 MXjDfZRwfG:6aXPpeJkhSXO|YYm= MWiyOEBp NUHhdWpmUUN3ME2wMlIyKM7:TR?= M1X3RVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MECwNlA4Lz5{MkCwNFIxPzxxYU6=
MCF-7 NGTvNIREgXSxdH;4bYNqfHliQYPzZZk> M2C2eVI1KGh? NHjIZnFKSzVyPUCuPFMh|ryP NVvJVoI4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKwNFAzODdpPkKyNFAxOjB5PD;hQi=>
MDA-MB-23 MmfLR5l1d3SxeHnjbZR6KEG|c3H5 NXjTbpBXOjRiaB?= MYjJR|UxRTFwODFOwG0> NEXiWGw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkCwNFIxPyd-MkKwNFAzODd:L3G+
K562r MmjVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rkWmlEPTB;MUFCpO69VQ>? NV;4S2s5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5N|k1OThpPkK0PVM6PDF6PD;hQi=>
K562 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\Mc5Y{TUN3ME2wMlA6KM7:TR?= MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjZ5OESxOEc,OTZ4N{i0NVQ9N2F-
MCF-7 NFPzfYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrhVYUyOCEQvF2= NGTqW|A1QCCq NIjse5VjdG:la4OgZ4VtdCCycn;sbYZmemG2aX;uJIlv[3KnYYPlJIlv\HWlZXSgZpkhSkp|Wh?= MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ5NECzOEc,OjV{N{SwN|Q9N2F-
K-562  NI\GbGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnhSmlXUUN3ME2xJO69VQ>? NWXjdlVZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyN|k3PjJpPkK1NlM6PjZ{PD;hQi=>
K562  NIfjU5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvGRoFKSzVyPUCuOeKh|ryP M1H3ZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUO5OFE5Lz5{NEmzPVQyQDxxYU6=
PC3  NULGV4dDSXCxcITvd4l{KEG|c3H5 NYXnPWx{OjEkgJpOwG0> MoHsOFgwPzJiaB?= MlrobY5kemWjc3XzJINmdGxic4Xyeol3[Wx? NUjwTFBKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3PFY3PTZpPkK1O|g3PjV4PD;hQi=>
PC3  NFTV[|lE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MWCyNQKBkc7:TR?= MnjiOk04OiCq MkSzbY5kemWjc3XzJINmdGxidnnhZoltcXS7 NXjtTYRSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3PFY3PTZpPkK1O|g3PjV4PD;hQi=>
DU145 M1rWW2Fxd3C2b4Ppd{BCe3OjeR?= NVzycWlQOjEkgJpOwG0> M33YWVQ5Nzd{IHi= M2nLPYlv\HWlZYOgZ4VtdCCmZXH0bEBjgSCjcH;weI9{cXN? NFnFPY49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe4OlY2Pid-MkW3PFY3PTZ:L3G+
DU145 Ml7oR4VtdCCYaXHibYxqfHliQYPzZZk> MlOxNlDjiIoQvF2= NYTxV29zPi15MjDo MUjk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHl? M3\4NVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{i2OlU3Lz5{NUe4OlY2PjxxYU6=
Hep G2 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTNzIN88US=> NFnlRZc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUi2N|I{Oid-MkW4OlMzOzJ:L3G+
T47D  Ml[wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTVyIN88US=> M3\zWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OE[zNlMzLz5{NUi2N|I{OjxxYU6=
EOL-1 M37GeGN6fG:2b4jpZ4l1gSCjc4PhfS=> MlTrO|IhcHK| MkLER5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gSW9NNTFiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JIFt[W2jcj3icJVmKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxKD1iMD6wNFAzKM7:TT6= MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTNyMUmwNkc,OTl|MEG5NFI9N2F-
EOL-1 NUCySI9USW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= Mn:2O|IhcHK| NU\YNnZXSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDFU2wuOSClZXzsd{Bi\nSncjC3NkBpenNiYomgR4VtdFSrdHXyMWdtdyCxcjDDR2suQCCjc4PhfUwhT0l3MDC9JFAvODBzIN88UU4> NELzWVA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUW0OFE1QSd-Mkm1OFQyPDl:L3G+
GISTT1 M3XaXmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NV3KTGZGPzJiaILz NISzVFZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFfJV3RVOSClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDj[YxtKHSrdHXyMYdtdyCjc4PhfUwhT0l3MDC9JFAvODB|IN88UU4> MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDV2MU[5OUc,Ojh3NEG2PVU9N2F-
Sf9 NYPNe3lQTnWwY4Tpc44h[XO|YYm= MWPCbY5lcW6pIHHm[olvcXS7IITvJIh2dWGwIHHjeIl3\SC|aYTlJI9nKE5vdHXycYlv[WxiaHX4ZYhqe3SrZHnu[U11[WepZXSgRWJNOiCneIDy[ZN{\WRiaX6gWJJq[2ixcHz1d4liKG6rIHnu[oVkfGWmIGPmPUBk\WyuczDifUBqe2:2aHXycYFtKHSrdILheIlwdiClYXzvdolu\XS{aXOgZZN{[XluIFvkJF0hOC5yME[g{txONg>? MoDxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF2MUezOFMoRjJzNEG3N|Q{RC:jPh?=
K562 M3TSUWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NVzw[WhkSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDpcYF1cW6rYj3y[ZNqe3SjboSgT|U3OiClZXzsd{whUUN3MDC9JFAvODB4MEWg{txONg>? M4DZZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{e2OVg4Lz5{MUO3OlU5PzxxYU6=
GISTT1 NFXZUlJCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NV24bpRvPzJiaILz MX;BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHPLTXQh\GWyZX7k[Y51KGi3bXHuJGdKW1SWMTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4h[2WubDD2bYFjcWyrdImgZYZ1\XJiN{KgbJJ{KGK7IHPlcIx1cXSncj3ncI8wS0ONODDhd5NigSxiR1m1NEA:KDBwMEC4JO69VS5? MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzB5N{ewOUc,OjdyN{e3NFU9N2F-
GISTT1 NIHVdFJCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NF;2dYQ4OiCqcoO= MkXxRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCJSWPUWFEh[2WubIOgcYVie3W{ZXSgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8hd3JiQ1PLPEBie3OjeTygS2k2OCB;IECuNFA5KM7:TT6= M{\0VVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OU[2PVU1Lz5{N{m2Olk2PDxxYU6=
GISTT1 NXTGem53TnWwY4Tpc44h[XO|YYm= MYq3NkBpenN? NXLBT4lvUW6qaXLpeIlwdiCxZjDLTXQhcW5iaIXtZY4hT0mVVGSxJINmdGy|IHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDTVmIh[XO|YYmsJGdKPTBiPTCwMlAyKM7:TT6= M4HRXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{ezNVU{Lz5{M{e3N|E2OzxxYU6=
BAF3 MVfGeY5kfGmxbjDhd5NigQ>? M1LY[lczKGi{cx?= NFTQUXhKdmirYnn0bY9vKG:oIGTFUE1nfXOnZDDQSGdHWmGucHjhJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW|c3XkJIlvKG2xdYPlJGJCTjNiY3XscJMh[XO|ZYPz[YQh[XNiY3XscEBoem:5dHigbY5pcWKrdHnvckBi\nSncjC3NkBpenNiYomgZ4VtdCC2aYTldk1odG9iYYPzZZktKEeLNUCgQUAxNjBzMEeg{txONg>? NUjuOWx2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki1OFE3QTVpPkK4OVQyPjl3PD;hQi=>
TF1 NHTEZ3pEgXSxdH;4bYNqfHliYYPzZZk> NYG0bVBpS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hXEZzIHPlcIx{KGW6cILld5NqdmdiYz3LTXQhdXW2YYTpc44h[XO|ZYPz[YQh[XNiY3XscEB3cWGkaXzpeJktKEmFNUCgQUAxNjBzMzFOwG0v NWjZNYlVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyNlEzODFpPkKyNlIyOjBzPD;hQi=>
GIST882 MX;BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MVm3NkBpenN? M17De2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgZ2tKXCCmZYDlcoRmdnRiaIXtZY4hT0mVVEi4NkBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgO|IhcHK|IHL5JINmdGy2aYTldk1odG9xQ1PLPEBie3OjeTygS2k2OCB;IECuNFE1KM7:TT6= MlflQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyN{e3NFUoRjJ5MEe3O|A2RC:jPh?=
GIST882 M3nme2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 NH76XWE4OiCqcoO= NVfGT5VMSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDHTXNVQDh{IHPlcIx{KG2nYYP1doVlKGGodHXyJFczKGi{czDifUBE\WyuVHn0[ZIuT2yxIH;yJGNEUzhiYYPzZZktKEeLNUCgQUAxNjBzNDFOwG0v NWXUSlNZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke5OlY6PTRpPkK3PVY3QTV2PD;hQi=>
BA/F3 M3HKNmZ2dmO2aX;uJIF{e2G7 MVy3NkBpenN? M4PKcGlvcGmkaYTpc44hd2ZiS3n0JIV5d25iMUGg[IVt\XSrb36gLFU2PyC2bzC1OVghemW|aXT1[ZMqKG23dHHueEApfW6tbn;3ckBwemmpaX6pJJRz[W6|ZnXjeIVlKGmwIH3veZNmKEKDL1[zJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3XscEBoem:5dHigbY5kfWKjdHXkJIZweiB5MjDodpMh[nliTWTTJIF{e2G7LDDHTVUxKD1iMD6wNVch|ryPLh?= MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJyNES0NUc,OzB{MES0OFE9N2F-
BA/F3 MXjGeY5kfGmxbjDhd5NigQ>? Mni3O|IhcHK| M4fYdmlvcGmkaYTpc44hd2ZiVFXMMYZ2e2WmIGDES2ZT[mW2YTCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBud3W|ZTDCRU9HOyClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOgZpkhS2WubGTpeIVzNUeubzDvdkBES0tvODDhd5NigSxiR1m1NEA:KDBwMEG5JO69VS5? NHjJeYk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUW0OFE1QSd-Mkm1OFQyPDl:L3G+
BAF3 M{nxfWZ2dmO2aX;uJIF{e2G7 MUi3NkBpenN? NXv1S5FYUW6qaXLpeIlwdiCxZjDU[Ywu\nW|ZXSgVGRITlJvYnX0ZUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCEQV[zJINmdGy|IHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJI1m[XO3cnXkJIFnfGW{IEeyJIhzeyCkeTDD[YxtXGm2ZYKtS4xwKG:{IFPDT|gh[XO|YYmsJGdKPTBiPTCwMlAyQSEQvF2u MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzl4Nkm1OEc,Ojd7Nk[5OVQ9N2F-
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BA/F3 M1PqcmN6fG:2b4jpZ4l1gSCjc4PhfS=> NIDGO241QCCqcoO= NVjkUIVuS3m2b4TvfIlkcXS7IHHnZYlve3RibX;1d4UhSkFxRkOgZ4VtdHNidILhcpNn\WO2ZXSge4l1cCC5aXzkJJR6eGViQnPyMWFjdCCjZoTldkA1QCCqcoOgZpkhYFSWIHHzd4F6NCCLQ{WwJF0hOC5yOUKg{txONg>? MlrZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MEC4NFYoRjJ|NkCwPFA3RC:jPh?=
GIST882 NHvzeZZHfW6ldHnvckBie3OjeR?= NEXiVVJKdmirYnn0bY9vKG:oIHj1cYFvKEuLVDDheZRweGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJGdKW1R6OEKgZ4VtdHNiYomgSWxKW0FuIFnDOVAhRSByLkC5O{DPxE1w MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODhzN{WzPEc,OjB6MUe1N|g9N2F-
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insect NH7NbZBHfW6ldHnvckBie3OjeR?= NUXQUW9JOzBibXnudy=> MoLHTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCC5aXzkJJR6eGViQVLMNUBmgHC{ZYPz[YQhcW5iaX7z[YN1KGOnbHzzJIFnfGW{IEOwJI1qdnNiYomgSnJGXCCjc4PhfUwhUUN3MDC9JFAvODl6MjFOwG0v NEL6UWw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{OwNVcxOyd-MkOzNFE4ODN:L3G+
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BA/F3 NV[3NFJqTnWwY4Tpc44h[XO|YYm= MoTzO|IhcHK| M1XvdmlvcGmkaYTpc44hd2ZiVFXMMYZ2e2WmIGDES2ZT[mW2YTCoeY5sdm:5bjDvdolocW5rIITyZY5{\mWldHXkJIlvKG2xdYPlJGJCN0Z|IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh[2WubDDndo94fGhiaX7jeYJifGWmIH\vdkA4OiCqcoOgZpkhVVSVIHHzd4F6NCCJSUWwJF0hOC5zMEKg{txONg>? MmXKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{MES0OFEoRjNyMkC0OFQyRC:jPh?=
BAF3 NHXmXmxHfW6ldHnvckBie3OjeR?= NWe4[mFqPzJiaILz M1vSVWlvcGmkaYTpc44hd2ZiVHXsMYZ2e2WmIHOtT2lVKEx3N{\QJI12fGGwdDCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBDSUZ|IHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIH3lZZN2emWmIHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJvR3zvJI9zKEOFS{igZZN{[XluIFfJOVAhRSByLkGwNkDPxE1w MnrpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7Nk[5OVQoRjJ5OU[2PVU1RC:jPh?=
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GIST882 NEHG[IpHfW6ldHnvckBie3OjeR?= NEHDeVBKdmirYnn0bY9vKG:oIFvJWEBMPjR{RTDteZRidnRiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gbJVu[W5iR1nTWFg5OiClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIJ6KEGWUD3k[ZBt\XSrb36gZZN{[XluIFnDOVAhRSByLkGwPEDPxE1w MmjJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MUG3O|EoRjJ|NkGxO|cyRC:jPh?=
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insect cells NFTBbVdHfW6ldHnvckBie3OjeR?= NYrabGhDOzBibXnudy=> MlntTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCDQlyxJG0{PTGWIH31eIFvfCCneIDy[ZN{\WRiaX6gbY5{\WO2IHPlcIx{KGGodHXyJFMxKG2rboOgZpkhTlKHVDDhd5NigSxiSVO1NEA:KDBwMUG0N{DPxE1w MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzNyMUewN{c,OjN|MEG3NFM9N2F-
insect cells NEDYd4RHfW6ldHnvckBie3OjeR?= NWSx[G5vOzBibXnudy=> NX3OXGhrUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDBRmwyKFF{NULIJI12fGGwdDDlfJBz\XO|ZXSgbY4hcW6|ZXP0JINmdGy|IHHmeIVzKDNyIH3pcpMh[nliRmLFWEBie3OjeTygTWM2OCB;IECuNVE2KM7:TT6= NEP4V2c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{OwNVcxOyd-MkOzNFE4ODN:L3G+
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... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-STAT3 / STAT3 / p-STAT5 / STAT5; 

PubMed: 18981115     


For phospho-STAT3 and Phospho-STAT5 detection, cells were then activated for 6 hrs with anti-CD3 and anti-CD28 Ab. Equivalent amounts of protein from cell lysates were separated by SDS-PAGE and western blot analysis was then performed using anti-phospho S䲧疝Ỵ疞㧀疜膉痘 瘿뙠ෆᾰƌෆĀ 㺣痖帉痖

p-ZAP70 / ZAP70 / p-LAT / LAT; 

PubMed: 18981115     


For the analysis of imatinib interference with early TCR signaling events, cells were activated for 5 min with anti-CD3 and anti-CD28 Abs and blots were probed with anti-phospho ZAP70, anti-ZAP70, anti-phospho LAT or anti-LAT antibodies. Untreated, non-ac䲧疝Ỵ疞㧀疜膉痘 瘿�෋ᾰƌ෋à 

18981115
Immunofluorescence
RelB; 

PubMed: 20371728     


Nuclear proteins were extracted from the untreated and treated cells and nuclear levels of RelA and RelB were confirmed by immunocytochemistry 

Cortactin / F-actin; 

PubMed: 20937825     


NIH3T3-SrcY527F cells were treated with DMSO or with 10 μm STI571 for 16 h, fixed and co-stained for cortactin (red, left panels) and F-actin (green, middle panels). Merged fields (right panels) demonstrate co-localization between cortactin and F-actin at䲧疝Ỵ疞㧀疜

20371728 20937825
Growth inhibition assay
Cell viability ; 

PubMed: 28435223     


(C) K562 cells were treated with imatinib (0–10 μM) alone or imatinib and BEZ235 (0.2 μM) for 48 h and subjected to MTS assay. (D) KBM7R cells were treated with imatinib (0–10 μM) alone or imatinib and BEZ235 (0.2 μM) for 48 h and subjected to MTS assay. 䲧疝Ỵ疞㧀疜膉痘 瘿�෋ᾰƌ෋à 㺣痖帉痖Ѐ瑖堘𢡄빢᎒෋à鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤瘯Ɖ뾠Ղ䐺

28435223
体内研究 Imatinib抑制从新鲜的人小细胞肺癌外科样品来源的SCLC6,SCLC61和SCLC108异种移植肿瘤,抑制率分别是80%,40%和78%,且对SCLC74生长长无显著抑制。[5] 在高脂肪喂养的ApoE(-/-)小鼠中,通过管饲法给药10 mg/kg,20 mg/kg和40 mg/kg Imatinib,和对照组相比高脂诱导的脂质染色区域减少了30%,27%和35%,并且颈动脉脂质积聚得到抑制。[6]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
- 合并

PDGF受体激酶活性 :

PDGF受体是由BALB / c3T3细胞提取物免疫共沉淀所得,通过兔抗PDGF受体冰上处理2小时所得。蛋白A-琼脂糖珠被用于收集抗原-抗体复合物。免疫沉淀物用TNET(50 mM Tris,pH 7.5,140 mM氯化钠,5mM的EDTA,1%的Triton X-100)洗涤两次,用TNE(50 mM Tris,pH 7.5,140 mM EDTA)洗涤一次,并用激酶缓冲液(20 mM的Tris,pH 7.5, 10 mM氯化镁)洗涤一次。用PDGF(50 ng/mL)在4℃下刺激10分钟后,不同浓度的药物加入到反应混合物中。PDGF受体激酶活性是通过温浴10 μCi [33P]-ATP和l μM ATP 10分钟来确定。免疫复合物经SDS-PAGE上的7.5%凝胶上分离。
细胞实验:[3]
- 合并
  • Cell lines: BON-1 和 NCI-H727细胞
  • Concentrations: 约100 μM
  • Incubation Time: 48小时
  • Method: BON-1细胞和NCI-H727细胞接种到平底96孔板中三个复孔,并在含10%胎牛血清的DMEM或RPMI1640完全培养基中贴壁过夜,然后更换为血清培养基(阴性对照)或含不同浓度梯度Imatinib的无血清培养基。48小时(对照培养物没有达到汇合)后,代谢活性细胞的数量是由3-(4,5-二甲基吡啶-2-基)-2,5-二苯基溴化测定,由帕卡德光谱酶标仪测定540nm处吸光度。生长抑制通过以下公式计算:抑制率=(1 − a / b) × 100%,其中a和b分别是治疗组和对照组的吸光度值。
    (Only for Reference)
动物实验:[5]
- 合并
  • Animal Models: SCLC6, SCLC61, SCLC 74 and SCLC108 小细胞肺癌注入瑞士小鼠 (nu/nu, 雌性)。
  • Dosages: 70或100 mg/kg
  • Administration: 腹腔注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 118 mg/mL (200.09 mM)
Water 118 mg/mL (200.09 mM)
Ethanol Insoluble

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 589.71
化学式

C29H31N7O.CH4SO3

CAS号 220127-57-1
储存条件 粉状
溶于溶剂
别名 Gleevec, Glivec, CGP-57148B

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02687425 Unknown status Drug: Pioglitazone|Drug: imatinib mesylate Leukemia Myelogenous Chronic BCR-ABL Positive Meng Li|Tongji Hospital February 2016 Phase 2
NCT02303899 Unknown status Drug: Gemcitabine|Drug: Imatinib mesylate Mesothelioma Malignant Istituto Clinico Humanitas November 2014 Phase 2
NCT01898377 Terminated Drug: Imatinib mesylate Mycophenolate mofetil Chronic Graft-versus-host Disease Seoul National University Hospital August 2013 Phase 2
NCT02891395 Completed Drug: Imatinib Mesylate and Nilotinib Graft Versus Host Disease University Hospital Lille|Novartis December 24 2012 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID