Imatinib (STI571) Mesylate

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

仅限科研使用

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。

Imatinib (STI571) Mesylate Chemical Structure

CAS: 220127-57-1

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
大包装 有超大折扣
大剂量询单有大折扣!

今日订购,明日送达 全国免运费 分装免费 分装成小规格产品(单支最小为1mg)
如1支10mg产品可分装为10支1mg产品

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的Imatinib (STI571) Mesylate发表文献212篇:

产品安全说明书

Bcr-Abl抑制剂选择性比较

相关Bcr-Abl产品

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 NFPBRpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LlXVk3KGh? M3vKeGlEPTB;MT63JO69VQ>? NX7xdFdFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFAzOTJpPkK0PVAxOjF{PD;hQi=>
K562 MoXzR5l1d3SxeHnjbZR6KEG|c3H5 NWTs[WNiOjRiaB?= NYXqRlF7UUN3ME2wMlIyKM7:TR?= M4DhWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MECwNlA4Lz5{MkCwNFIxPzxxYU6=
MCF-7 MVPDfZRwfG:6aXPpeJkhSXO|YYm= M{S2W|I1KGh? M{TFO2lEPTB;MD64N{DPxE1? NV3kPG03RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKwNFAzODdpPkKyNFAxOjB5PD;hQi=>
MDA-MB-23 MnvkR5l1d3SxeHnjbZR6KEG|c3H5 NF;xTm8zPCCq NYXMV5NuUUN3ME2xMlgh|ryP M33VdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MECwNlA4Lz5{MkCwNFIxPzxxYU6=
K562r NWTI[5hzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWrqcllxUUN3ME2xNOKh|ryP MoD6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7M{m0NVgoRjJ2OUO5OFE5RC:jPh?=
K562 NEfZfHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rER2VEPTB;MD6wPUDPxE1? NWr4NIQyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[2O|g1OTRpPkG2Olc5PDF2PD;hQi=>
MCF-7 Mly2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XHXlExKM7:TR?= MVu0PEBp NEXOdI9jdG:la4OgZ4VtdCCycn;sbYZmemG2aX;uJIlv[3KnYYPlJIlv\HWlZXSgZpkhSkp|Wh?= MnHUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{N{SwN|QoRjJ3Mke0NFM1RC:jPh?=
K-562  NXf5V2p7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHHTWM2OD1zIN88US=> NFG1PIg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKzPVY3Oid-MkWyN|k3PjJ:L3G+
K562  M3vrbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXTb4JKSzVyPUCuOeKh|ryP MmPoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7M{m0NVgoRjJ2OUO5OFE5RC:jPh?=
PC3  M{i3UmFxd3C2b4Ppd{BCe3OjeR?= M{\vd|Ix6oDLzszN NUHv[nZSPDhxN{KgbC=> NXP4SJdFcW6lcnXhd4V{KGOnbHygd5Vzfmm4YXy= M1\kNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{i2OlU3Lz5{NUe4OlY2PjxxYU6=
PC3  MnzkR4VtdCCYaXHibYxqfHliQYPzZZk> NYTqU5dLOjEkgJpOwG0> MmS1Ok04OiCq NVfYXHhpcW6lcnXhd4V{KGOnbHygeoli[mmuaYT5 NVfC[FU3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3PFY3PTZpPkK1O|g3PjV4PD;hQi=>
DU145 NHjicIJCeG:ydH;zbZMhSXO|YYm= NWDtW4hYOjEkgJpOwG0> NYHtfIk1PDhxN{KgbC=> NHTjelNqdmS3Y3XzJINmdGxiZHXheIgh[nliYYDvdJRwe2m| MmP4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5OE[2OVYoRjJ3N{i2OlU3RC:jPh?=
DU145 M3PMW2NmdGxiVnnhZoltcXS7IFHzd4F6 NVrDfJUzOjEkgJpOwG0> MmPHOk04OiCq NYjXRnBO\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5 MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd6Nk[1Okc,OjV5OE[2OVY9N2F-
Hep G2 NHztUlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoG3TWM2OD1|MTFOwG0> NU\YOohkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4OlMzOzJpPkK1PFY{OjN{PD;hQi=>
T47D  MlLoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonYTWM2OD13MDFOwG0> NIrpUm49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUi2N|I{Oid-MkW4OlMzOzJ:L3G+
EOL-1 MmewR5l1d3SxeHnjbZR6KGG|c3H5 MoO3O|IhcHK| NInp[WxEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBGV0xvMTDj[YxteyCjZoTldkA4OiCqcoOgZpkh[WyjbXHyMYJtfWViY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTBiPTCwMlAxODJizszNMi=> M{LQRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7M{CxPVAzLz5zOUOwNVkxOjxxYU6=
EOL-1 MlTGRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MnHEO|IhcHK| MoT1RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCHT1ytNUBk\WyuczDh[pRmeiB5MjDodpMh[nliQ3XscHRqfGW{LVfsc{BweiCFQ1utPEBie3OjeTygS2k2OCB;IECuNFAyKM7:TT6= M1;mWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUS0NVQ6Lz5{OUW0OFE1QTxxYU6=
GISTT1 MYDBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NUHZS4hyPzJiaILz MoGwRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCJSWPUWFEh[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliY3XscEB1cXSncj3ncI8h[XO|YYmsJGdKPTBiPTCwMlAxOyEQvF2u NUCySY17RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki1OFE3QTVpPkK4OVQyPjl3PD;hQi=>
Sf9 M4XZcmZ2dmO2aX;uJIF{e2G7 MWTCbY5lcW6pIHHm[olvcXS7IITvJIh2dWGwIHHjeIl3\SC|aYTlJI9nKE5vdHXycYlv[WxiaHX4ZYhqe3SrZHnu[U11[WepZXSgRWJNOiCneIDy[ZN{\WRiaX6gWJJq[2ixcHz1d4liKG6rIHnu[oVkfGWmIGPmPUBk\WyuczDifUBqe2:2aHXycYFtKHSrdILheIlwdiClYXzvdolu\XS{aXOgZZN{[XluIFvkJF0hOC5yME[g{txONg>? NVLSSG82RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG0NVc{PDNpPkKxOFE4OzR|PD;hQi=>
K562 NH3LcW5CdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MmPQRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCrbXH0bY5q[i2{ZYPpd5RidnRiS{W2NkBk\WyuczygTWM2OCB;IECuNFA3ODVizszNMi=> MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN5NkW4O{c,OjF|N{[1PFc9N2F-
GISTT1 NEGyZWtCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NVTGXWlCPzJiaILz M1q0[mFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgZ2tKXCCmZYDlcoRmdnRiaIXtZY4hT0mVVGSxJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBi\nSncjC3NkBpenNiYomgZ4VtdHSrdHXyMYdtdy:FQ1u4JIF{e2G7LDDHTVUxKD1iMD6wNFgh|ryPLh?= MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzB5N{ewOUc,OjdyN{e3NFU9N2F-
GISTT1 M{TkW2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 MUG3NkBpenN? NVT0epJESW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDHTXNVXDFiY3XscJMhdWWjc4Xy[YQh[W[2ZYKgO|IhcHK|IHL5JGNmdGyWaYTldk1IdG9ib4KgR2NMQCCjc4PhfUwhT0l3MDC9JFAvODB6IN88UU4> MkTyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7Nk[5OVQoRjJ5OU[2PVU1RC:jPh?=
GISTT1 NHv4XVlHfW6ldHnvckBie3OjeR?= MXy3NkBpenN? NHvq[ZlKdmirYnn0bY9vKG:oIFvJWEBqdiCqdX3hckBIUVOWVEGgZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IGPSRkBie3OjeTygS2k2OCB;IECuNFEh|ryPLh?= M13HUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{ezNVU{Lz5{M{e3N|E2OzxxYU6=
BAF3 NH\Nb|ZHfW6ldHnvckBie3OjeR?= M1WyWlczKGi{cx?= M1HOOGlvcGmkaYTpc44hd2ZiVFXMMYZ2e2WmIGDES2ZT[WyyaHGgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4hdW:3c3WgRmFHOyClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDj[YxtKHSrdHXyMYdtdyCjc4PhfUwhT0l3MDC9JFAvODFyNzFOwG0v MkLyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh3NEG2PVUoRjJ6NUSxOlk2RC:jPh?=
TF1 MVfDfZRwfG:6aXPpeJkh[XO|YYm= NHPLZ3pEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBVTjFiY3XscJMh\XiycnXzd4lv\yClLVvJWEBufXSjdHnvckBie3Onc4Pl[EBieyClZXzsJJZq[WKrbHn0fUwhUUN3MDC9JFAvODF|IN88UU4> M2HUc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MkKxNlAyLz5{MkKyNVIxOTxxYU6=
GIST882 MV7BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MX:3NkBpenN? MVrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHPLTXQh\GWyZX7k[Y51KGi3bXHuJGdKW1R6OEKgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGOnbHygeoli[mmuaYT5JIFnfGW{IEeyJIhzeyCkeTDj[YxtfGm2ZYKt[4xwN0OFS{igZZN{[XluIFfJOVAhRSByLkCxOEDPxE1w Mn;iQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyN{e3NFUoRjJ5MEe3O|A2RC:jPh?=
GIST882 M3HhOGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NYfpR3U5PzJiaILz MWnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEeLU2S4PFIh[2WubIOgcYVie3W{ZXSgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8hd3JiQ1PLPEBie3OjeTygS2k2OCB;IECuNFE1KM7:TT6= NYDjPWVORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke5OlY6PTRpPkK3PVY3QTV2PD;hQi=>
BA/F3 M2OxOWZ2dmO2aX;uJIF{e2G7 NGjqbZA4OiCqcoO= M3SzUWlvcGmkaYTpc44hd2ZiS3n0JIV5d25iMUGg[IVt\XSrb36gLFU2PyC2bzC1OVghemW|aXT1[ZMqKG23dHHueEApfW6tbn;3ckBwemmpaX6pJJRz[W6|ZnXjeIVlKGmwIH3veZNmKEKDL1[zJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3XscEBoem:5dHigbY5kfWKjdHXkJIZweiB5MjDodpMh[nliTWTTJIF{e2G7LDDHTVUxKD1iMD6wNVch|ryPLh?= M1\oNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkC0OFQyLz5|MEKwOFQ1OTxxYU6=
BA/F3 M2TJW2Z2dmO2aX;uJIF{e2G7 NX\TSWJoPzJiaILz NX3HOGRUUW6qaXLpeIlwdiCxZjDUSWwu\nW|ZXSgVGRITlKkZYThJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW|c3XkJIlvKG2xdYPlJGJCN0Z|IHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJvR3zvJI9zKEOFSz24JIF{e2G7LDDHTVUxKD1iMD6wNVkh|ryPLh?= NXrFWVB{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1OFQyPDlpPkK5OVQ1OTR7PD;hQi=>
BAF3 NFLnbmVHfW6ldHnvckBie3OjeR?= Ml;1O|IhcHK| MUXJcohq[mm2aX;uJI9nKFSnbD3meZNm\CCSRFfGVk1j\XSjIDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJGJCTjNiY3XscJMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25ibXXhd5Vz\WRiYX\0[ZIhPzJiaILzJIJ6KEOnbHzUbZRmei2JbH:gc5IhS0ONODDhd5NigSxiR1m1NEA:KDBwMEG5JO69VS5? MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzl4Nkm1OEc,Ojd7Nk[5OVQ9N2F-
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primary leukemia cells M3HSWGN6fG:2b4jpZ4l1gSCjc4PhfS=> MWK3NkBpenN? NH\uVnlEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBxemmvYYL5JIxmfWunbXnhJINmdGy|IHnzc4xifGWmIH\yc40h[WO3dHWgcZlmdG:rZDDs[ZVs\W2rYTDwZZRq\W62IHX4dJJme3Orbnege4lt\CC2eYDlJGZNXDNiYYPz[ZN{\WRiYYOgZ4VtdCC4aXHibYxqfHliYX\0[ZIhPzJiaILzJIJ6KGy3Y3nm[ZJie2ViYYPzZZktKEmFNUCgQUAxNjFizszNMi=> NX7aXG86RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyNlEzODFpPkKyNlIyOjBzPD;hQi=>
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insect cells NFXpTYlHfW6ldHnvckBie3OjeR?= NIO0cXM{OCCvaX7z MlXaTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCDQlyxJG0{PTGWIH31eIFvfCCneIDy[ZN{\WRiaX6gbY5{\WO2IHPlcIx{KGGodHXyJFMxKG2rboOgZpkhTlKHVDDhd5NigSxiSVO1NEA:KDBwMUG0N{DPxE1w MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzNyMUewN{c,OjN|MEG3NFM9N2F-
insect cells M1GzRmZ2dmO2aX;uJIF{e2G7 NV\IXmhqOzBibXnudy=> MkLoTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCDQlyxJHEzPTKKIH31eIFvfCCneIDy[ZN{\WRiaX6gbY5{\WO2IHPlcIx{KGGodHXyJFMxKG2rboOgZpkhTlKHVDDhd5NigSxiSVO1NEA:KDBwMUG1JO69VS5? M1GyTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{CxO|A{Lz5{M{OwNVcxOzxxYU6=
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Assay
Methods Test Index PMID
Western blot p-STAT3 / STAT3 / p-STAT5 / STAT5 p-ZAP70 / ZAP70 / p-LAT / LAT 18981115
Immunofluorescence RelB Cortactin / F-actin 20371728 20937825
Growth inhibition assay Cell viability 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]
  • 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]
  • 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。
动物实验:[5]
  • 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

溶解度(25°C)

体外

* 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 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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)

mg/kg g μL

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
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

摩尔浓度计算器

质量 浓度 体积 分子量

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 Completed 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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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