Imatinib (STI571)

For research use only. Not for use in humans.

目录号:S2475 别名: Gleevec, Glivec, CGP057148B 中文名称:伊马替尼

Imatinib (STI571) Chemical Structure

CAS No. 152459-95-5

Imatinib (STI571, CGP057148B, ST-1571)是一种多靶点酪氨酸激酶抑制剂,抑制v-Abl、c-Kit和PDGFR的IC50分别为0.6,0.1和0.1 μM。Imatinib (STI571) 可诱导自噬。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 746.33 现货
RMB 571.38 现货
RMB 980.11 现货
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客户使用Selleck生产的Imatinib (STI571)发表文献222篇:

产品安全说明书

PDGFR抑制剂选择性比较

生物活性

产品描述 Imatinib (STI571, CGP057148B, ST-1571)是一种多靶点酪氨酸激酶抑制剂,抑制v-Abl、c-Kit和PDGFR的IC50分别为0.6,0.1和0.1 μM。Imatinib (STI571) 可诱导自噬。
特性 Imatinib 是多靶点酪氨酸激酶抑制剂。
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

体外抑制一组酪氨酸和丝/苏氨酸蛋白激酶实验,说明Imatinib有效抑制v-Abl 酪氨酸激酶和PDGFR,IC50 分别为 0.6 和 0.1 μM。[1]Imatinib抑制 野生型 c-kit激酶活性的SLF依赖性激活,IC50约为0.1 μM, 与抑制PDGFR所需的浓度相似。[2] Imatinib 抑制人类支气管类癌细胞NCI-H727和胰腺类癌细胞 BON-1生长,IC50分别为 32.4 和 32.8 μM。[3] 最新研究显示Imatinib作用于慢性粒细胞白血病,通过下调hERG1 K(+)通道,具有恢复其抗白血病效果的潜力,而hERG1 K(+) 通道在白血病细胞中高表达,且易引发白血病。[4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
LAMA-84 MnTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvvR3pKSzVyPUCuNFc{ODRizszN NGjrSXA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6PDFxJ{7TRW5ITVJ:L3G+
EM-2 NFe3bldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknRTWM2OD1yLkC4PFgh|ryP MmHmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVQyNyd-U1HOS2VTRC:jPh?=
MEG-01 Ml;CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnlWoFHUUN3ME2wMlA5QTJzIN88US=> NIDFeXk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6PDFxJ{7TRW5ITVJ:L3G+
BV-173 M4Hldmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTBwMUi3OEDPxE1? MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5OFEwLz6VQV7HSXI9N2F-
K-562 M1fJeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vDUmlEPTB;MD6yNlQ{OiEQvF2= MljyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVQyNyd-U1HOS2VTRC:jPh?=
CGTH-W-1 NV35SmY4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2X5V2lEPTB;MD6zPFM4PCEQvF2= NIG4WnM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6PDFxJ{7TRW5ITVJ:L3G+
ST486 M4rlZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXxTWRKSzVyPUCuOlg2PCEQvF2= MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5OFEwLz6VQV7HSXI9N2F-
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NCI-H1770 NIHtNZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEe2S5lKSzVyPUWuOVczPjJizszN NELpZW49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6PDFxJ{7TRW5ITVJ:L3G+
IMR-5 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;ZR3hKSzVyPU[uNlIyPDdizszN Mo\2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVQyNyd-U1HOS2VTRC:jPh?=
LB2241-RCC NEjkemhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\DPGlEPTB;OD6wO|M5PCEQvF2= NE\XN3A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6PDFxJ{7TRW5ITVJ:L3G+
TGBC24TKB NFXMNIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYH3TFhNUUN3ME24MlM1ODV{IN88US=> MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5OFEwLz6VQV7HSXI9N2F-
SCC-15 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7ETW5KSzVyPUGwMlc4QDhizszN M3foXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk1OS9pPmPBUmdGWjxxYU6=
BB49-HNC NEXERWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TLNWlEPTB;MUSuN|M{PSEQvF2= MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5OFEwLz6VQV7HSXI9N2F-
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LB2518-MEL M3j1O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTF4Lk[wPVQh|ryP MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5OFEwLz6VQV7HSXI9N2F-
NCI-H510A NVqxUI1QT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPjTYNYUUN3ME2xO{4zPDR{IN88US=> M{\2WlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk1OS9pPmPBUmdGWjxxYU6=
TE-441-T NFvtUodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYrsVIdEUUN3ME2xO{4zQDh4IN88US=> NEj2cpU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6PDFxJ{7TRW5ITVJ:L3G+
HH MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPLTWM2OD1zNz6zPVk6KM7:TR?= NW\keHA1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTRzLze+V2FPT0WUPD;hQi=>
LC4-1 M{iwfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTF6LkC2OVIh|ryP M1\iWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk1OS9pPmPBUmdGWjxxYU6=
KARPAS-45 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfXe3REUUN3ME2xPE4yQDR6IN88US=> MljTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVQyNyd-U1HOS2VTRC:jPh?=
LB1047-RCC MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7IeGtKSzVyPUG4MlQ1PTJizszN MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5OFEwLz6VQV7HSXI9N2F-
NKM-1 M3TBfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3NTWM2OD1zOT6zOVUzKM7:TR?= MlXDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVQyNyd-U1HOS2VTRC:jPh?=
SCLC-21H NHq4T2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\5cWlEPTB;MkCuNVI1PiEQvF2= NIjpXGg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6PDFxJ{7TRW5ITVJ:L3G+
RS4-11 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTJyLkOzNFgh|ryP NY\wTFVZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTRzLze+V2FPT0WUPD;hQi=>
ALL-PO MoSzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\wTWM2OD1{MD64NVQ6KM7:TR?= NEfZWI09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6PDFxJ{7TRW5ITVJ:L3G+
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DMS-79 M2LGXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIO4OohKSzVyPUK0MlQ6OzRizszN NGLk[II9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6PDFxJ{7TRW5ITVJ:L3G+
MPP-89 NWLUVFNKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXNN3dLUUN3ME2yOU43QDd2IN88US=> Ml7rQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVQyNyd-U1HOS2VTRC:jPh?=
NB10 NV7aZpZUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzGWHZxUUN3ME2yOk41Pjl7IN88US=> MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5OFEwLz6VQV7HSXI9N2F-
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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 STAT3, anti-STAT3, anti-phospho STAT5 or anti-STAT5 Abs.

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-activated cells were used as controls (NA).

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 STAT3, anti-STAT3, anti-phospho STAT5 or anti-STAT5 Abs.

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-activated cells were used as controls (NA).

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 invadopodia.

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 invadopodia.

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. Mean ± SD. n=3. *P<0.05, compared to the control group. #P<0.05, compared to the group of IM alone. Abbreviations: IM, imatinib; SD, standard deviation.

28435223
体内研究

Imatinib作用于三种从新鲜人类小细胞肺癌衍生的移植瘤,具有不同的抗肿瘤效果,抑制SCLC6, SCLC61和 SCLC108 肿瘤生长分别达80%, 40% 和78%,而对SCLC74 生长没有明显抑制效果。[5] Imatinib 处理高脂肪饲喂的ApoE(-/-)小鼠, 显著降低高脂肪诱导的脂质染色区,按10,20和 40 mg/kg剂量饲喂,与未经高脂肪饮食处理的对照组相比,脂质染色区分别降低 30%, 27% 和 35%,且抑制颈动脉脂质堆积。[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 :

从BALB/c 3T3 细胞抽提物中使用兔抗血清免疫沉淀PDGF受体,然后小鼠PDGF受体置于冰上2小时。使用蛋白A-琼脂糖磁珠,用于收集抗原-抗体复合体。使用TNET (50 mM Tris, pH 7.5, 140 mM NaCl, 5 mM EDTA, 1% Triton X-100)冲洗免疫沉淀反应两次,,使用TNE (50 mM Tris, pH 7.5, 140 mM EDTA)冲洗一次,再使用激酶 buffer (20 mM Tris, pH 7.5,10 mM MgCl2)冲洗一次。在 4oC下使用PDGF(50 ng/mL)刺激10分钟,在反应混合物中加入不同浓度Imatinib。与10 μCi [7-33P]-ATP及l μM ATP 在4oC下温育10分钟,然后测定PDGF受体激酶活性。通过 SDS-PAGE 在7.5% 凝胶上分离免疫复合物。
细胞实验:

[3]

- 合并
  • Cell lines: BON-1 和 NCI-H727 细胞
  • Concentrations: 0 到 100 μM
  • Incubation Time: 48 小时
  • Method:

    BON-1 细胞和 NCI-H727 细胞按一式三份接种在平底96孔板上,分别在补充10%胎牛血清的 DMEM 或 RPMI 1640 完全培养基中粘附过夜,更换培养基为无血清培养基(阴性对照) 或含连续稀释Imatinib的无血清培养基。48小时后 (对照组细胞不汇合),通过MTT实验测定代谢活性细胞数,使用Packard Spectra 酶标仪在540 nm处测定吸光值。按如下公式计算抑制生长率: 抑制率=(1 − a / b) × 100%, a 和 b 分别为实验组和对照组的吸光值。


    (Only for Reference)

溶解度 (25°C)

体外 DMSO 33 mg/mL (66.85 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
2mg/mL

* 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 493.6
化学式

C29H31N7O

CAS号 152459-95-5
储存条件 粉状
溶于溶剂
别名 Gleevec, Glivec, CGP057148B

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