BI 2536

For research use only. Not for use in humans.

目录号:S1109

BI 2536 Chemical Structure

CAS No. 755038-02-9

BI-2536是一种有效的Plk1抑制剂,无细胞试验中IC50为0.83 nM。BI-2536可抑制 Bromodomain 4 (BRD4) ,其Kd值为37 nM,并有效地抑制 c-Myc 的表达。BI-2536可诱导凋亡而减弱自噬。Phase 2。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1978.87 现货
RMB 981.57 现货
RMB 1704.35 现货
RMB 5492.59 现货
RMB 8160.83 现货
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客户使用Selleck生产的BI 2536发表文献209篇:

产品安全说明书

PLK抑制剂选择性比较

生物活性

产品描述 BI-2536是一种有效的Plk1抑制剂,无细胞试验中IC50为0.83 nM。BI-2536可抑制 Bromodomain 4 (BRD4) ,其Kd值为37 nM,并有效地抑制 c-Myc 的表达。BI-2536可诱导凋亡而减弱自噬。Phase 2。
特性 BI 2536是第一个有效的Plk1选择性抑制剂,抑制 Plk1的标记。
靶点
c-Myc [3]
()
PLK1 [1]
(Cell-free assay)
PLK2 [1]
(Cell-free assay)
PLK3 [1]
(Cell-free assay)
BRD4 [3]
(Cell-free assay)
0.83 nM 3.5 nM 9.0 nM 37 nM(Kd)
体外研究

除了Plk1, BI 2536也抑制 Plk2 和Plk3活性,只是抑制程度低点,IC50分别为3.5 nM和9.0 nM。BI 2536比一组63种其他蛋白激酶(IC50>10 μM)选择性高1000多倍。BI 2536 按10 nM 到 100 nM剂量作用于HeLa细胞,抑制有丝分裂中心体中γ-微管蛋白招募和Apc6 磷酸化,抑制染色体臂中释放黏结蛋白, 诱导产生单极主轴,及一些依赖Plk1的其他有丝分裂过程。与作用于Plk1 RNAi效果相一致, BI 2536处理HeLa细胞,使细胞周期停在G2/M期, 随后DNA分解及凋亡,且累积断裂的PARP p85片段,这种作用存在浓度依赖性。BI 2536抑制一组32种人肿瘤细胞系生长,EC50为2-25 nM,抑制指数生长的hTERT-RPE1,人脐静脉内皮细胞 (HUVECs),和正常大鼠肾脏(NRK) 细胞的增殖,EC50为12-31 nM。[1] BI 2536 抑制Plk1,降低甲状腺未分化癌(ATC)细胞如 CAL62, OCUT-1, SW1736, 8505C,和 ACT-1 的生长的生长和活力,EC50为1.4-5.6 nM。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
PSN1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3nieGlEPTB;MD6wNFc4PiEQvF2= NGrXSIM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2OTN7MEmvK|5USU6JRWK8M4E,
ACN MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfaTHpmUUN3ME2wMlAxQDR|IN88US=> MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1NVM6ODlxJ{7TRW5ITVJ:L3G+
TE-8 NX7CZ2xIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPsPVRKSzVyPUCuNFA6PDFizszN MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1NVM6ODlxJ{7TRW5ITVJ:L3G+
LC-2-ad NWLrWFJ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTBwMEGwPVMh|ryP MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1NVM6ODlxJ{7TRW5ITVJ:L3G+
ALL-PO MmPxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HLdWlEPTB;MD6wNVMh|ryP NFXG[Ik9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2OTN7MEmvK|5USU6JRWK8M4E,
EW-16 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjwTWM2OD1yLkCxN|M3KM7:TR?= NGi0UVA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2OTN7MEmvK|5USU6JRWK8M4E,
KM12 NFn4SIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3L[VdFUUN3ME2wMlAyOzR6IN88US=> NIq2SXM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2OTN7MEmvK|5USU6JRWK8M4E,
GI-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPQOHV6UUN3ME2wMlAyOzh|IN88US=> NF\kUFg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2OTN7MEmvK|5USU6JRWK8M4E,
LS-411N NFfNdHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;uc4lKSzVyPUCuNFE1ODdizszN MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1NVM6ODlxJ{7TRW5ITVJ:L3G+
ES8 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPlUJhKSzVyPUCuNFE1QTRizszN M3vRV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFUyOzlyOT:nQnNCVkeHUkyvZV4>
SNU-C2B MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{Di[2lEPTB;MD6wNVUzPiEQvF2= MnTuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVE{QTB7Lze+V2FPT0WUPD;hQi=>
CESS NHjLWpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLzV|ZKSzVyPUCuNFE3ODJizszN NVz0THllRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTF|OUC5M{c,W0GQR1XSQE9iRg>?
697 NG[1NnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmSyTWM2OD1yLkCxOlY5KM7:TR?= MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1NVM6ODlxJ{7TRW5ITVJ:L3G+
NCI-H1963 MoXzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\LTWM2OD1yLkCxOlc{KM7:TR?= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1NVM6ODlxJ{7TRW5ITVJ:L3G+
IA-LM NWHiO3pNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LRRmlEPTB;MD6wNVY5QCEQvF2= MnrjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVE{QTB7Lze+V2FPT0WUPD;hQi=>
SW954 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVS1RnpjUUN3ME2wMlAyPzB3IN88US=> NEXoc4Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2OTN7MEmvK|5USU6JRWK8M4E,
RL95-2 M2fzWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPp[ZlyUUN3ME2wMlAyPzN6IN88US=> MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1NVM6ODlxJ{7TRW5ITVJ:L3G+
LXF-289 NGXSSZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTBwMEG3O{DPxE1? M4HUSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFUyOzlyOT:nQnNCVkeHUkyvZV4>
OCUB-M NYPCNYpsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTBwMEG4NlYh|ryP MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1NVM6ODlxJ{7TRW5ITVJ:L3G+
RKO M3Hjfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjnTJR{UUN3ME2wMlAyQTh5IN88US=> M1nse|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFUyOzlyOT:nQnNCVkeHUkyvZV4>
LOUCY NXLOeGl5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXie3QyUUN3ME2wMlAzODVizszN NG\IS|E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2OTN7MEmvK|5USU6JRWK8M4E,
NOS-1 MofMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIrWcGZKSzVyPUCuNFIxQTNizszN MlTJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVE{QTB7Lze+V2FPT0WUPD;hQi=>
A4-Fuk M1yyfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFe4TI9KSzVyPUCuNFIzOThizszN M1PqeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFUyOzlyOT:nQnNCVkeHUkyvZV4>
A388 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{[1fmlEPTB;MD6wNlIzPyEQvF2= NGfpemc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2OTN7MEmvK|5USU6JRWK8M4E,
TE-9 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzMTWM2OD1yLkCyNlYyKM7:TR?= MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1NVM6ODlxJ{7TRW5ITVJ:L3G+
KURAMOCHI M1LCOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGT3fYVKSzVyPUCuNFIzQDVizszN MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1NVM6ODlxJ{7TRW5ITVJ:L3G+
KALS-1 NI\QNIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPHdGN5UUN3ME2wMlAzOzN6IN88US=> MmrzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVE{QTB7Lze+V2FPT0WUPD;hQi=>
HOP-62 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\0T2ZKSzVyPUCuNFI1OiEQvF2= MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1NVM6ODlxJ{7TRW5ITVJ:L3G+
RPMI-8402 NX;5ZmJ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnBVZAxUUN3ME2wMlAzPTB6IN88US=> MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1NVM6ODlxJ{7TRW5ITVJ:L3G+
TE-1 MmjmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4ToRmlEPTB;MD6wNlUyOiEQvF2= MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1NVM6ODlxJ{7TRW5ITVJ:L3G+
CCRF-CEM NIC1U5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTBwMEK1OFMh|ryP M3nUb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFUyOzlyOT:nQnNCVkeHUkyvZV4>
HUTU-80 MofaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYK2PZlyUUN3ME2wMlAzPjJ2IN88US=> NF7qW3U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2OTN7MEmvK|5USU6JRWK8M4E,
NCI-H1648 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTBwMEK2OFch|ryP Mm\DQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVE{QTB7Lze+V2FPT0WUPD;hQi=>
HCE-4 M4L2PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorvTWM2OD1yLkCyOlgzKM7:TR?= MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1NVM6ODlxJ{7TRW5ITVJ:L3G+
ETK-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnG4TWM2OD1yLkCyO|M3KM7:TR?= MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1NVM6ODlxJ{7TRW5ITVJ:L3G+
TE-15 MnPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTBwMEK3N|gh|ryP M2[1TlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFUyOzlyOT:nQnNCVkeHUkyvZV4>
BE-13 NFT6NGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHyV3QzUUN3ME2wMlAzPzRizszN NGrLXnQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2OTN7MEmvK|5USU6JRWK8M4E,
KE-37 M2ixW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17leWlEPTB;MD6wNlc1OSEQvF2= NXjzNpIzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTF|OUC5M{c,W0GQR1XSQE9iRg>?
NCI-H1355 NID4cmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTBwMEK3PFMh|ryP NV25VmRRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTF|OUC5M{c,W0GQR1XSQE9iRg>?
TE-11 NEHxdpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVrheoFUUUN3ME2wMlAzQDB7IN88US=> MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1NVM6ODlxJ{7TRW5ITVJ:L3G+
BL-70 NWHHTI9CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;wWGlEPTB;MD6wNlg2PyEQvF2= MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1NVM6ODlxJ{7TRW5ITVJ:L3G+
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SIL-ALL NY\WOVBmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYqyOEBp MYLJR|UxRTF7OT63O{BvVQ>? NWnQNGZHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1NVk6QTVpPkK0OVE6QTl3PD;hQi=>
CEM M4rwZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEn2elQzPCCq MX;JR|UxRTV{LkG4JI5O MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDVzOUm5OUc,OjR3MUm5PVU9N2F-
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SIL-ALL MkP4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HVWlQ5KGh? NIXRSGdKSzVyPUe0MlYzKG6P M{TwN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUG5PVk2Lz5{NEWxPVk6PTxxYU6=
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... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
pro-caspase-8 / cleaved caspase-8 / cleaved caspase-3 / cleaved caspase-9; 

PubMed: 27699933     


PLKi‐induced caspase activation. HeLa cells were treated with BI 2536 (10 nmol/L), BI 6727 (68 nmol/L), or GSK461364 (11 nmol/L), and HCT 116 cells were treated with BI 2536 (20 nmol/L), BI 6727 (70 nmol/L), or GSK461364 (12 nmol/L) for 48 h. The levels of cleaved caspase (CASP)‐3, ‐8, and ‐9 were examined by Western blot analysis.

p-HH3 / PARP / Myc / p-Myc; 

PubMed: 24771642     


Western blotting showing more mitotic arrested (shown by phospho-histone H3) and apoptotic (shown by PARP) cells as well as lower MYC levels in LNCaP-Pim1 cells after BI 2536 treatment compared with LNCaP-Neo cells. The difference is obvious at lower dose of BI 2536 (10 nM). Both total MYC expression and phosphor-MYC levels were lower in Pim1 cells than Neo cells after BI 2536 treatment.

pMEK / MEK / pERK / ERK / pRSK1 / RSK1; 

PubMed: 28430578     


(A) and (B) Western blot analysis of the expression and activation of components of the MEK-ERK-RSK1 pathway in MKN45 and MKN74 cancer cells treated with BI 2536 and BI 6727 for 24 and 48 hours, respectively.

pPlk1 / Plk1 / pMyt1; 

PubMed: 28430578     


(A) and (B) Western blot analysis of the expression and phosphorylation of Plk1, and phosphorylation of Myt1 in the CSC-like and cancer cells after treatment with BI 2536 and BI 6727 for 24 and 48 hours, respectively.

Aurora B / pAurora B / pAurora C / pH3 / Cyclin B1 / Securin / pBcl-XL / MPM2; 

PubMed: 25169932     


Western blot analysis of cells treated for 24 h with the indicated inhibitor concentrations. Cell lysates were immunoblotted for Plk1, Phospho-Aurora B (T232)/Aurora C (T198), Aurora B, histone H3 phosphorylated at S10 (pH3), Cdk1, Cyclin B1, Securin, Phospho-Bcl-XL, Induced myeloid leukemia cell differentiation protein Mcl-1, MPM-2 and β-Actin. Left (Hela cells); Right (HUVEC)

27699933 24771642 28430578 25169932
Immunofluorescence
p-H2AX / propidium iodide; 

PubMed: 22309939     


Apoptotic images of the cells after BI 2536 treatment, as revealed by HCS (high-content screening) instrument (×10) with phospho-H2AX antibody or PI (propidium iodide) intake. 

Pericentrin / α-tubulin; 

PubMed: 21772266     


MEFs were labelled using Plk1, pericentrin and α-tubulin antibodies and 4,6-diamidino-2-phenylindole for the analysis by immunofluorescence microscopy. Representative examples of BI 2536-treated and control MEFs are depicted. Scale bar, 5 μm.

22309939 21772266
Growth inhibition assay
Cell viability; 

PubMed: 21772266     


Proliferative activity of MEFs at different BI 2536 concentrations (25–250 nM; means±s.d., n=3, for each concentration). *P<0.05, **P<0.01, ***P<0.001, Student's t-test, unpaired and two-tailed.

21772266
体内研究

BI 2536静脉注射给药多种移植瘤模型,每周一次或两次,效果都很好,通过使细胞周期停滞而抑制细胞增殖,随后诱导肿瘤细胞死亡。BI 2536按 50 mg/kg剂量处理HCT 116移植瘤,每周一次或两次,显著抑制肿瘤生长,T/C 分别为15%和0.3%。BI 2536每周处理两次BxPC-3和A549模型,也显著抑制肿瘤生长,T/C分别为5% 和14%。[1]

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

体外Plk1激酶实验:

重组人Plk1 (1-603残基) 作为氮端,携带杆状病毒表达系统的GST-标记的融合蛋白通过亲和层析,使用谷胱甘肽-琼脂糖而纯化。在梯度稀释的BI 2536存在时,使用 20 ng 重组激酶,及10 μg牛奶中的酪蛋白作为底物进行Plk1 酶活性实验。在终体积为60 μL 的混合物(15 mM MgCl2, 25 mM MOPS [pH 7.0], 1 mM DTT, 1% DMSO, 7.5 mM ATP, 0.3 μCi γ-33P-ATP)中30oC下进行激酶反应45分钟。加入 125 μL 冰冻的5% TCA终止反应。沉淀物转移到混合酯纤维素的多屏过滤板上,使用1% TCA冲洗实验板,然后利用放射性进行测量。绘制剂量反应曲线,而计算IC50值。
细胞实验:

[1]

- 合并
  • Cell lines: HeLa, A43, SKOV-3, HT-29, K562, A549, Saos-2, MCF7, HCT116, COLO 205, Hep G2, Raji, PC-3,等等
  • Concentrations: 溶于DMSO, 终浓度为~1 μM
  • Incubation Time: 24,和72小时
  • Method:

    使用不同浓度BI 2536处理细胞24和72小时。 在荧光分光光度计中测量Alamar Blue染料转换而测定细胞生长。为了测定培养基中DNA含量,细胞悬液在80%乙醇中混合, 使用溶于PBS的0.25% Triton X-100处理5分钟,然后与0.1% RNase 和溶于PBS的 10 μg/mL碘化丙啶在室温下温育20分钟。通过流式细胞仪分析而测定细胞周期谱。


    (Only for Reference)
动物实验:

[1]

- 合并
  • Animal Models: 皮下注射HCT 116, NCI-H460, 或A549 细胞的雌性BomTac:NMRI-Foxn1nu 小鼠
  • Dosages: ~50 mg/kg
  • Administration: 静脉注射,每周一到两次
    (Only for Reference)

溶解度 (25°C)

体外 Ethanol 100 mg/mL (191.69 mM)
DMSO 21 mg/mL (40.25 mM)
Water 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):
30% PEG 400+0.5% Tween 80+5% Propylene glycol
15mg/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 521.66
化学式

C28H39N7O3

CAS号 755038-02-9
储存条件 粉状
溶于溶剂
别名 N/A

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
NCT02215044 Terminated Drug: BI 2536 intravenous|Drug: Gemcitabine intravenous Pancreatic Neoplasms Boehringer Ingelheim June 2007 Phase 1
NCT02211833 Completed Drug: BI 2536|Drug: Pemetrexed Carcinoma Non-Small-Cell Lung Boehringer Ingelheim October 2006 Phase 1
NCT00701766 Completed Drug: BI 2536 Leukemia Myeloid Acute Boehringer Ingelheim October 2006 Phase 2
NCT00706498 Completed Drug: BI 2536 Prostatic Neoplasms Boehringer Ingelheim September 2006 Phase 2
NCT00376623 Completed Drug: BI 2536 Carcinoma Non-Small-Cell Lung Boehringer Ingelheim July 2006 Phase 2
NCT02211872 Completed Drug: BI 2536 BS intravenous Neoplasms Boehringer Ingelheim August 2004 Phase 1

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

    We need to use BI 2536 in preclinical studies using mice, how to formulate the inhibitor for this in vivo study?

  • 回答:

    For in vivo study, DMSO should not be more than 5% because the toxicity. You can formulated BI2536 in hydrochloric acid (0.1 N), and diluted with 0.9% NaCl for animal study according to the reference :( Supplemental Data) http://linkinghub.elsevier.com/retrieve/pii/S0960-9822(06)02671-6

PLK Signaling Pathway Map

PLK Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID