Tozasertib (VX-680, MK-0457)

For research use only. Not for use in humans.

目录号:S1048 中文名称:陶扎色替

Tozasertib (VX-680, MK-0457) Chemical Structure

CAS No. 639089-54-6

Tozasertib (VX-680, MK-0457)是一种pan-Aurora抑制剂,对Aurora A作用最强,无细胞试验中Kiapp为0.6 nM,而对Aurora B/Aurora C的作用较弱,对Aurora A选择性比其他55种激酶高100倍。唯二的例外是 Fms-related tyrosine kinase-3 (FLT-3)BCR-ABL tyrosine kinase,也可被 Tozasertib 抑制,对应的Ki值均为30 nM和30 nM。Tozasertib 可诱导凋亡和自噬。Phase 2。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1098.34 现货
RMB 1211.51 现货
RMB 3833.09 现货
RMB 4316.13 现货
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客户使用Selleck生产的Tozasertib (VX-680, MK-0457)发表文献114篇:

产品安全说明书

Aurora Kinase抑制剂选择性比较

生物活性

产品描述 Tozasertib (VX-680, MK-0457)是一种pan-Aurora抑制剂,对Aurora A作用最强,无细胞试验中Kiapp为0.6 nM,而对Aurora B/Aurora C的作用较弱,对Aurora A选择性比其他55种激酶高100倍。唯二的例外是 Fms-related tyrosine kinase-3 (FLT-3)BCR-ABL tyrosine kinase,也可被 Tozasertib 抑制,对应的Ki值均为30 nM和30 nM。Tozasertib 可诱导凋亡和自噬。Phase 2。
靶点
Aurora A [1]
(Cell-free assay)
Aurora C [1]
(Cell-free assay)
Aurora B [1]
(Cell-free assay)
FLT3 [4]
(Cell-free assay)
Bcr-Abl [4]
(Cell-free assay)
0.6 nM(Ki app) 4.6 nM(Ki app) 18 nM(Ki app) 30 nM(Ki) 30 nM(Ki)
体外研究

虽然VX-680具有多激酶特性,VX-680却诱导相似的细胞毒性,IC50约为300 nM,在G2/M期,核内复制期,及转染ABL或FLT-3激酶的BaF3细胞凋亡时,显示一个Aurora B 类似的抑制表现型。VX-680抑制CAL-62细胞增殖,这种作用存在时间依赖性。用VX-680处理14天,明显降低群体的数量和大小,处理8305C下降达到70%,处理CAL-62, 8505C,和BHT-101下降达到90%。用VX-680处理不同ATC细胞,抑制细胞增殖,IC50为25到150  nM,这种作用存在时间和剂量依赖性。在软琼脂中,VX-680明显削弱不同细胞系形成群落的能力。caspase-3的活性分析显示VX-680诱导不同细胞凋亡。VX-680处理CAL-62 细胞12小时,形成DNA含量≥4N细胞累积物。微速摄影分析显示VX-680处理的CAL-62细胞离开细胞中期。VX-680可以抑制组蛋白H3的磷酸化作用。[2] VX-680作用于携带T315I突变的BCR-Abl的病人样本,具有明显抑制活性。[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BE-13 M{PwXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7uTWM2OD1yLkCwN|M5KM7:TR?= NXLLWJU{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd{OEe4M{c,W0GQR2LFVlww[T5?
RS4-11 NFfuRW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTBwMEC0NFQh|ryP NWH6RnlJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd{OEe4M{c,W0GQR2LFVlww[T5?
MFH-ino M1LrXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XHNGlEPTB;MD6wNFk6KM7:TR?= M2X3TlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4Ojh5OD:nQnNCVkeURWK8M4E,
NTERA-S-cl-D1 NGezbpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PZfGlEPTB;MD6wNVQ{PCEQvF2= NEe3bFU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzJ6N{ivK|5USU6JUlXSQE9iRg>?
697 M{PoN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fzSWlEPTB;MD6wNlQ4OSEQvF2= M3;SNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4Ojh5OD:nQnNCVkeURWK8M4E,
NALM-6 Mmn1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfITFV3UUN3ME2wMlAzPTV{IN88US=> MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O|I5PzhxJ{7TRW5IWkWUPD;hQi=>
ES8 NXXnOo82T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\2WnlKSzVyPUCuNFQ3OTNizszN MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O|I5PzhxJ{7TRW5IWkWUPD;hQi=>
HUTU-80 NYHaTFdXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDXOoxSUUN3ME2wMlA2Ojl7IN88US=> MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O|I5PzhxJ{7TRW5IWkWUPD;hQi=>
MV-4-11 NUDH[GE2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLuSGdtUUN3ME2wMlA4Pzh{IN88US=> MojhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVczQDd6Lze+V2FPT1KHUkyvZV4>
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BL-41 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTBwMUC0OFUh|ryP MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O|I5PzhxJ{7TRW5IWkWUPD;hQi=>
A4-Fuk MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7DTWM2OD1yLkGxOVY{KM7:TR?= MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O|I5PzhxJ{7TRW5IWkWUPD;hQi=>
SW954 NEnRV|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTvPXRKSzVyPUCuNVIzOjlizszN MnnnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVczQDd6Lze+V2FPT1KHUkyvZV4>
BV-173 NYDJNng3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3ZbY1KSzVyPUCuNVI3PDFizszN MnTMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVczQDd6Lze+V2FPT1KHUkyvZV4>
TE-11 M1fsbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXsV|lKSzVyPUCuNVQ6QDJizszN NFOwOWI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzJ6N{ivK|5USU6JUlXSQE9iRg>?
SK-UT-1 MnLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTBwMUW5OlUh|ryP M3nicFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4Ojh5OD:nQnNCVkeURWK8M4E,
SIG-M5 NVvoSnJMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTBwMU[3NFch|ryP NH6zR|I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzJ6N{ivK|5USU6JUlXSQE9iRg>?
OCUB-M MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HIXGlEPTB;MD6xOlk5OyEQvF2= NFryPWc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzJ6N{ivK|5USU6JUlXSQE9iRg>?
K052 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3Hm[2lEPTB;MD6xPVQ5KM7:TR?= NVTwOox4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd{OEe4M{c,W0GQR2LFVlww[T5?
VA-ES-BJ MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTBwMkCwPFYh|ryP M4DZO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4Ojh5OD:nQnNCVkeURWK8M4E,
SW982 M3vkNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3Tr[mlEPTB;MD6yNVM5KM7:TR?= NEDFNFg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzJ6N{ivK|5USU6JUlXSQE9iRg>?
LB647-SCLC M2rFeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7VV3g{UUN3ME2wMlIyPTJ|IN88US=> MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O|I5PzhxJ{7TRW5IWkWUPD;hQi=>
PSN1 NYjvbGJrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEC0boNKSzVyPUCuNlIxOjZizszN NIPpfWw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzJ6N{ivK|5USU6JUlXSQE9iRg>?
BB30-HNC M13YTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUfIVmpFUUN3ME2wMlIzPTlzIN88US=> Mmi5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVczQDd6Lze+V2FPT1KHUkyvZV4>
ST486 MmPaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTBwMkOwPFch|ryP NUSwXYtGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd{OEe4M{c,W0GQR2LFVlww[T5?
MOLT-4 NVHEdnE1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTKTWM2OD1yLkKzN|M4KM7:TR?= Ml[wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVczQDd6Lze+V2FPT1KHUkyvZV4>
EW-16 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTBwMkO3Olgh|ryP NIL2R249[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzJ6N{ivK|5USU6JUlXSQE9iRg>?
KS-1 MkXUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\qTWM2OD1yLkKzO|g2KM7:TR?= MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O|I5PzhxJ{7TRW5IWkWUPD;hQi=>
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KM12 MoX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPCXWw5UUN3ME2wMlI3OzZizszN MnvrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVczQDd6Lze+V2FPT1KHUkyvZV4>
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MEG-01 NF\OUYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;JeY54UUN3ME2wMlI4QDR7IN88US=> MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O|I5PzhxJ{7TRW5IWkWUPD;hQi=>
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CESS M1zNcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTBwM{GzNlgh|ryP M2DLWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4Ojh5OD:nQnNCVkeURWK8M4E,
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DOHH-2 NV\SUZlzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7CRnlKSzVyPUCuN|M4QDFizszN NF\rSVA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzJ6N{ivK|5USU6JUlXSQE9iRg>?
A388 NXnwNIhCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nUfGlEPTB;MD6zOFA5PiEQvF2= M2X1VFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4Ojh5OD:nQnNCVkeURWK8M4E,
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OCI-AML2 MnfIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInsSIVKSzVyPUCuOlQ1ODNizszN Mon4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVczQDd6Lze+V2FPT1KHUkyvZV4>
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IST-SL2 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vhSWlEPTB;MD63NVk5OiEQvF2= NF7vdYQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzJ6N{ivK|5USU6JUlXSQE9iRg>?
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HL-60 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HocWlEPTB;MT6wOlU4PCEQvF2= MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O|I5PzhxJ{7TRW5IWkWUPD;hQi=>
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ETK-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjpTWM2OD1zLkGzOlE{KM7:TR?= MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O|I5PzhxJ{7TRW5IWkWUPD;hQi=>
HAL-01 NXT3Vm9sT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFz1RpZKSzVyPUGuNVY4ODlizszN M1K3PVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4Ojh5OD:nQnNCVkeURWK8M4E,
BB65-RCC MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTmbWpKSzVyPUGuNVgxODVizszN MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O|I5PzhxJ{7TRW5IWkWUPD;hQi=>
EW-1 MlvKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3PTWhZUUN3ME2xMlE5PTZ{IN88US=> MlvoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVczQDd6Lze+V2FPT1KHUkyvZV4>
SK-NEP-1 MoXwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mni3TWM2OD1zLkKxNVEyKM7:TR?= M1TkOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4Ojh5OD:nQnNCVkeURWK8M4E,
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HCT116 MnHpSpVv[3Srb36gZZN{[Xl? NULXUIR5OyCqcoO= MWjJcohq[mm2aX;uJI9nKEG3cn;yZUBCKHCqb4PwbI9zgWyjdHnvckBifCCWaIKyPFghemW|aXT1[UBqdiCqdX3hckBJS1RzMU[gZ4VtdHNidYCgeI8hOSC3TTDh[pRmeiB|IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= NX:zPGh2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CxOFM1OjNpPkOwNVQ{PDJ|PD;hQi=>
HCT116 MkPrSpVv[3Srb36gZZN{[Xl? NHG0SZk{KGi{cx?= MoK3TY5pcWKrdHnvckBw\iCDdYLvdoEhSiCyaH;zdIhwenmuYYTpc44h[XRiVHjyNlMzKHKnc3nkeYUhcW5iaIXtZY4hUEOWMUG2JINmdGy|IIXwJJRwKDFidV2gZYZ1\XJiMzDodpMh[nliV3XzeIVzdiCkbH;0JI1mfGixZB?= NEHjTJE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEG0N|QzOyd-M{CxOFM1OjN:L3G+
Sf9 MnnySpVv[3Srb36gZZN{[Xl? NED0[4hKdmirYnn0bY9vKG:oIFfTWE11[WepZXSgRXVTV1KDIFGgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4h[mGldXzveolzfXNiaX7m[YN1\WRiU3[5JINmdGy|IIXzbY5oKE2EUDDhd{B{fWK|dILheIUtKEmFNUC9NE4xOjQQvF2= MkjzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{M{S5PFcoRjNyMkO0PVg4RC:jPh?=
HeLa NYL6SIVbTnWwY4Tpc44h[XO|YYm= NHPpNYUyOiCqcoO= NUHMVIVxUW6qaXLpeIlwdiCxZjDBeZJwemFiQTDwbI9{eGixconsZZRqd25iYYSgWIhzOjh6IILld4llfWViaX6gbJVu[W5iSHXMZUBk\WyuczDh[pRmeiBzMjDodpMh[nliRVzJV2EtKEmFNUC9NE4xOTQQvF2= NGrOOIE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEWwNlEyPSd-M{C1NFIyOTV:L3G+
HeLa NELoR4NHfW6ldHnvckBie3OjeR?= MlnYNVIhcHK| MWjJcohq[mm2aX;uJI9nKEG3cn;yZUBDKHCqb4PwbI9zgWyjdHnvckBifCCWaIKyN|IhemW|aXT1[UBqdiCqdX3hckBJ\UyjIHPlcIx{KGGodHXyJFEzKGi{czDifUBGVEmVQTygTWM2OD1yLkG0PO69VQ>? NYeyepBuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C1NFIyOTVpPkOwOVAzOTF3PD;hQi=>
A549 NXHwV4lISW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NFnxO2o1QCCqcoO= NV3kNHdsSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGdKPTB;M{WuPO69VQ>? MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODVyMkGxOUc,OzB3MEKxNVU9N2F-
LoVo NYDxS2ZvSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= Mn\XOFghcHK| NXrJTFM4SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDMc3ZwKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGdKPTB;NEWuN:69VQ>? MnTmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB3MEKxNVUoRjNyNUCyNVE2RC:jPh?=
HeLa NITwUFdCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MVy0PEBpenN? NXrBdVBpSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDI[WxiKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGdKPTB;NE[uNu69VQ>? NU\HXWt3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C1NFIyOTVpPkOwOVAzOTF3PD;hQi=>
HeLa M1;FXWNmdGxiY4njcIUh[XO|YYm= NHXGXYM2KHWP MkLnNVIhcHK| MYjD[YxtKGO7Y3zlJIFzemW|dDDpckBpfW2jbjDI[WxiKGOnbHzzJIF{e2W|c3XkJIF{KGSnY4LlZZNmKGmwIHP5Z4xqdiCEMTDwdo91\WmwIHX4dJJme3Orb36gZZQhPSC3TTDh[pRmeiBzMjDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz NX36VmZZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C1NFIyOTVpPkOwOVAzOTF3PD;hQi=>
HeLa MkHUR4VtdCCleXPs[UBie3OjeR?= MYe1JJVO NWXibWhROTJiaILz NUTXN2dyS2WubDDjfYNt\SCjcoLld5QhcW5iaIXtZY4hUGWOYTDj[YxteyCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckBk\GN{IIDyc5RmcW5iZYjwdoV{e2mxbjDheEA2KHWPIHHmeIVzKDF{IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= Mn7iQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB3MEKxNVUoRjNyNUCyNVE2RC:jPh?=
HeLa NWXafph4TnWwY4Tpc44h[XO|YYm= NIniZXU2KHWP NYnFd|ZDOTJiaILz M2i1TGlvcGmkaYTpc44hd2ZiQYXyc5JiKEFicHjvd5Bpd3K7bHH0bY9vKGG2IGTodlI5QCC{ZYPp[JVmKGmwIHj1cYFvKEinTHGgZ4VtdHNiYYSgOUB2VSCjZoTldkAyOiCqcoOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| M4DaUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNUCyNVE2Lz5|MEWwNlEyPTxxYU6=
HeLa M3izeGZ2dmO2aX;uJIF{e2G7 MX:1JJVO NFTOWHYyOiCqcoO= NUnYSnNKUW6qaXLpeIlwdiCxZjDBeZJwemFiQjDwbI9{eGixconsZZRqd25iYYSgWIhzOjN{IILld4llfWViaX6gbJVu[W5iSHXMZUBk\WyuczDheEA2KHWPIHHmeIVzKDF{IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= M4WwbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNUCyNVE2Lz5|MEWwNlEyPTxxYU6=
A549 MmqwRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MnO5OFghcHK| MWfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF3NEmgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0{PS56zszN M33Ec|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyN{K4NVEzLz5|MEeyPFEyOjxxYU6=
LoVo NWfEZoFnSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M4XWOlQ5KGi{cx?= M1SwTWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTH;Wc{Bk\WyuczDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTR3LkROwG0> NUjCfFNRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C3NlgyOTJpPkOwO|I5OTF{PD;hQi=>
HeLa MnvORY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M3Wz[VQ5KGi{cx?= M{P4PGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSHXMZUBk\WyuczDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTR4LkNOwG0> MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODd{OEGxNkc,OzB5MkixNVI9N2F-

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
DLK / p-MKK7 / MKK7 / p-JNK / JNK ; 

PubMed: 23431148     


Western blot of the DLK pathway members in RGCs (retinal ganglion cells) 4 h after immunopanning in the presence of 0, 0.03, 0.06, 0.125, 0.25, 0.5, 1, or 2 μM tozasertib. 

p-AURKA / AURKA / Survivin ; 

PubMed: 28218735     


BGC823 cells were incubated with indicated doses of VX-680 for 24 h before subjected to western blotting with the indicated antibodies. Densitometry was used to quantify the Survivin and GAPDH levels. The relative expression shown (right panel) are means±s.e.m. of the ratios of Survivin to GAPDH. 

YAP; 

PubMed: 31160567     


Western blot analysis of YAP protein level in A549 cells treated with indicated doses of VX-680 for 24 h. 

p-AKT / p-GSK3β / Cleaved caspase-3 / Cleaved PARP ; 

PubMed: 21600017     


NB4-R2 cells were collected, lysed and subjected to Western blot analysis with cleaved caspase-3, cleaved-PARP, pAkt-1 (Ser473), pGSK-3β (Ser9) specific antibodies. GAPDH was used as a loading control. Data shown is a representative of three independent experiments.

23431148 28218735 31160567 21600017
Immunofluorescence
α-tubulin / Aurora-A ; 

PubMed: 21600017     


The morphology of mitotic spindle was shown by immunofluorescence staining with anti-α-tubulin antibody and anti-Aur-A antibodies. Microtubules were stained as green, Aur-A protein as red, and nucleus as blue.

21600017
Growth inhibition assay
Cell viability; 

PubMed: 21600017     


VX-680 significantly suppresses the proliferation in a number of leukemic cell types. OCI-AML3, NB4, HL-60 and ML-1 cells were incubated with increasing doses of VX-680 (1, 2, 5 and 10 nM) for 24 hr. Cell viability was measured by MTT assay. Data summarized three independent experiments, *p < 0.05, **p < 0.01, compared to control.

21600017
体内研究 VX-680作用于人类AML(HL-60)移植瘤模型明显降低肿瘤尺寸。VX-680按75 mg/kg剂量给药实验鼠,每天腹腔注射两次,持续13天,与对照组相比,平均肿瘤体积下降达98%。肿瘤体积比实验之前初始体积小很多。按12.5 mg/kg剂量每天给药两次,肿瘤生长也明显降低,这种作用存在剂量依赖性。VX-680耐受性很好,只有在使用高剂量时可以观察到实验动物体重稍微降低。通过比较cisplatin,按5.4 mg/kg剂量给药,每四天腹腔注射一次,一共进行三次,抑制肿瘤生长只达9%。VX-680作用于胰脏和结肠移植瘤,也引起肿瘤衰退。VX-680静脉注射给药携带HCT116肿瘤的实验鼠,显示很强的抗癌活性。使用高剂量VX-680(每小时2 mg/kg)处理,明显提高效果,比实验钱的初始肿瘤平均尺寸下降56%。[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:

[3]

- 合并

激酶抑制实验:

丙酮酸激酶/乳酸脱氢酶催化NADH的氧化,伴随着ATP的消耗,观察340 nm 处吸光值的降低。反应包括100 mM Tris (pH 为 8), 10 mM MgCl2, 2.2 mM ATP, 1 mM磷酸烯醇丙酮酸, 0.6 mg/ml NADH, 75 ml丙酮酸激酶, 105 ml 乳酸脱氢酶,和0.5 mM 基底肽(序列为EAIYAAPFAKKK)。加入足够的激酶开始反应,反应的激酶浓度达到30 nM,用微量滴定板分光光度计在30oC进行30分钟,观察吸收率的降低。通过加入3.75 μl 溶于100% DMSO的VX-680 或单独DMSO,获得抑制常数。按如下公式计算Ki值,Ki = IC50/(1+[S]/Kd),[S]=[ATP]=2.2 mM, Kd=70 μM。假定作用于野生型和H396P Abl 激酶域的Kd(ATP)为70 μM,计算以上各值。
细胞实验:

[2]

- 合并
  • Cell lines: CAL-62细胞
  • Concentrations: 5-500 nM
  • Incubation Time: 4天
  • Method:

    对照组CAL-62细胞培养在二甲亚砜和DMSO中,实验组加入500 nM VX-680,处理1到5天。加入不同浓度(5到500 nM) Aurora抑制剂处理不同ATC细胞4天,用来测定VX-680作用于细胞增殖的剂量依赖性。细胞在温育结束前加30 mM BrdU标记,脉冲2小时。通过比色免疫分析使用细胞增殖ELISA试剂盒分析BrdU的合并率。通过比较VX-680处理的细胞和对照组细胞得到结果,


    (Only for Reference)
动物实验:

[1]

- 合并
  • Animal Models: 右侧腋窝处皮下注射107 HL-60白血病细胞的雌性无胸腺NCr-nu鼠
  • Dosages: 50 mg/kg, 75 mg/kg
  • Administration: 腹腔注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 93 mg/mL (200.17 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):
5% DMSO+30% PEG 300+2% Tween 80+ddH2O
3.75 mg/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 464.59
化学式

C23H28N8OS

CAS号 639089-54-6
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、SDS / 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、SDS / 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
NCT00290550 Terminated Drug: MK0457 Carcinoma Non-Small-Cell Lung Merck Sharp & Dohme Corp. June 2006 Phase 2
NCT00111683 Completed Drug: MK0457 Chronic Myelogenous Leukemia in Blast Crisis|Lymphocytic Leukemia B Cell Acute|Myelodysplastic Syndromes|Myelogenous Leukemia Chronic Merck Sharp & Dohme Corp. June 2005 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
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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID