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117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 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPNTWM2OD1yLkCwN|M5KM7:TR?= M1XuRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4Ojh5OD:nQnNCVkeURWK8M4E,
RS4-11 M4LXSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zM[WlEPTB;MD6wNFQxPCEQvF2= MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O|I5PzhxJ{7TRW5IWkWUPD;hQi=>
MFH-ino MkDSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTBwMEC5PUDPxE1? NEnkXpY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzJ6N{ivK|5USU6JUlXSQE9iRg>?
NTERA-S-cl-D1 MoXJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTBwMEG0N|Qh|ryP M4TJWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4Ojh5OD:nQnNCVkeURWK8M4E,
697 NX[zeohtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHLTWM2OD1yLkCyOFcyKM7:TR?= M{exV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4Ojh5OD:nQnNCVkeURWK8M4E,
NALM-6 NVLVW5YzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2[4ZmlEPTB;MD6wNlU2OiEQvF2= MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O|I5PzhxJ{7TRW5IWkWUPD;hQi=>
ES8 NWfOV3dtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjuTWM2OD1yLkC0OlE{KM7:TR?= M4XTUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4Ojh5OD:nQnNCVkeURWK8M4E,
HUTU-80 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3vTWM2OD1yLkC1Nlk6KM7:TR?= M3nOZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4Ojh5OD:nQnNCVkeURWK8M4E,
MV-4-11 MofpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrhbGF6UUN3ME2wMlA4Pzh{IN88US=> MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O|I5PzhxJ{7TRW5IWkWUPD;hQi=>
MONO-MAC-6 NGXBNFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfITWM2OD1yLkC3PFc6KM7:TR?= NXnK[lNvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd{OEe4M{c,W0GQR2LFVlww[T5?
LC-2-ad NEfmN5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4P3eWlEPTB;MD6wPFc5QSEQvF2= NIjadlY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzJ6N{ivK|5USU6JUlXSQE9iRg>?
BL-41 Ml3kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXh[Y5KSzVyPUCuNVA1PDVizszN M3XiOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4Ojh5OD:nQnNCVkeURWK8M4E,
A4-Fuk MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLBUHp4UUN3ME2wMlEyPTZ|IN88US=> M13MNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4Ojh5OD:nQnNCVkeURWK8M4E,
SW954 M1fSXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELSW|JKSzVyPUCuNVIzOjlizszN NGO1cVI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzJ6N{ivK|5USU6JUlXSQE9iRg>?
BV-173 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFL3OWtKSzVyPUCuNVI3PDFizszN MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O|I5PzhxJ{7TRW5IWkWUPD;hQi=>
TE-11 NYDaNpVpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfPb4Z4UUN3ME2wMlE1QTh{IN88US=> NHi5R2E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzJ6N{ivK|5USU6JUlXSQE9iRg>?
SK-UT-1 NXzkUFd4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HvcGlEPTB;MD6xOVk3PSEQvF2= MmH1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVczQDd6Lze+V2FPT1KHUkyvZV4>
SIG-M5 M4TrPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1H2bWlEPTB;MD6xOlcxPyEQvF2= NH3JWnQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzJ6N{ivK|5USU6JUlXSQE9iRg>?
OCUB-M MnvDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHacnRXUUN3ME2wMlE3QTh|IN88US=> M{XpWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4Ojh5OD:nQnNCVkeURWK8M4E,
K052 NHyyR|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLRXIo{UUN3ME2wMlE6PDhizszN MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O|I5PzhxJ{7TRW5IWkWUPD;hQi=>
VA-ES-BJ MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTBwMkCwPFYh|ryP NH\XVWE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzJ6N{ivK|5USU6JUlXSQE9iRg>?
SW982 NEn0ZVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3Xm[2lEPTB;MD6yNVM5KM7:TR?= Ml[0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVczQDd6Lze+V2FPT1KHUkyvZV4>
LB647-SCLC MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnXbIRKSzVyPUCuNlE2OjNizszN Mn:2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVczQDd6Lze+V2FPT1KHUkyvZV4>
PSN1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4Wx[WlEPTB;MD6yNlAzPiEQvF2= MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O|I5PzhxJ{7TRW5IWkWUPD;hQi=>
BB30-HNC MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHf5XoVKSzVyPUCuNlI2QTFizszN NWrVdpdmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd{OEe4M{c,W0GQR2LFVlww[T5?
ST486 M4L2O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1ztUmlEPTB;MD6yN|A5PyEQvF2= MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O|I5PzhxJ{7TRW5IWkWUPD;hQi=>
MOLT-4 M3HpRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTBwMkOzN|ch|ryP MoLDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVczQDd6Lze+V2FPT1KHUkyvZV4>
EW-16 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\NVHBKSzVyPUCuNlM4PjhizszN MnyxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVczQDd6Lze+V2FPT1KHUkyvZV4>
KS-1 NVW3NoZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jSZ2lEPTB;MD6yN|c5PSEQvF2= M1K2VFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4Ojh5OD:nQnNCVkeURWK8M4E,
SR NX7QbFM3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jT[WlEPTB;MD6yOFU3PCEQvF2= NU\BeoVFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd{OEe4M{c,W0GQR2LFVlww[T5?
KM12 NFe2R29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDIWGRUUUN3ME2wMlI3OzZizszN NHfqfmQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzJ6N{ivK|5USU6JUlXSQE9iRg>?
EM-2 MnHjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\Ndm8{UUN3ME2wMlI3PjRzIN88US=> NF3xfYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzJ6N{ivK|5USU6JUlXSQE9iRg>?
MEG-01 MkHtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIWxcWdKSzVyPUCuNlc5PDlizszN M3rXblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4Ojh5OD:nQnNCVkeURWK8M4E,
NB13 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;vWWlEPTB;MD6yO|k5PCEQvF2= NEHGdms9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzJ6N{ivK|5USU6JUlXSQE9iRg>?
RKO NXnoPWJnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nnZWlEPTB;MD6zNFgyOyEQvF2= NYDCVlZmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd{OEe4M{c,W0GQR2LFVlww[T5?
CESS Mn\CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTBwM{GzNlgh|ryP NFzCbnU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzJ6N{ivK|5USU6JUlXSQE9iRg>?
EoL-1-cell NIjl[|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDiZYE3UUN3ME2wMlM{PDV7IN88US=> NX\5eWxvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd{OEe4M{c,W0GQR2LFVlww[T5?
DOHH-2 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTBwM{O3PFEh|ryP MnywQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVczQDd6Lze+V2FPT1KHUkyvZV4>
A388 NVT1UHp5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTBwM{SwPFYh|ryP NYHZd21XRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd{OEe4M{c,W0GQR2LFVlww[T5?
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HCT116 NXjrPY91TnWwY4Tpc44h[XO|YYm= NXrCPIw4OSC3TR?= NFjPSXMzPCCqcoO= NU\uU4JJUW6qaXLpeIlwdiCxZjDjfZRwc2mwZYPpd{BqdiCqdX3hckBJS1RzMU[gZ4VtdHNiYYSgNUB2VSCjZoTldkAzPCCqcoOgZpkheHKxcHnkbZVuKGmxZHnk[U9TVmG|ZTDzeIFqdmmwZz3iZZNm\CCobH;3JIN6fG:vZYTybYMh[W6jbInzbZM> NID6ZWo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEG0N|QzOyd-M{CxOFM1OjN:L3G+
HCT116 NH3Ce|dHfW6ldHnvckBie3OjeR?= MXexJJVO NF7lOXA{KGi{cx?= M1HqZ2lvcGmkaYTpc44hd2ZiQYXyc5JiKEJiaX6gbJVu[W5iSFPUNVE3KGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDobZN1d26nIFizJJBpd3OyaH;yfYxifGmxbjDheEBU\XJzMDDy[ZNq\HWnIIXwJJRwKDFidV2gZYZ1\XJiMzDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz NVnvOVFNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CxOFM1OjNpPkOwNVQ{PDJ|PD;hQi=>
HCT116 M{Lyc2Z2dmO2aX;uJIF{e2G7 M2\zU|MhcHK| M3f0eGlvcGmkaYTpc44hd2ZiQYXyc5JiKEFicHjvd5Bpd3K7bHH0bY9vKGG2IGTodlI5QCC{ZYPp[JVmKGmwIHj1cYFvKEiFVEGxOkBk\WyuczD1dEB1dyBzIIXNJIFnfGW{IEOgbJJ{KGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=> MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODF2M{SyN{c,OzBzNEO0NlM9N2F-
HCT116 NWrMR4U1TnWwY4Tpc44h[XO|YYm= NX7ybml7OyCqcoO= NH7aPWtKdmirYnn0bY9vKG:oIFH1do9z[SCEIIDoc5NxcG:{eXzheIlwdiCjdDDUbJIzOzJicnXzbYR2\SCrbjDoeY1idiCKQ2SxNVYh[2WubIOgeZAhfG9iMTD1UUBi\nSncjCzJIhzeyCkeTDX[ZN1\XKwIHLsc5QhdWW2aH;k MlTHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzBzNEO0NlMoRjNyMUSzOFI{RC:jPh?=
Sf9 NH7jdmxHfW6ldHnvckBie3OjeR?= MYjJcohq[mm2aX;uJI9nKEeVVD30ZYdo\WRiQWXSU3JCKEFiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gZoFkfWyxdnnyeZMhcW6oZXP0[YQhW2Z7IHPlcIx{KHW|aX7nJG1DWCCjczDzeYJ{fHKjdHWsJGlEPTB;MD6wNlPPxE1? M13Me|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkO0PVg4Lz5|MEKzOFk5PzxxYU6=
HeLa M{fzVWZ2dmO2aX;uJIF{e2G7 MYqxNkBpenN? Ml3MTY5pcWKrdHnvckBw\iCDdYLvdoEhSSCyaH;zdIhwenmuYYTpc44h[XRiVHjyNlg5KHKnc3nkeYUhcW5iaIXtZY4hUGWOYTDj[YxteyCjZoTldkAyOiCqcoOgZpkhTUyLU1GsJGlEPTB;MD6wNVPPxE1? M3rYUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNUCyNVE2Lz5|MEWwNlEyPTxxYU6=
HeLa NUfDc3piTnWwY4Tpc44h[XO|YYm= NVrsV2pWOTJiaILz NGW4NZpKdmirYnn0bY9vKG:oIFH1do9z[SCEIIDoc5NxcG:{eXzheIlwdiCjdDDUbJIzOzJicnXzbYR2\SCrbjDoeY1idiCKZVzhJINmdGy|IHHmeIVzKDF{IHjyd{BjgSCHTFnTRUwhUUN3ME2wMlE1QM7:TR?= NVr1SZZURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C1NFIyOTVpPkOwOVAzOTF3PD;hQi=>
A549 MUnBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? Mn2wOFghcHK| M3fWcWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\WyuczDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDHTVUxRTN3LklOwG0> MnP0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB3MEKxNVUoRjNyNUCyNVE2RC:jPh?=
LoVo NGC4cVBCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MWe0PEBpenN? NUfjXXZWSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDMc3ZwKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGdKPTB;NEWuN:69VQ>? MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODVyMkGxOUc,OzB3MEKxNVU9N2F-
HeLa MljTRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MmDwOFghcHK| M2ruOWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSHXMZUBk\WyuczDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDHTVUxRTR4LkNOwG0> MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODVyMkGxOUc,OzB3MEKxNVU9N2F-
HeLa M3PkU2NmdGxiY4njcIUh[XO|YYm= MXu1JJVO M{PiPVEzKGi{cx?= MULD[YxtKGO7Y3zlJIFzemW|dDDpckBpfW2jbjDI[WxiKGOnbHzzJIF{e2W|c3XkJIF{KGSnY4LlZZNmKGmwIHP5Z4xqdiCEMTDwdo91\WmwIHX4dJJme3Orb36gZZQhPSC3TTDh[pRmeiBzMjDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz NHqwXXo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEWwNlEyPSd-M{C1NFIyOTV:L3G+
HeLa NFToOWpE\WyuIHP5Z4xmKGG|c3H5 NUC1S2diPSC3TR?= NEDN[ZYyOiCqcoO= MlTCR4VtdCCleXPs[UBienKnc4SgbY4hcHWvYX6gTIVN[SClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDj[IMzKHC{b4TlbY4h\XiycnXzd4lwdiCjdDC1JJVOKGGodHXyJFEzKGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? M3jtSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNUCyNVE2Lz5|MEWwNlEyPTxxYU6=
HeLa MljCSpVv[3Srb36gZZN{[Xl? M{TWZVUhfU1? NYTx[4FpOTJiaILz MYLJcohq[mm2aX;uJI9nKEG3cn;yZUBCKHCqb4PwbI9zgWyjdHnvckBifCCWaIKyPFghemW|aXT1[UBqdiCqdX3hckBJ\UyjIHPlcIx{KGG2IEWgeW0h[W[2ZYKgNVIhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODVyMkGxOUc,OzB3MEKxNVU9N2F-
HeLa NX\VPXJsTnWwY4Tpc44h[XO|YYm= MVm1JJVO M3e2WFEzKGi{cx?= NYjPUo9kUW6qaXLpeIlwdiCxZjDBeZJwemFiQjDwbI9{eGixconsZZRqd25iYYSgWIhzOjN{IILld4llfWViaX6gbJVu[W5iSHXMZUBk\WyuczDheEA2KHWPIHHmeIVzKDF{IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= Mor1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB3MEKxNVUoRjNyNUCyNVE2RC:jPh?=
A549 NHPGc|FCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NV3QWId5PDhiaILz M1fXSWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\WyuczDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTN3LklOwG0> M3n1dFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyN{K4NVEzLz5|MEeyPFEyOjxxYU6=
LoVo NIHkZ|ZCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MVq0PEBpenN? MWDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEyxVn:gZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF01PS5|zszN NFjXe3k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEeyPFEyOid-M{C3NlgyOTJ:L3G+
HeLa MmLJRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MnLoOFghcHK| Mn;oRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKZVzhJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:PDZwMt88US=> MmrFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB5MkixNVIoRjNyN{K4NVEzRC:jPh?=

... 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

Aurora Kinase Signaling Pathway Map

Aurora Kinase Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID