AZD7762

For research use only. Not for use in humans.

目录号:S1532

AZD7762 Chemical Structure

CAS No. 860352-01-8

AZD7762是一种有效的,选择性Chk1抑制剂,无细胞试验中IC50为5 nM,作用于Chk2也同样有效,对CAM, Yes, Fyn, Lyn, Hck和Lck作用效果稍弱。Phase 1。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1562.52 现货
RMB 576.88 现货
RMB 974.33 现货
RMB 3040.33 现货
RMB 13243.23 现货
有超大折扣
今日订购,明日送达 全国免运费 分装免费
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客户使用Selleck生产的AZD7762发表文献105篇:

产品安全说明书

Chk抑制剂选择性比较

生物活性

产品描述 AZD7762是一种有效的,选择性Chk1抑制剂,无细胞试验中IC50为5 nM,作用于Chk2也同样有效,对CAM, Yes, Fyn, Lyn, Hck和Lck作用效果稍弱。Phase 1。
靶点
Chk1 [1]
(Cell-free assay)
Chk2 [1]
(Cell-free assay)
5 nM <10 nM
体外研究

AZD7762是Chk1选择性抑制剂, 通过与Chk1的ATP结合位点可逆结合而抑制cdc25C肽段的Chk1磷酸化,IC50 为5 nM,Ki为 3.6 nM。AZD7762诱导细胞周期停滞,EC50为0.620 μM, 且通过阻断cdc25A依赖chk1的降解 和Cyclin A的激活,显著废除Camptothecin诱导的G2期停滞,EC50为10 nM。300 nM AZD7762增强Gemcitabine作用于SW620的抗癌活性,也增强 Topotecan作用于MDA-MB-231 的抗癌活性,通过降低 GI50 值,分别从24.1 nM和2.25 μM 降到1.08 nM 和0.15 μM。[1] AZD7762 作用于多种携带p53野生型,p53突变型,MDM2增添,或p14 缺失的神经母细胞瘤细胞系,IC50为82.6 nM 到505.9 nM。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
KASUMI-1 NYPye25nT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fIb2lEPTB;MD6wNFAzOzRizszN MmC2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
NKM-1 NIG3b3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTwTWM2OD1yLkCwNFQyPSEQvF2= MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
MV-4-11 M{ftUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTBwMECwOFI2KM7:TR?= Mnm2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
NCI-H1703 NHvFT2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXFTWM2OD1yLkCwOlQ{KM7:TR?= MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
A204 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2H5OWlEPTB;MD6wNFg2PiEQvF2= MmnnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
CGTH-W-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTsXZVKSzVyPUCuNFE1OiEQvF2= M1TIVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
MLMA NVrUUYxqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2q5e2lEPTB;MD6wNlg1QSEQvF2= MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
GOTO NFfyd2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TIOmlEPTB;MD6wN|EzKM7:TR?= MlPrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
KE-37 NH7FdW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfRTWM2OD1yLkCzNVQzKM7:TR?= MmnqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
ES4 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlX5TWM2OD1yLkCzNlUyKM7:TR?= NEjGcVE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
ATN-1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7ZTWM2OD1yLkCzOFE4KM7:TR?= NHPJOYU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
MHH-PREB-1 Ml35S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjaXmFKSzVyPUCuNFM1PDJizszN M4nKcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
SW756 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULNV|B[UUN3ME2wMlA{PTd7IN88US=> M2PlfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
CTV-1 NGKwRppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrSTWM2OD1yLkCzPFk3KM7:TR?= NISyPHg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
HCC1806 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTBwMESwNlIh|ryP M2rOe|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
NEC8 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4G0XmlEPTB;MD6wOFIxOyEQvF2= NIrNSmk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
P12-ICHIKAWA NFflb3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nVOGlEPTB;MD6wOFMyPiEQvF2= MnruQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
DEL M1jtVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTBwMES1PVIh|ryP NHLocHM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
KM12 MmDlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHmTWM2OD1yLkC1NVU5KM7:TR?= Mn;WQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
LB1047-RCC MkXUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTBwME[wNlUh|ryP MkjhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
LB2241-RCC NYOzbo5TT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2CzVGlEPTB;MD6wOlExOiEQvF2= MnHKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
NOMO-1 MlrrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDORWhKSzVyPUCuNFYyOTVizszN M3[5UlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
NB14 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTBwME[xN|Yh|ryP M3\HWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
ONS-76 NXjNXnBRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPVTWM2OD1yLkC2NVk3KM7:TR?= MmDZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
HD-MY-Z M1rSZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTBwME[yOVUh|ryP Mnz6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
G-402 NWTkZoMzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnyTWM2OD1yLkC2OFYh|ryP NVjMN3hoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
ES1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXmxbXZCUUN3ME2wMlA4OTR4IN88US=> MmrLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
L-363 NVrxSFdVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmq4TWM2OD1yLkC3N|kh|ryP NHi4[3I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
A4-Fuk M3X0bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{D1SWlEPTB;MD6wO|Q5PiEQvF2= M3jTO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
OC-314 MlziS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\aNmlTUUN3ME2wMlA4QDB5IN88US=> NFiwcGY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
SK-LU-1 M3jiWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\admlEPTB;MD6wPFQzOSEQvF2= NET4WVA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
MDA-MB-157 NGrkNYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTHVZB2UUN3ME2wMlA5PjV7IN88US=> MmrLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
HuP-T3 MonES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTrTWM2OD1yLkC4O|Eh|ryP MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
A3-KAW M4Pq[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HTNWlEPTB;MD6wPFgxPiEQvF2= NH31ems9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
MOLT-16 MkLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfHW4NSUUN3ME2wMlA5QDB5IN88US=> Mmf1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
COLO-679 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjPTWM2OD1yLkC5NFkyKM7:TR?= MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
EM-2 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHkTGVCUUN3ME2wMlA6QTB|IN88US=> NWXUfpc1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
ES8 NYGx[WJQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfsTWM2OD1yLkC5PVE5KM7:TR?= MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
SK-MEL-2 NX:4e|E1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTBwMUCwN|Mh|ryP NWLROZdmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
ES3 NEXMfJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzEZ4R3UUN3ME2wMlExOiEQvF2= NF7oT409[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
HSC-4 NYfXd2t5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\wTWM2OD1yLkGwOVU1KM7:TR?= MleyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
697 NHvr[IpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jvVGlEPTB;MD6xNVA3OyEQvF2= MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
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... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
pChk1 / Chk1 / Wee1 / p21 / p53 ; 

PubMed: 29963769     


Immunoblotting analysis of CAL39 and SW954 cells showing increase in CHK1 phosphorylation after exposure to AZD7762 for 24 hours. β‐actin is used as loading control. Representative data from n = 3 experiments.

29963769
Growth inhibition assay
Cell viability; 

PubMed: 23715154     


Lkb1-wt (634, 855, and 857) and Lkb1-null (t2, t4, and t5) cell lines were plated into 96-well plates at 2000 cells/well in 150 ml medium containing the indicated concentrations of AZD7762 or CHIR124 for 3 days. Viable cells were then counted with Dojindo’s Cell Counting Kit-8 assay. The data represent mean ± SD for 3 repeats. GI50 was calculated with GraphPad.

23715154
体内研究 AZD7762 按25 mg/kg剂量单独作用于携带H460-DNp53移植瘤的小鼠和携带SW620移植瘤的小鼠,显示很弱的抗癌活性,但是和Gemcitabine(60 mg/kg)联用处理这两种携带移植瘤的小鼠,则具有强抗癌活性。AZD7762和Gemcitabine(10 mg/kg) 联用作用于携带H460-DNp53移植瘤大鼠,抑制肿瘤体积,这种作用存在剂量依赖性。AZD7762 (25 mg/kg)和Irinotecan (25或50 mg/kg) 联用作用于携带SW620移植瘤的小鼠,引起全部肿瘤衰退。[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

Chk1激酶实验:

使用杆状病毒载体,融合在昆虫细胞中,重组人类Chk1表达作为谷胱甘肽S转移酶,通过胱甘肽亲和层析纯化。合成的肽底物 (N-biotinylaminohexanoyl-KKVSRSGLYRSPMPENLNRPR)用于Chk1 合成。实验中,肽和ATP(完全和40 nCi [33P]ATP) 的终浓度分别为0.8和1 μM。不同浓度AZD7762, 含肽和chk1激酶和ATP的buffer相继加到384孔板中。然后温育2小时,加入含EDTA和邻近闪烁分析(SPA)圆球微粒的buffer终止反应, 然后使用TopCount计数器读数。进行数据分析,测定IC50值。
细胞实验:[1]
- 合并
  • Cell lines: HT29,SW620和MDA-MB-231细胞
  • Concentrations: 溶于DMSO, 终浓度为12.5 μM 左右
  • Incubation Time: 20或48小时
  • Method: 检测点废除实验中, 用Camptothecin(拓扑异构酶I 抑制剂;0.07 μg/mL)处理HT29细胞2小时,诱导产生G2期检测点。然后用AZD7762(12.5 μM 到6 nM)12点滴定法和Nocodazole处理细胞20分钟。细胞和3.7%甲醛混合1小时,用含0.05% Triton X的PBS渗透处理, 然后与anti-phH3抗体温育1小时,然后用Hoechst染料染色1小时。使用ArrayScan测定有丝分裂指数,作为进行有丝分裂细胞的百分数。增强实验中,用Gemcitabine 9点滴定(0.01到 100 nM)和固定剂量AZD7762(300 nM)处理SW620或MDA-MB-231细胞24小时。24小时后, 移除培养基,单独加入AZD7762,再处理24小时。细胞在无AZD7762培养基中再温育72小时,通过MTT测定细胞增殖。
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: 皮下注射H460-DNp53细胞或SW620细胞的雄性NCr小鼠, 或皮下注射H460-DNp53细胞的雄性rnu大鼠
  • Dosages: ~25 mg/kg
  • Administration: 静脉注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 50 mg/mL (137.96 mM)
Water Insoluble
Ethanol Insoluble

* 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 362.42
化学式

C17H19FN4O2S

CAS号 860352-01-8
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
NCT00937664 Terminated Drug: AZD7762|Drug: gemcitabine Cancer|Solid Tumors|Advanced Solid Malignancies AstraZeneca July 2009 Phase 1
NCT00473616 Terminated Drug: AZD7762|Drug: Irinotecan Advanced Solid Tumors|Cancer|Advanced Solid Malignancies AstraZeneca May 2007 Phase 1
NCT00413686 Completed Drug: AZD7762|Drug: Gemcitabine Solid Tumors AstraZeneca December 2006 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:

    If I want to use the inhibitor for i.p. injection, can I use DMSO to dissolve it?

  • 回答:

    Since DMSO has low toxicity with i.p. injection, hydroxyproplyl-β-cyclodextrin is consider a safer co-solvent in compound formulation. In a previous literature report, 11.3% hydroxyproplyl-β-cyclodextrin was used to formulate this compound for i.v. injection.

Chk Signaling Pathway Map

Chk Inhibitors with Unique Features

相关Chk产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID