AZD7762

For research use only.

Catalog No.S1532

94 publications

AZD7762 Chemical Structure

CAS No. 860352-01-8

AZD7762 is a potent and selective inhibitor of Chk1 with IC50 of 5 nM in a cell-free assay. It is equally potent against Chk2 and less potent against CAM, Yes, Fyn, Lyn, Hck and Lck. Phase 1.

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Selleck's AZD7762 has been cited by 94 publications

Purity & Quality Control

Choose Selective Chk Inhibitors

Biological Activity

Description AZD7762 is a potent and selective inhibitor of Chk1 with IC50 of 5 nM in a cell-free assay. It is equally potent against Chk2 and less potent against CAM, Yes, Fyn, Lyn, Hck and Lck. Phase 1.
Targets
Chk1 [1]
(Cell-free assay)
Chk2 [1]
(Cell-free assay)
5 nM <10 nM
In vitro

AZD7762, a more selective Chk1 inhibitor, inhibits Chk1 phosphorylation of a cdc25C peptide by reversibly binding to the ATP-binding site of Chk1, with IC50 of 5 nM and Ki of 3.6 nM. AZD7762 induces cell arrest with EC50 of 0.620 μM, and significantly abrogates the camptothecin induced G2 arrest with an EC50 of 10 nM, by blocking the chk1 dependent degradation of Cdc25A and activation of Cyclin A. AZD7762 (300 nM) enhances the antitumor efficacy of gemcitabine against SW620 and topotecan against MDA-MB-231 by reducing the GI50 values from 24.1 nM and 2.25 μM to 1.08 nM and 0.15 μM, respectively. [1] AZD7762 shows cytotoxicity against a variety of neuroblastoma cell lines bearing p53 wild type, p53 mutation, Mdm2 amplification or p14 deletion with IC50 values ranging from 82.6-505.9 nM. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
KASUMI-1 NF;1cWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPuTWM2OD1yLkCwNFI{PCEQvF2= Mme5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
NKM-1 M17MPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XrVGlEPTB;MD6wNFA1OTVizszN Ml;FQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
MV-4-11 M1j4Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTBwMECwOFI2KM7:TR?= NXvudnVyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
NCI-H1703 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPuTWM2OD1yLkCwOlQ{KM7:TR?= NIjvb2w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
A204 NGfxN4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\3U4x2UUN3ME2wMlAxQDV4IN88US=> NInHdIo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
CGTH-W-1 MlPlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfheHJKSzVyPUCuNFE1OiEQvF2= NETOVFE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
MLMA NUHRbVl1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYP1XpRwUUN3ME2wMlAzQDR7IN88US=> Mn;1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
GOTO NU\1SoJvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTBwMEOxNkDPxE1? MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
KE-37 NVH1WYtxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrSdpNKSzVyPUCuNFMyPDJizszN M4myelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
ES4 M3r4N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vXXmlEPTB;MD6wN|I2OSEQvF2= MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
ATN-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXGV5M3UUN3ME2wMlA{PDF5IN88US=> M37RZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
MHH-PREB-1 NWL2VpoxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnnZoUzUUN3ME2wMlA{PDR{IN88US=> NEfpcoc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
SW756 NVmyPJh3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYr0fnNlUUN3ME2wMlA{PTd7IN88US=> M37pVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
CTV-1 NIL4O|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF[5XZhKSzVyPUCuNFM5QTZizszN NIX1Wlg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
HCC1806 M{LqNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEntbpNKSzVyPUCuNFQxOjJizszN MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
NEC8 NX;vXJA5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkD0TWM2OD1yLkC0NlA{KM7:TR?= NFH1RoU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
P12-ICHIKAWA M1G5Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHe2XpFKSzVyPUCuNFQ{OTZizszN Mo[zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
DEL NH7hc4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTBwMES1PVIh|ryP M1PB[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
KM12 NEHpe2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIK0V3JKSzVyPUCuNFUyPThizszN MoPuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
LB1047-RCC NWjHdnZ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUntcYxjUUN3ME2wMlA3ODJ3IN88US=> MnznQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
LB2241-RCC MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjaeYdDUUN3ME2wMlA3OTB{IN88US=> M2XPUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
NOMO-1 NXm4TWtpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTUTWM2OD1yLkC2NVE2KM7:TR?= M3XJOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
NB14 NHPNWJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnOzTWM2OD1yLkC2NVM3KM7:TR?= MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
ONS-76 M1SwRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\3[YlNUUN3ME2wMlA3OTl4IN88US=> NGDOXHI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
HD-MY-Z M1LiUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3hTWM2OD1yLkC2NlU2KM7:TR?= M1XBS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
G-402 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTBwME[0OkDPxE1? NXjhOWNQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
ES1 NFXMbJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHrRVhKSzVyPUCuNFcyPDZizszN MlL6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
L-363 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHKTWM2OD1yLkC3N|kh|ryP M{XWRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
A4-Fuk MluxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPxVotKSzVyPUCuNFc1QDZizszN MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
OC-314 M{XkWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTKTWM2OD1yLkC3PFA4KM7:TR?= M1LRd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
SK-LU-1 NGnvW2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTBwMEi0NlEh|ryP MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
MDA-MB-157 M{LZXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPDTWM2OD1yLkC4OlU6KM7:TR?= M3P2dlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
HuP-T3 NFLlO4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTzU4pVUUN3ME2wMlA5PzFizszN M2S3TVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
A3-KAW M{fMc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnxTWM2OD1yLkC4PFA3KM7:TR?= MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
MOLT-16 NH\KenJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LNcmlEPTB;MD6wPFgxPyEQvF2= Mni2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
COLO-679 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2C5UGlEPTB;MD6wPVA6OSEQvF2= NHvveoo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
EM-2 MnrWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3jXFdKSzVyPUCuNFk6ODNizszN MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
ES8 M2TXc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTMcIwxUUN3ME2wMlA6QTF6IN88US=> NWD1dlhPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
SK-MEL-2 M4jX[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LnNmlEPTB;MD6xNFA{OyEQvF2= MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
ES3 NV3QfoRCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTYZYpkUUN3ME2wMlExOiEQvF2= MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
HSC-4 NUjzPVFrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPwU|h6UUN3ME2wMlExPTV2IN88US=> MknCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
697 NUTwXlNST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHFTWM2OD1yLkGxNFY{KM7:TR?= NHnGNXU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
TGBC11TKB MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEOwUI9KSzVyPUCuNVExQTNizszN M4rvPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
SK-PN-DW Ml;5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTBwMUG4OkDPxE1? Ml\rQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
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JEG-3 NF3zVoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\hW2lEPTB;MkCuN|U4PyEQvF2= NH\qToI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
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SK-HEP-1 M1PDXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\kXWlEPTB;MkGuOVU1OSEQvF2= MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
NCI-H1770 NEPQcopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTJ|LkSwPFYh|ryP MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
MG-63 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXO[o5KUUN3ME2yN{44Pjd|IN88US=> NEHGbmQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
ECC10 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3roOWlEPTB;MkWuOVcyKM7:TR?= M1THcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
SW1463 M2LoW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnFTWM2OD1{Nz64N|E3KM7:TR?= MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
JVM-2 NYPudXhVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjZTWM2OD1{OD6zNlQ5KM7:TR?= NEOxfYQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
HCT-15 M3PtRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjrTWM2OD1{OD60NVkzKM7:TR?= NVTF[lBjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
CAL-72 NIS1T2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjXd3RQUUN3ME2zNU41QTF{IN88US=> M2\DUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
HCC2218 M{XDXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvVflg6UUN3ME2zNk45QDV6IN88US=> NUD1ZpF1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
BT-474 NEXWVGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TFcmlEPTB;M{OuNFg1OyEQvF2= MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
NCI-H1092 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTN|LkWxOFUh|ryP NF;sfZA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
Mo-T NIj3OolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\ITWM2OD1|Nz6zOVg2KM7:TR?= MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
DU-145 NWe2OJdKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TvNGlEPTB;NECuOlI6PSEQvF2= NWmzOYtxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
NCI-H1666 NIPuXGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TTWmlEPTB;NEKuOFQ5QCEQvF2= MmC3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
IST-MES1 M2Xhfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonqTWM2OD12Nj60NVk3KM7:TR?= MlXtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
SW1116 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTR6LkG3OVYh|ryP MorwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
MZ2-MEL NYnhXJpwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTR6LkWwNlYh|ryP MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>

... 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
In vivo AZD7762 alone at 25 mg/kg shows little antitumor activity in the H460-DNp53 xenograft mice and SW620 xenograft mice, but when administrated in combination with gemcitabine (60 mg/kg), AZD7762 shows significant antitumor efficacy in the two xenografts mice with a log cell kill of 0.9 or percent treated/control (%T/C) of 26 even at low dose of 12.5 mg. Dosing of AZD7762 in combination with gemcitabine (10 mg/kg) in the H460-DNp53 xenograft rat inhibits the tumor volume in a dose-dependent manner with the %T/C values of 48 and 32 for 10 and 20 mg/kg AZD7762, respectively. AZD7762 (25 mg/kg) in combination with irinotecan (25 or 50 mg/kg) causes complete tumor regression in the SW620 xenograft mice with the %T/C increasing significantly to -66% and -67%, respectively. [1]

Protocol

Kinase Assay:[1]
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Chk1 Kinase Assay:

Recombinant human Chk1 is expressed as a glutathione S-transferase fusion in insect cells using a baculovirus vector and purified by glutathione affinity chromatography. A synthetic peptide substrate (N-biotinylaminohexanoyl-KKVSRSGLYRSPMPENLNRPR) for Chk1 is synthesized. Final assay concentrations of peptide and ATP (cold + 40 nCi [33P]ATP) are 0.8 and 1 μM, respectively. Different concentrations of AZD7762, buffer containing peptide and chk1 kinase and ATP, are added sequentially to a 384-well assay plate. The plate is incubated for 2 hours, reaction is stopped by the addition of buffer containing EDTA and scintillation proximity assay beads, and plates are read using a TopCount reader. Data analysis is carried out to determinate a dose response (IC50).
Cell Research:[1]
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  • Cell lines: HT29, SW620 and MDA-MB-231 cells
  • Concentrations: Dissolved in DMSO, final concentration ~12.5 μM
  • Incubation Time: 20 or 48 hours
  • Method: For the checkpoint abrogation assay, HT29 cells are treated for 2 hours with camptothecin (topoisomerase I inhibitor; 0.07 μg/mL) to induce the G2 checkpoint. Cells are then treated for 20 hours with a 12-point titration of AZD7762 (12.5 μM to 6 nM) plus nocodazole. Cells are fixed with 3.7% formaldehyde for 1 hour, permeabilized with PBS containing 0.05% Triton X, and incubated with anti-phH3 antibody for 1 hour followed by Alexa Fluor 488 anti-rabbit and Hoechst stain for 1 hour. Mitotic index is determined on the ArrayScan and expressed as the percentage of cells undergoing mitosis. For the potentiation assays, SW620 or MDA-MB-231 cells are dosed for 24 hours with a 9-point titration of gemcitabine ranging from 0.01 to 100 nM with a constant dose of AZD7762 (300 nM). After 24 hours, medium is removed and AZD7762 alone is added back to the wells for an additional 24 hours. Cells are then incubated in AZD7762-free medium for an additional 72 hours. The effect on cell proliferation is determined by MTT.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Male NCr mice implanted s.c. with H460-DNp53 cells or SW620, and male rnu rats implanted s.c. with H460-DNp53 cells
  • Dosages: ~25 mg/kg
  • Administration: Injection i.v.
    (Only for Reference)

Solubility (25°C)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 362.42
Formula

C17H19FN4O2S

CAS No. 860352-01-8
Storage powder
in solvent
Synonyms N/A
Smiles C1CC(CNC1)NC(=O)C2=C(C=C(S2)C3=CC(=CC=C3)F)NC(=O)N

In vivo Formulation Calculator (Clear solution)

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Clinical Trial Information

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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Frequently Asked Questions

  • Question 1:

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

  • Answer:

    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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID