AZD7762

For research use only.

Catalog No.S1532

98 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.

Selleck's AZD7762 has been cited by 98 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 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFHVfppKSzVyPUCuNFAxOjN2IN88US=> NUjkcFBDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
NKM-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13RbGlEPTB;MD6wNFA1OTVizszN Ml:yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
MV-4-11 MmftS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mkm4TWM2OD1yLkCwNFQzPSEQvF2= NV2yOIJqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
NCI-H1703 M{S1dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\VeGlEPTB;MD6wNFY1OyEQvF2= NVrDOlRCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
A204 Mn3vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vhTWlEPTB;MD6wNFg2PiEQvF2= NELVOGk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
CGTH-W-1 M3;JT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPJTWM2OD1yLkCxOFIh|ryP MmHYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
MLMA NYK4U|NkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17FWWlEPTB;MD6wNlg1QSEQvF2= NUXTSFlVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
GOTO MoTNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTBwMEOxNkDPxE1? MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
KE-37 M2XFe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDETWM2OD1yLkCzNVQzKM7:TR?= MnKxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
ES4 Mo\0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTBwMEOyOVEh|ryP MnnIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
ATN-1 NVfMZpEyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{C2T2lEPTB;MD6wN|QyPyEQvF2= MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
MHH-PREB-1 NFXJ[phIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\5WnJWUUN3ME2wMlA{PDR{IN88US=> NV;2WFJoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
SW756 NUftb4lOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfEUms4UUN3ME2wMlA{PTd7IN88US=> NF;HfVE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
CTV-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYO4fIJHUUN3ME2wMlA{QDl4IN88US=> MnO3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
HCC1806 M4Pi[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\MTWM2OD1yLkC0NFIzKM7:TR?= MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
NEC8 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1Xa[2lEPTB;MD6wOFIxOyEQvF2= M{jPVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
P12-ICHIKAWA MnL4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPNb5NKSzVyPUCuNFQ{OTZizszN NW[ye5V2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
DEL NH\MTlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmmyTWM2OD1yLkC0OVkzKM7:TR?= NH\LO|g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
KM12 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTBwMEWxOVgh|ryP NYPlcW1JRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
LB1047-RCC M17Qdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfQTFloUUN3ME2wMlA3ODJ3IN88US=> MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
LB2241-RCC NYTsUllPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDXTWM2OD1yLkC2NVAzKM7:TR?= M3\SWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
NOMO-1 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3DWY9uUUN3ME2wMlA3OTF3IN88US=> MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
NB14 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mne0TWM2OD1yLkC2NVM3KM7:TR?= MnLvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
ONS-76 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\QTWM2OD1yLkC2NVk3KM7:TR?= M33Yb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
HD-MY-Z NGr1[oZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVLNRWYzUUN3ME2wMlA3OjV3IN88US=> Mn3OQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
G-402 M1XPeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTQTWM2OD1yLkC2OFYh|ryP MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
ES1 NEj2dZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoT1TWM2OD1yLkC3NVQ3KM7:TR?= NWXlPYFpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
L-363 NEKzfHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mkf0TWM2OD1yLkC3N|kh|ryP NHPyZok9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
A4-Fuk NEOzNotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPtTWM2OD1yLkC3OFg3KM7:TR?= NGPwd2Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
OC-314 NWP1R|h6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\RRoZKSzVyPUCuNFc5ODdizszN NWSxOYxURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
SK-LU-1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU[5dWNRUUN3ME2wMlA5PDJzIN88US=> NX;rTlU3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
MDA-MB-157 NWDUSGk{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfFZ|lqUUN3ME2wMlA5PjV7IN88US=> NHfNZ2M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
HuP-T3 MlP3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTBwMEi3NUDPxE1? MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
A3-KAW NG\QeI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTlTWM2OD1yLkC4PFA3KM7:TR?= M{jkWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
MOLT-16 M{DEXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlP4TWM2OD1yLkC4PFA4KM7:TR?= MnPwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
COLO-679 M3fPVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7UdFRKSzVyPUCuNFkxQTFizszN MnnuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
EM-2 M3q5TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmmzTWM2OD1yLkC5PVA{KM7:TR?= NULxS2d4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
ES8 NWPB[XVnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLWT4xLUUN3ME2wMlA6QTF6IN88US=> NWfoUW1LRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
SK-MEL-2 M1jubGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjNUWtKSzVyPUCuNVAxOzNizszN NX3kXVFwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
ES3 NF7hSHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\FTnpMUUN3ME2wMlExOiEQvF2= NY\iO4hrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
HSC-4 NUjlW|R3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTBwMUC1OVQh|ryP NEnkfpk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
697 NF3ZcW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlr4TWM2OD1yLkGxNFY{KM7:TR?= MkTHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
TGBC11TKB NFnYdpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInhNIJKSzVyPUCuNVExQTNizszN M1eydVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
SK-PN-DW M3nzW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkOwTWM2OD1yLkGxPFYh|ryP NHi4UHY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
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C3A NI\zPYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTF{LkOxO|Ih|ryP M1rjRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
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LU-139 M4TFXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LlO2lEPTB;MUKuOlM{OyEQvF2= MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
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MCF7 MlS5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTF|LkKzOlUh|ryP MlzPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
SW872 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTF2LkW0OlEh|ryP M3jibVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
HT-1376 MmPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn[0TWM2OD1zND64OVgzKM7:TR?= MlTNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
NCI-SNU-5 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVv3bI1KUUN3ME2xOU4yPzRzIN88US=> NHPxO4U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
NCI-H2405 M{LSbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGD4TWtKSzVyPUG1MlQ1PzRizszN MoDNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
KYSE-150 NVKyTnV5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTF3Lke2NVEh|ryP NF7Pfm09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
SW837 M{HCT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLMVZZKSzVyPUG2MlAyOjRizszN Ml6yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
LU-65 MornS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTF7LkeyOkDPxE1? M1fqTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
JEG-3 Mn\US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTJyLkO1O|ch|ryP NWLERVF5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
SK-MEL-1 MkjVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTJyLke4N|Yh|ryP MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
SK-HEP-1 MkDrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTJzLkW1OFEh|ryP MlzyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
NCI-H1770 M2DZeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk[4TWM2OD1{Mz60NFg3KM7:TR?= M{jSbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
MG-63 MmGwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVO3TIFnUUN3ME2yN{44Pjd|IN88US=> MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
ECC10 MmHNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TFZWlEPTB;MkWuOVcyKM7:TR?= NXjWTGNTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
SW1463 NHrGOnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\2VWlEPTB;MkeuPFMyPiEQvF2= MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
JVM-2 M1TSdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3mzRWlEPTB;MkiuN|I1QCEQvF2= MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
HCT-15 NXLIblB[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;KXY1KSzVyPUK4MlQyQTJizszN NHTlems9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
CAL-72 NYS2emh6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTze4tKUUN3ME2zNU41QTF{IN88US=> NVjqdI1{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
HCC2218 Mn\pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnBS5ZZUUN3ME2zNk45QDV6IN88US=> MlHaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
BT-474 M3r3fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTN|LkC4OFMh|ryP NFPlS5E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
NCI-H1092 NELoNIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFn2VoRKSzVyPUOzMlUyPDVizszN NUTHbnduRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
Mo-T NFu3SnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3ryVmlEPTB;M{euN|U5PSEQvF2= MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
DU-145 Ml3JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LGcGlEPTB;NECuOlI6PSEQvF2= MlviQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
NCI-H1666 NX\EW|N6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfuTWM2OD12Mj60OFg5KM7:TR?= NG\MV|c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
IST-MES1 M4j0Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TLO2lEPTB;NE[uOFE6PiEQvF2= NEjWUG09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
SW1116 M{\pVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjxTWM2OD12OD6xO|U3KM7:TR?= M4T0V|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
MZ2-MEL M3;yOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTR6LkWwNlYh|ryP NGn6UGY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?

... 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)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

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Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

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Mass Concentration Volume Molecular Weight

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.

Handling Instructions

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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