AZD7762

For research use only.

Catalog No.S1532

92 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 92 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 MmHaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3TTWM2OD1yLkCwNFI{PCEQvF2= MmCzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
NKM-1 MljPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33IcWlEPTB;MD6wNFA1OTVizszN M3nndlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
MV-4-11 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojUTWM2OD1yLkCwNFQzPSEQvF2= M4LBfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
NCI-H1703 Mn\3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn21TWM2OD1yLkCwOlQ{KM7:TR?= NWLkZ3hHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
A204 MmPvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jMPWlEPTB;MD6wNFg2PiEQvF2= NV;0W3BtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
CGTH-W-1 MmW0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTBwMEG0NkDPxE1? NVzxdW14RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
MLMA NVPaPWQ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTvNphKSzVyPUCuNFI5PDlizszN NYjjSHdvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
GOTO NUHqN|J1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mor6TWM2OD1yLkCzNVIh|ryP MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
KE-37 MnTxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTBwMEOxOFIh|ryP NXO3N4FLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
ES4 M{[0[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3sSZVSUUN3ME2wMlA{OjVzIN88US=> NUPYR5JYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
ATN-1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\RVJNKSzVyPUCuNFM1OTdizszN M2PRNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
MHH-PREB-1 Mkf3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nYUGlEPTB;MD6wN|Q1OiEQvF2= NYPhZ2FrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
SW756 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUTjV3FKUUN3ME2wMlA{PTd7IN88US=> NW[5NGtSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
CTV-1 NHXBNnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnn5TWM2OD1yLkCzPFk3KM7:TR?= M1La[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
HCC1806 MlHUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFH4Om1KSzVyPUCuNFQxOjJizszN MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
NEC8 NIS2[ZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjvcVZKSzVyPUCuNFQzODNizszN M1j0dVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
P12-ICHIKAWA MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTBwMESzNVYh|ryP NUfaeHFxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
DEL NEWxO2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTBwMES1PVIh|ryP M4\BT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
KM12 M4H5Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTBwMEWxOVgh|ryP NXnqTldRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
LB1047-RCC NHPq[VhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVe4TW13UUN3ME2wMlA3ODJ3IN88US=> Ml7tQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
LB2241-RCC MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELPU|ZKSzVyPUCuNFYyODJizszN M1zUclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
NOMO-1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fpXmlEPTB;MD6wOlEyPSEQvF2= M2nLOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
NB14 NIK4[YJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTBwME[xN|Yh|ryP M4fIeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
ONS-76 M1W0[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{jlNmlEPTB;MD6wOlE6PiEQvF2= NUTyZmhrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
HD-MY-Z Mme0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPvPIVKSzVyPUCuNFYzPTVizszN M2XwOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
G-402 NX\FU4poT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\p[GlEPTB;MD6wOlQ3KM7:TR?= M3;6eVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
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L-363 Mn;JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TDWmlEPTB;MD6wO|M6KM7:TR?= NYH4c4I{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
A4-Fuk M2L5TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\ueGlEPTB;MD6wO|Q5PiEQvF2= NV3WTXFbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
OC-314 NUXF[IlpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1q5XGlEPTB;MD6wO|gxPyEQvF2= NVrqWXQ4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
SK-LU-1 NHqyUo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDzTWM2OD1yLkC4OFIyKM7:TR?= MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
MDA-MB-157 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3XoWmlEPTB;MD6wPFY2QSEQvF2= NGGzUI49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
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COLO-679 NIPucGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHyO5JKSzVyPUCuNFkxQTFizszN MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
EM-2 NFfud5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PnOWlEPTB;MD6wPVkxOyEQvF2= M1\GNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
ES8 MlG1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmm5TWM2OD1yLkC5PVE5KM7:TR?= M3PCSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
SK-MEL-2 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTBwMUCwN|Mh|ryP M{TWelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
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HSC-4 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTBwMUC1OVQh|ryP M1[w[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
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SK-PN-DW MmfMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDmZmtKSzVyPUCuNVE5PiEQvF2= MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
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MCF7 MkTyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjIZ5JKSzVyPUGzMlI{PjVizszN MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
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NCI-SNU-5 NI[4Z4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTF3LkG3OFEh|ryP NEHQbVA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
NCI-H2405 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLPTWM2OD1zNT60OFc1KM7:TR?= NFPaWYs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
KYSE-150 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPNTWM2OD1zNT63OlEyKM7:TR?= MofBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
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LU-65 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTF7LkeyOkDPxE1? MmHLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
JEG-3 M1vVRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml60TWM2OD1{MD6zOVc4KM7:TR?= MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
SK-MEL-1 NV3XfnlTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;hVnRKSzVyPUKwMlc5OzZizszN MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
SK-HEP-1 NYjpdW5mT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTJzLkW1OFEh|ryP NYP6co5FRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
NCI-H1770 Mn;iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4ezNGlEPTB;MkOuOFA5PiEQvF2= M3;wN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
MG-63 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnSxTWM2OD1{Mz63Olc{KM7:TR?= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
ECC10 NWPzPJNwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXyyXXdSUUN3ME2yOU42PzFizszN NW[3[VhZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
SW1463 NHvaNm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LtNGlEPTB;MkeuPFMyPiEQvF2= M2j0OFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
JVM-2 NF\aWmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPLb|dDUUN3ME2yPE4{OjR6IN88US=> MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
HCT-15 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUT6S2RXUUN3ME2yPE41OTl{IN88US=> MlvwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
CAL-72 NHu2XFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjVXmZzUUN3ME2zNU41QTF{IN88US=> MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN|Lze+V2FPT0WUPD;hQi=>
HCC2218 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HycWlEPTB;M{KuPFg2QCEQvF2= MlvHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
BT-474 NWPQUY9uT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1W1ZmlEPTB;M{OuNFg1OyEQvF2= Mmq0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
NCI-H1092 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rCRWlEPTB;M{OuOVE1PSEQvF2= NWKxc3E6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
Mo-T MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\wUmlEPTB;M{euN|U5PSEQvF2= Mnn4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
DU-145 NFTqTVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfRc3dKSzVyPUSwMlYzQTVizszN M1nYb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK|5USU6JRWK8M4E,
NCI-H1666 NHfOV3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPmfWtKSzVyPUSyMlQ1QDhizszN NHT3dXM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
IST-MES1 Mn;ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTR4LkSxPVYh|ryP MmO5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl|Mz:nQnNCVkeHUkyvZV4>
SW1116 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWT1cIxjUUN3ME20PE4yPzV4IN88US=> NIGyZY09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
MZ2-MEL NVTBVmpMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\NR2NWUUN3ME20PE42ODJ4IN88US=> NGK0Z|A9[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)

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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