AZD7762

Catalog No.S1532

AZD7762 Chemical Structure

Molecular Weight(MW): 362.42

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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Cited by 52 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 M{TVRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTBwMECwNlM1KM7:TR?= MY\TRW5ITVJ?
NKM-1 NG\tTFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXsUlFKSzVyPUCuNFAxPDF3IN88US=> M{DIUHNCVkeHUh?=
MV-4-11 M4XZPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXziOWxXUUN3ME2wMlAxODR{NTFOwG0> MVTTRW5ITVJ?
NCI-H1703 NG\ZOllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnFT|JVUUN3ME2wMlAxPjR|IN88US=> NGTpUWNUSU6JRWK=
A204 M3fjNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzoWm5KSzVyPUCuNFA5PTZizszN NXL1fVdxW0GQR1XS
CGTH-W-1 NXPQZ2VsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTBwMEG0NkDPxE1? M3HPeHNCVkeHUh?=
MLMA NWjBd4FZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTBwMEK4OFkh|ryP NVzObWRkW0GQR1XS
GOTO MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;pfItUUUN3ME2wMlA{OTJizszN NUHDVGxHW0GQR1XS
KE-37 MlGyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTBwMEOxOFIh|ryP NH3iNGVUSU6JRWK=
ES4 M2GwO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LRNmlEPTB;MD6wN|I2OSEQvF2= MmC4V2FPT0WU
ATN-1 M1zUNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXnco8zUUN3ME2wMlA{PDF5IN88US=> NYS0PW1uW0GQR1XS
MHH-PREB-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojkTWM2OD1yLkCzOFQzKM7:TR?= M4j3c3NCVkeHUh?=
SW756 NF:1PIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHoTWM2OD1yLkCzOVc6KM7:TR?= MnrPV2FPT0WU
CTV-1 NHj4W2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXwTWM2OD1yLkCzPFk3KM7:TR?= MWHTRW5ITVJ?
HCC1806 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXCTWM2OD1yLkC0NFIzKM7:TR?= M3vvfHNCVkeHUh?=
NEC8 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFT6T4dKSzVyPUCuNFQzODNizszN NWjkNm0yW0GQR1XS
P12-ICHIKAWA M2jyN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvVbFh3UUN3ME2wMlA1OzF4IN88US=> NFLUfmpUSU6JRWK=
DEL MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HvZWlEPTB;MD6wOFU6OiEQvF2= M{TzRnNCVkeHUh?=
KM12 NFn6V5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{WzWGlEPTB;MD6wOVE2QCEQvF2= MlXIV2FPT0WU
LB1047-RCC MnrTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTBwME[wNlUh|ryP MknHV2FPT0WU
LB2241-RCC NHjnZW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nSZ2lEPTB;MD6wOlExOiEQvF2= Ml\1V2FPT0WU
NOMO-1 NHj2Z2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFKwWY5KSzVyPUCuNFYyOTVizszN M1e5W3NCVkeHUh?=
NB14 M2H3XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mki2TWM2OD1yLkC2NVM3KM7:TR?= M2PPO3NCVkeHUh?=
ONS-76 M{XoXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rM[WlEPTB;MD6wOlE6PiEQvF2= MmPpV2FPT0WU
HD-MY-Z NV[xPGJET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXMTWM2OD1yLkC2NlU2KM7:TR?= NWW4VJNQW0GQR1XS
G-402 NH3H[IRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTBwME[0OkDPxE1? M3n0fnNCVkeHUh?=
ES1 NHnQWGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrHTWM2OD1yLkC3NVQ3KM7:TR?= M1K4Z3NCVkeHUh?=
L-363 M3vOfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3v0cGlEPTB;MD6wO|M6KM7:TR?= NEXHOI9USU6JRWK=
A4-Fuk MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{[1U2lEPTB;MD6wO|Q5PiEQvF2= NGHSfHFUSU6JRWK=
OC-314 NXX0Z|UzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTBwMEe4NFch|ryP NWnh[llsW0GQR1XS
SK-LU-1 MoPpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHPd3J3UUN3ME2wMlA5PDJzIN88US=> M1X6eHNCVkeHUh?=
MDA-MB-157 MkLVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTBwMEi2OVkh|ryP MWTTRW5ITVJ?
HuP-T3 NI\4UlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzXb|hrUUN3ME2wMlA5PzFizszN NIexVpZUSU6JRWK=
A3-KAW MmLmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TnUGlEPTB;MD6wPFgxPiEQvF2= M2[1UHNCVkeHUh?=
MOLT-16 NVL3So1[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoGzTWM2OD1yLkC4PFA4KM7:TR?= NWru[2c{W0GQR1XS
COLO-679 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTBwMEmwPVEh|ryP NVTIXYlqW0GQR1XS
EM-2 M2\CWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTBwMEm5NFMh|ryP NFvQV21USU6JRWK=
ES8 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTWbWRKSzVyPUCuNFk6OThizszN NVH1dFhiW0GQR1XS
SK-MEL-2 M{W0TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHCZlg4UUN3ME2wMlExODN|IN88US=> NGe5SmRUSU6JRWK=
ES3 MmTBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlK3TWM2OD1yLkGwNkDPxE1? MmW1V2FPT0WU
HSC-4 NUP3R3hiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlm0TWM2OD1yLkGwOVU1KM7:TR?= NVfQUGJEW0GQR1XS
697 NYLBNlNGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmS0TWM2OD1yLkGxNFY{KM7:TR?= NVTuZmRNW0GQR1XS
TGBC11TKB Mof3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGri[GlKSzVyPUCuNVExQTNizszN MlnrV2FPT0WU
SK-PN-DW M4jFTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\jfmZKSzVyPUCuNVE5PiEQvF2= MWLTRW5ITVJ?
H9 NW\S[3hGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2OwU2lEPTB;MD6xNlE3PSEQvF2= NHn5R4lUSU6JRWK=
NCI-H2122 NIH4OIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTBwMUKyOUDPxE1? MXLTRW5ITVJ?
ML-2 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTqdXhKSzVyPUCuNVI1QDRizszN NV[yU|ZuW0GQR1XS
MC-IXC NILaTWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlT4TWM2OD1yLkGyPFQ{KM7:TR?= M3LrZnNCVkeHUh?=
KYSE-140 NIHUVmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHT6VFNKSzVyPUCuNVMxPDFizszN M3XQR3NCVkeHUh?=
DOHH-2 NITKSWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mne0TWM2OD1yLkGzNFY1KM7:TR?= NInrOGFUSU6JRWK=
MEL-JUSO MmfsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlGyTWM2OD1yLkGzNVI5KM7:TR?= NW\WSGRTW0GQR1XS
P30-OHK MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfvVlBKSzVyPUCuNVMyPiEQvF2= M{joNHNCVkeHUh?=
CTB-1 MlLtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHiTWM2OD1yLkGzN|I2KM7:TR?= M{jPN3NCVkeHUh?=
ACHN NEDCdnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDEbHNKSzVyPUCuNVM{PjlizszN M2nwPHNCVkeHUh?=
ES5 NGrZTXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjWdXdKSzVyPUCuNVM1PzZizszN NV\oZ3IxW0GQR1XS
SF539 NHLJdZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVLWd5hZUUN3ME2wMlE{PjhizszN NWrsNmlTW0GQR1XS
D-283MED M2P5Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTBwMUO2PFch|ryP NH3FdHZUSU6JRWK=
OVCAR-5 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDGfIFKSzVyPUCuNVM5QTRizszN MlzFV2FPT0WU
RPMI-8866 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTBwMUO5NlUh|ryP NGi1TZpUSU6JRWK=
PANC-03-27 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzGSJc4UUN3ME2wMlE1Ojh6IN88US=> MlHPV2FPT0WU
M14 M3vv[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4f1TWlEPTB;MD6xOFQ3OyEQvF2= M2DpfnNCVkeHUh?=
D-566MG MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LZ[WlEPTB;MD6xOFY6KM7:TR?= M3;lVnNCVkeHUh?=
Ramos-2G6-4C10 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;SRWlEPTB;MD6xOFg1OiEQvF2= MXnTRW5ITVJ?
NOS-1 NUf0eGp7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LlSWlEPTB;MD6xOFk3PyEQvF2= MVzTRW5ITVJ?
YH-13 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7EfIduUUN3ME2wMlE2Pjd2IN88US=> NWmxcJZyW0GQR1XS
NB17 NWe5eot7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLUSo1KSzVyPUCuNVU4QDZizszN M4XDUXNCVkeHUh?=
U-2-OS NX;ySFBPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTBwMUW4OFch|ryP NHm1b|JUSU6JRWK=
ES7 MnfmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTBwMU[wNVEh|ryP NVrFdnJ7W0GQR1XS
LoVo MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjJfXhLUUN3ME2wMlE3OTZ4IN88US=> MorMV2FPT0WU
QIMR-WIL NF\IUHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHiVWpKSzVyPUCuNVY{OTFizszN MXTTRW5ITVJ?
ESS-1 NV\XN3lvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTiVWduUUN3ME2wMlE3PDF|IN88US=> M1fWb3NCVkeHUh?=
LAMA-84 MoOxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\QTWM2OD1yLkG2OVA{KM7:TR?= NYr1Zop6W0GQR1XS
TGBC24TKB NEXaOZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjKTWM2OD1yLkG2OVM2KM7:TR?= NEnrcGFUSU6JRWK=
KU812 NFTvcGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTBwMU[4N{DPxE1? NVPHWo44W0GQR1XS
KARPAS-45 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfONWtxUUN3ME2wMlE3QDR5IN88US=> NGnWdldUSU6JRWK=
ACN NFO2cmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrmOY1KSzVyPUCuNVcyPzFizszN M4HDS3NCVkeHUh?=
RPMI-8226 NFjpN5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2radGlEPTB;MD6xO|Q3PCEQvF2= M4TXbnNCVkeHUh?=
GR-ST M1:wT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDUTWM2OD1yLkG3PFI4KM7:TR?= NXvNdY17W0GQR1XS
SK-UT-1 M1vPd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3yxZmlEPTB;MD6xPFU6QSEQvF2= NYjVZ2ZLW0GQR1XS
SK-N-AS NFrNToVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTBwMUi4NVUh|ryP NYjUUnpLW0GQR1XS
EW-1 NHvURVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjYcXNKSzVyPUCuNVg6ODVizszN MX;TRW5ITVJ?
5637 M3PpTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml2yTWM2OD1yLkG5Nlc5KM7:TR?= MoLsV2FPT0WU
GI-1 NGnSc4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonnTWM2OD1yLkG5OVYyKM7:TR?= MWfTRW5ITVJ?
NCI-H1395 NIW1SINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoK1TWM2OD1yLkG5O|YyKM7:TR?= Ml61V2FPT0WU
CHP-212 NIXUWXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnZfpFKSzVyPUCuNVk4QDJizszN NVrpOFJSW0GQR1XS
A427 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYH3OZJ2UUN3ME2wMlE6QDN{IN88US=> NGS3OFBUSU6JRWK=
BE-13 MoHuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HnXGlEPTB;MD6yNFEyPyEQvF2= NYXGVGNUW0GQR1XS
RS4-11 NHnENmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnO3TWM2OD1yLkKwN|E5KM7:TR?= M13BSXNCVkeHUh?=
TI-73 NUW5WIxIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPsTWM2OD1yLkKwPFc{KM7:TR?= M3LMdHNCVkeHUh?=
HAL-01 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWO2eFVvUUN3ME2wMlIxQTdizszN NVj1SWVtW0GQR1XS
KY821 NG\6bIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvhVIVKSzVyPUCuNlE1OjlizszN NWrZXHhbW0GQR1XS
H4 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrObYJXUUN3ME2wMlIzODZ{IN88US=> NITVU2JUSU6JRWK=
EPLC-272H NV;zUlZ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIH0UIxKSzVyPUCuNlIxPjhizszN NEXB[m5USU6JRWK=
COR-L105 NHjtbpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTBwMkKyN|Uh|ryP Mnn2V2FPT0WU
769-P MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{Hj[2lEPTB;MD6yNlI6QCEQvF2= M4XYW3NCVkeHUh?=
HEL NYPhT2puT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXXemZKSzVyPUCuNlI1PTRizszN MmjxV2FPT0WU
VA-ES-BJ NHPmcoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTBwMkK1OVch|ryP NUHyeJc{W0GQR1XS
IST-MEL1 M2rLdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPDN49KSzVyPUCuNlI2PyEQvF2= NXTpV455W0GQR1XS
KYSE-270 NXW3WHBQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljETWM2OD1yLkKyOlM{KM7:TR?= NFX0bFdUSU6JRWK=
RH-1 M3SzTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXhZlFQUUN3ME2wMlIzPjZ4IN88US=> NH\nSZlUSU6JRWK=
JVM-3 NGDnSFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLOc|RYUUN3ME2wMlI{ODN4IN88US=> NEXSR3JUSU6JRWK=
RPMI-7951 M4fJTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHuTWM2OD1yLkKzNFU3KM7:TR?= NXPWVmhDW0GQR1XS
JAR MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUn5fmloUUN3ME2wMlI{OjN6IN88US=> NULOdXRwW0GQR1XS
MOLT-4 NVjxb|B1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVXPfmx[UUN3ME2wMlI{QDVizszN M3OyXnNCVkeHUh?=
ALL-PO NEjFb2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYWzVnNbUUN3ME2wMlI1OjR|IN88US=> NYLYTlFZW0GQR1XS
SNU-387 NWXFPGVwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTBwMkSzN|kh|ryP M{mwWHNCVkeHUh?=
IGROV-1 NGnQTXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDHc3N4UUN3ME2wMlI1PDBzIN88US=> NUO2eY93W0GQR1XS
MPP-89 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVf1eII6UUN3ME2wMlI1PDVzIN88US=> MVrTRW5ITVJ?
T98G NFzzR|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnz3TWM2OD1yLkK0OVY5KM7:TR?= M3PWVnNCVkeHUh?=
NCI-H510A MnK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYD4[4NDUUN3ME2wMlI1PjJ4IN88US=> M{XqcHNCVkeHUh?=
KOSC-2 MkS5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnQN49KSzVyPUCuNlQ3PzFizszN M1vqfXNCVkeHUh?=
NCI-H23 NWXkfnVNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrUZot{UUN3ME2wMlI1PzZzIN88US=> M3S3V3NCVkeHUh?=
MC116 MlPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTBwMkW2OVQh|ryP M{fl[3NCVkeHUh?=
8-MG-BA M2THcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXH4VHJoUUN3ME2wMlI2PzZ6IN88US=> NFHZZVFUSU6JRWK=
ABC-1 MmnUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\rTWM2OD1yLkK2NFY1KM7:TR?= MVHTRW5ITVJ?
J-RT3-T3-5 NYK4TFRtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPKTWM2OD1yLkK2Olc5KM7:TR?= M{nmRnNCVkeHUh?=
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CAL-120 M{fl[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nDNGlEPTB;ND64OFk6OSEQvF2= Mm\aV2FPT0WU
DMS-114 NHG3WGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITCXVFKSzVyPUWuNVQ2ODZizszN MoW4V2FPT0WU
KYSE-70 Mn:1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nX[mlEPTB;NT6xOFg2QSEQvF2= NVj2OFJ[W0GQR1XS
NCI-H1648 Ml\sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIns[2tKSzVyPUWuNlk4QDJizszN NHXofllUSU6JRWK=
MDA-MB-175-VII MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTVwNESwNVQh|ryP MlHVV2FPT0WU
NCI-H2029 MknTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPyTWM2OD13LkS4NFIzKM7:TR?= NInHdYZUSU6JRWK=
LS-1034 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLrOo9KSzVyPUWuOlY5QDlizszN Ml;ZV2FPT0WU
LB831-BLC NGi3SGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTVwN{CzOFUh|ryP NG\lWXNUSU6JRWK=
MDA-MB-415 NUfjcmxST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHOxb3lKSzVyPUWuO|A5OSEQvF2= NUS5SI9PW0GQR1XS
TE-6 MlnvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPwRWc{UUN3ME21Mlc1OTh{IN88US=> MlfiV2FPT0WU
SK-MEL-24 M2TBTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfpWHd1UUN3ME21Mlc1PTZ2IN88US=> MlfXV2FPT0WU
HUTU-80 NELLOIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MorGTWM2OD13Lke1N|M{KM7:TR?= NUDWfJRrW0GQR1XS
OCUB-M NGTi[XdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHoTWM2OD13Lke3OVY{KM7:TR?= M3zWOHNCVkeHUh?=
IGR-1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PDNGlEPTB;NT64Olg6PCEQvF2= Ml;CV2FPT0WU
NCI-H747 Mk\WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2Pp[mlEPTB;Nj6yOFU5PSEQvF2= NGjhW|FUSU6JRWK=
COLO-680N MmG3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLmTWM2OD14LkO5OFA{KM7:TR?= MVPTRW5ITVJ?
NB12 M1\jfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;rcmlEPTB;Nj63PVczOiEQvF2= NH;Q[5JUSU6JRWK=
SNU-449 NULYS5kxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFy3e5lKSzVyPU[uPVk2QTFizszN M2jEWHNCVkeHUh?=
D-542MG M{fnOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXLTWM2OD15LkGyNlk6KM7:TR?= NUjzcGZkW0GQR1XS
COLO-792 MkDYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PuOmlEPTB;Nz64O|EzPyEQvF2= NFXLVlFUSU6JRWK=
NCI-H810 NYXqOJpTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnmxTWM2OD16LkCyPVg1KM7:TR?= NEXPeVVUSU6JRWK=
T47D NYDCNHlKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M36yUmlEPTB;OD6xOlAzPCEQvF2= MnPDV2FPT0WU
Calu-3 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnS1TWM2OD16LkK4PFg3KM7:TR?= M4jOcnNCVkeHUh?=
COLO-741 MoLKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRThwOUOwPVMh|ryP NF\IN2RUSU6JRWK=
LU-135 NU\SV|hJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTlwMEO0OVIh|ryP MUTTRW5ITVJ?
COLO-678 MomzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTlwMki4OFQh|ryP MmL0V2FPT0WU
NCI-H2126 NYXwO4htT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDrWpZKSzVyPUmuN|M6OTlizszN Mm\uV2FPT0WU
SK-MEL-28 M4[4bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\mcJFKSzVyPUmuOVM2QTZizszN NYnzflhWW0GQR1XS
MFE-280 NVH0c5dMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTFyLkCyNlkh|ryP NIHTfVNUSU6JRWK=
DBTRG-05MG MorLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{W3N2lEPTB;MUCuOFM3QSEQvF2= M1v2O3NCVkeHUh?=
RCC10RGB MoWxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TtT2lEPTB;MUCuOVI2PSEQvF2= NFrCXGZUSU6JRWK=
NTERA-S-cl-D1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjJb3BCUUN3ME2xNE43QDV{IN88US=> NW[0RpN{W0GQR1XS
C3A NXPCWGE4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnmcZRKSzVyPUGyMlMyPzJizszN MW\TRW5ITVJ?
MHH-ES-1 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTF{LkWyPFQh|ryP NFnifFNUSU6JRWK=
LU-139 MnfJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTF{Lk[zN|Mh|ryP Ml7tV2FPT0WU
KNS-42 MmHIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vhT2lEPTB;MUKuPFc4OSEQvF2= NUC1fHNGW0GQR1XS
MCF7 M2XBRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3nSbmlEPTB;MUOuNlM3PSEQvF2= NXjnUHJDW0GQR1XS
SW872 NWHJXG1MT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoqyTWM2OD1zND61OFYyKM7:TR?= M{jSWHNCVkeHUh?=
HT-1376 M{T6WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvhOlZCUUN3ME2xOE45PTh{IN88US=> NX7Tb|l7W0GQR1XS
NCI-SNU-5 M4PH[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTF3LkG3OFEh|ryP M1yzNHNCVkeHUh?=
NCI-H2405 NXzpcXR4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfwfFQzUUN3ME2xOU41PDd2IN88US=> MYXTRW5ITVJ?
KYSE-150 M4jqR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHXd5RKSzVyPUG1Mlc3OTFizszN MVHTRW5ITVJ?
SW837 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXZTWM2OD1zNj6wNVI1KM7:TR?= NIDI[JlUSU6JRWK=
LU-65 NYC3UlV[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\ETWM2OD1zOT63NlYh|ryP MUHTRW5ITVJ?
JEG-3 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fZWGlEPTB;MkCuN|U4PyEQvF2= NYPZOZdOW0GQR1XS
SK-MEL-1 NXq5N|JjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1POV2lEPTB;MkCuO|g{PiEQvF2= MonhV2FPT0WU
SK-HEP-1 M{nte2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDmTWM2OD1{MT61OVQyKM7:TR?= NXjn[ohMW0GQR1XS
NCI-H1770 M4rqSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;idlZnUUN3ME2yN{41ODh4IN88US=> MkH5V2FPT0WU
MG-63 MlnZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTJ|Lke2O|Mh|ryP NXPPOnlRW0GQR1XS
ECC10 M{TRfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfONnlbUUN3ME2yOU42PzFizszN Mm\lV2FPT0WU
SW1463 NFvkXXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrQTWM2OD1{Nz64N|E3KM7:TR?= MknuV2FPT0WU
JVM-2 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTLTWM2OD1{OD6zNlQ5KM7:TR?= MY\TRW5ITVJ?
HCT-15 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTJ6LkSxPVIh|ryP NHnRPIhUSU6JRWK=
CAL-72 NV7o[ohbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV20fIJVUUN3ME2zNU41QTF{IN88US=> NHnRc4VUSU6JRWK=
HCC2218 NXrH[nk2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnGO4dQUUN3ME2zNk45QDV6IN88US=> MkfpV2FPT0WU
BT-474 NInwb3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHoTWM2OD1|Mz6wPFQ{KM7:TR?= Ml3lV2FPT0WU
NCI-H1092 MmnOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;rN2lEPTB;M{OuOVE1PSEQvF2= M{H3cHNCVkeHUh?=
Mo-T M2nGZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7WTWM2OD1|Nz6zOVg2KM7:TR?= MXHTRW5ITVJ?
DU-145 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWroSFV{UUN3ME20NE43Ojl3IN88US=> MUPTRW5ITVJ?
NCI-H1666 NHHyWWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEez[ZBKSzVyPUSyMlQ1QDhizszN NFftVFJUSU6JRWK=
IST-MES1 MkTtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEK0PXZKSzVyPUS2MlQyQTZizszN MmXDV2FPT0WU
SW1116 M4PI[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLqdmlzUUN3ME20PE4yPzV4IN88US=> NI\GVpFUSU6JRWK=
MZ2-MEL NFXwTIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTR6LkWwNlYh|ryP MUHTRW5ITVJ?

... 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
  • Formulation: Formulated in 11.3% hydroxyproplyl-β-cyclodextrin
  • 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

Bio Calculators

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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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

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