AZD7762

For research use only.

Catalog No.S1532

55 publications

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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Selleck's AZD7762 has been cited by 55 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 MnG3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1e0O2lEPTB;MD6wNFAzOzRizszN NYj3PGllW0GQR1XS
NKM-1 NEK3bI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHjNI1KSzVyPUCuNFAxPDF3IN88US=> NGT0dHdUSU6JRWK=
MV-4-11 M3\WNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTJc2M4UUN3ME2wMlAxODR{NTFOwG0> MWnTRW5ITVJ?
NCI-H1703 Mny3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTBwMEC2OFMh|ryP MYLTRW5ITVJ?
A204 MkS3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGj3cpRKSzVyPUCuNFA5PTZizszN MljFV2FPT0WU
CGTH-W-1 M3\EU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XRbWlEPTB;MD6wNVQzKM7:TR?= NFu4TFRUSU6JRWK=
MLMA MkToS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjoc5ZKSzVyPUCuNFI5PDlizszN Mo[0V2FPT0WU
GOTO MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4qzOGlEPTB;MD6wN|EzKM7:TR?= NUf2T2IyW0GQR1XS
KE-37 M1:3PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTBwMEOxOFIh|ryP NX\HTXR4W0GQR1XS
ES4 NHO0V|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7LfZNqUUN3ME2wMlA{OjVzIN88US=> NIDVO3lUSU6JRWK=
ATN-1 NY\1doJCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTmUWp2UUN3ME2wMlA{PDF5IN88US=> MXHTRW5ITVJ?
MHH-PREB-1 NYnsZlRjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLVTWM2OD1yLkCzOFQzKM7:TR?= M3XBSHNCVkeHUh?=
SW756 NEHGeVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\ZV4UzUUN3ME2wMlA{PTd7IN88US=> M1\LZXNCVkeHUh?=
CTV-1 NULTe4hKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPTZWFyUUN3ME2wMlA{QDl4IN88US=> M1K1NnNCVkeHUh?=
HCC1806 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDHTWM2OD1yLkC0NFIzKM7:TR?= MX\TRW5ITVJ?
NEC8 NYrIUXpsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvLTWM2OD1yLkC0NlA{KM7:TR?= M17uXHNCVkeHUh?=
P12-ICHIKAWA MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHDN|NjUUN3ME2wMlA1OzF4IN88US=> MXrTRW5ITVJ?
DEL NF[ze5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPyNYxkUUN3ME2wMlA1PTl{IN88US=> NEXnOGJUSU6JRWK=
KM12 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PtW2lEPTB;MD6wOVE2QCEQvF2= M3vIPHNCVkeHUh?=
LB1047-RCC NIPITIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHhTWM2OD1yLkC2NFI2KM7:TR?= NHn0OW9USU6JRWK=
LB2241-RCC M1nNZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTBwME[xNFIh|ryP MYDTRW5ITVJ?
NOMO-1 NUnMXmhET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILsb2dKSzVyPUCuNFYyOTVizszN M1;RenNCVkeHUh?=
NB14 NFSyS5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTBwME[xN|Yh|ryP M2\nUXNCVkeHUh?=
ONS-76 NHGzT4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLUUGp1UUN3ME2wMlA3OTl4IN88US=> M{fic3NCVkeHUh?=
HD-MY-Z MlXrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnjTWh4UUN3ME2wMlA3OjV3IN88US=> MUjTRW5ITVJ?
G-402 NHTLb41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3we3JKSzVyPUCuNFY1PiEQvF2= M4\Re3NCVkeHUh?=
ES1 M2G1RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTBwMEexOFYh|ryP MX3TRW5ITVJ?
L-363 MmXsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17MR2lEPTB;MD6wO|M6KM7:TR?= MmrXV2FPT0WU
A4-Fuk NE\KOlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI[yNlVKSzVyPUCuNFc1QDZizszN MWnTRW5ITVJ?
OC-314 MlrnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;0XJFQUUN3ME2wMlA4QDB5IN88US=> Ml36V2FPT0WU
SK-LU-1 NXfGXm5oT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nXfmlEPTB;MD6wPFQzOSEQvF2= NYPFW|BEW0GQR1XS
MDA-MB-157 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVGyc4Y3UUN3ME2wMlA5PjV7IN88US=> NVjGTYdRW0GQR1XS
HuP-T3 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml31TWM2OD1yLkC4O|Eh|ryP Mn3pV2FPT0WU
A3-KAW NV\CN4s{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITacG1KSzVyPUCuNFg5ODZizszN MV;TRW5ITVJ?
MOLT-16 M4[yVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXO[mdKSzVyPUCuNFg5ODdizszN M325VXNCVkeHUh?=
COLO-679 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrmTWM2OD1yLkC5NFkyKM7:TR?= M3u2cnNCVkeHUh?=
EM-2 MoPHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTBwMEm5NFMh|ryP M3:ye3NCVkeHUh?=
ES8 M1Ptcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlz5TWM2OD1yLkC5PVE5KM7:TR?= NWL2[o1VW0GQR1XS
SK-MEL-2 M{juSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;2U3JSUUN3ME2wMlExODN|IN88US=> NV3CWoJVW0GQR1XS
ES3 NVHkXnc6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUm4cpBEUUN3ME2wMlExOiEQvF2= MnTlV2FPT0WU
HSC-4 M13VNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlT0TWM2OD1yLkGwOVU1KM7:TR?= NEf6W5BUSU6JRWK=
697 NWWxOpFlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTRTpBTUUN3ME2wMlEyODZ|IN88US=> NGjRVXJUSU6JRWK=
TGBC11TKB MkLOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUK5bmtSUUN3ME2wMlEyODl|IN88US=> Ml;tV2FPT0WU
SK-PN-DW NITwcHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXr5XYd5UUN3ME2wMlEyQDZizszN NHXiW3JUSU6JRWK=
H9 M{TMVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjqPWJKSzVyPUCuNVIyPjVizszN MU\TRW5ITVJ?
NCI-H2122 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlv2TWM2OD1yLkGyNlUh|ryP M{jMUnNCVkeHUh?=
ML-2 NU[xUIZ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHm1SnFKSzVyPUCuNVI1QDRizszN NXrjUVNUW0GQR1XS
MC-IXC MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfJTWM2OD1yLkGyPFQ{KM7:TR?= NX\nOGx[W0GQR1XS
KYSE-140 NFfwfVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jxdmlEPTB;MD6xN|A1OSEQvF2= MXzTRW5ITVJ?
DOHH-2 M1i2[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7Q[YpKSzVyPUCuNVMxPjRizszN M2DMZ3NCVkeHUh?=
MEL-JUSO NXLXSFRtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWrrdGR4UUN3ME2wMlE{OTJ6IN88US=> Mmq4V2FPT0WU
P30-OHK Ml3ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFrveY1KSzVyPUCuNVMyPiEQvF2= M4jMVHNCVkeHUh?=
CTB-1 M3;1Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{m4RmlEPTB;MD6xN|MzPSEQvF2= NGHZPGhUSU6JRWK=
ACHN MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXININSUUN3ME2wMlE{OzZ7IN88US=> NYTl[HJIW0GQR1XS
ES5 M3jy[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHaNGc6UUN3ME2wMlE{PDd4IN88US=> NF75fJdUSU6JRWK=
SF539 MofTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{T1XmlEPTB;MD6xN|Y5KM7:TR?= NXnSRXVRW0GQR1XS
D-283MED MkW2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDJTXNKSzVyPUCuNVM3QDdizszN M3;pbHNCVkeHUh?=
OVCAR-5 NGPOPHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTBwMUO4PVQh|ryP M3TNfXNCVkeHUh?=
RPMI-8866 NXr4ZpVZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXH5N44yUUN3ME2wMlE{QTJ3IN88US=> NGG0TVBUSU6JRWK=
PANC-03-27 M1HRNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTBwMUSyPFgh|ryP MnraV2FPT0WU
M14 MmP4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljWTWM2OD1yLkG0OFY{KM7:TR?= NGCz[oNUSU6JRWK=
D-566MG NFjuT|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXi5N3lOUUN3ME2wMlE1PjlizszN NHfreZJUSU6JRWK=
Ramos-2G6-4C10 MnfWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTBwMUS4OFIh|ryP M2m1[3NCVkeHUh?=
NOS-1 M{Licmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3XTWM2OD1yLkG0PVY4KM7:TR?= M3ft[XNCVkeHUh?=
YH-13 M4r1Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{W3fGlEPTB;MD6xOVY4PCEQvF2= M2Ts[HNCVkeHUh?=
NB17 M1LFdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTBwMUW3PFYh|ryP MWnTRW5ITVJ?
U-2-OS M2nZeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTBwMUW4OFch|ryP M1jiZXNCVkeHUh?=
ES7 NX3pS4gxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTBwMU[wNVEh|ryP NXPDZ25nW0GQR1XS
LoVo MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHu4PWpKSzVyPUCuNVYyPjZizszN MY\TRW5ITVJ?
QIMR-WIL M4r5V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPO[op3UUN3ME2wMlE3OzFzIN88US=> Mn7WV2FPT0WU
ESS-1 Mne0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoL3TWM2OD1yLkG2OFE{KM7:TR?= MlvlV2FPT0WU
LAMA-84 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2D1PGlEPTB;MD6xOlUxOyEQvF2= NHPR[VNUSU6JRWK=
TGBC24TKB NGHvd2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknsTWM2OD1yLkG2OVM2KM7:TR?= M3H6UHNCVkeHUh?=
KU812 NYTFfZV{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\KTWM2OD1yLkG2PFMh|ryP Mo\EV2FPT0WU
KARPAS-45 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PGNGlEPTB;MD6xOlg1PyEQvF2= NVrxfo5iW0GQR1XS
ACN MkjyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfOflNjUUN3ME2wMlE4OTdzIN88US=> NHrXPIRUSU6JRWK=
RPMI-8226 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmS0TWM2OD1yLkG3OFY1KM7:TR?= NHnW[VlUSU6JRWK=
GR-ST MnTjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3aVIdjUUN3ME2wMlE4QDJ5IN88US=> MnLBV2FPT0WU
SK-UT-1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTBwMUi1PVkh|ryP MWLTRW5ITVJ?
SK-N-AS NY\FSG84T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvZO2RKSzVyPUCuNVg5OTVizszN M2LleHNCVkeHUh?=
EW-1 MkD4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTBwMUi5NFUh|ryP MoHiV2FPT0WU
5637 M1PNTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHFPW5uUUN3ME2wMlE6Ojd6IN88US=> MWLTRW5ITVJ?
GI-1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnHUZFKSzVyPUCuNVk2PjFizszN NFXtVGpUSU6JRWK=
NCI-H1395 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DONGlEPTB;MD6xPVc3OSEQvF2= M2j4cnNCVkeHUh?=
CHP-212 M3zkWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfkdlVKSzVyPUCuNVk4QDJizszN NHHFVnJUSU6JRWK=
A427 NHPXWmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fmc2lEPTB;MD6xPVg{OiEQvF2= NGjtXWJUSU6JRWK=
BE-13 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrDTWM2OD1yLkKwNVE4KM7:TR?= MXTTRW5ITVJ?
RS4-11 Mne4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{P1fWlEPTB;MD6yNFMyQCEQvF2= NYPROVBDW0GQR1XS
TI-73 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;2[GlEPTB;MD6yNFg4OyEQvF2= NY\DPWhxW0GQR1XS
HAL-01 MojLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHz3WoRKSzVyPUCuNlA6PyEQvF2= M2D6enNCVkeHUh?=
KY821 NEH4TYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PVfWlEPTB;MD6yNVQzQSEQvF2= M3PsV3NCVkeHUh?=
H4 NXHnXI5FT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljXTWM2OD1yLkKyNFYzKM7:TR?= MoGzV2FPT0WU
EPLC-272H M{DWNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHOyemtKSzVyPUCuNlIxPjhizszN NHfy[HFUSU6JRWK=
COR-L105 NWm0WIhCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HNTmlEPTB;MD6yNlI{PSEQvF2= M{nS[3NCVkeHUh?=
769-P NITqXIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTBwMkKyPVgh|ryP NInqPGFUSU6JRWK=
HEL M1GxWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LUNWlEPTB;MD6yNlQ2PCEQvF2= MoTTV2FPT0WU
VA-ES-BJ NF\4VnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXoTWM2OD1yLkKyOVU4KM7:TR?= NXnTNXpCW0GQR1XS
IST-MEL1 NVnwd45CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LqSmlEPTB;MD6yNlU4KM7:TR?= NGTLOVZUSU6JRWK=
KYSE-270 MnLpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXnTWM2OD1yLkKyOlM{KM7:TR?= M{X3OnNCVkeHUh?=
RH-1 NHLSTIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTBwMkK2OlYh|ryP NHfxfHNUSU6JRWK=
JVM-3 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTBwMkOwN|Yh|ryP MWPTRW5ITVJ?
RPMI-7951 M2jI[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jBOGlEPTB;MD6yN|A2PiEQvF2= MkPwV2FPT0WU
JAR MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkG2TWM2OD1yLkKzNlM5KM7:TR?= NHntU4tUSU6JRWK=
MOLT-4 NFf2Om9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjBRnRnUUN3ME2wMlI{QDVizszN MmqxV2FPT0WU
ALL-PO NHfzc|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGGxdlRKSzVyPUCuNlQzPDNizszN MkWwV2FPT0WU
SNU-387 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjIfWV2UUN3ME2wMlI1OzN7IN88US=> MnGxV2FPT0WU
IGROV-1 MlT0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mkn4TWM2OD1yLkK0OFAyKM7:TR?= NH2ye|RUSU6JRWK=
MPP-89 M1noRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LuSGlEPTB;MD6yOFQ2OSEQvF2= M1rN[nNCVkeHUh?=
T98G MmTtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTBwMkS1Olgh|ryP NXj5T2hxW0GQR1XS
NCI-H510A NXTXUJdIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7kTWM2OD1yLkK0OlI3KM7:TR?= MWjTRW5ITVJ?
KOSC-2 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTBwMkS2O|Eh|ryP MlrWV2FPT0WU
NCI-H23 M4DnZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfCOVNtUUN3ME2wMlI1PzZzIN88US=> MoPTV2FPT0WU
MC116 MnXiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jnR2lEPTB;MD6yOVY2PCEQvF2= NX\tXJpNW0GQR1XS
8-MG-BA MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTjTWM2OD1yLkK1O|Y5KM7:TR?= MXPTRW5ITVJ?
ABC-1 M4HUfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnSTFlmUUN3ME2wMlI3ODZ2IN88US=> MmD5V2FPT0WU
J-RT3-T3-5 MoD6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUSyWpZkUUN3ME2wMlI3Pjd6IN88US=> M2\wVnNCVkeHUh?=
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TK10 M{nWdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUD3fpptUUN3ME2wMlM4QTR6IN88US=> MVPTRW5ITVJ?
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G-401 NVW5[FAyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfUbmFnUUN3ME20Mlg{QDRzIN88US=> M1OxdXNCVkeHUh?=
CAL-120 MmHlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mne0TWM2OD12Lki0PVkyKM7:TR?= M2PjenNCVkeHUh?=
DMS-114 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTUTWM2OD13LkG0OVA3KM7:TR?= M1HEU3NCVkeHUh?=
KYSE-70 NETKOZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfTcmhKSzVyPUWuNVQ5PTlizszN NV\N[oVKW0GQR1XS
NCI-H1648 NWmx[ZZUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4nHTWlEPTB;NT6yPVc5OiEQvF2= M1vKXnNCVkeHUh?=
MDA-MB-175-VII MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTVwNESwNVQh|ryP MYHTRW5ITVJ?
NCI-H2029 NG\qWJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXH1WWxLUUN3ME21MlQ5ODJ{IN88US=> NI[ySWpUSU6JRWK=
LS-1034 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojzTWM2OD13Lk[2PFg6KM7:TR?= NWjSV5BLW0GQR1XS
LB831-BLC NH\kSlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4T2NmlEPTB;NT63NFM1PSEQvF2= MoD1V2FPT0WU
MDA-MB-415 NXfiO2pMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jGN2lEPTB;NT63NFgyKM7:TR?= NWjTPWRVW0GQR1XS
TE-6 M2DzfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\5cZFXUUN3ME21Mlc1OTh{IN88US=> MUXTRW5ITVJ?
SK-MEL-24 MlftS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LvTmlEPTB;NT63OFU3PCEQvF2= NUS0c5JpW0GQR1XS
HUTU-80 NXnrcVF2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXCdXdKSzVyPUWuO|U{OzNizszN NFHDZ2RUSU6JRWK=
OCUB-M M2DQUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEm0UVJKSzVyPUWuO|c2PjNizszN NYnkOWVtW0GQR1XS
IGR-1 NU\ZUnN5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfPXFlKSzVyPUWuPFY5QTRizszN NX7kdG9uW0GQR1XS
NCI-H747 M{DvSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY[wVpU2UUN3ME22MlI1PTh3IN88US=> NI\nfXhUSU6JRWK=
COLO-680N MkTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnCeXJGUUN3ME22MlM6PDB|IN88US=> MljLV2FPT0WU
NB12 NFXpXXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVf4O2FoUUN3ME22Mlc6PzJ{IN88US=> NFP3[mVUSU6JRWK=
SNU-449 NIOxTm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2foVGlEPTB;Nj65PVU6OSEQvF2= NHnXOmZUSU6JRWK=
D-542MG NEPrZ4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\UeGlEPTB;Nz6xNlI6QSEQvF2= Mo\0V2FPT0WU
COLO-792 NVfCWIZ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DhNWlEPTB;Nz64O|EzPyEQvF2= NHTCfWtUSU6JRWK=
NCI-H810 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnFTWM2OD16LkCyPVg1KM7:TR?= NX\2dJhsW0GQR1XS
T47D MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\veHBEUUN3ME24MlE3ODJ2IN88US=> MorqV2FPT0WU
Calu-3 NWPD[WRpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfMTWM2OD16LkK4PFg3KM7:TR?= NGPISZRUSU6JRWK=
COLO-741 M{jt[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRThwOUOwPVMh|ryP NUXycGlHW0GQR1XS
LU-135 MoPNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYmwSHFjUUN3ME25MlA{PDV{IN88US=> M3fNPXNCVkeHUh?=
COLO-678 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3voRmlEPTB;OT6yPFg1PCEQvF2= NGfzWJpUSU6JRWK=
NCI-H2126 MmP1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\mT|JjUUN3ME25MlM{QTF7IN88US=> Ml7tV2FPT0WU
SK-MEL-28 Mn\NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDHdnpKSzVyPUmuOVM2QTZizszN NWf0UolxW0GQR1XS
MFE-280 NVPBUJFiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jQbWlEPTB;MUCuNFIzQSEQvF2= NX;jUJBqW0GQR1XS
DBTRG-05MG MlfRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTFyLkSzOlkh|ryP MVXTRW5ITVJ?
RCC10RGB NEWzTVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPaTWM2OD1zMD61NlU2KM7:TR?= NXe1WmxpW0GQR1XS
NTERA-S-cl-D1 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWq1UmpKUUN3ME2xNE43QDV{IN88US=> Mk\sV2FPT0WU
C3A MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfwTWM2OD1zMj6zNVczKM7:TR?= NWLITVJyW0GQR1XS
MHH-ES-1 MnHtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHRTWM2OD1zMj61Nlg1KM7:TR?= M1PpV3NCVkeHUh?=
LU-139 MkfVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjITWM2OD1zMj62N|M{KM7:TR?= MV\TRW5ITVJ?
KNS-42 M4joemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;sTWM2OD1zMj64O|cyKM7:TR?= M3foXHNCVkeHUh?=
MCF7 NUPrS5BWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTF|LkKzOlUh|ryP MoewV2FPT0WU
SW872 NGPEVJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTF2LkW0OlEh|ryP MWXTRW5ITVJ?
HT-1376 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnriTWM2OD1zND64OVgzKM7:TR?= M4HNbXNCVkeHUh?=
NCI-SNU-5 NHHFR3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfENWdPUUN3ME2xOU4yPzRzIN88US=> M1vZenNCVkeHUh?=
NCI-H2405 MnXZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPpTWM2OD1zNT60OFc1KM7:TR?= NX:xdI1[W0GQR1XS
KYSE-150 MmSwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPqUZdVUUN3ME2xOU44PjFzIN88US=> NEnOVZZUSU6JRWK=
SW837 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2Dmb2lEPTB;MU[uNFEzPCEQvF2= M2SzXHNCVkeHUh?=
LU-65 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXvTWM2OD1zOT63NlYh|ryP NF2zOZJUSU6JRWK=
JEG-3 NIPJd4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTJyLkO1O|ch|ryP M2DCd3NCVkeHUh?=
SK-MEL-1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmC5TWM2OD1{MD63PFM3KM7:TR?= MlHjV2FPT0WU
SK-HEP-1 NIS2[|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTJzLkW1OFEh|ryP M3rRZ3NCVkeHUh?=
NCI-H1770 M1yxW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVm2T495UUN3ME2yN{41ODh4IN88US=> NX2zdY9RW0GQR1XS
MG-63 MlK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfoTFBKSzVyPUKzMlc3PzNizszN MmrhV2FPT0WU
ECC10 NUXNdWsxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4O3cWlEPTB;MkWuOVcyKM7:TR?= M13IZ3NCVkeHUh?=
SW1463 M2PDdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGCwOFRKSzVyPUK3Mlg{OTZizszN M1i0cnNCVkeHUh?=
JVM-2 MkLBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTJ6LkOyOFgh|ryP MWfTRW5ITVJ?
HCT-15 MlH6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPSb5dKSzVyPUK4MlQyQTJizszN M3\0c3NCVkeHUh?=
CAL-72 NFHVeZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTNzLkS5NVIh|ryP Mon4V2FPT0WU
HCC2218 Mln6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPISGlKSzVyPUOyMlg5PThizszN M3nyUHNCVkeHUh?=
BT-474 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrDTWM2OD1|Mz6wPFQ{KM7:TR?= MVrTRW5ITVJ?
NCI-H1092 NVfMOZF[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1v2b2lEPTB;M{OuOVE1PSEQvF2= M3:wd3NCVkeHUh?=
Mo-T NEfPeZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHKcG9KSzVyPUO3MlM2QDVizszN NX;4W4V{W0GQR1XS
DU-145 NYi4[2dxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2L1fmlEPTB;NECuOlI6PSEQvF2= NXroeZNKW0GQR1XS
NCI-H1666 Mnv4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTJTWM2OD12Mj60OFg5KM7:TR?= NEf6Z|ZUSU6JRWK=
IST-MES1 NUXOcGdMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHhTWM2OD12Nj60NVk3KM7:TR?= MWXTRW5ITVJ?
SW1116 M2GyOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M136NmlEPTB;NEiuNVc2PiEQvF2= NFTjWZhUSU6JRWK=
MZ2-MEL MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTR6LkWwNlYh|ryP NILQSZRUSU6JRWK=

... 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
Smiles NC(=O)NC1=C(SC(=C1)C2=CC(=CC=C2)F)C(=O)NC3CCCNC3

Bio Calculators

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

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

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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