Choose Your Country or Region

AZD7762

Name: AZD7762
Brand: Selleck Chemicals
SKU: S1532
Rating: 5 (131 reviews)

Catalog No.S1532 Purity:99.98%

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.

AZD7762 Chemical Structure

CAS No. 860352-01-8

Purity & Quality Control

Batch: Purity: 99.98%

99.98

AZD7762 Related Products

Related Targets	Chk1 Chk2	Click to Expand
Related Products	Rabusertib (LY2603618) MK-8776 (SCH 900776) CHIR-124 Prexasertib HCl (LY2606368) PF-477736 BML-277 (Chk2 Inhibitor II) Prexasertib (LY2606368) CCT245737 (SRA737) GDC-0575	Click to Expand
Related Compound Libraries	Kinase Inhibitor Library PI3K/Akt Inhibitor Library MAPK Inhibitor Library DNA Damage/DNA Repair compound Library Cell Cycle compound library	Click to Expand

Signaling Pathway

Chk Signaling Pathway

Cell Data

Cell Lines	Assay Type	Activity Description	PMID
KASUMI-1	Growth Inhibition Assay	IC50=0.000234 μM	SANGER
NKM-1	Growth Inhibition Assay	IC50=0.000415 μM	SANGER
MV-4-11	Growth Inhibition Assay	IC50=0.000425 μM	SANGER
NCI-H1703	Growth Inhibition Assay	IC50=0.00643 μM	SANGER
A204	Growth Inhibition Assay	IC50=0.00856 μM	SANGER
CGTH-W-1	Growth Inhibition Assay	IC50=0.0142 μM	SANGER
MLMA	Growth Inhibition Assay	IC50=0.02849 μM	SANGER
GOTO	Growth Inhibition Assay	IC50=0.0312 μM	SANGER
KE-37	Growth Inhibition Assay	IC50=0.03142 μM	SANGER
ES4	Growth Inhibition Assay	IC50=0.03251 μM	SANGER
ATN-1	Growth Inhibition Assay	IC50=0.03417 μM	SANGER
MHH-PREB-1	Growth Inhibition Assay	IC50=0.03442 μM	SANGER
SW756	Growth Inhibition Assay	IC50=0.03579 μM	SANGER
CTV-1	Growth Inhibition Assay	IC50=0.03896 μM	SANGER
HCC1806	Growth Inhibition Assay	IC50=0.04022 μM	SANGER
NEC8	Growth Inhibition Assay	IC50=0.04203 μM	SANGER
P12-ICHIKAWA	Growth Inhibition Assay	IC50=0.04316 μM	SANGER
DEL	Growth Inhibition Assay	IC50=0.04592 μM	SANGER
KM12	Growth Inhibition Assay	IC50=0.05158 μM	SANGER
LB1047-RCC	Growth Inhibition Assay	IC50=0.06025 μM	SANGER
LB2241-RCC	Growth Inhibition Assay	IC50=0.06102 μM	SANGER
NOMO-1	Growth Inhibition Assay	IC50=0.06115 μM	SANGER
NB14	Growth Inhibition Assay	IC50=0.06136 μM	SANGER
ONS-76	Growth Inhibition Assay	IC50=0.06196 μM	SANGER
HD-MY-Z	Growth Inhibition Assay	IC50=0.06255 μM	SANGER
G-402	Growth Inhibition Assay	IC50=0.0646 μM	SANGER
ES1	Growth Inhibition Assay	IC50=0.07146 μM	SANGER
L-363	Growth Inhibition Assay	IC50=0.0739 μM	SANGER
A4-Fuk	Growth Inhibition Assay	IC50=0.07486 μM	SANGER
OC-314	Growth Inhibition Assay	IC50=0.07807 μM	SANGER
SK-LU-1	Growth Inhibition Assay	IC50=0.08421 μM	SANGER
MDA-MB-157	Growth Inhibition Assay	IC50=0.08659 μM	SANGER
HuP-T3	Growth Inhibition Assay	IC50=0.0871 μM	SANGER
A3-KAW	Growth Inhibition Assay	IC50=0.08806 μM	SANGER
MOLT-16	Growth Inhibition Assay	IC50=0.08807 μM	SANGER
COLO-679	Growth Inhibition Assay	IC50=0.09091 μM	SANGER
EM-2	Growth Inhibition Assay	IC50=0.09903 μM	SANGER
ES8	Growth Inhibition Assay	IC50=0.09918 μM	SANGER
SK-MEL-2	Growth Inhibition Assay	IC50=0.10033 μM	SANGER
ES3	Growth Inhibition Assay	IC50=0.102 μM	SANGER
HSC-4	Growth Inhibition Assay	IC50=0.10554 μM	SANGER
697	Growth Inhibition Assay	IC50=0.11063 μM	SANGER
TGBC11TKB	Growth Inhibition Assay	IC50=0.11093 μM	SANGER
SK-PN-DW	Growth Inhibition Assay	IC50=0.1186 μM	SANGER
H9	Growth Inhibition Assay	IC50=0.12165 μM	SANGER
NCI-H2122	Growth Inhibition Assay	IC50=0.1225 μM	SANGER
ML-2	Growth Inhibition Assay	IC50=0.12484 μM	SANGER
MC-IXC	Growth Inhibition Assay	IC50=0.12843 μM	SANGER
KYSE-140	Growth Inhibition Assay	IC50=0.13041 μM	SANGER
DOHH-2	Growth Inhibition Assay	IC50=0.13064 μM	SANGER
MEL-JUSO	Growth Inhibition Assay	IC50=0.13128 μM	SANGER
P30-OHK	Growth Inhibition Assay	IC50=0.1316 μM	SANGER
CTB-1	Growth Inhibition Assay	IC50=0.13325 μM	SANGER
ACHN	Growth Inhibition Assay	IC50=0.13369 μM	SANGER
ES5	Growth Inhibition Assay	IC50=0.13476 μM	SANGER
SF539	Growth Inhibition Assay	IC50=0.1368 μM	SANGER
D-283MED	Growth Inhibition Assay	IC50=0.13687 μM	SANGER
OVCAR-5	Growth Inhibition Assay	IC50=0.13894 μM	SANGER
RPMI-8866	Growth Inhibition Assay	IC50=0.13925 μM	SANGER
PANC-03-27	Growth Inhibition Assay	IC50=0.14288 μM	SANGER
M14	Growth Inhibition Assay	IC50=0.14463 μM	SANGER
D-566MG	Growth Inhibition Assay	IC50=0.1469 μM	SANGER
Ramos-2G6-4C10	Growth Inhibition Assay	IC50=0.14842 μM	SANGER
NOS-1	Growth Inhibition Assay	IC50=0.14967 μM	SANGER
YH-13	Growth Inhibition Assay	IC50=0.15674 μM	SANGER
NB17	Growth Inhibition Assay	IC50=0.15786 μM	SANGER
U-2-OS	Growth Inhibition Assay	IC50=0.15847 μM	SANGER
ES7	Growth Inhibition Assay	IC50=0.16011 μM	SANGER
LoVo	Growth Inhibition Assay	IC50=0.16166 μM	SANGER
QIMR-WIL	Growth Inhibition Assay	IC50=0.16311 μM	SANGER
ESS-1	Growth Inhibition Assay	IC50=0.16413 μM	SANGER
LAMA-84	Growth Inhibition Assay	IC50=0.16503 μM	SANGER
TGBC24TKB	Growth Inhibition Assay	IC50=0.16535 μM	SANGER
KU812	Growth Inhibition Assay	IC50=0.1683 μM	SANGER
KARPAS-45	Growth Inhibition Assay	IC50=0.16847 μM	SANGER
ACN	Growth Inhibition Assay	IC50=0.17171 μM	SANGER
RPMI-8226	Growth Inhibition Assay	IC50=0.17464 μM	SANGER
GR-ST	Growth Inhibition Assay	IC50=0.17827 μM	SANGER
SK-UT-1	Growth Inhibition Assay	IC50=0.18599 μM	SANGER
SK-N-AS	Growth Inhibition Assay	IC50=0.18815 μM	SANGER
EW-1	Growth Inhibition Assay	IC50=0.18905 μM	SANGER
5637	Growth Inhibition Assay	IC50=0.19278 μM	SANGER
GI-1	Growth Inhibition Assay	IC50=0.19561 μM	SANGER
NCI-H1395	Growth Inhibition Assay	IC50=0.19761 μM	SANGER
CHP-212	Growth Inhibition Assay	IC50=0.19782 μM	SANGER
A427	Growth Inhibition Assay	IC50=0.19832 μM	SANGER
BE-13	Growth Inhibition Assay	IC50=0.20117 μM	SANGER
RS4-11	Growth Inhibition Assay	IC50=0.20318 μM	SANGER
TI-73	Growth Inhibition Assay	IC50=0.20873 μM	SANGER
HAL-01	Growth Inhibition Assay	IC50=0.2097 μM	SANGER
KY821	Growth Inhibition Assay	IC50=0.21429 μM	SANGER
H4	Growth Inhibition Assay	IC50=0.22062 μM	SANGER
EPLC-272H	Growth Inhibition Assay	IC50=0.22068 μM	SANGER
COR-L105	Growth Inhibition Assay	IC50=0.22235 μM	SANGER
769-P	Growth Inhibition Assay	IC50=0.22298 μM	SANGER
HEL	Growth Inhibition Assay	IC50=0.22454 μM	SANGER
VA-ES-BJ	Growth Inhibition Assay	IC50=0.22557 μM	SANGER
IST-MEL1	Growth Inhibition Assay	IC50=0.2257 μM	SANGER
KYSE-270	Growth Inhibition Assay	IC50=0.22633 μM	SANGER
RH-1	Growth Inhibition Assay	IC50=0.22666 μM	SANGER
JVM-3	Growth Inhibition Assay	IC50=0.23036 μM	SANGER
RPMI-7951	Growth Inhibition Assay	IC50=0.23056 μM	SANGER
JAR	Growth Inhibition Assay	IC50=0.23238 μM	SANGER
MOLT-4	Growth Inhibition Assay	IC50=0.2385 μM	SANGER
ALL-PO	Growth Inhibition Assay	IC50=0.24243 μM	SANGER
SNU-387	Growth Inhibition Assay	IC50=0.24339 μM	SANGER
IGROV-1	Growth Inhibition Assay	IC50=0.24401 μM	SANGER
MPP-89	Growth Inhibition Assay	IC50=0.24451 μM	SANGER
T98G	Growth Inhibition Assay	IC50=0.24568 μM	SANGER
NCI-H510A	Growth Inhibition Assay	IC50=0.24626 μM	SANGER
KOSC-2	Growth Inhibition Assay	IC50=0.24671 μM	SANGER
NCI-H23	Growth Inhibition Assay	IC50=0.24761 μM	SANGER
MC116	Growth Inhibition Assay	IC50=0.25654 μM	SANGER
8-MG-BA	Growth Inhibition Assay	IC50=0.25768 μM	SANGER
ABC-1	Growth Inhibition Assay	IC50=0.26064 μM	SANGER
J-RT3-T3-5	Growth Inhibition Assay	IC50=0.26678 μM	SANGER
NCI-SNU-1	Growth Inhibition Assay	IC50=0.27059 μM	SANGER
HCC1395	Growth Inhibition Assay	IC50=0.27089 μM	SANGER
BB65-RCC	Growth Inhibition Assay	IC50=0.27097 μM	SANGER
NCI-H1755	Growth Inhibition Assay	IC50=0.27304 μM	SANGER
OVCAR-3	Growth Inhibition Assay	IC50=0.27385 μM	SANGER
MKN45	Growth Inhibition Assay	IC50=0.2798 μM	SANGER
TYK-nu	Growth Inhibition Assay	IC50=0.2806 μM	SANGER
SNU-C2B	Growth Inhibition Assay	IC50=0.28134 μM	SANGER
H-EMC-SS	Growth Inhibition Assay	IC50=0.28354 μM	SANGER
CAKI-1	Growth Inhibition Assay	IC50=0.2868 μM	SANGER
EW-24	Growth Inhibition Assay	IC50=0.2891 μM	SANGER
RXF393	Growth Inhibition Assay	IC50=0.29008 μM	SANGER
CCRF-CEM	Growth Inhibition Assay	IC50=0.29154 μM	SANGER
HOP-92	Growth Inhibition Assay	IC50=0.29279 μM	SANGER
COLO-684	Growth Inhibition Assay	IC50=0.29406 μM	SANGER
NCI-H28	Growth Inhibition Assay	IC50=0.29704 μM	SANGER
HuO9	Growth Inhibition Assay	IC50=0.29793 μM	SANGER
SF295	Growth Inhibition Assay	IC50=0.29802 μM	SANGER
COLO-829	Growth Inhibition Assay	IC50=0.29845 μM	SANGER
MSTO-211H	Growth Inhibition Assay	IC50=0.29855 μM	SANGER
MDA-MB-361	Growth Inhibition Assay	IC50=0.29896 μM	SANGER
FTC-133	Growth Inhibition Assay	IC50=0.30265 μM	SANGER
Mewo	Growth Inhibition Assay	IC50=0.30431 μM	SANGER
HCC70	Growth Inhibition Assay	IC50=0.30665 μM	SANGER
BB30-HNC	Growth Inhibition Assay	IC50=0.31525 μM	SANGER
LCLC-97TM1	Growth Inhibition Assay	IC50=0.31566 μM	SANGER
HCC2998	Growth Inhibition Assay	IC50=0.3165 μM	SANGER
NBsusSR	Growth Inhibition Assay	IC50=0.31819 μM	SANGER
OVCAR-4	Growth Inhibition Assay	IC50=0.32021 μM	SANGER
NCI-H209	Growth Inhibition Assay	IC50=0.32353 μM	SANGER
ChaGo-K-1	Growth Inhibition Assay	IC50=0.32489 μM	SANGER
KALS-1	Growth Inhibition Assay	IC50=0.32594 μM	SANGER
D-423MG	Growth Inhibition Assay	IC50=0.33142 μM	SANGER
Detroit562	Growth Inhibition Assay	IC50=0.33343 μM	SANGER
HT-144	Growth Inhibition Assay	IC50=0.3381 μM	SANGER
MEG-01	Growth Inhibition Assay	IC50=0.34584 μM	SANGER
BV-173	Growth Inhibition Assay	IC50=0.34596 μM	SANGER
MZ7-mel	Growth Inhibition Assay	IC50=0.34677 μM	SANGER
C32	Growth Inhibition Assay	IC50=0.34682 μM	SANGER
DU-4475	Growth Inhibition Assay	IC50=0.34875 μM	SANGER
KP-N-YN	Growth Inhibition Assay	IC50=0.34887 μM	SANGER
MKN1	Growth Inhibition Assay	IC50=0.35002 μM	SANGER
8505C	Growth Inhibition Assay	IC50=0.35002 μM	SANGER
OVCAR-8	Growth Inhibition Assay	IC50=0.35584 μM	SANGER
NH-12	Growth Inhibition Assay	IC50=0.35696 μM	SANGER
COR-L88	Growth Inhibition Assay	IC50=0.36482 μM	SANGER
T-24	Growth Inhibition Assay	IC50=0.36985 μM	SANGER
MIA-PaCa-2	Growth Inhibition Assay	IC50=0.37497 μM	SANGER
LS-411N	Growth Inhibition Assay	IC50=0.37606 μM	SANGER
TK10	Growth Inhibition Assay	IC50=0.37948 μM	SANGER
SW1990	Growth Inhibition Assay	IC50=0.38353 μM	SANGER
GAMG	Growth Inhibition Assay	IC50=0.38567 μM	SANGER
G-361	Growth Inhibition Assay	IC50=0.38712 μM	SANGER
Ca-Ski	Growth Inhibition Assay	IC50=0.38792 μM	SANGER
786-0	Growth Inhibition Assay	IC50=0.38823 μM	SANGER
MHH-NB-11	Growth Inhibition Assay	IC50=0.3897 μM	SANGER
OE33	Growth Inhibition Assay	IC50=0.39118 μM	SANGER
SW954	Growth Inhibition Assay	IC50=0.40131 μM	SANGER
KYSE-180	Growth Inhibition Assay	IC50=0.40151 μM	SANGER
NCI-H720	Growth Inhibition Assay	IC50=0.40191 μM	SANGER
COR-L23	Growth Inhibition Assay	IC50=0.40286 μM	SANGER
PFSK-1	Growth Inhibition Assay	IC50=0.41092 μM	SANGER
FADU	Growth Inhibition Assay	IC50=0.41172 μM	SANGER
GP5d	Growth Inhibition Assay	IC50=0.41225 μM	SANGER
PC-14	Growth Inhibition Assay	IC50=0.41661 μM	SANGER
SJSA-1	Growth Inhibition Assay	IC50=0.41714 μM	SANGER
D-336MG	Growth Inhibition Assay	IC50=0.42138 μM	SANGER
LOXIMVI	Growth Inhibition Assay	IC50=0.42885 μM	SANGER
EFO-27	Growth Inhibition Assay	IC50=0.43049 μM	SANGER
A2780	Growth Inhibition Assay	IC50=0.43162 μM	SANGER
CAL-12T	Growth Inhibition Assay	IC50=0.43288 μM	SANGER
ES6	Growth Inhibition Assay	IC50=0.44185 μM	SANGER
HCE-T	Growth Inhibition Assay	IC50=0.44187 μM	SANGER
SK-MES-1	Growth Inhibition Assay	IC50=0.44293 μM	SANGER
Daoy	Growth Inhibition Assay	IC50=0.45103 μM	SANGER
A2058	Growth Inhibition Assay	IC50=0.45136 μM	SANGER
Hs-578-T	Growth Inhibition Assay	IC50=0.45278 μM	SANGER
TE-11	Growth Inhibition Assay	IC50=0.45293 μM	SANGER
GI-ME-N	Growth Inhibition Assay	IC50=0.4546 μM	SANGER
D-392MG	Growth Inhibition Assay	IC50=0.45612 μM	SANGER
MOLT-13	Growth Inhibition Assay	IC50=0.46294 μM	SANGER
SK-NEP-1	Growth Inhibition Assay	IC50=0.46419 μM	SANGER
KS-1	Growth Inhibition Assay	IC50=0.46603 μM	SANGER
HuP-T4	Growth Inhibition Assay	IC50=0.46868 μM	SANGER
NCI-H1563	Growth Inhibition Assay	IC50=0.47035 μM	SANGER
U031	Growth Inhibition Assay	IC50=0.48234 μM	SANGER
HSC-3	Growth Inhibition Assay	IC50=0.48626 μM	SANGER
HT-3	Growth Inhibition Assay	IC50=0.4903 μM	SANGER
HGC-27	Growth Inhibition Assay	IC50=0.49115 μM	SANGER
HT-1080	Growth Inhibition Assay	IC50=0.4927 μM	SANGER
RT-112	Growth Inhibition Assay	IC50=0.49921 μM	SANGER
A375	Growth Inhibition Assay	IC50=0.49922 μM	SANGER
SW626	Growth Inhibition Assay	IC50=0.50633 μM	SANGER
SBC-5	Growth Inhibition Assay	IC50=0.51344 μM	SANGER
CAL-51	Growth Inhibition Assay	IC50=0.51437 μM	SANGER
RKO	Growth Inhibition Assay	IC50=0.52019 μM	SANGER
HC-1	Growth Inhibition Assay	IC50=0.52114 μM	SANGER
CHL-1	Growth Inhibition Assay	IC50=0.52551 μM	SANGER
SK-N-DZ	Growth Inhibition Assay	IC50=0.53078 μM	SANGER
SNU-423	Growth Inhibition Assay	IC50=0.53466 μM	SANGER
NB13	Growth Inhibition Assay	IC50=0.53657 μM	SANGER
EW-16	Growth Inhibition Assay	IC50=0.53774 μM	SANGER
A704	Growth Inhibition Assay	IC50=0.53881 μM	SANGER
Ca9-22	Growth Inhibition Assay	IC50=0.54077 μM	SANGER
NCI-H1299	Growth Inhibition Assay	IC50=0.5558 μM	SANGER
LB771-HNC	Growth Inhibition Assay	IC50=0.55933 μM	SANGER
EW-11	Growth Inhibition Assay	IC50=0.56326 μM	SANGER
LC-2-ad	Growth Inhibition Assay	IC50=0.56522 μM	SANGER
KNS-62	Growth Inhibition Assay	IC50=0.56553 μM	SANGER
CAL-62	Growth Inhibition Assay	IC50=0.57121 μM	SANGER
SF126	Growth Inhibition Assay	IC50=0.57421 μM	SANGER
OMC-1	Growth Inhibition Assay	IC50=0.57497 μM	SANGER
AGS	Growth Inhibition Assay	IC50=0.58162 μM	SANGER
EW-22	Growth Inhibition Assay	IC50=0.58375 μM	SANGER
KP-N-YS	Growth Inhibition Assay	IC50=0.58382 μM	SANGER
BFTC-909	Growth Inhibition Assay	IC50=0.58833 μM	SANGER
PSN1	Growth Inhibition Assay	IC50=0.59118 μM	SANGER
NB10	Growth Inhibition Assay	IC50=0.59129 μM	SANGER
COLO-800	Growth Inhibition Assay	IC50=0.60328 μM	SANGER
647-V	Growth Inhibition Assay	IC50=0.61787 μM	SANGER
VM-CUB-1	Growth Inhibition Assay	IC50=0.61861 μM	SANGER
OS-RC-2	Growth Inhibition Assay	IC50=0.6201 μM	SANGER
IST-SL1	Growth Inhibition Assay	IC50=0.62788 μM	SANGER
NCI-H661	Growth Inhibition Assay	IC50=0.63712 μM	SANGER
ETK-1	Growth Inhibition Assay	IC50=0.63721 μM	SANGER
SW1710	Growth Inhibition Assay	IC50=0.64023 μM	SANGER
GCT	Growth Inhibition Assay	IC50=0.64935 μM	SANGER
SKG-IIIa	Growth Inhibition Assay	IC50=0.65036 μM	SANGER
LU-134-A	Growth Inhibition Assay	IC50=0.6565 μM	SANGER
Becker	Growth Inhibition Assay	IC50=0.65805 μM	SANGER
PANC-08-13	Growth Inhibition Assay	IC50=0.66068 μM	SANGER
SW620	Growth Inhibition Assay	IC50=0.66223 μM	SANGER
AsPC-1	Growth Inhibition Assay	IC50=0.66361 μM	SANGER
LXF-289	Growth Inhibition Assay	IC50=0.67625 μM	SANGER
RERF-LC-MS	Growth Inhibition Assay	IC50=0.67671 μM	SANGER
NCI-H1355	Growth Inhibition Assay	IC50=0.67852 μM	SANGER
23132-87	Growth Inhibition Assay	IC50=0.68306 μM	SANGER
BHY	Growth Inhibition Assay	IC50=0.68804 μM	SANGER
C2BBe1	Growth Inhibition Assay	IC50=0.68928 μM	SANGER
A172	Growth Inhibition Assay	IC50=0.69217 μM	SANGER
NCI-H727	Growth Inhibition Assay	IC50=0.69812 μM	SANGER
NB69	Growth Inhibition Assay	IC50=0.70549 μM	SANGER
HCC1937	Growth Inhibition Assay	IC50=0.70631 μM	SANGER
HuCCT1	Growth Inhibition Assay	IC50=0.70765 μM	SANGER
HH	Growth Inhibition Assay	IC50=0.70781 μM	SANGER
MN-60	Growth Inhibition Assay	IC50=0.72124 μM	SANGER
CFPAC-1	Growth Inhibition Assay	IC50=0.72257 μM	SANGER
HOP-62	Growth Inhibition Assay	IC50=0.7262 μM	SANGER
EW-3	Growth Inhibition Assay	IC50=0.73552 μM	SANGER
SW1417	Growth Inhibition Assay	IC50=0.73593 μM	SANGER
NCI-H1155	Growth Inhibition Assay	IC50=0.73864 μM	SANGER
CAL-54	Growth Inhibition Assay	IC50=0.7403 μM	SANGER
Saos-2	Growth Inhibition Assay	IC50=0.74584 μM	SANGER
NCI-H446	Growth Inhibition Assay	IC50=0.74806 μM	SANGER
LS-513	Growth Inhibition Assay	IC50=0.74908 μM	SANGER
PA-1	Growth Inhibition Assay	IC50=0.74968 μM	SANGER
HCC38	Growth Inhibition Assay	IC50=0.74984 μM	SANGER
DMS-273	Growth Inhibition Assay	IC50=0.75456 μM	SANGER
U-266	Growth Inhibition Assay	IC50=0.76262 μM	SANGER
HL-60	Growth Inhibition Assay	IC50=0.77355 μM	SANGER
UACC-62	Growth Inhibition Assay	IC50=0.77553 μM	SANGER
DoTc2-4510	Growth Inhibition Assay	IC50=0.78211 μM	SANGER
SW982	Growth Inhibition Assay	IC50=0.78432 μM	SANGER
8305C	Growth Inhibition Assay	IC50=0.78939 μM	SANGER
SW48	Growth Inhibition Assay	IC50=0.7924 μM	SANGER
NB5	Growth Inhibition Assay	IC50=0.79651 μM	SANGER
J82	Growth Inhibition Assay	IC50=0.80487 μM	SANGER
HDLM-2	Growth Inhibition Assay	IC50=0.81349 μM	SANGER
HEC-1	Growth Inhibition Assay	IC50=0.81371 μM	SANGER
AU565	Growth Inhibition Assay	IC50=0.8244 μM	SANGER
KYSE-520	Growth Inhibition Assay	IC50=0.82636 μM	SANGER
HTC-C3	Growth Inhibition Assay	IC50=0.83474 μM	SANGER
AN3-CA	Growth Inhibition Assay	IC50=0.83711 μM	SANGER
KG-1	Growth Inhibition Assay	IC50=0.84484 μM	SANGER
NCI-N87	Growth Inhibition Assay	IC50=0.84556 μM	SANGER
HN	Growth Inhibition Assay	IC50=0.84591 μM	SANGER
SiHa	Growth Inhibition Assay	IC50=0.85882 μM	SANGER
C-33-A	Growth Inhibition Assay	IC50=0.86185 μM	SANGER
A673	Growth Inhibition Assay	IC50=0.86536 μM	SANGER
HSC-2	Growth Inhibition Assay	IC50=0.87334 μM	SANGER
LN-405	Growth Inhibition Assay	IC50=0.87731 μM	SANGER
HOS	Growth Inhibition Assay	IC50=0.87995 μM	SANGER
SF268	Growth Inhibition Assay	IC50=0.88097 μM	SANGER
DJM-1	Growth Inhibition Assay	IC50=0.88602 μM	SANGER
HT-29	Growth Inhibition Assay	IC50=0.89417 μM	SANGER
NCI-H292	Growth Inhibition Assay	IC50=0.89777 μM	SANGER
UM-UC-3	Growth Inhibition Assay	IC50=0.90316 μM	SANGER
VMRC-RCZ	Growth Inhibition Assay	IC50=0.90578 μM	SANGER
D-263MG	Growth Inhibition Assay	IC50=0.90943 μM	SANGER
TE-10	Growth Inhibition Assay	IC50=0.90984 μM	SANGER
SW1088	Growth Inhibition Assay	IC50=0.91552 μM	SANGER
NCI-H1048	Growth Inhibition Assay	IC50=0.91852 μM	SANGER
A431	Growth Inhibition Assay	IC50=0.92452 μM	SANGER
SW1783	Growth Inhibition Assay	IC50=0.93251 μM	SANGER
NCI-H2452	Growth Inhibition Assay	IC50=0.93557 μM	SANGER
OAW-42	Growth Inhibition Assay	IC50=0.93665 μM	SANGER
HuO-3N1	Growth Inhibition Assay	IC50=0.94092 μM	SANGER
K5	Growth Inhibition Assay	IC50=0.94127 μM	SANGER
SW1573	Growth Inhibition Assay	IC50=0.94227 μM	SANGER
NCI-H1792	Growth Inhibition Assay	IC50=0.94237 μM	SANGER
HCC1187	Growth Inhibition Assay	IC50=0.96749 μM	SANGER
HCE-4	Growth Inhibition Assay	IC50=0.9696 μM	SANGER
HPAF-II	Growth Inhibition Assay	IC50=0.97028 μM	SANGER
MEL-HO	Growth Inhibition Assay	IC50=0.97945 μM	SANGER
LCLC-103H	Growth Inhibition Assay	IC50=0.98027 μM	SANGER
CAL-33	Growth Inhibition Assay	IC50=0.98378 μM	SANGER
NB6	Growth Inhibition Assay	IC50=0.98462 μM	SANGER
BFTC-905	Growth Inhibition Assay	IC50=0.98473 μM	SANGER
NMC-G1	Growth Inhibition Assay	IC50=0.98592 μM	SANGER
RCM-1	Growth Inhibition Assay	IC50=0.99258 μM	SANGER
COLO-320-HSR	Growth Inhibition Assay	IC50=1.00412 μM	SANGER
NCI-H2030	Growth Inhibition Assay	IC50=1.01813 μM	SANGER
SCC-4	Growth Inhibition Assay	IC50=1.01859 μM	SANGER
KYSE-410	Growth Inhibition Assay	IC50=1.0352 μM	SANGER
NCI-H1650	Growth Inhibition Assay	IC50=1.03971 μM	SANGER
S-117	Growth Inhibition Assay	IC50=1.04 μM	SANGER
GAK	Growth Inhibition Assay	IC50=1.05075 μM	SANGER
KYSE-450	Growth Inhibition Assay	IC50=1.05336 μM	SANGER
M059J	Growth Inhibition Assay	IC50=1.06828 μM	SANGER
LAN-6	Growth Inhibition Assay	IC50=1.07773 μM	SANGER
NCI-H1651	Growth Inhibition Assay	IC50=1.09352 μM	SANGER
KMOE-2	Growth Inhibition Assay	IC50=1.10973 μM	SANGER
SN12C	Growth Inhibition Assay	IC50=1.11785 μM	SANGER
SW900	Growth Inhibition Assay	IC50=1.12251 μM	SANGER
TE-8	Growth Inhibition Assay	IC50=1.12291 μM	SANGER
HO-1-N-1	Growth Inhibition Assay	IC50=1.14353 μM	SANGER
BHT-101	Growth Inhibition Assay	IC50=1.14714 μM	SANGER
639-V	Growth Inhibition Assay	IC50=1.1667 μM	SANGER
RVH-421	Growth Inhibition Assay	IC50=1.19347 μM	SANGER
SW780	Growth Inhibition Assay	IC50=1.19515 μM	SANGER
SNB75	Growth Inhibition Assay	IC50=1.19819 μM	SANGER
U-87-MG	Growth Inhibition Assay	IC50=1.21334 μM	SANGER
TE-1	Growth Inhibition Assay	IC50=1.21367 μM	SANGER
CAS-1	Growth Inhibition Assay	IC50=1.21418 μM	SANGER
MKN7	Growth Inhibition Assay	IC50=1.21478 μM	SANGER
KM-H2	Growth Inhibition Assay	IC50=1.21773 μM	SANGER
NCI-H1693	Growth Inhibition Assay	IC50=1.22758 μM	SANGER
KGN	Growth Inhibition Assay	IC50=1.23359 μM	SANGER
NCI-H2347	Growth Inhibition Assay	IC50=1.23525 μM	SANGER
MFM-223	Growth Inhibition Assay	IC50=1.24343 μM	SANGER
OCI-AML2	Growth Inhibition Assay	IC50=1.26666 μM	SANGER
SAS	Growth Inhibition Assay	IC50=1.26672 μM	SANGER
BT-549	Growth Inhibition Assay	IC50=1.26782 μM	SANGER
NCI-H2228	Growth Inhibition Assay	IC50=1.2864 μM	SANGER
BxPC-3	Growth Inhibition Assay	IC50=1.30672 μM	SANGER
SCH	Growth Inhibition Assay	IC50=1.32503 μM	SANGER
GMS-10	Growth Inhibition Assay	IC50=1.34551 μM	SANGER
GB-1	Growth Inhibition Assay	IC50=1.37564 μM	SANGER
NCI-H520	Growth Inhibition Assay	IC50=1.38168 μM	SANGER
GCIY	Growth Inhibition Assay	IC50=1.39051 μM	SANGER
HuH-7	Growth Inhibition Assay	IC50=1.39501 μM	SANGER
IA-LM	Growth Inhibition Assay	IC50=1.39986 μM	SANGER
BB49-HNC	Growth Inhibition Assay	IC50=1.40231 μM	SANGER
Calu-6	Growth Inhibition Assay	IC50=1.41187 μM	SANGER
NCI-H650	Growth Inhibition Assay	IC50=1.41795 μM	SANGER
TE-5	Growth Inhibition Assay	IC50=1.41954 μM	SANGER
KINGS-1	Growth Inhibition Assay	IC50=1.42018 μM	SANGER
HCT-116	Growth Inhibition Assay	IC50=1.42176 μM	SANGER
NCI-H1573	Growth Inhibition Assay	IC50=1.42257 μM	SANGER
NCI-H358	Growth Inhibition Assay	IC50=1.43128 μM	SANGER
LNCaP-Clone-FGC	Growth Inhibition Assay	IC50=1.44319 μM	SANGER
KP-4	Growth Inhibition Assay	IC50=1.46151 μM	SANGER
LK-2	Growth Inhibition Assay	IC50=1.46382 μM	SANGER
EFM-19	Growth Inhibition Assay	IC50=1.48104 μM	SANGER
GT3TKB	Growth Inhibition Assay	IC50=1.48613 μM	SANGER
A549	Growth Inhibition Assay	IC50=1.48833 μM	SANGER
no-11	Growth Inhibition Assay	IC50=1.49026 μM	SANGER
SK-N-FI	Growth Inhibition Assay	IC50=1.4938 μM	SANGER
NCI-H2170	Growth Inhibition Assay	IC50=1.52313 μM	SANGER
NCI-H460	Growth Inhibition Assay	IC50=1.52961 μM	SANGER
NCI-H526	Growth Inhibition Assay	IC50=1.53706 μM	SANGER
KYSE-510	Growth Inhibition Assay	IC50=1.5825 μM	SANGER
YKG-1	Growth Inhibition Assay	IC50=1.58328 μM	SANGER
EW-18	Growth Inhibition Assay	IC50=1.60227 μM	SANGER
MDA-MB-231	Growth Inhibition Assay	IC50=1.6038 μM	SANGER
HT55	Growth Inhibition Assay	IC50=1.60591 μM	SANGER
NCI-H1793	Growth Inhibition Assay	IC50=1.61345 μM	SANGER
TE-9	Growth Inhibition Assay	IC50=1.63456 μM	SANGER
DSH1	Growth Inhibition Assay	IC50=1.69256 μM	SANGER
A101D	Growth Inhibition Assay	IC50=1.69983 μM	SANGER
DB	Growth Inhibition Assay	IC50=1.70067 μM	SANGER
ME-180	Growth Inhibition Assay	IC50=1.71785 μM	SANGER
BT-20	Growth Inhibition Assay	IC50=1.72407 μM	SANGER
A498	Growth Inhibition Assay	IC50=1.72963 μM	SANGER
UMC-11	Growth Inhibition Assay	IC50=1.76749 μM	SANGER
EC-GI-10	Growth Inhibition Assay	IC50=1.77556 μM	SANGER
NCI-H630	Growth Inhibition Assay	IC50=1.78642 μM	SANGER
EGI-1	Growth Inhibition Assay	IC50=1.80267 μM	SANGER
22RV1	Growth Inhibition Assay	IC50=1.80853 μM	SANGER
LS-123	Growth Inhibition Assay	IC50=1.81214 μM	SANGER
OAW-28	Growth Inhibition Assay	IC50=1.84746 μM	SANGER
CaR-1	Growth Inhibition Assay	IC50=1.8707 μM	SANGER
HT	Growth Inhibition Assay	IC50=1.87342 μM	SANGER
BCPAP	Growth Inhibition Assay	IC50=1.88676 μM	SANGER
RMG-I	Growth Inhibition Assay	IC50=1.90787 μM	SANGER
C8166	Growth Inhibition Assay	IC50=1.90932 μM	SANGER
TGBC1TKB	Growth Inhibition Assay	IC50=1.92035 μM	SANGER
SCC-9	Growth Inhibition Assay	IC50=1.99105 μM	SANGER
EKVX	Growth Inhibition Assay	IC50=2.00154 μM	SANGER
KU-19-19	Growth Inhibition Assay	IC50=2.00372 μM	SANGER
K-562	Growth Inhibition Assay	IC50=2.00898 μM	SANGER
SW962	Growth Inhibition Assay	IC50=2.04059 μM	SANGER
MDA-MB-453	Growth Inhibition Assay	IC50=2.05442 μM	SANGER
BPH-1	Growth Inhibition Assay	IC50=2.07098 μM	SANGER
DK-MG	Growth Inhibition Assay	IC50=2.08603 μM	SANGER
Capan-2	Growth Inhibition Assay	IC50=2.10041 μM	SANGER
SCC-15	Growth Inhibition Assay	IC50=2.12541 μM	SANGER
DOK	Growth Inhibition Assay	IC50=2.13147 μM	SANGER
YAPC	Growth Inhibition Assay	IC50=2.15307 μM	SANGER
AM-38	Growth Inhibition Assay	IC50=2.17015 μM	SANGER
EFO-21	Growth Inhibition Assay	IC50=2.17788 μM	SANGER
A388	Growth Inhibition Assay	IC50=2.19271 μM	SANGER
RH-18	Growth Inhibition Assay	IC50=2.19369 μM	SANGER
NCI-H1581	Growth Inhibition Assay	IC50=2.19596 μM	SANGER
COLO-668	Growth Inhibition Assay	IC50=2.29973 μM	SANGER
RPMI-2650	Growth Inhibition Assay	IC50=2.32659 μM	SANGER
HMV-II	Growth Inhibition Assay	IC50=2.33868 μM	SANGER
NCI-H2342	Growth Inhibition Assay	IC50=2.34603 μM	SANGER
SH-4	Growth Inhibition Assay	IC50=2.38204 μM	SANGER
L-428	Growth Inhibition Assay	IC50=2.38794 μM	SANGER
U-118-MG	Growth Inhibition Assay	IC50=2.39805 μM	SANGER
RO82-W-1	Growth Inhibition Assay	IC50=2.43727 μM	SANGER
NCI-H2291	Growth Inhibition Assay	IC50=2.46994 μM	SANGER
SK-OV-3	Growth Inhibition Assay	IC50=2.50249 μM	SANGER
NCI-H441	Growth Inhibition Assay	IC50=2.50305 μM	SANGER
NCI-H2009	Growth Inhibition Assay	IC50=2.52934 μM	SANGER
LB2518-MEL	Growth Inhibition Assay	IC50=2.53747 μM	SANGER
PANC-10-05	Growth Inhibition Assay	IC50=2.61116 μM	SANGER
CAL-85-1	Growth Inhibition Assay	IC50=2.66161 μM	SANGER
PC-3	Growth Inhibition Assay	IC50=2.66611 μM	SANGER
COLO-824	Growth Inhibition Assay	IC50=2.67374 μM	SANGER
D-502MG	Growth Inhibition Assay	IC50=2.70406 μM	SANGER
SBC-1	Growth Inhibition Assay	IC50=2.71627 μM	SANGER
CAPAN-1	Growth Inhibition Assay	IC50=2.71949 μM	SANGER
D-247MG	Growth Inhibition Assay	IC50=2.73756 μM	SANGER
CAL-39	Growth Inhibition Assay	IC50=2.86389 μM	SANGER
NCI-H2087	Growth Inhibition Assay	IC50=2.88431 μM	SANGER
NB7	Growth Inhibition Assay	IC50=2.92139 μM	SANGER
NCI-H1437	Growth Inhibition Assay	IC50=2.92257 μM	SANGER
RD	Growth Inhibition Assay	IC50=2.99939 μM	SANGER
TCCSUP	Growth Inhibition Assay	IC50=3.02636 μM	SANGER
MKN28	Growth Inhibition Assay	IC50=3.03463 μM	SANGER
NCI-H596	Growth Inhibition Assay	IC50=3.0671 μM	SANGER
SW948	Growth Inhibition Assay	IC50=3.09693 μM	SANGER
WM-115	Growth Inhibition Assay	IC50=3.11827 μM	SANGER
HCC1954	Growth Inhibition Assay	IC50=3.12141 μM	SANGER
MS-1	Growth Inhibition Assay	IC50=3.18474 μM	SANGER
SW13	Growth Inhibition Assay	IC50=3.2326 μM	SANGER
OE19	Growth Inhibition Assay	IC50=3.28489 μM	SANGER
HT-1197	Growth Inhibition Assay	IC50=3.29179 μM	SANGER
HLE	Growth Inhibition Assay	IC50=3.3281 μM	SANGER
NUGC-3	Growth Inhibition Assay	IC50=3.44761 μM	SANGER
UACC-257	Growth Inhibition Assay	IC50=3.52417 μM	SANGER
SK-MEL-3	Growth Inhibition Assay	IC50=3.53214 μM	SANGER
KNS-81-FD	Growth Inhibition Assay	IC50=3.562 μM	SANGER
MZ1-PC	Growth Inhibition Assay	IC50=3.57986 μM	SANGER
KLE	Growth Inhibition Assay	IC50=3.59867 μM	SANGER
NCI-H2052	Growth Inhibition Assay	IC50=3.60009 μM	SANGER
NCI-H1838	Growth Inhibition Assay	IC50=3.81119 μM	SANGER
NCI-H1623	Growth Inhibition Assay	IC50=4.01396 μM	SANGER
SCC-25	Growth Inhibition Assay	IC50=4.23597 μM	SANGER
CP66-MEL	Growth Inhibition Assay	IC50=4.25191 μM	SANGER
TE-12	Growth Inhibition Assay	IC50=4.29271 μM	SANGER
LU-99A	Growth Inhibition Assay	IC50=4.31345 μM	SANGER
CAMA-1	Growth Inhibition Assay	IC50=4.352 μM	SANGER
SK-MEL-30	Growth Inhibition Assay	IC50=4.41913 μM	SANGER
KURAMOCHI	Growth Inhibition Assay	IC50=4.45528 μM	SANGER
BEN	Growth Inhibition Assay	IC50=4.52362 μM	SANGER
NCI-H226	Growth Inhibition Assay	IC50=4.54871 μM	SANGER
CAL-27	Growth Inhibition Assay	IC50=4.71694 μM	SANGER
G-401	Growth Inhibition Assay	IC50=4.83841 μM	SANGER
CAL-120	Growth Inhibition Assay	IC50=4.84991 μM	SANGER
DMS-114	Growth Inhibition Assay	IC50=5.14506 μM	SANGER
KYSE-70	Growth Inhibition Assay	IC50=5.14859 μM	SANGER
NCI-H1648	Growth Inhibition Assay	IC50=5.29782 μM	SANGER
MDA-MB-175-VII	Growth Inhibition Assay	IC50=5.44014 μM	SANGER
NCI-H2029	Growth Inhibition Assay	IC50=5.48022 μM	SANGER
LS-1034	Growth Inhibition Assay	IC50=5.66889 μM	SANGER
LB831-BLC	Growth Inhibition Assay	IC50=5.70345 μM	SANGER
MDA-MB-415	Growth Inhibition Assay	IC50=5.7081 μM	SANGER
TE-6	Growth Inhibition Assay	IC50=5.74182 μM	SANGER
SK-MEL-24	Growth Inhibition Assay	IC50=5.74564 μM	SANGER
HUTU-80	Growth Inhibition Assay	IC50=5.75333 μM	SANGER
OCUB-M	Growth Inhibition Assay	IC50=5.77563 μM	SANGER
IGR-1	Growth Inhibition Assay	IC50=5.86894 μM	SANGER
NCI-H747	Growth Inhibition Assay	IC50=6.24585 μM	SANGER
COLO-680N	Growth Inhibition Assay	IC50=6.39403 μM	SANGER
NB12	Growth Inhibition Assay	IC50=6.79722 μM	SANGER
SNU-449	Growth Inhibition Assay	IC50=6.99591 μM	SANGER
D-542MG	Growth Inhibition Assay	IC50=7.12299 μM	SANGER
COLO-792	Growth Inhibition Assay	IC50=7.87127 μM	SANGER
NCI-H810	Growth Inhibition Assay	IC50=8.02984 μM	SANGER
T47D	Growth Inhibition Assay	IC50=8.16024 μM	SANGER
Calu-3	Growth Inhibition Assay	IC50=8.28886 μM	SANGER
COLO-741	Growth Inhibition Assay	IC50=8.93093 μM	SANGER
LU-135	Growth Inhibition Assay	IC50=9.03452 μM	SANGER
COLO-678	Growth Inhibition Assay	IC50=9.28844 μM	SANGER
NCI-H2126	Growth Inhibition Assay	IC50=9.33919 μM	SANGER
SK-MEL-28	Growth Inhibition Assay	IC50=9.53596 μM	SANGER
MFE-280	Growth Inhibition Assay	IC50=10.0229 μM	SANGER
DBTRG-05MG	Growth Inhibition Assay	IC50=10.4369 μM	SANGER
RCC10RGB	Growth Inhibition Assay	IC50=10.5255 μM	SANGER
NTERA-S-cl-D1	Growth Inhibition Assay	IC50=10.6852 μM	SANGER
C3A	Growth Inhibition Assay	IC50=12.3172 μM	SANGER
MHH-ES-1	Growth Inhibition Assay	IC50=12.5284 μM	SANGER
LU-139	Growth Inhibition Assay	IC50=12.6333 μM	SANGER
KNS-42	Growth Inhibition Assay	IC50=12.8771 μM	SANGER
MCF7	Growth Inhibition Assay	IC50=13.2365 μM	SANGER
SW872	Growth Inhibition Assay	IC50=14.5461 μM	SANGER
HT-1376	Growth Inhibition Assay	IC50=14.8582 μM	SANGER
NCI-SNU-5	Growth Inhibition Assay	IC50=15.1741 μM	SANGER
NCI-H2405	Growth Inhibition Assay	IC50=15.4474 μM	SANGER
KYSE-150	Growth Inhibition Assay	IC50=15.7611 μM	SANGER
SW837	Growth Inhibition Assay	IC50=16.0124 μM	SANGER
LU-65	Growth Inhibition Assay	IC50=19.726 μM	SANGER
JEG-3	Growth Inhibition Assay	IC50=20.3577 μM	SANGER
SK-MEL-1	Growth Inhibition Assay	IC50=20.7836 μM	SANGER
SK-HEP-1	Growth Inhibition Assay	IC50=21.5541 μM	SANGER
NCI-H1770	Growth Inhibition Assay	IC50=23.4086 μM	SANGER
MG-63	Growth Inhibition Assay	IC50=23.7673 μM	SANGER
ECC10	Growth Inhibition Assay	IC50=25.571 μM	SANGER
SW1463	Growth Inhibition Assay	IC50=27.8316 μM	SANGER
JVM-2	Growth Inhibition Assay	IC50=28.3248 μM	SANGER
HCT-15	Growth Inhibition Assay	IC50=28.4192 μM	SANGER
CAL-72	Growth Inhibition Assay	IC50=31.4912 μM	SANGER
HCC2218	Growth Inhibition Assay	IC50=32.8858 μM	SANGER
BT-474	Growth Inhibition Assay	IC50=33.0843 μM	SANGER
NCI-H1092	Growth Inhibition Assay	IC50=33.5145 μM	SANGER
Mo-T	Growth Inhibition Assay	IC50=37.3585 μM	SANGER
DU-145	Growth Inhibition Assay	IC50=40.6295 μM	SANGER
NCI-H1666	Growth Inhibition Assay	IC50=42.4488 μM	SANGER
IST-MES1	Growth Inhibition Assay	IC50=46.4196 μM	SANGER
SW1116	Growth Inhibition Assay	IC50=48.1756 μM	SANGER
MZ2-MEL	Growth Inhibition Assay	IC50=48.5026 μM	SANGER
Click to View More Cell Line Experimental Data

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
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 K_i 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 against SW620 and 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]
Kinase Assay	Chk1 Kinase Assay
Kinase Assay	Recombinant human Chk1 is expressed as a S-transferase fusion in insect cells using a baculovirus vector and purified by 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	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 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.
Experimental Result Images	Methods	Biomarkers	Images	PMID
	Western blot	pChk1 / Chk1 / Wee1 / p21 / p53		29963769
	Growth inhibition assay	Cell viability		23715154

In Vivo
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, 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 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 causes complete tumor regression in the SW620 xenograft mice with the %T/C increasing significantly to -66% and -67%, respectively. ^[1]
Animal Research	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.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT00937664	Terminated	Cancer\|Solid Tumors\|Advanced Solid Malignancies	AstraZeneca	July 2009	Phase 1
NCT00473616	Terminated	Advanced Solid Tumors\|Cancer\|Advanced Solid Malignancies	AstraZeneca	May 2007	Phase 1
NCT00413686	Completed	Solid Tumors	AstraZeneca	December 2006	Phase 1

References

[1] Zabludoff SD, et al. Mol Cancer Ther, 2008, 7(9), 2955-2966.

Chemical Information & Solubility

Molecular Weight	362.42	Formula	C₁₇H₁₉FN₄O₂S
CAS No.	860352-01-8	SDF	Download AZD7762 SDF
Smiles	C1CC(CNC1)NC(=O)C2=C(C=C(S2)C3=CC(=CC=C3)F)NC(=O)N
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 73 mg/mL ( (201.42 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.				In vivo Formulation Calculator
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):