AZD7762

Name: AZD7762
Brand: Selleck Chemicals
SKU: S1532
Rating: 5 (87 reviews)

For research use only.

Catalog No.S1532

87 publications

CAS No. 860352-01-8

AZD7762 is a potent and selective inhibitor of Chk1 with IC50 of 5 nM in a cell-free assay. It is equally potent against Chk2 and less potent against CAM, Yes, Fyn, Lyn, Hck and Lck. Phase 1.

Selleck's AZD7762 has been cited by 87 publications

Cancer Cell, 2019, 35(6):851-867

PubMed: 31185210 ( click the link to review the publication )

Cancer Cell, 2019, 36(2):179-193

PubMed: 31378681 ( click the link to review the publication )

Cell, 2019, 36(2):179-193

PubMed: 28162770 ( click the link to review the publication )

Cancer Cell, 2019, 35(5):752-766

PubMed: 31085176 ( click the link to review the publication )

Cancer Discov, 2012, 2(6):524-39

PubMed: 22628408 ( click the link to review the publication )

Nat Biotechnol, 2011, 29(6):542-6

PubMed: 21623355 ( click the link to review the publication )

Theranostics, 2021, 11(4):1795-1813

PubMed: 33408782 ( click the link to review the publication )

Mol Cell, 2020, 22 pii: S1097-2765(20)30231-8

PubMed: 32353258 ( click the link to review the publication )

J Clin Invest, 2020, 139080

PubMed: 33016928 ( click the link to review the publication )

Nat Commun, 2020, 29;11(1):2086

PubMed: 32350249 ( click the link to review the publication )

Nucleic Acids Res, 2020, 48(17):9710-9723

PubMed: 32890395 ( click the link to review the publication )

Biomaterials, 2020, 248:120032

PubMed: 32304937 ( click the link to review the publication )

Cell Rep, 2020, 31(12):107800

PubMed: 32579927 ( click the link to review the publication )

Cell Rep, 2020, 12;31(6):107632

PubMed: 32402277 ( click the link to review the publication )

Cell Rep, 2020, 30(7):2416-2429

PubMed: 32075739 ( click the link to review the publication )

Haematologica, 2020, 105(3):784-795

PubMed: 31289205 ( click the link to review the publication )

Oncogene, 2020, 10.1038/s41388-020-1300-x

PubMed: 32335582 ( click the link to review the publication )

Cancers (Basel), 2020, 12(9)E2498

PubMed: 32899210 ( click the link to review the publication )

Cell Death Dis, 2020, 28;11(4):298

PubMed: 32345958 ( click the link to review the publication )

Mol Oncol, 2020, 10.1002/1878-0261.12882

PubMed: 33320980 ( click the link to review the publication )

Int J Mol Sci, 2020, 21(18)E6692

PubMed: 32932732 ( click the link to review the publication )

Radiat Environ Biophys, 2020,

PubMed: 32857208 ( click the link to review the publication )

Cancers (Basel), 2020, 12(7):1726

PubMed: 32610557 ( click the link to review the publication )

Life Sci Alliance, 2020, 3(8):e202000671

PubMed: 32571801 ( click the link to review the publication )
Nat Cell Biol, 2019, 21(6):778-790

PubMed: 31160710 ( click the link to review the publication )

J Thorac Oncol, 2019, 14(6):1032-1045

PubMed: 30771522 ( click the link to review the publication )

Clin Cancer Res, 2019, 25(7):2290-2304

PubMed: 30538111 ( click the link to review the publication )

Cancers (Basel), 2019, 11(8)

PubMed: 31362447 ( click the link to review the publication )

Mol Cancer Ther, 2019, 18(4):762-770

PubMed: 30872379 ( click the link to review the publication )

Mol Cancer Ther, 2019, 18(8):1439-1450

PubMed: 31142662 ( click the link to review the publication )

Mol Cancer Ther, 2019, 10.1158/1535-7163.MCT-19-0474

PubMed: 31597711 ( click the link to review the publication )

Mol Cancer Res, 2019, 17(10):1985-1998

PubMed: 31300540 ( click the link to review the publication )

Cancer Cell Int, 2019, 19:195

PubMed: 31372095 ( click the link to review the publication )

Cell Cycle, 2019, 18(8):834-847

PubMed: 30943845 ( click the link to review the publication )

Br J Pharmacol, 2019, 10.1111/bph.14916

PubMed: 31670839 ( click the link to review the publication )

Mol Cancer Ther, 2019, 10.1158/1535-7163.MCT-19-0290

PubMed: 31871265 ( click the link to review the publication )

Oncotarget, 2019, 10(62):6691-6712

PubMed: 31803363 ( click the link to review the publication )

Nucleic Acids Res, 2018, 46(10):5029-5049

PubMed: 29596642 ( click the link to review the publication )

Clin Cancer Res, 2018, 24(7):1629-1643

PubMed: 29326282 ( click the link to review the publication )

Cell Rep, 2018, 24(13):3393-3403.e5

PubMed: 30257201 ( click the link to review the publication )

Diabetes, 2018, 67(11):2319-2328

PubMed: 30104248 ( click the link to review the publication )

Cancer Lett, 2018, 431:142-149

PubMed: 29859297 ( click the link to review the publication )

Chem Res Toxicol, 2018, 31(7):612-618

PubMed: 29897742 ( click the link to review the publication )

Cancer Med, 2018, 7(8):3955-3964

PubMed: 29963769 ( click the link to review the publication )

Oncotarget, 2018, 9(71):33589-33600

PubMed: 30323901 ( click the link to review the publication )

Nat Commun, 2017, 8(1):1392

PubMed: 29123096 ( click the link to review the publication )

Proc Natl Acad Sci U S A, 2017, 114(24):E4782-E4791

PubMed: 28533414 ( click the link to review the publication )

Haematologica, 2017, 102(5):826-834

PubMed: 28154085 ( click the link to review the publication )
Cell Syst, 2017,

PubMed: 28017544 ( click the link to review the publication )

Cell Rep, 2017, 18(8):1970-1981

PubMed: 28228262 ( click the link to review the publication )

Cancer Lett, 2017, 392:71-82

PubMed: 28126323 ( click the link to review the publication )

J Exp Clin Cancer Res, 2017, 36(1):1

PubMed: 28049532 ( click the link to review the publication )

Eur J Pharm Sci, 2017, 109:223-232

PubMed: 28822757 ( click the link to review the publication )

Oncotarget, 2017, 8(7):10966-10979

PubMed: 28030798 ( click the link to review the publication )

Tumour Biol, 2017, 39(3):1010428317694307

PubMed: 28347251 ( click the link to review the publication )

Cancer Res, 2016, 76(11):3319-31

PubMed: 26988986 ( click the link to review the publication )

Oncogene, 2016, 35(36):4689-97

PubMed: 26804177 ( click the link to review the publication )

PLoS Pathog, 2016, 12(2):e1005424

PubMed: 26891221 ( click the link to review the publication )

Mol Cancer Res, 2016, 14(5):437-47

PubMed: 26979711 ( click the link to review the publication )

J Biol Chem, 2016, 291(17):9330-42

PubMed: 26940878 ( click the link to review the publication )

Anticancer Res, 2016, 36(6):2649-57

PubMed: 27272773 ( click the link to review the publication )

Oncotarget, 2016, 7(23):34688-702

PubMed: 27167194 ( click the link to review the publication )

Oncotarget, 2016, 7(14):18159-70

PubMed: 26921248 ( click the link to review the publication )

J Pathol, 2015, 10.1002/path.4528

PubMed: 25757065 ( click the link to review the publication )

Biochem Pharmacol, 2015, 93(2):210-20

PubMed: 25478729 ( click the link to review the publication )

Biochem Pharmacol, 2015, 93(2):210-20

PubMed: ( click the link to review the publication )

J Biol Chem, 2015, 290(3):1874-84

PubMed: 25480786 ( click the link to review the publication )

PLoS One, 2015, 10(6):e0129090

PubMed: 26046346 ( click the link to review the publication )

Oncotarget, 2015,

PubMed: 25544753 ( click the link to review the publication )

Oncotarget, 2015, 6(35):37229-40

PubMed: 26439697 ( click the link to review the publication )

Oncotarget, 2015, 6(25):21074-84

PubMed: 26025928 ( click the link to review the publication )

BMC Cancer, 2015, 15:462

PubMed: 26054341 ( click the link to review the publication )
Cell Rep, 2014, 10.1016/j.celrep.2014.10.024

PubMed: ( click the link to review the publication )

Cell Rep, 2014, 9(4):1375-86

PubMed: 25456132 ( click the link to review the publication )

Sci Signal, 2014, 7(326):ra47

PubMed: 24847116 ( click the link to review the publication )

Cell Death Dis, 2014, 5:e1223

PubMed: 24810059 ( click the link to review the publication )

Cell Death Dis, 2014, 5:e1253

PubMed: 24853431 ( click the link to review the publication )

Int J Oncol, 2014, 45(3):1159-66

PubMed: 24969815 ( click the link to review the publication )

PLoS One, 2014, 9(10):e111146

PubMed: 25343454 ( click the link to review the publication )

Int J Gynecol Cancer, 2014, 24(5):838-43

PubMed: 24804869 ( click the link to review the publication )

Oncotarget, 2014, 5(21):10546-57

PubMed: 25301733 ( click the link to review the publication )

Br J Cancer, 2013, 110(2):510-9

PubMed: 24327015 ( click the link to review the publication )

J Cell Mol Med, 2013, 18(1):143-55

PubMed: 24238094 ( click the link to review the publication )

PLoS One, 2013, 8(2):e55493

PubMed: 23405159 ( click the link to review the publication )

Cancer Biol Ther, 2012, 13(6):379-88

PubMed: 22313687 ( click the link to review the publication )

Cancer Biol Ther, 2011, 12(3):215-28

PubMed: 21642769 ( click the link to review the publication )

PLoS One, 2010, 5(12):e14335

PubMed: 21179472 ( click the link to review the publication )

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 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 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	Activity Description	PMID
KASUMI-1	MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MYXJR\|UxRTBwMECwNlM1KM7:TR?=	M{noeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK\|5USU6JRWK8M4E,
NKM-1	M{[0W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MX\JR\|UxRTBwMECwOFE2KM7:TR?=	M2W0clxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK\|5USU6JRWK8M4E,
MV-4-11	MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MoHsTWM2OD1yLkCwNFQzPSEQvF2=	NWO5XGNERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
NCI-H1703	MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MULJR\|UxRTBwMEC2OFMh\|ryP	Mn7QQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl\|Mz:nQnNCVkeHUkyvZV4>
A204	M3rDfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MX\JR\|UxRTBwMEC4OVYh\|ryP	MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN\|Lze+V2FPT0WUPD;hQi=>
CGTH-W-1	MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MmXXTWM2OD1yLkCxOFIh\|ryP	NWPpeoNCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
MLMA	MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MoDVTWM2OD1yLkCyPFQ6KM7:TR?=	NEHsU2Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
GOTO	Mn\1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NF\PSoFKSzVyPUCuNFMyOiEQvF2=	MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN\|Lze+V2FPT0WUPD;hQi=>
KE-37	NIHvRohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NVHvWGRvUUN3ME2wMlA{OTR{IN88US=>	NIHLTY89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
ES4	Ml;xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M{SxbWlEPTB;MD6wN\|I2OSEQvF2=	M3vpd\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK\|5USU6JRWK8M4E,
ATN-1	NEjGS5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NVSzNpNZUUN3ME2wMlA{PDF5IN88US=>	MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN\|Lze+V2FPT0WUPD;hQi=>
MHH-PREB-1	M2P5b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M1;i[GlEPTB;MD6wN\|Q1OiEQvF2=	NFXIc5U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
SW756	NGPqeFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MkK3TWM2OD1yLkCzOVc6KM7:TR?=	NWPBZoRxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
CTV-1	NX;QTHA5T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M3;NXWlEPTB;MD6wN\|g6PiEQvF2=	MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN\|Lze+V2FPT0WUPD;hQi=>
HCC1806	MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NV;xZYNMUUN3ME2wMlA1ODJ{IN88US=>	MlzUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl\|Mz:nQnNCVkeHUkyvZV4>
NEC8	Mlu3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NFn1SmpKSzVyPUCuNFQzODNizszN	M4n4XlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK\|5USU6JRWK8M4E,
P12-ICHIKAWA	M1PHfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MYXJR\|UxRTBwMESzNVYh\|ryP	NI[zRlI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
DEL	NGj5Z\|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	Mn2zTWM2OD1yLkC0OVkzKM7:TR?=	NIfXWII9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
KM12	M{D2cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NVzidnZKUUN3ME2wMlA2OTV6IN88US=>	M3X5ZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK\|5USU6JRWK8M4E,
LB1047-RCC	MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M2ixT2lEPTB;MD6wOlAzPSEQvF2=	MojJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl\|Mz:nQnNCVkeHUkyvZV4>
LB2241-RCC	NUjXe29qT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M2XpdGlEPTB;MD6wOlExOiEQvF2=	MnS4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl\|Mz:nQnNCVkeHUkyvZV4>
NOMO-1	M3HmWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MVPJR\|UxRTBwME[xNVUh\|ryP	NXHsS5U1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
NB14	NXfpUXdlT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M3:1TmlEPTB;MD6wOlE{PiEQvF2=	MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN\|Lze+V2FPT0WUPD;hQi=>
ONS-76	NGPjdlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MVfJR\|UxRTBwME[xPVYh\|ryP	NU\wXZlwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
HD-MY-Z	MoLNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NYHjTVV2UUN3ME2wMlA3OjV3IN88US=>	MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN\|Lze+V2FPT0WUPD;hQi=>
G-402	M{SxUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M{LrN2lEPTB;MD6wOlQ3KM7:TR?=	M4\iNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK\|5USU6JRWK8M4E,
ES1	M4\rXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NX3kOIlrUUN3ME2wMlA4OTR4IN88US=>	M{fZblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK\|5USU6JRWK8M4E,
L-363	NXTKeXFsT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MUjJR\|UxRTBwMEezPUDPxE1?	NEKyRZM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
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A427	Mln1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NF:ydZVKSzVyPUCuNVk5OzJizszN	NHLwdlI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
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HAL-01	NH7P[nBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MmHUTWM2OD1yLkKwPVch\|ryP	Ml\yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl\|Mz:nQnNCVkeHUkyvZV4>
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MPP-89	MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M{HpOWlEPTB;MD6yOFQ2OSEQvF2=	M1jKOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK\|5USU6JRWK8M4E,
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NCI-H510A	NWDFWmRET3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MWHJR\|UxRTBwMkS2NlYh\|ryP	NFzR[Wc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
KOSC-2	NEPKbVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NWLmXYh5UUN3ME2wMlI1PjdzIN88US=>	NGnhZ2c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
NCI-H23	MnTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M2jHVGlEPTB;MD6yOFc3OSEQvF2=	M335XVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK\|5USU6JRWK8M4E,
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ABC-1	Mn7IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MUDJR\|UxRTBwMk[wOlQh\|ryP	M1fkWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK\|5USU6JRWK8M4E,
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MG-63	NXu3V2FKT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NE\jVXlKSzVyPUKzMlc3PzNizszN	Mnf0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl\|Mz:nQnNCVkeHUkyvZV4>
ECC10	NYXITXZNT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NVW2UG1PUUN3ME2yOU42PzFizszN	NI\pXHk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
SW1463	NF\VOZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NV3UcYU4UUN3ME2yO{45OzF4IN88US=>	MoHhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl\|Mz:nQnNCVkeHUkyvZV4>
JVM-2	M1XNTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	Mn3VTWM2OD1{OD6zNlQ5KM7:TR?=	MojRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl\|Mz:nQnNCVkeHUkyvZV4>
HCT-15	NI\0RXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NXLjZXg5UUN3ME2yPE41OTl{IN88US=>	NHzUfG49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
CAL-72	MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NHf0UXhKSzVyPUOxMlQ6OTJizszN	MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN\|Lze+V2FPT0WUPD;hQi=>
HCC2218	NWDET\|F3T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NUjaZmFZUUN3ME2zNk45QDV6IN88US=>	NGfwSm09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzODRzOUOzM{c,W0GQR1XSQE9iRg>?
BT-474	MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NFrCU3lKSzVyPUOzMlA5PDNizszN	MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN\|Lze+V2FPT0WUPD;hQi=>
NCI-H1092	NFL1[ZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M1O5WWlEPTB;M{OuOVE1PSEQvF2=	M{f2UFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIxPDF7M{OvK\|5USU6JRWK8M4E,
Mo-T	MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NWXxO5YyUUN3ME2zO{4{PTh3IN88US=>	NULkfWgyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
DU-145	M{DWXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	Mm\zTWM2OD12MD62Nlk2KM7:TR?=	MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFQyQTN\|Lze+V2FPT0WUPD;hQi=>
NCI-H1666	MkDPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NIWw[WlKSzVyPUSyMlQ1QDhizszN	MnvhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl\|Mz:nQnNCVkeHUkyvZV4>
IST-MES1	M2PWWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MX7JR\|UxRTR4LkSxPVYh\|ryP	NYPDXmpVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
SW1116	Ml;jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NH65NWZKSzVyPUS4MlE4PTZizszN	NX\zdogxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjB2MUmzN{8oRlODTlfFVlww[T5?
MZ2-MEL	NVLIUWNlT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MnjRTWM2OD12OD61NFI3KM7:TR?=	MoLnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA1OTl\|Mz:nQnNCVkeHUkyvZV4>

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	pChk1 / Chk1 / Wee1 / p21 / p53 ; PubMed: 29963769 Cancer Med 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 Cancer Discov 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]	- Collapse 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]	- Collapse 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]	- Collapse 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)

References

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

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 Download AZD7762 SDF

Molecular Weight	362.42
Formula	C₁₇H₁₉FN₄O₂S
CAS No.	860352-01-8
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	N/A
Smiles	C1CC(CNC1)NC(=O)C2=C(C=C(S2)C3=CC(=CC=C3)F)NC(=O)N

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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.

Chk Signaling Pathway Map

Chk Inhibitors with Unique Features

Selective CHK Inhibitor

MK-8776 (SCH 900776) : Chk1-selective, IC50=3 nM.
Most Potent CHK Inhibitor

CHIR-124 : Chk1, IC50=0.3 nM.
CHK Inhibitor in Clinical Trial

MK-8776 (SCH 900776) : Phase II for Relapsed Acute Myeloid Leukemia.
Classic CHK Inhibitor

PF-477736 : Selective, potent and ATP-competitive Chk1 inhibitor with K_i of 0.49 nM and also inhibits VEGFR2, Aurora-A, FGFR3, Flt3, Fms (CSF1R), Ret and Yes.

Related Chk Products

Ro-3306 ^New

RO-3306 is an ATP-competitive, and selective CDK1 inhibitor with K_i of 20 nM, >15-fold selectivity against a diverse panel of human kinases. RO-3306 enhances p53-mediated Bax activation and mitochondrial apoptosis.
CCG-1423 ^New

CCG-1423 is a specific RhoA pathway inhibitor, which inhibits SRF-mediated transcription.
ML141 ^New

ML141 (CID-2950007) is demonstrated to be a potent, selective and reversible non-competitive inhibitor of Cdc42 GTPase suitable for in vitro assays, with IC50 of 200 nM and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). ML141 is associated with an increase in p38 activation and may induce p38-dependent apoptosis/senescence. ML141 also protects neuroblastoma cells from metformin-induced apoptosis.
Rabusertib (LY2603618)

Rabusertib (LY2603618, IC-83) is a highly selective Chk1 inhibitor with potential anti-tumor activity in a cell-free assay. IC50=7 nM, showing approximately 100-fold more potent against Chk1 than against any of the other protein kinases evaluated. Rabusertib (LY2603618) induces cell cycle arrest, DNA damage response and autophagy in cancer cells. Rabusertib (LY2603618) induces bak-dependent apoptosis in AML cell lines.
CHIR-124

CHIR-124 is a novel and potent Chk1 inhibitor with IC50 of 0.3 nM in a cell-free assay. It shows 2,000-fold selectivity against Chk2, 500- to 5,000-fold less activity against CDK2/4 and Cdc2.
MK-8776 (SCH 900776)

MK-8776 (SCH 900776) is a selective Chk1 inhibitor with IC50 of 3 nM in a cell-free assay. It shows 500-fold selectivity against Chk2. Phase 2.
PF-477736

PF-477736 (PF-736, PF-00477736) is a selective, potent and ATP-competitive Chk1 inhibitor with K_i of 0.49 nM in a cell-free assay and also inhibits VEGFR2, Aurora-A, FGFR3, Flt3, Fms (CSF1R), Ret and Yes. It shows ~100-fold selectivity for Chk1 than Chk2. Phase 1.
Y-27632 2HCl

Y-27632 2HCl is a selective ROCK1 (p160ROCK) inhibitor with K_i of 140 nM in a cell-free assay, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK.
Palbociclib (PD-0332991) HCl

Palbociclib (PD-0332991) HCl is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays, respectively. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3.

Features:Non-cytotoxic, and halts cancer cell growth & could be used in glioblastoma that has relapsed after temozolomide treatment (a chemotherapeutic used to treat many cancers).
Alisertib (MLN8237)

Alisertib (MLN8237) is a selective Aurora A inhibitor with IC50 of 1.2 nM in a cell-free assay. It has >200-fold higher selectivity for Aurora A than Aurora B. Alisertib induces cell cycle arrest, apoptosis and autophagy. Phase 3.

Features:First orally available inhibitor of Aurora A.

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