Capivasertib (AZD5363)

Name: Capivasertib (AZD5363)
Brand: Selleck Chemicals
SKU: S8019
Rating: 5 (88 reviews)

For research use only.

Catalog No.S8019

88 publications

Capivasertib (AZD5363) Chemical Structure

CAS No. 1143532-39-1

Capivasertib (AZD5363) potently inhibits all isoforms of Akt(Akt1/Akt2/Akt3) with IC50 of 3 nM/8 nM/8 nM in cell-free assays, similar to P70S6K/PKA and lower activity towards ROCK1/2. Phase 2.

Selleck's Capivasertib (AZD5363) has been cited by 88 publications

Nature, 2020, 583(7817):620-624

PubMed: 32669709 ( click the link to review the publication )

Cell, 2020, 182(3):685-712.e19

PubMed: 32645325 ( click the link to review the publication )

Cancer Cell, 2017, 32(6):869-883

PubMed: 29232557 ( click the link to review the publication )

Mol Cell, 2021, S1097-2765(21)00264-1

PubMed: 33878293 ( click the link to review the publication )

Cancer Res, 2021, canres.3232.2020

PubMed: 33685991 ( click the link to review the publication )

J Exp Clin Cancer Res, 2021, 40(1):168

PubMed: 33990217 ( click the link to review the publication )

Cell Death Dis, 2021, 12(4):400

PubMed: 33854046 ( click the link to review the publication )

Mol Oncol, 2021, 10.1002/1878-0261.13046

PubMed: 34165921 ( click the link to review the publication )

Antiviral Res, 2021, 194:105145

PubMed: 34303747 ( click the link to review the publication )

Cancer Med, 2021, 10(7):2370-2379

PubMed: 33665980 ( click the link to review the publication )

Exp Ther Med, 2021, 22(3):973

PubMed: 34335915 ( click the link to review the publication )

Commun Biol, 2021, 4(1):416

PubMed: 33772116 ( click the link to review the publication )

NPJ Precis Oncol, 2021, 5(1):65

PubMed: 34267282 ( click the link to review the publication )

Mol Cell, 2020, 80(6):1104-1122.e9

PubMed: 33259812 ( click the link to review the publication )

Nat Commun, 2020, 11(1):5982

PubMed: 33239617 ( click the link to review the publication )

Genome Med, 2020, 18;12(1):17

PubMed: 32070411 ( click the link to review the publication )

Eur J Cancer, 2020, 126:93-103

PubMed: 31927215 ( click the link to review the publication )

J Exp Clin Cancer Res, 2020, 39(1):33

PubMed: 32041631 ( click the link to review the publication )

Cancers (Basel), 2020, 12(9)E2500

PubMed: 32899250 ( click the link to review the publication )

Br J Cancer, 2020, 22

PubMed: 32439931 ( click the link to review the publication )

Cells, 2020, 9(3)

PubMed: 32106632 ( click the link to review the publication )

Mol Oncol, 2020, 10.1002/1878-0261.12888

PubMed: 33338300 ( click the link to review the publication )

Mol Oncol, 2020, 26

PubMed: 32336009 ( click the link to review the publication )

J Recept Signal Transduct Res, 2020, 1-11

PubMed: 33108937 ( click the link to review the publication )
Mol Cancer Res, 2020, molcanres.0623.2020

PubMed: 33303690 ( click the link to review the publication )

J Cell Mol Med, 2020, 10.1111/jcmm.15830

PubMed: 32914934 ( click the link to review the publication )

Int J Mol Sci, 2020, 18;21(8):2825

PubMed: 32325639 ( click the link to review the publication )

Sci Rep, 2020, 10(1):21762

PubMed: 33303839 ( click the link to review the publication )

Stem Cells Int, 2020, 6;2020:7073805

PubMed: 32322280 ( click the link to review the publication )

Nature, 2020, 583(7817):620-624

PubMed: 32669709 ( click the link to review the publication )

Life Sci Alliance, 2020, 31;3(5) pii: e202000648

PubMed: 32234750 ( click the link to review the publication )

Clin Transl Med, 2020, 10(1):363-373

PubMed: 32508049 ( click the link to review the publication )

Oncotarget, 2020, 17;11(11):969-981

PubMed: 32215185 ( click the link to review the publication )

FASEB Bioadv, 2020, 2(2):126-144

PubMed: 32123862 ( click the link to review the publication )

Cancer Res, 2019, 79(9):2367-2378

PubMed: 30858154 ( click the link to review the publication )

J Hematol Oncol, 2019, 12(1):132

PubMed: 31805962 ( click the link to review the publication )

Oncogene, 2019, 38(26):5294-5307

PubMed: 30914799 ( click the link to review the publication )

EBioMedicine, 2019, 40:77-91

PubMed: 30594554 ( click the link to review the publication )

Cancers (Basel), 2019, 11(9)

PubMed: 31540244 ( click the link to review the publication )

Cancers (Basel), 2019, 30;12(1) pii: E89

PubMed: 31905918 ( click the link to review the publication )

Cell Prolif, 2019, 52(3):e12584

PubMed: 30834619 ( click the link to review the publication )

Biochem Pharmacol, 2019, 169:113640

PubMed: 31536726 ( click the link to review the publication )

Sci Rep, 2019, 9(1):13308

PubMed: 31527768 ( click the link to review the publication )

Nat Commun, 2018, 9(1):5200

PubMed: 30518851 ( click the link to review the publication )

Oncogene, 2018, 10.1038/s41388-018-0498-3

PubMed: 30228349 ( click the link to review the publication )

Oncogene, 2018,

PubMed: 29059160 ( click the link to review the publication )

Gastric Cancer, 2018, 10.1007/s10120-018-0859-1

PubMed: 30066183 ( click the link to review the publication )

J Immunol, 2018, 201(5):1510-1521

PubMed: 30037846 ( click the link to review the publication )
J Proteomics, 2018, 170:130-140

PubMed: 28842319 ( click the link to review the publication )

Cancer Biol Ther, 2018, 19(7):584-589

PubMed: 29708815 ( click the link to review the publication )

Oncol Rep, 2018, 40(6):3561-3572

PubMed: 30272296 ( click the link to review the publication )

PLoS One, 2018, 13(2):e0191890

PubMed: 29389967 ( click the link to review the publication )

Nat Commun, 2017, 8(1):410

PubMed: 28871105 ( click the link to review the publication )

Nucleic Acids Res, 2017, 45(16):9654-9678

PubMed: 28934469 ( click the link to review the publication )

Dev Cell, 2017, 43(6):673-688

PubMed: 29103956 ( click the link to review the publication )

Cell Rep, 2017, 20(13):3212-3222

PubMed: 28954236 ( click the link to review the publication )

Elife, 2017, 6e30640

PubMed: 29173281 ( click the link to review the publication )

Breast Cancer Res, 2017, 19(1):74

PubMed: 28666462 ( click the link to review the publication )

J Neuroinflammation, 2017, 14(1):228

PubMed: 29178967 ( click the link to review the publication )

Int J Mol Sci, 2017, 18(10)E2114

PubMed: 28991210 ( click the link to review the publication )

Biomed Pharmacother, 2017, 90:414-420

PubMed: 28391163 ( click the link to review the publication )

PLoS One, 2017, 12(10):e0186106

PubMed: 28982179 ( click the link to review the publication )

Immunol Lett, 2017, 184:7-14

PubMed: 28223102 ( click the link to review the publication )

Int J Gynecol Cancer, 2017, 27(2):196-205

PubMed: 27870715 ( click the link to review the publication )

Exp Ther Med, 2017, 13(6):3021-3031

PubMed: 28587375 ( click the link to review the publication )

Oncotarget, 2017, 8(6):9739-9751

PubMed: 28039457 ( click the link to review the publication )

EMBO J, 2016, 35(20):2192-2212

PubMed: 27625374 ( click the link to review the publication )

Clin Cancer Res, 2016, 22(4):1018-27

PubMed: 26490311 ( click the link to review the publication )

Cancer Res, 2016, pii: canres.3393

PubMed: 27197158 ( click the link to review the publication )

Int J Oncol, 2016, 49(3):953-60

PubMed: 27572939 ( click the link to review the publication )

Eur J Pharmacol, 2016, 788:90-97

PubMed: 27321870 ( click the link to review the publication )

Biochem Biophys Res Commun, 2016, 477(1):1-8

PubMed: 26970307 ( click the link to review the publication )
Oncol Lett, 2016, 11(3):1685-1692

PubMed: 26998062 ( click the link to review the publication )

Anticancer Res, 2016, 36(11):5849-5858

PubMed: 27793908 ( click the link to review the publication )

Oncotarget, 2016, 7(24):36971-36987

PubMed: 27175591 ( click the link to review the publication )

Oncotarget, 2016, 7(12):13651-66

PubMed: 26871944 ( click the link to review the publication )

J Immunol Res, 2016, 2016:5281823

PubMed: 28116319 ( click the link to review the publication )

Nat Commun, 2015, 6:6750

PubMed: 25857523 ( click the link to review the publication )

Elife, 2015, 4:e10510

PubMed: 26523394 ( click the link to review the publication )

Oncogene, 2015, 10.1038/onc.2015.226

PubMed: 26165839 ( click the link to review the publication )

Oncoimmunology, 2015, 10.1080/2162402X.2015.1005448

PubMed: ( click the link to review the publication )

Hum Mol Genet, 2015, 24(23):6687-98

PubMed: 26362254 ( click the link to review the publication )

Front Oncol, 2015, 4:343

PubMed: 25520943 ( click the link to review the publication )

Anticancer Res, 2015,

PubMed: 26254364 ( click the link to review the publication )

Vanderbilt University, 2015, /

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

Cell Commun Signal, 2014, 12(1):61

PubMed: 25248616 ( click the link to review the publication )

J Biol Chem, 2014, 289(49):34189-204

PubMed: 25331943 ( click the link to review the publication )

PLoS One, 2014, 9(10):e108780

PubMed: 25360799 ( click the link to review the publication )

Purity & Quality Control

Choose Selective Akt Inhibitors

Biological Activity

Description

Features

Moderate preclinical tolerability, and PD characteristics of an AKT inhibitor. Distinct profile from other AKT inhibitors in clinical development.

Targets

Akt1 ^[1] (Cell-free assay)	Akt2 ^[1] (Cell-free assay)	Akt3 ^[1] (Cell-free assay)	ROCK2 ^[1] (Cell-free assay)
3 nM	8 nM	8 nM	56 nM

In vitro

AZD5363 is a potent Akt inhibitor with IC50 of 3 nM, 8 nM and 8 nM for Akt1, Akt2 and Akt3, respectively. ^[1] AZD5363 inhibits phosphorylation of AKT substrates in cells with a potency of approximately 0.3 to 0.8 μM. AZD5363 inhibits the proliferation of 41 of 182 solid and hematologic tumor cell lines with a potency of < 3 μM. ^[2] Activating mutations in PIK3CA, loss or inactivation of tumor suppressor PTEN, or HER2 amplification all are significantly predictive of responsiveness to AZD5363. Additionally, correlation is also seen between the RAS mutation status of cell lines and resistance to AZD5363. ^[1]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
PC-3	M4fQ[GZ2dmO2aX;uJGF{e2G7	MV6xNEDPxE1?	M2LU[VEzKGh?	MX3pcoR2[2W\|IHH1eI9xcGGpeR?=	MnTIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN{NUi3OFAoRjJ\|MkW4O\|QxRC:jPh?=
LNCaP	NWS4dphRS2WubDDWbYFjcWyrdImgRZN{[Xl?	MWCwMVExODBibl2=	MonCNE01KGR?	NXH2NIN6emWmdXPl[EBNVkOjUDDj[YxtKH[rYXLpcIl1gSCrbjDhJIRwe2VvIHHu[EB1cW2nLXTldIVv\GWwdDDtZY5v\XMEoB?=	NXTrTZcxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyOVg4PDBpPkKzNlU5PzRyPD;hQi=>
DU145	NVnRVpZLTnWwY4Tpc44hSXO\|YYm=	M4DuUFAvPS9zL{GwJO69VQ>?	MYC0PEBp	MlPP[I94dnKnZ4XsZZRmeyC2aHWgdIhwe3Cqb4L5cIF1cW:wIH;mJIRwf26\|dILlZY0heGG2aIfhfUBxem:2ZXnud{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>	M2e5NFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|MkW4O\|QxLz5{M{K1PFc1ODxxYU6=
PC-3	NH\DdVRHfW6ldHnvckBCe3OjeR?=	NELt[3IxNjVxMT:xNEDPxE1?	MoHPOFghcA>?	M4fLZ4Rwf26{ZXf1cIF1\XNidHjlJJBpd3OyaH;yfYxifGmxbjDv[kBld3ewc4Ty[YFuKHCjdHj3ZZkheHKxdHXpcpMhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI>	M2DteVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|MkW4O\|QxLz5{M{K1PFc1ODxxYU6=
C4-2	MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MW[xNFAuPTByMDDuUS=>	MUG3NkBp	NFnLUmZqdmO{ZXHz[ZMhfGinIH\yZYN1cW:wIH;mJINmdGy\|IIXu[IVz\2:rbnegZ4VtdCCmZXH0bC=>	MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl4Nk[yNUc,OjN7Nk[2NlE9N2F-
LNCaP	MkHpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NE\xUYoyODBvNUCwNEBvVQ>?	NXTOPFc5PzJiaB?=	MUjpcoNz\WG\|ZYOgeIhmKG[{YXP0bY9vKG:oIHPlcIx{KHWwZHXy[49qdmdiY3XscEBl\WG2aB?=	MnGyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7Nk[2NlEoRjJ\|OU[2OlIyRC:jPh?=
C4-2	NWraOWNCT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M1;jPVEuOTByMECgcm0>	NXjWN2pmOC1\|IHS=	MlTIbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>?	M{\Pe\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|OU[2OlIyLz5{M{m2OlYzOTxxYU6=
LNCaP	Mnv3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M3XSc\|EuOTByMECgcm0>	MmHoNE0{KGR?	M4HNWYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl?	MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl4Nk[yNUc,OjN7Nk[2NlE9N2F-
C4-2	MXTGeY5kfGmxbjDBd5NigQ>?	NX;Jb4lXPSEQvF2=	NVi4foVlOC1{NDDo	NWrDU2hCcW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKHSqZTDkbZN1[WxiQVvUMZBifGi5YYmgZolwdWG{a3Xyd{BqdmOudXTpcochWFKDU{SwMEBmUUZ2RTygOGUuSlBzLDDtWG9TNCCjbnSgVFcxKFN4IHvpcoF{\SCrbjDhJJRqdWVvZHXw[Y5l\W62IH3hco5meg>?	M{\6Z\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|OU[2OlIyLz5{M{m2OlYzOTxxYU6=
LNCaP	NYLJb4doTnWwY4Tpc44hSXO\|YYm=	MUO1JO69VQ>?	MnSyNE0zPCCq	MonSbY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJJRp\SCmaYP0ZYwhSUuWLYDheIh4[XliYnnvcYFzc2W{czDpcoNtfWSrbnegVHJCWzRyLDDlTWY1TSxiNFWtRnAyNCCvVF;SMEBidmRiUEewJHM3KGurbnHz[UBqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7ldi=>	NF\SUYc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m2OlYzOSd-MkO5OlY3OjF:L3G+
C4-2	M2OzNWZ2dmO2aX;uJGF{e2G7	MmPtOUDPxE1?	NH7FfFQxNTJ2IHi=	NWW4bFRScW6mdXPld{BCU1SVNEezJIFv\CCDS2TUN\|A5KHCqb4PwbI9zgWyjdHnvckBqdiCjIITpcYUh\GWyZX7k[Y51KG2jbn7ldi=>	MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl4Nk[yNUc,OjN7Nk[2NlE9N2F-
LNCaP	MnzXSpVv[3Srb36gRZN{[Xl?	NIXXTZI2KM7:TR?=	NIHwO4QxNTJ2IHi=	NYjsb5ZHcW6mdXPld{BCU1SVNEezJIFv\CCDS2TUN\|A5KHCqb4PwbI9zgWyjdHnvckBqdiCjIITpcYUh\GWyZX7k[Y51KG2jbn7ldi=>	MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl4Nk[yNUc,OjN7Nk[2NlE9N2F-
PAMC82	M3rz[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			Moe2TWM2OD1\|MDFOwG0>	NUDacnRHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwPFg{QDJpPkK0NFg5Ozh{PD;hQi=>
MKN74	MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NFrvNHpKSzVyPUOwJO69VQ>?	NYPxTZRMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwPFg{QDJpPkK0NFg5Ozh{PD;hQi=>
GTL-16	M1O3eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NGHKdWlKSzVyPUOwJO69VQ>?	MnvlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyOEizPFIoRjJ2MEi4N\|gzRC:jPh?=
SNU-5	NITiU4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NXTx[HRIUUN3ME2zNEDPxE1?	NUHPeGdqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwPFg{QDJpPkK0NFg5Ozh{PD;hQi=>
NUGC-4	NGXic3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NIHxb2FKSzVyPUOwJO69VQ>?	NGfmTYw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC4PFM5Oid-MkSwPFg{QDJ:L3G+
SNU-216	MknYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			MmOwTWM2OD1\|MDFOwG0>	MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB6OEO4Nkc,OjRyOEizPFI9N2F-
AZ521	M4Xub2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NWHjb29MUUN3ME2yOU41PDhizszN	M4Lxb\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEi4N\|gzLz5{NEC4PFM5OjxxYU6=
NUGC-3	NHXVT5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			M3rt[WlEPTB;MkGuPFc{KM7:TR?=	NFvlWHQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC4PFM5Oid-MkSwPFg{QDJ:L3G+
OCUM-1	MlKwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			MXrJR\|UxRTF2LkWxOUDPxE1?	MkC4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyOEizPFIoRjJ2MEi4N\|gzRC:jPh?=
SNU-16	Ml3oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			MXfJR\|UxRTFzLkC5O{DPxE1?	M4XT[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEi4N\|gzLz5{NEC4PFM5OjxxYU6=
SNU-484	M1TGVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			M1vMNWlEPTB;Nz6zPVIh\|ryP	MkT1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyOEizPFIoRjJ2MEi4N\|gzRC:jPh?=
KATO III	M1\x[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			MmjqTWM2OD15LkK2O{DPxE1?	NGC1XZg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC4PFM5Oid-MkSwPFg{QDJ:L3G+
HS746T	M4HNV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NEXHNIdKSzVyPU[uNFg1KM7:TR?=	NWLKV45LRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwPFg{QDJpPkK0NFg5Ozh{PD;hQi=>
SNU-668	NEGxOIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NWjwW4Q6UUN3ME22MlAxOyEQvF2=	M{X1SlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEi4N\|gzLz5{NEC4PFM5OjxxYU6=
SNU-601	M2TFRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			MlT1TWM2OD13LkmzPEDPxE1?	NHfLW\|Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC4PFM5Oid-MkSwPFg{QDJ:L3G+
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DAOY	NFnGe\|VyUFSVIHHzd4F6			MkTndWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKESDT2mgZ4VtdHN?	M3nucFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Saos-2	NG\CdmZyUFSVIHHzd4F6			MYXxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW2Gxcz2yJINmdGy\|	MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
SK-N-SH	MYLxTHRUKGG\|c3H5			MnzQdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tV2gh[2WubIO=	NELr[GU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
NB1643	M2LuepFJXFNiYYPzZZk>			MkSzdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6EMU[0N{Bk\Wyucx?=	Mn\zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
MG 63 (6-TG R)	M3HIb5FJXFNiYYPzZZk>			MW\xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN?	NHWwWZk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
Rh41	M3zCVpFJXFNiYYPzZZk>			MUTxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmh2MTDj[Yxtew>?	Mlv3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC	NX\OTXFjeUiWUzDhd5NigQ>?			M3jseZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMW1EKGOnbHzz	MoCyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
NB-EBc1	NXvkbIdXeUiWUzDhd5NigQ>?			NFTCVGtyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKtSWJkOSClZXzsdy=>	M1uwc\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
LAN-5	NH\PWXVyUFSVIHHzd4F6			M{\XPZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCOQV6tOUBk\Wyucx?=	NYezTFR3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh18	MlTzdWhVWyCjc4PhfS=>			NUm5T2VMeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IGLoNVgh[2WubIO=	NHr4[lE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	pAKT / AKT / pGSK3β / GSK3β; PubMed: 26998062 Oncol Lett AZD5363 inhibited the phosphorylation of GSK3β, but increased the phosphorylation of AKT in a time-dependent manner in the (A) Hep-G2 cells. HER3 / pHER3 / HER2 / pHER2 / pPRAS40 / pS6 / p-4EBP1 / pFOXO / pERK / PARP / Cleaved PARP; PubMed: 26095475 Int J Oncol (A) BT474c or HCC1954 cells were treated for 24 h with increasing concentrations of AZD5363 ±0.3 μM or 1 μM AZD8931, respectively. Protein lysates were analysed by immunoblot with the indicated antibodies. Blots are representative of blots from 2–3 separate experiments.	26998062 26095475
Immunofluorescence	p-Chk2 / γ-H2AX; PubMed: 29879757 Cancer Res Treat (C) Cells were treated with AZD1208 and AZD5363 alone or in combination for 5 days, and immunofluorescence analysis was subsequently performed. Confocal microscopy was used to observe the signals corresponding to p-Chk2 (red) and γ-H2AX (green). DAPI (blue) was used as a nuclear counterstain. CI, combination index. Scale bars=5 μm.	29879757
Growth inhibition assay	Cell viability; PubMed: 29879757 Cancer Res Treat Cells were seeded and cultured with increasing concentrations of AZD5363 and 1 μM AZD1208 every 3 days. The cells were cultured for 14 days until colonies formed and were then stained. The percentages of surviving cells were calculated by counting the number of colonies and are presented in a bar graph with standard error bars (n=3). a)p < 0.005.	29879757

In vivo

Oral dosing of AZD5363 (100, 300 mg/kg) to nude mice causes dose- and time-dependent reduction of PRAS40, GSK3β, and S6 phosphorylation in BT474c xenografts, reversible increases in blood glucose concentrations, and dose-dependent decreases in 2[¹⁸F]fluoro-2-deoxy-d-glucose (¹⁸F-FDG) uptake in U87-MG xenografts. Chronic oral dosing of AZD5363 (130, 200, and 300 mg/kg) causes dose-dependent growth inhibition of xenografts derived from various tumor types, including HER2+ breast cancer models that are resistant to trastuzumab. AZD5363 also significantly enhances the antitumor activity of docetaxel, lapatinib, and trastuzumab in breast cancer xenografts. ^[2]

Protocol

Kinase Assay:^[1]	- Collapse Caliper Off-Chip Incubation Mobility Shift assay: The ability of AZD5363 and other compounds to inhibit the activity of AKT1, AKT2, and AKT3 is evaluated by the Caliper Off-Chip Incubation Mobility Shift assay. Active recombinant AKT1, AKT2, or AKT3 are incubated with a 5-FAM-labeled custom-synthesized peptide substrate together with increasing concentrations of inhibitor. Final reactions contained 1 to 3 nM AKT1, AKT2, or AKT3 enzymes; 1.5 mM peptide substrate; ATP at K _m for each AKT isoform; 10 mM MgCl₂, 4 mM DTT, 100 mM HEPES, and 0.015% Brij-35. The reactions are incubated at room temperature for 1 hour and stopped by the addition of buffer containing 100 mM HEPES, 0.015% Brij-35 solution, 0.1% coating reagent, 40 mM EDTA, and 5% DMSO. Plates are then analyzed using a Caliper LC3000, allowing for separation of peptide substrate and phosphorylated product by electrophoresis with subsequent detection and quantification of laser induced fluorescence.
Cell Research: ^[2]	- Collapse Cell lines: 182 solid and hematologic tumor cell lines Concentrations: ~30 μM Incubation Time: 72 hours Method: Cell proliferation assay is determined by 2 methods, MTS and Sytox Green. Briefly, cells are seeded in 96-well plates and incubated overnight at 37 ℃, 5% CO₂. Cells are then exposed to concentrations of AZD5363 ranging from 30 to 0.003μM for 72 hours. For the MTS endpoint, cell proliferation is measured by the CellTiter AQueous Non-Radioactive Cell Proliferation Assay reagent in accordance with the manufacturer's protocol. For the Sytox Green endpoint, Sytox Green nucleic acid dye diluted in TBS-EDTA buffer is added to cells (final concentration of 0.13 μM) and the number of dead cells detected using an Acumen Explorer. Cells are then permeabilized by the addition of saponin (0.03% final concentration, diluted in TBS-EDTA buffer), incubated overnight and a total cell count measured. Predose measurements are made for both MTS and Sytox Green endpoints, and concentration needed to reduce the growth of treated cells to half that of untreated cells values are determined using absorbance readings (MTS) or live cell counts. (Only for Reference)
Animal Research:^[2]	- Collapse Animal Models: Female nude mice and male SCID mice with BT474c, U87MG, KPL-4, HCC-1187 xenografts. Dosages: 130 mg/Kg - 300 mg/Kg Administration: p.o. (Only for Reference)

References

Solubility (25°C)

In vitro	DMSO	86 mg/mL (200.5 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 Capivasertib (AZD5363) SDF

Molecular Weight	428.92
Formula	C₂₁H₂₅ClN₆O₂
CAS No.	1143532-39-1
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	N/A
Smiles	C1CN(CCC1(C(=O)NC(CCO)C2=CC=C(C=C2)Cl)N)C3=NC=NC4=C3C=CN4

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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.

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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2021-09-06)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03310541	Active not recruiting	Drug: AZD5363\|Drug: Enzalutamide\|Drug: Fulvestrant	Breast Cancer\|Prostate Cancer\|Advanced Solid Tumors	Memorial Sloan Kettering Cancer Center	October 11 2017	Phase 1
NCT01992952	Active not recruiting	Drug: AZD5363\|Drug: Placebo\|Drug: Fulvestrant	Estrogen Receptor Positive Breast Cancer	Velindre NHS Trust\|AstraZeneca\|Cenduit LLC\|Covance\|Cardiff and Vale University Health Board	May 2014	Phase 1\|Phase 2
NCT02338622	Completed	Drug: olaparib\|Drug: AZD5363	Advanced Cancer	Royal Marsden NHS Foundation Trust\|Institute of Cancer Research United Kingdom\|AstraZeneca	March 31 2014	Phase 1
NCT02121639	Active not recruiting	Drug: Placebo\|Drug: AZD5363	Prostate Cancer	University Hospital Southampton NHS Foundation Trust\|AstraZeneca\|Cancer Research UK	January 29 2014	Phase 1\|Phase 2
NCT02077569	Completed	Drug: AZD5363	Invasive Breast Cancer	University of Nottingham\|AstraZeneca\|Cancer Research UK\|National Cancer Research Network	January 2014	Phase 2
NCT01692262	Completed	Drug: Intermittent dosing of AZD5363	Metastatic Castrate-Resistant Prostate Cancer (mCRPC)\|Efficacy\|Safety and Tolerability\|Pharmacokinetics\|Pharmacodynamics\|Tumour Response.	AstraZeneca	November 2012	Phase 1

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Akt Signaling Pathway Map

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Akt Inhibitor in Clinical Trial

Perifosine (KRX-0401) : Phase III for relapsed and refractory multiple myeloma.
Classic Akt Inhibitor

MK-2206 2HCl : Highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM, respectively; no inhibitory activities against 250 other protein kinases observed. Phase 2.

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Capivasertib (AZD5363)