Capivasertib (AZD5363)

For research use only. Not for use in humans.

目录号：S8019

Capivasertib (AZD5363) Chemical Structure

CAS No. 1143532-39-1

Capivasertib (AZD5363)有效抑制Akt(Akt1/Akt2/3)的所有亚型，在无细胞试验中IC50为3 nM/8 nM/8 nM，对P70S6K/PKA也具有相似的抑制效果，而对ROCK1/2抑制活性较低。Phase 2。

规格

价格

库存

购买数量

10mM (1mL in DMSO)	RMB 1926.33	现货
5mg	RMB 1216.65	现货
25mg	RMB 3865.98	现货
100mg	RMB 9582.3	现货
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客户使用Selleck生产的Capivasertib (AZD5363)发表文献75篇：

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

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Nat Commun, 2020, 11(1):5982

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

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Eur J Cancer, 2020, 126:93-103

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Br J Cancer, 2020, 22

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Cells, 2020, 9(3)

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Mol Oncol, 2020, 10.1002/1878-0261.12888

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J Recept Signal Transduct Res, 2020, 1-11

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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

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

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Sci Rep, 2020, 10(1):21762

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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

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

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

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

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

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EBioMedicine, 2019, 40:77-91

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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

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Sci Rep, 2019, 9(1):13308

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Nat Commun, 2018, 9(1):5200

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

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Oncogene, 2018,

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

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

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Eur J Pharmacol, 2016, 788:90-97

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

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PubMed: 26970307 ( click the link to review the publication )

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Vanderbilt University, 2015, /

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产品安全说明书

Akt抑制剂选择性比较

生物活性

产品描述

特性

AZD5363具有良好的临床前期耐受性，和AKT抑制剂的药效学特性，且不同于其他AKT抑制剂具有卓越的特性，已经进入临床开发阶段。^[2]

靶点

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

体外研究

AZD5363是有效的Akt抑制剂，抑制Akt1, Akt2 和 Akt3时，IC50分别为3 nM, 8 nM 和 8 nM。PIK3CA突变的激活，肿瘤抑制基因PTEN的丢失或失活，或HER2的扩增，都与AZD5363有着显著的关系。此外，还可以看出细胞系的RAS突变状态与抗AZD5363之间的相关性。^[1]AZD5363在细胞中抑制AKT底物的磷酸化，效价约为0.3〜0.8μM。AZD5363抑制182种实体和血液肿瘤细胞系中的41种细胞增殖，效价为< 3 μM。^[2]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
PC-3	NX6wVG5STnWwY4Tpc44hSXO\|YYm=	MkLCNVAh\|ryP	MVOxNkBp	MUHpcoR2[2W\|IHH1eI9xcGGpeR?=	MoO4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN{NUi3OFAoRjJ\|MkW4O\|QxRC:jPh?=
LNCaP	MVHD[YxtKF[rYXLpcIl1gSCDc4PhfS=>	NG\BR44xNTFyMECgcm0>	NUDpeJl1OC12IHS=	MVPy[YR2[2WmIFzOR4FRKGOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U0h[W6mIITpcYUu\GWyZX7k[Y51KG2jbn7lduKh	MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzJ3OEe0NEc,OjN{NUi3OFA9N2F-
DU145	NWTVPIFJTnWwY4Tpc44hSXO\|YYm=	M4fDRVAvPS9zL{GwJO69VQ>?	NWnUXnp1PDhiaB?=	NEXiUnVld3ewcnXneYxifGW\|IITo[UBxcG:\|cHjvdplt[XSrb36gc4Yh\G:5boP0doVidSCyYYToe4F6KHC{b4TlbY5{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz	M3TNbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|MkW4O\|QxLz5{M{K1PFc1ODxxYU6=
PC-3	MWLGeY5kfGmxbjDBd5NigQ>?	MVewMlUwOS9zMDFOwG0>	NVX2N4dzPDhiaB?=	M3vrOIRwf26{ZXf1cIF1\XNidHjlJJBpd3OyaH;yfYxifGmxbjDv[kBld3ewc4Ty[YFuKHCjdHj3ZZkheHKxdHXpcpMhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI>	M4PKflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|MkW4O\|QxLz5{M{K1PFc1ODxxYU6=
C4-2	M3T2dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NUTJOZluOTByLUWwNFAhdk1?	NFvMXZk4OiCq	NFm5cFhqdmO{ZXHz[ZMhfGinIH\yZYN1cW:wIH;mJINmdGy\|IIXu[IVz\2:rbnegZ4VtdCCmZXH0bC=>	MmnZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7Nk[2NlEoRjJ\|OU[2OlIyRC:jPh?=
LNCaP	NXPxRoU2T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NGHJOlIyODBvNUCwNEBvVQ>?	MXK3NkBp	NV7tRmlIcW6lcnXhd4V{KHSqZTDmdoFkfGmxbjDv[kBk\WyuczD1coRmemexaX7nJINmdGxiZHXheIg>	MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl4Nk[yNUc,OjN7Nk[2NlE9N2F-
C4-2	MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NX\STpAxOS1zMECwNEBvVQ>?	MkXkNE0{KGR?	NGTR[oNqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7	MkXsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7Nk[2NlEoRjJ\|OU[2OlIyRC:jPh?=
LNCaP	MlXrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	Mn7yNU0yODByMDDuUS=>	NYW5fms{OC1\|IHS=	MXXpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6	MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl4Nk[yNUc,OjN7Nk[2NlE9N2F-
C4-2	MWnGeY5kfGmxbjDBd5NigQ>?	M{HXcFUh\|ryP	MX:wMVI1KGh?	Ml25bY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJJRp\SCmaYP0ZYwhSUuWLYDheIh4[XliYnnvcYFzc2W{czDpcoNtfWSrbnegVHJCWzRyLDDlTWY1TSxiNFWtRnAyNCCvVF;SMEBidmRiUEewJHM3KGurbnHz[UBqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7ldi=>	M2P4eFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|OU[2OlIyLz5{M{m2OlYzOTxxYU6=
LNCaP	NWTWfmNITnWwY4Tpc44hSXO\|YYm=	MUO1JO69VQ>?	NXfC[VB2OC1{NDDo	MnT1bY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJJRp\SCmaYP0ZYwhSUuWLYDheIh4[XliYnnvcYFzc2W{czDpcoNtfWSrbnegVHJCWzRyLDDlTWY1TSxiNFWtRnAyNCCvVF;SMEBidmRiUEewJHM3KGurbnHz[UBqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7ldi=>	MoP3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7Nk[2NlEoRjJ\|OU[2OlIyRC:jPh?=
C4-2	M2X3Z2Z2dmO2aX;uJGF{e2G7	NYPyO4JtPSEQvF2=	NUDkWYhMOC1{NDDo	Mn\LbY5lfWOnczDBT3RUPDd\|IHHu[EBCU1SWM{C4JJBpd3OyaH;yfYxifGmxbjDpckBiKHSrbXWg[IVx\W6mZX70JI1idm6nch?=	NUPBVYVtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5OlY3OjFpPkKzPVY3PjJzPD;hQi=>
LNCaP	MXXGeY5kfGmxbjDBd5NigQ>?	MUi1JO69VQ>?	MmW3NE0zPCCq	Ml3ybY5lfWOnczDBT3RUPDd\|IHHu[EBCU1SWM{C4JJBpd3OyaH;yfYxifGmxbjDpckBiKHSrbXWg[IVx\W6mZX70JI1idm6nch?=	NEHyfpE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m2OlYzOSd-MkO5OlY3OjF:L3G+
PAMC82	MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			MYfJR\|UxRTNyIN88US=>	NHTQ[Yo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC4PFM5Oid-MkSwPFg{QDJ:L3G+
MKN74	NGTCXIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MlPMTWM2OD1\|MDFOwG0>	NFGxe\|c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC4PFM5Oid-MkSwPFg{QDJ:L3G+
GTL-16	NXGzSoZrT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			M3eyV2lEPTB;M{Cg{txO	NV24cGdFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwPFg{QDJpPkK0NFg5Ozh{PD;hQi=>
SNU-5	NVLaWI9NT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			MmX6TWM2OD1\|MDFOwG0>	MnTRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyOEizPFIoRjJ2MEi4N\|gzRC:jPh?=
NUGC-4	Moj1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			M4nZNmlEPTB;M{Cg{txO	M{jTXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEi4N\|gzLz5{NEC4PFM5OjxxYU6=
SNU-216	Mn\qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			MorvTWM2OD1\|MDFOwG0>	NILuXmg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC4PFM5Oid-MkSwPFg{QDJ:L3G+
AZ521	NEXjVW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MkHoTWM2OD1{NT60OFgh\|ryP	NEi0eWw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC4PFM5Oid-MkSwPFg{QDJ:L3G+
NUGC-3	MoXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			MkPWTWM2OD1{MT64O\|Mh\|ryP	NIK5RYM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC4PFM5Oid-MkSwPFg{QDJ:L3G+
OCUM-1	MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NVPoW2VKUUN3ME2xOE42OTVizszN	NYLQO5p3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwPFg{QDJpPkK0NFg5Ozh{PD;hQi=>
SNU-16	NX\MW4dNT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NWDLPG85UUN3ME2xNU4xQTdizszN	NIHXUGQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC4PFM5Oid-MkSwPFg{QDJ:L3G+
SNU-484	MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NHnacWhKSzVyPUeuN\|kzKM7:TR?=	MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB6OEO4Nkc,OjRyOEizPFI9N2F-
KATO III	M3vYUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			MWPJR\|UxRTdwMk[3JO69VQ>?	M2nKPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEi4N\|gzLz5{NEC4PFM5OjxxYU6=
HS746T	M2\6ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			MkDKTWM2OD14LkC4OEDPxE1?	NWTsNmJnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwPFg{QDJpPkK0NFg5Ozh{PD;hQi=>
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DAOY	NVy0ZY0xeUiWUzDhd5NigQ>?			M3XV[ZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCGQV;ZJINmdGy\|	NF3JbVI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
Saos-2	M{TYcpFJXFNiYYPzZZk>			M2rGS5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVYX;zMVIh[2WubIO=	NX[0Xm5tRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-SH	MU\xTHRUKGG\|c3H5			NXT3VYE5eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IGPLMW4uW0hiY3XscJM>	NFrKV3U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
NB1643	NYO5OIppeUiWUzDhd5NigQ>?			M{WxUZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQkG2OFMh[2WubIO=	NIju[o09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
MG 63 (6-TG R)	NHHnZlhyUFSVIHHzd4F6			MYfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN?	Mn3wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
Rh41	MVPxTHRUKGG\|c3H5			M3XBOZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCUaESxJINmdGy\|	NYjERYVQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC	NXLkcYhPeUiWUzDhd5NigQ>?			NHjw[ZVyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1OSyClZXzsdy=>	MnTTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
NB-EBc1	M2rTRpFJXFNiYYPzZZk>			NHLxNIRyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKtSWJkOSClZXzsdy=>	MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
LAN-5	MoHodWhVWyCjc4PhfS=>			Mke5dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKEyDTj21JINmdGy\|	NXfueo9vRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh18	MYfxTHRUKGG\|c3H5			NGHPS4pyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUnixPEBk\Wyucx?=	MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-

... 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

体内研究

AZD5363按100, 300 mg/kg剂量口服给药裸鼠，降低BT474c移植瘤中PRAS40, GSK3β,和 S6的磷酸化，这种作用具有剂量和时间依赖性，也可逆性地增加血糖浓度，且降低U87-MG移植瘤中2[¹⁸F]氟-2-脱氧-d-葡萄糖(¹⁸F-FDG)的摄取，这种作用存在剂量依赖性。AZD5363按130, 200, 和300 mg/kg剂量慢性口服给药从各种肿瘤类型衍生的移植瘤，包括抗Trastuzumab的HER2⁺乳腺癌模型，抑制移植瘤的生长，这种作用存在剂量依赖性。AZD5363在乳腺癌移植瘤中也显著增强 Docetaxel, Lapatinib, 和 Trastuzumab的抗肿瘤活性。^[2]

激酶实验：^[1]	- 合并 Caliper Off-Chip Incubation迁移率变动分析: 通过 Caliper Off-Chip Incubation迁移率变动分析测评AZD5363和其他化合物抑制AKT1, AKT2, 和 AKT3活性的能力。活跃的重组AKT1，AKT2，或AKT3与5-FAM标记的定制合成的肽底物，及浓度不断增加的抑制剂温育。最终反应包含1 到 3 nM AKT1, AKT2, 或AKT3 酶; 1.5 mM 肽底物; AKT亚型的ATP为K_m; 10 mM MgCl₂, 4 mM DTT, 100 mM HEPES, 及0.015% Brij-35。反应在室温下温育1小时，然后加入含100 mM HEPES, 0.015% Brij-35 溶液, 0.1% 涂层试剂， 40 mM EDTA, 和5% DMSO的buffer终止反应。使用Caliper LC3000分析实验板，进行肽底物的分离，对磷酸化的产物进行电泳和激光诱导荧光的检测和量化。
细胞实验： ^[2]	- 合并 Cell lines: 182种实体和血液肿瘤细胞系 Concentrations: 0.003 μM-30 μM Incubation Time: 72 小时 Method: 通过MTS和Sytox Green2种方法测定细胞增殖实验。细胞接种在96孔板中，在37°C下,含 5% CO₂的环境中温育过夜。使用浓度为30 到 0.003μM的 AZD5363处理细胞72小时。对于MTS端点，通过CellTiter AQueous非放射性细胞增殖检测试剂测量细胞增殖。对于Sytox Green 端点，在TBS-EDTA buffer 中稀释的Sytox Green核酸染料加到细胞中（终浓度为0.13μM），使用Acumen Explorer测定死亡细胞数。通过加入Saponin（终浓度0.03％，在TBS-EDTA buffer中稀释）使细胞具有渗透性，温育过夜，并测量总细胞数。MTS 和Sytox Green 端点都是给药前测量，使用吸光度读数（MTS）或活细胞计数测定将实验组细胞的生长降低到未处理组细胞的一半所需要的浓度值。 (Only for Reference)
动物实验：^[2]	- 合并 Animal Models: 携带 BT474c, U87MG, KPL-4, HCC-1187 移植瘤的雌性裸鼠和雄性SCID小鼠 Dosages: 130 mg/Kg-300 mg/Kg Administration: 口服处理 (Only for Reference)

参考文献

溶解度 (25°C)

体外	DMSO	86 mg/mL (200.5 mM)
	Water	Insoluble
	Ethanol	Insoluble

* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据 Download Capivasertib (AZD5363) SDF

分子量	428.92
化学式	C₂₁H₂₅ClN₆O₂
CAS号	1143532-39-1
储存条件	3年-20°C 粉状 2年-80°C 溶于溶剂
别名	N/A

动物体内配方计算器 (澄清溶液)

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO+ % + % Tween 80+ % ddH₂O

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

质量

浓度

体积

分子量
=

×

×

*在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入输出 )

C1

V1

C2

V2
×

=

×

在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.

连续稀释计算器方程

连续稀释
初始浓度:
稀释倍数:

计算结果

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):

分子量计算器

通过输入化合物的化学式来计算其分子量：

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×
计算

临床试验信息 (data from https://clinicaltrials.gov, updated on 2020-01-06)

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

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

Akt Signaling Pathway Map

Akt Inhibitors with Unique Features

选择性强的Akt抑制剂

CCT128930 : Akt2-selective, IC50=6 nM.
活性最高的Akt抑制剂

GSK690693 : Akt1, IC50=2 nM; Akt2, IC50=13 nM; Akt3, IC50=9 nM.
用于临床的Akt抑制剂

Perifosine (KRX-0401) : Phase III for relapsed and refractory multiple myeloma.
经典的Akt抑制剂

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.

研究领域

产品类型

定制您的化合物库

Capivasertib (AZD5363)

客户使用Selleck生产的Capivasertib (AZD5363)发表文献75篇：

产品安全说明书

Akt抑制剂选择性比较

生物活性

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

参考文献

溶解度 (25°C)

化学数据 Download Capivasertib (AZD5363) SDF

动物体内配方计算器 (澄清溶液)

计算器

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

稀释计算器

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

连续稀释计算器方程

连续稀释

计算结果

分子量计算器

总分子量：g/mol

摩尔浓度计算器

临床试验信息 (data from https://clinicaltrials.gov, updated on 2020-01-06)

技术支持

Akt Signaling Pathway Map

Akt Inhibitors with Unique Features

相关Akt产品