Capivasertib (AZD5363)

目录号:S8019

仅限科研使用

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。

Capivasertib (AZD5363) Chemical Structure

CAS: 1143532-39-1

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 1926.33 现货
RMB 1216.65 现货
RMB 3865.98 现货
RMB 9582.3 现货
大包装 有超大折扣
大剂量询单有大折扣!

今日订购,明日送达 全国免运费 分装免费 分装成小规格产品(单支最小为1mg)
如1支10mg产品可分装为10支1mg产品

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客户使用Selleck生产的Capivasertib (AZD5363)发表文献101篇:

产品安全说明书

Akt抑制剂选择性比较

相关Akt产品

生物活性

产品描述 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。
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 Formulation Activity Description PMID
PC-3  MXHGeY5kfGmxbjDBd5NigQ>? NEDQ[pAyOCEQvF2= NV7rToNUOTJiaB?= Ml:2bY5lfWOnczDheZRweGijZ4m= NIPMZo09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{K1PFc1OCd-MkOyOVg4PDB:L3G+
LNCaP M13KfGNmdGxiVnnhZoltcXS7IFHzd4F6 MoD0NE0yODByIH7N MX2wMVQh\A>? M2PMdZJm\HWlZXSgUG5E[VBiY3XscEB3cWGkaXzpeJkhcW5iYTDkc5NmNSCjbnSgeIlu\S2mZYDlcoRmdnRibXHucoVzyqB? M1TpVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MkW4O|QxLz5{M{K1PFc1ODxxYU6=
DU145  M1;LbWZ2dmO2aX;uJGF{e2G7 M2nEcVAvPS9zL{GwJO69VQ>? M1;uU|Q5KGh? Mknw[I94dnKnZ4XsZZRmeyC2aHWgdIhwe3Cqb4L5cIF1cW:wIH;mJIRwf26|dILlZY0heGG2aIfhfUBxem:2ZXnud{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzJ3OEe0NEc,OjN{NUi3OFA9N2F-
PC-3 MVrGeY5kfGmxbjDBd5NigQ>? MXWwMlUwOS9zMDFOwG0> MnziOFghcA>? NVPzVnY6\G:5boLl[5Vt[XSnczD0bIUheGixc4Doc5J6dGG2aX;uJI9nKGSxd37zeJJm[W1icHH0bJdigSCycn;0[YlveyCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzJ3OEe0NEc,OjN{NUi3OFA9N2F-
C4-2  M37zOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYOxNFAuPTByMDDuUS=> MVm3NkBp MoT3bY5kemWjc3XzJJRp\SCocnHjeIlwdiCxZjDj[YxteyC3bnTldodwcW6pIHPlcIwh\GWjdHi= NIrVcIM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m2OlYzOSd-MkO5OlY3OjF:L3G+
LNCaP MoTaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3ZNVAxNTVyMECgcm0> NXn2S4lGPzJiaB?= MkjDbY5kemWjc3XzJJRp\SCocnHjeIlwdiCxZjDj[YxteyC3bnTldodwcW6pIHPlcIwh\GWjdHi= MoD5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7Nk[2NlEoRjJ|OU[2OlIyRC:jPh?=
C4-2  NFH2co9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXyxMVExODByIH7N NF;OcpIxNTNiZB?= NVzSWlRUcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NYXB[3VMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5OlY3OjFpPkKzPVY3PjJzPD;hQi=>
LNCaP Ml;FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVn0Wo42OS1zMECwNEBvVQ>? M1nWUVAuOyCm M{XhNYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NX7qXmRxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5OlY3OjFpPkKzPVY3PjJzPD;hQi=>
C4-2  M3vsN2Z2dmO2aX;uJGF{e2G7 MlvnOUDPxE1? NFfPb3ExNTJ2IHi= MWHpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[geIhmKGSrc4ThcEBCU1RvcHH0bJdigSCkaX;tZZJs\XK|IHnuZ4x2\GmwZzDQVmFUPDBuIHXJSlRGNCB2RT3CVFEtKG2WT2KsJIFv\CCSN{CgV|Yhc2mwYYPlJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy M2LxNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OU[2OlIyLz5{M{m2OlYzOTxxYU6=
LNCaP MmXzSpVv[3Srb36gRZN{[Xl? MlzCOUDPxE1? MkTrNE0zPCCq MYrpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[geIhmKGSrc4ThcEBCU1RvcHH0bJdigSCkaX;tZZJs\XK|IHnuZ4x2\GmwZzDQVmFUPDBuIHXJSlRGNCB2RT3CVFEtKG2WT2KsJIFv\CCSN{CgV|Yhc2mwYYPlJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy M{PJWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OU[2OlIyLz5{M{m2OlYzOTxxYU6=
C4-2  NUPQdHc1TnWwY4Tpc44hSXO|YYm= MnnKOUDPxE1? MlzzNE0zPCCq MWrpcoR2[2W|IFHLWHM1PzNiYX7kJGFMXFR|MEigdIhwe3Cqb4L5cIF1cW:wIHnuJIEhfGmvZTDk[ZBmdmSnboSgcYFvdmW{ NEflSFI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m2OlYzOSd-MkO5OlY3OjF:L3G+
LNCaP NX7GUWF2TnWwY4Tpc44hSXO|YYm= Mk\tOUDPxE1? M2HKfFAuOjRiaB?= NVj4NnZJcW6mdXPld{BCU1SVNEezJIFv\CCDS2TUN|A5KHCqb4PwbI9zgWyjdHnvckBqdiCjIITpcYUh\GWyZX7k[Y51KG2jbn7ldi=> M3zrTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OU[2OlIyLz5{M{m2OlYzOTxxYU6=
PAMC82 MnSwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPVTWM2OD1|MDFOwG0> NWjJT5pORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwPFg{QDJpPkK0NFg5Ozh{PD;hQi=>
MKN74 NIDiO3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1:5R2lEPTB;M{Cg{txO NVTpeWRVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwPFg{QDJpPkK0NFg5Ozh{PD;hQi=>
GTL-16 Ml\kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXL3XGNjUUN3ME2zNEDPxE1? M1XSdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEi4N|gzLz5{NEC4PFM5OjxxYU6=
SNU-5 NGfmcZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTNyIN88US=> NECybZM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC4PFM5Oid-MkSwPFg{QDJ:L3G+
NUGC-4 MnTNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTNyIN88US=> NIfRc5k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC4PFM5Oid-MkSwPFg{QDJ:L3G+
SNU-216 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrmc45qUUN3ME2zNEDPxE1? MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB6OEO4Nkc,OjRyOEizPFI9N2F-
AZ521 MlrFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;WdmlEPTB;MkWuOFQ5KM7:TR?= NX\zcIg5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwPFg{QDJpPkK0NFg5Ozh{PD;hQi=>
NUGC-3 NHK0To9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\lUGlEPTB;MkGuPFc{KM7:TR?= M3v3SFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEi4N|gzLz5{NEC4PFM5OjxxYU6=
OCUM-1 MlvCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTF2LkWxOUDPxE1? NX7lVJJXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwPFg{QDJpPkK0NFg5Ozh{PD;hQi=>
SNU-16 M1L0Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3ycYNKSzVyPUGxMlA6PyEQvF2= M3f5eVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEi4N|gzLz5{NEC4PFM5OjxxYU6=
SNU-484 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fRUmlEPTB;Nz6zPVIh|ryP M3L4dVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEi4N|gzLz5{NEC4PFM5OjxxYU6=
KATO III NXThW3c1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3Px[mlEPTB;Nz6yOlch|ryP Mk\OQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyOEizPFIoRjJ2MEi4N|gzRC:jPh?=
HS746T Mn7lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlP3TWM2OD14LkC4OEDPxE1? Ml36QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyOEizPFIoRjJ2MEi4N|gzRC:jPh?=
SNU-668 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HGd2lEPTB;Nj6wNFMh|ryP NV7WSlZxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwPFg{QDJpPkK0NFg5Ozh{PD;hQi=>
SNU-601 NFPuPZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnkTZhKSzVyPUWuPVM5KM7:TR?= Mn3SQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyOEizPFIoRjJ2MEi4N|gzRC:jPh?=
SNU-1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLQO4RKSzVyPUWuNlU5KM7:TR?= NGrQVGE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC4PFM5Oid-MkSwPFg{QDJ:L3G+
SNU-638 M2XuT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnNVpJKSzVyPUSuOVI{KM7:TR?= MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB6OEO4Nkc,OjRyOEizPFI9N2F-
SNU-620 NX3z[XdOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3nuRWlEPTB;Mz6zPFQh|ryP MlTwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyOEizPFIoRjJ2MEi4N|gzRC:jPh?=
MKN1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PyeWlEPTB;Mj60NlEh|ryP NH25NY89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC4PFM5Oid-MkSwPFg{QDJ:L3G+
23132/87 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3ITWM2OD1zLk[3NUDPxE1? MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB6OEO4Nkc,OjRyOEizPFI9N2F-
NCI-N87 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTFwMEO3JO69VQ>? MoH0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyOEizPFIoRjJ2MEi4N|gzRC:jPh?=
AGS MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MorETWM2OD1yLkW1NkDPxE1? M{LUO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEi4N|gzLz5{NEC4PFM5OjxxYU6=
IM95m MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPBZlVKSzVyPUCuOVEh|ryP M1vLclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEi4N|gzLz5{NEC4PFM5OjxxYU6=
HGC27 M4i1fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTBwNES1JO69VQ>? M3HYVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEi4N|gzLz5{NEC4PFM5OjxxYU6=
PC-9 MUnGeY5kfGmxbjDBd5NigQ>? NVnDPY41OS93L{GwJO69VQ>? M2j6SFQwOjRiaB?= MYDpcoNz\WG|ZYOgRWtVKHCqb4PwbI9zgWyjdHnvci=> NHfycpA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm1O|Y5Oid-MkS5OVc3QDJ:L3G+
NCI-H522 NVf0ZnE1TnWwY4Tpc44hSXO|YYm= MYGxM|UwOTBizszN NUfFdIs1PC9{NDDo MljmbY5kemWjc3XzJGFMXCCyaH;zdIhwenmuYYTpc44> M4[5elxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUW3OlgzLz5{NEm1O|Y5OjxxYU6=
PC-9 MmqwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPtTWM2OD17LkOgLOKyOS5{KTFOwG0> NX\4XIVORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5OVc3QDJpPkK0PVU4Pjh{PD;hQi=>
NCI-H522 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTFzLkOgLOKyOi55KTFOwG0> MnrpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7NUe2PFIoRjJ2OUW3OlgzRC:jPh?=
MR49F MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW[wMVUh|ryP NH7GblM1QCCq NGC1bWpqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NI\NSmM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUG1NVAyOid-MkWxOVExOTJ:L3G+
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Assay
Methods Test Index PMID
Western blot pAKT / AKT / pGSK3β / GSK3β HER3 / pHER3 / HER2 / pHER2 / pPRAS40 / pS6 / p-4EBP1 / pFOXO / pERK / PARP / Cleaved PARP 26998062 26095475
Immunofluorescence p-Chk2 / γ-H2AX 29879757
Growth inhibition assay Cell viability 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]

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)

激酶实验:[1]
  • 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Km; 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]
  • 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。
动物实验:[2]
  • 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

溶解度(25°C)

体外

* 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

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

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)

mg/kg g μL

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
%DMSO %

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,: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: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。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,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。

摩尔浓度计算器

质量 浓度 体积 分子量

临床试验信息

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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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