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
RMB 1216.65 现货
RMB 3865.98 现货
RMB 9582.3 现货
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客户使用Selleck生产的Capivasertib (AZD5363)发表文献88篇:

产品安全说明书

Akt抑制剂选择性比较

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  M2nCb2Z2dmO2aX;uJGF{e2G7 NVTWWm1KOTBizszN M3LUeVEzKGh? MnjwbY5lfWOnczDheZRweGijZ4m= MkDqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN{NUi3OFAoRjJ|MkW4O|QxRC:jPh?=
LNCaP NXjhUo9tS2WubDDWbYFjcWyrdImgRZN{[Xl? NIDPWWYxNTFyMECgcm0> NWTYV5FZOC12IHS= NHvTOmNz\WS3Y3XkJGxPS2GSIHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S1iYX7kJJRqdWVvZHXw[Y5l\W62IH3hco5mesLi Ml\rQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN{NUi3OFAoRjJ|MkW4O|QxRC:jPh?=
DU145  M1u1cWZ2dmO2aX;uJGF{e2G7 NUfFW3JkOC53L{GvNVAh|ryP NVT1PHI{PDhiaB?= Mmrp[I94dnKnZ4XsZZRmeyC2aHWgdIhwe3Cqb4L5cIF1cW:wIH;mJIRwf26|dILlZY0heGG2aIfhfUBxem:2ZXnud{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NVHR[pNlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyOVg4PDBpPkKzNlU5PzRyPD;hQi=>
PC-3 NGHnPWxHfW6ldHnvckBCe3OjeR?= NEnzfXUxNjVxMT:xNEDPxE1? M2[3S|Q5KGh? MYPkc5dvemWpdXzheIV{KHSqZTDwbI9{eGixconsZZRqd25ib3[g[I94dnO2cnXhcUBx[XSqd3H5JJBzd3SnaX7zJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M1XWVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MkW4O|QxLz5{M{K1PFc1ODxxYU6=
C4-2  NEL3VYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2q3S|ExOC13MECwJI5O M4DxR|czKGh? MVrpcoNz\WG|ZYOgeIhmKG[{YXP0bY9vKG:oIHPlcIx{KHWwZHXy[49qdmdiY3XscEBl\WG2aB?= NWf4TFJ[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5OlY3OjFpPkKzPVY3PjJzPD;hQi=>
LNCaP Mk[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfyb3N5OTByLUWwNFAhdk1? NVLjVnRlPzJiaB?= MnrqbY5kemWjc3XzJJRp\SCocnHjeIlwdiCxZjDj[YxteyC3bnTldodwcW6pIHPlcIwh\GWjdHi= MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl4Nk[yNUc,OjN7Nk[2NlE9N2F-
C4-2  NV;vZ2dKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzqdplrOS1zMECwNEBvVQ>? M1\IcFAuOyCm NFTSO3JqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MkLjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7Nk[2NlEoRjJ|OU[2OlIyRC:jPh?=
LNCaP M1vYOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHT6NmwyNTFyMECwJI5O MV2wMVMh\A>? NEnE[XlqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 M1P3Z|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OU[2OlIyLz5{M{m2OlYzOTxxYU6=
C4-2  NEn4[nJHfW6ldHnvckBCe3OjeR?= MmDvOUDPxE1? NUW1RYprOC1{NDDo MmG2bY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJJRp\SCmaYP0ZYwhSUuWLYDheIh4[XliYnnvcYFzc2W{czDpcoNtfWSrbnegVHJCWzRyLDDlTWY1TSxiNFWtRnAyNCCvVF;SMEBidmRiUEewJHM3KGurbnHz[UBqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7ldi=> MorlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7Nk[2NlEoRjJ|OU[2OlIyRC:jPh?=
LNCaP MXLGeY5kfGmxbjDBd5NigQ>? MorPOUDPxE1? MknENE0zPCCq MoLHbY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJJRp\SCmaYP0ZYwhSUuWLYDheIh4[XliYnnvcYFzc2W{czDpcoNtfWSrbnegVHJCWzRyLDDlTWY1TSxiNFWtRnAyNCCvVF;SMEBidmRiUEewJHM3KGurbnHz[UBqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7ldi=> M{n1Z|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OU[2OlIyLz5{M{m2OlYzOTxxYU6=
C4-2  M1jybWZ2dmO2aX;uJGF{e2G7 NXjWflNmPSEQvF2= NY\wb45IOC1{NDDo MXfpcoR2[2W|IFHLWHM1PzNiYX7kJGFMXFR|MEigdIhwe3Cqb4L5cIF1cW:wIHnuJIEhfGmvZTDk[ZBmdmSnboSgcYFvdmW{ M3[zZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OU[2OlIyLz5{M{m2OlYzOTxxYU6=
LNCaP NYnwOJVSTnWwY4Tpc44hSXO|YYm= Mnu3OUDPxE1? M2jMeVAuOjRiaB?= NGLKPGFqdmS3Y3XzJGFMXFN2N{OgZY5lKEGNVGSzNFgheGixc4Doc5J6dGG2aX;uJIlvKGFidHnt[UBl\XCnbnTlcpQhdWGwbnXy MnX5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7Nk[2NlEoRjJ|OU[2OlIyRC:jPh?=
PAMC82 MonQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV[wSlEyUUN3ME2zNEDPxE1? M13w[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEi4N|gzLz5{NEC4PFM5OjxxYU6=
MKN74 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILu[2dKSzVyPUOwJO69VQ>? MlTwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyOEizPFIoRjJ2MEi4N|gzRC:jPh?=
GTL-16 NH:1N2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIj1SmdKSzVyPUOwJO69VQ>? MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB6OEO4Nkc,OjRyOEizPFI9N2F-
SNU-5 MnTzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTNyIN88US=> MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB6OEO4Nkc,OjRyOEizPFI9N2F-
NUGC-4 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTNyIN88US=> MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB6OEO4Nkc,OjRyOEizPFI9N2F-
SNU-216 NXXKR5ZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvC[GhKUUN3ME2zNEDPxE1? M4jtT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEi4N|gzLz5{NEC4PFM5OjxxYU6=
AZ521 NV\MXVN6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIWyb4JKSzVyPUK1MlQ1QCEQvF2= NUHnPG5MRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwPFg{QDJpPkK0NFg5Ozh{PD;hQi=>
NUGC-3 NE\j[2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3NTWM2OD1{MT64O|Mh|ryP NF\1SJY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC4PFM5Oid-MkSwPFg{QDJ:L3G+
OCUM-1 NFTFeoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzQbVBKSzVyPUG0MlUyPSEQvF2= MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB6OEO4Nkc,OjRyOEizPFI9N2F-
SNU-16 NH7ac|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnlTWM2OD1zMT6wPVch|ryP NILBVo49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC4PFM5Oid-MkSwPFg{QDJ:L3G+
SNU-484 Mn\tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTdwM{myJO69VQ>? MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB6OEO4Nkc,OjRyOEizPFI9N2F-
KATO III MmDCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;qTWM2OD15LkK2O{DPxE1? NXLYVoFSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwPFg{QDJpPkK0NFg5Ozh{PD;hQi=>
HS746T NVjUV5F[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIX2[GxKSzVyPU[uNFg1KM7:TR?= Mn;aQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyOEizPFIoRjJ2MEi4N|gzRC:jPh?=
SNU-668 NFi1S2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTZwMECzJO69VQ>? NVjYZZVNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwPFg{QDJpPkK0NFg5Ozh{PD;hQi=>
SNU-601 M2mwbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTVwOUO4JO69VQ>? NHfCb5Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC4PFM5Oid-MkSwPFg{QDJ:L3G+
SNU-1 NYixNlFVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTVwMkW4JO69VQ>? M4XCUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEi4N|gzLz5{NEC4PFM5OjxxYU6=
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SNU-620 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTNwM{i0JO69VQ>? MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB6OEO4Nkc,OjRyOEizPFI9N2F-
MKN1 Mlv1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rxR2lEPTB;Mj60NlEh|ryP NYLmVWlIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwPFg{QDJpPkK0NFg5Ozh{PD;hQi=>
23132/87 NVGyXHRiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXXTWM2OD1zLk[3NUDPxE1? NFnWNms9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC4PFM5Oid-MkSwPFg{QDJ:L3G+
NCI-N87 NWiwWnl4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzjTWM2OD1zLkCzO{DPxE1? M4HUfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEi4N|gzLz5{NEC4PFM5OjxxYU6=
AGS NU[4d3JGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml65TWM2OD1yLkW1NkDPxE1? MkDDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyOEizPFIoRjJ2MEi4N|gzRC:jPh?=
IM95m NEfsZodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTCfXp[UUN3ME2wMlUyKM7:TR?= M3HBUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEi4N|gzLz5{NEC4PFM5OjxxYU6=
HGC27 MnrlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33ES2lEPTB;MD60OFUh|ryP M2PMSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEi4N|gzLz5{NEC4PFM5OjxxYU6=
PC-9 NXTCSIYyTnWwY4Tpc44hSXO|YYm= NGPLdYQyNzVxMUCg{txO Mm\6OE8zPCCq M3S1fYlv[3KnYYPld{BCU1RicHjvd5Bpd3K7bHH0bY9v MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl3N{[4Nkc,OjR7NUe2PFI9N2F-
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NB-EBc1 NF3p[JRyUFSVIHHzd4F6 M{fxOJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQj3FRoMyKGOnbHzz NFj5Row9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
LAN-5 M4HtcJFJXFNiYYPzZZk> MnuydWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEyDTj21JINmdGy| MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh18 Mo\ldWhVWyCjc4PhfS=> NGLrU4FyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUnixPEBk\Wyucx?= NYnNdXBRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
pAKT / AKT / pGSK3β / GSK3β; 

PubMed: 26998062     


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     


(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     


(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     


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]

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]
- 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]
- 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)

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

分子量 428.92
化学式

C21H25ClN6O2

CAS号 1143532-39-1
储存条件 粉状
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 g 每只动物给药体积 ul 动物数量
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

计算器

摩尔浓度计算器

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、SDS / 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

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、SDS / 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

  • 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

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

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

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID