AZD8055

For research use only. Not for use in humans.

目录号:S1555

AZD8055 Chemical Structure

CAS No. 1009298-09-2

AZD8055是一种新型的,ATP竞争性mTOR抑制剂,在MDA-MB-468 细胞中IC50为0.8 nM,与作用于PI3K亚型和ATM/DNA-PK相比,具有优异的选择性(约1000倍)。AZD8055可诱导半胱天冬酶依赖的凋亡和自噬。Phase 1。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1265.49 现货
RMB 712.53 现货
RMB 988.31 现货
RMB 3048.72 现货
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客户使用Selleck生产的AZD8055发表文献171篇:

产品安全说明书

mTOR抑制剂选择性比较

生物活性

产品描述 AZD8055是一种新型的,ATP竞争性mTOR抑制剂,在MDA-MB-468 细胞中IC50为0.8 nM,与作用于PI3K亚型和ATM/DNA-PK相比,具有优异的选择性(约1000倍)。AZD8055可诱导半胱天冬酶依赖的凋亡和自噬。Phase 1。
特性 AZD8055是第一种抑制两种类型mTOR蛋白的药物,被认为可能比之前mTOR抑制剂更有效。
靶点
mTOR (truncated) [1]
(MDA-MB-468 cells)
mTOR (full length) [1]
(MDA-MB-468 cells)
0.13 nM 0.8 nM
体外研究

AZD8055作用于所有 PI3K亚型 (α, β, γ, δ) 和其他近PI3K激酶家族(ATM和DNA-PK)显示出低活性。AZD8055抑制mTORC1(p70S6K 和4E-BP1) ,mTORC2 (AKT) 和下游蛋白的磷酸化。AZD8055完全抑制4E-BP1抗Rapamycin 的T37/46 磷酸化位点, 导致明显抑制cap-dependent 转译作用。AZD8055有效抑制U87MG, A549和H838 细胞增殖, IC50分别为53, 50,和20 nM。AZD8055作用于H838和A549细胞,也诱导自体吞噬和增加LC3-II 水平。[1] AZD8055降低白血病细胞增殖和细胞周期进展, 降低白血病祖细胞的无性系生长,且在白血病细胞中诱导caspase依赖的细胞凋亡,但是作用于正常未成熟的CD34+ 细胞时不会产生这种诱导作用。[2] AZD8055 抑制儿科临床前期测试计划(PPTP)细胞系,IC50 为24.7 nM,且在EFS 分布时诱导产生明显区别。[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
LU-139 M1;WV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3L2c2lEPTB;MD6wNlM{OSEQvF2= MWjTRW5ITVJ?
NCI-H720 M{LTW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTBwMEK5N|gh|ryP Moj3V2FPT0WU
KARPAS-45 Mlm4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1ziW2lEPTB;MD6wN|M4OSEQvF2= MV7TRW5ITVJ?
EW-3 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrmTmxKSzVyPUCuNFQxPTZizszN NF\KSGpUSU6JRWK=
SBC-1 M2fwcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnm0TWM2OD1yLkC0OVgyKM7:TR?= MYPTRW5ITVJ?
NCI-H209 M1PlVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3p[21UUUN3ME2wMlA2PDV|IN88US=> M1z6cXNCVkeHUh?=
EoL-1-cell MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELRdVZKSzVyPUCuNFY2PjlizszN MnO4V2FPT0WU
H9 MojrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\PU41KSzVyPUCuNFY3QTJizszN NICyOYxUSU6JRWK=
AN3-CA NVjLXWJ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvHdolKSzVyPUCuNFc6PTFizszN NXH1RYFCW0GQR1XS
HH MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHv5O4xKSzVyPUCuNFgxODlizszN M1zSWHNCVkeHUh?=
KU812 M331VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfPNFVKSzVyPUCuNFgxPDNizszN M33idnNCVkeHUh?=
DU-4475 M2q5Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TJT2lEPTB;MD6wPFA1PyEQvF2= MV3TRW5ITVJ?
CTV-1 NV\EUFNKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTBwMEi2OFEh|ryP MX;TRW5ITVJ?
BV-173 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTBwMEmwOlEh|ryP MnLOV2FPT0WU
ES5 NHjqPJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTBwMEmzOUDPxE1? M{HMNXNCVkeHUh?=
G-402 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vtcGlEPTB;MD6wPVk5KM7:TR?= M4DCe3NCVkeHUh?=
MV-4-11 Mmm3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTBwMUCzOFch|ryP M13sVnNCVkeHUh?=
NB69 M4XGPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzUTWM2OD1yLkGzOUDPxE1? MYHTRW5ITVJ?
EGI-1 NF;SeI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{j0PWlEPTB;MD6xN|U{OSEQvF2= NGnqUXRUSU6JRWK=
EW-18 NH\aeGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTBwMUSwO|Mh|ryP MVnTRW5ITVJ?
ME-180 NEThR|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPPTWM2OD1yLkG0OlgyKM7:TR?= MonhV2FPT0WU
D-283MED NGGweIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzoflBKSzVyPUCuNVQ4OjNizszN MlK2V2FPT0WU
NB14 M4qxXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fDS2lEPTB;MD6xOlQ1PyEQvF2= NF\u[|JUSU6JRWK=
Ramos-2G6-4C10 Mk\oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrEVmFZUUN3ME2wMlE3QTh|IN88US=> MXzTRW5ITVJ?
NBsusSR MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7pVXpKSzVyPUCuNVcxOTlizszN NGG2[lNUSU6JRWK=
LAMA-84 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LFc2lEPTB;MD6xPFA{OiEQvF2= M3nYenNCVkeHUh?=
NCI-H1581 NFvyVVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGizU|ZKSzVyPUCuNVg6PjZizszN MYLTRW5ITVJ?
A204 NF3GR5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTBwMUi5O{DPxE1? NH2xRoJUSU6JRWK=
A549 NXj5[XZ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jIdWlEPTB;MD6xPVU2KM7:TR?= M{O3[HNCVkeHUh?=
CAL-51 NXHId2VHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;TNGlEPTB;MD6xPVY2OSEQvF2= M4jWT3NCVkeHUh?=
NKM-1 M{fMXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTBwMkCwNlkh|ryP NVHF[2tNW0GQR1XS
LoVo MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTBwMkCyNFIh|ryP MYLTRW5ITVJ?
HAL-01 NH7nSHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPPSHI3UUN3ME2wMlIxOjl5IN88US=> MUHTRW5ITVJ?
HCC2218 M37lfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M330N2lEPTB;MD6yNFY5QCEQvF2= MnjlV2FPT0WU
BEN NV\JSJlqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXuZXNKSzVyPUCuNlEzQTNizszN NWrhUXZDW0GQR1XS
LC-2-ad M2rhVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\Be5djUUN3ME2wMlIzODh2IN88US=> NYixZWJDW0GQR1XS
LXF-289 NEGwe5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTBwMkWwOFEh|ryP MV7TRW5ITVJ?
HGC-27 NUTQ[HBHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjhT4ZZUUN3ME2wMlI3PDF2IN88US=> MX\TRW5ITVJ?
LK-2 NIPUVWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTkXXdKSzVyPUCuNlY5OjRizszN NGTYWXVUSU6JRWK=
CTB-1 NYHF[3JjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTBwMkeyNVUh|ryP MnjZV2FPT0WU
697 NVnyd|JlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jjVGlEPTB;MD6yO|M3PyEQvF2= MnvpV2FPT0WU
ES7 M{\We2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPqTWM2OD1yLkK3N|g{KM7:TR?= NUHMNVFyW0GQR1XS
MG-63 NXfFVIlXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTBwMke0NFch|ryP NYSzUXhsW0GQR1XS
T47D MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXriSoVUUUN3ME2wMlI4PDd3IN88US=> MVjTRW5ITVJ?
RPMI-8226 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTBwMki1PFkh|ryP MlHJV2FPT0WU
NCI-H292 MlHlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\6RVhKSzVyPUCuNlkyPjRizszN NVfvfllxW0GQR1XS
HT MlnrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXtW4xKSzVyPUCuNlk{QCEQvF2= M3XGS3NCVkeHUh?=
A3-KAW MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTBwMkm3OEDPxE1? NGDFS49USU6JRWK=
LB2241-RCC M4P0bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHLWFRKSzVyPUCuN|AyQThizszN NWnUelR[W0GQR1XS
BB65-RCC Mn;tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTBwM{C4NFUh|ryP NEPGVIdUSU6JRWK=
G-401 Moj6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULQRXFvUUN3ME2wMlMxQTh4IN88US=> NXzmOXRWW0GQR1XS
TYK-nu MkPqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDxTWM2OD1yLkOxPFY1KM7:TR?= NX7QTZR5W0GQR1XS
NCI-SNU-1 NYDIOGdxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLlUVlKSzVyPUCuN|I{OzFizszN NV[1UItqW0GQR1XS
CHL-1 NVLNW48yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzhN|RKSzVyPUCuN|I4ODNizszN M3fPbHNCVkeHUh?=
P30-OHK NIq1SINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHRTWM2OD1yLkOyO|A2KM7:TR?= MUXTRW5ITVJ?
PA-1 MkD2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTBwM{O2NVkh|ryP MYTTRW5ITVJ?
LB1047-RCC M2\1XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\zTWM2OD1yLkO0NFQ4KM7:TR?= NGP5dHhUSU6JRWK=
EM-2 NGSzVINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGX6UFBKSzVyPUCuN|QyQDhizszN NYLZWFVrW0GQR1XS
VA-ES-BJ NF65eY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFP4WZhKSzVyPUCuN|QzPjhizszN M{nWWnNCVkeHUh?=
NCI-H520 NGm3UHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37zUmlEPTB;MD6zOFg{PCEQvF2= M4\pdHNCVkeHUh?=
ECC10 Mn61S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\ZVGdNUUN3ME2wMlM2ODN3IN88US=> NHLMdWxUSU6JRWK=
LNCaP-Clone-FGC NWXjd4J3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vVemlEPTB;MD6zOVMyPCEQvF2= NYjsVHZlW0GQR1XS
ES8 NGjk[WVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTBwM{[1OVMh|ryP MX7TRW5ITVJ?
HuO-3N1 MmLRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvidHJKSzVyPUCuN|g{PzlizszN MXjTRW5ITVJ?
L-363 NVTDSmJpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTqeZMzUUN3ME2wMlM6ODJ4IN88US=> NVvRRVl2W0GQR1XS
SK-LU-1 NVrBNplTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XtNWlEPTB;MD6zPVIxQCEQvF2= M{TxXXNCVkeHUh?=
MCF7 Ml3qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEX4cpRKSzVyPUCuOFA2OyEQvF2= M4P1NXNCVkeHUh?=
HuO9 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3hTFFKSzVyPUCuOFA3PjdizszN NUWxT3hvW0GQR1XS
BHT-101 MoXCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojpTWM2OD1yLkSwO|g4KM7:TR?= M2rSSnNCVkeHUh?=
MZ2-MEL NYXBZ|RyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TWW2lEPTB;MD60NFg5OiEQvF2= NI\xNnVUSU6JRWK=
NOS-1 NWPITlVUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLTcGFKSzVyPUCuOFExPzRizszN NHjRd|ZUSU6JRWK=
NEC8 MmTXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYm0NodsUUN3ME2wMlQyPjl3IN88US=> NULQfIx[W0GQR1XS
COR-L88 Mkj0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTBwNEKyOlch|ryP NXjmVlhzW0GQR1XS
MFM-223 MlvKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTBwNEK2NVch|ryP NX\PUVc3W0GQR1XS
HSC-3 M374dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTBwNEK5NFgh|ryP MmDOV2FPT0WU
OVCAR-5 NFXaR2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPTV5pxUUN3ME2wMlQzQTN|IN88US=> MnHHV2FPT0WU
MFE-280 MnvFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1n1OWlEPTB;MD60N|A{OiEQvF2= NXfm[JRMW0GQR1XS
KP-N-YS NE\lb4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTBwNEOwO{DPxE1? M4r5U3NCVkeHUh?=
EPLC-272H MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV34O2NyUUN3ME2wMlQ{ODd5IN88US=> MnLWV2FPT0WU
KE-37 M4fNbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPXTWM2OD1yLkSzNlQ4KM7:TR?= NGriWlFUSU6JRWK=
HuH-7 MmPWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPFTWM2OD1yLkSzN|czKM7:TR?= MVHTRW5ITVJ?
CHP-212 MkXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mly4TWM2OD1yLkSzOlk4KM7:TR?= M3voUnNCVkeHUh?=
SK-MES-1 NWPWc29ET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvIbVJKSzVyPUCuOFM5PDhizszN M{fHRnNCVkeHUh?=
SJSA-1 M3jaN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4KzXmlEPTB;MD60OFU2PCEQvF2= NXvEXJNKW0GQR1XS
QIMR-WIL M4XEVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWH1cYRIUUN3ME2wMlQ2OTVizszN NGHT[ZhUSU6JRWK=
ES4 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrtWWhKSzVyPUCuOFU{OzZizszN NFLvdXdUSU6JRWK=
TI-73 NI\jbYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTBwNEW2PFYh|ryP M4jZUXNCVkeHUh?=
COLO-684 NYLkTII6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jmcWlEPTB;MD60OVczPiEQvF2= MkPpV2FPT0WU
GCIY M4XmNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mny3TWM2OD1yLkS1O|U1KM7:TR?= MmnrV2FPT0WU
JVM-3 NXfxVW9YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTBwNE[yPVIh|ryP NYLMeIhSW0GQR1XS
MPP-89 NXThWlEyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfxTWM2OD1yLkS2PVQ4KM7:TR?= NUfqb244W0GQR1XS
M14 NUDTTFU4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\pTWM2OD1yLkS3NVch|ryP M4LjfHNCVkeHUh?=
SW962 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\XTWM2OD1yLkS3NVkh|ryP NUHob|d6W0GQR1XS
VM-CUB-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PDZWlEPTB;MD60O|I5PiEQvF2= NFjhbIFUSU6JRWK=
A101D NFjKb2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXx[GdTUUN3ME2wMlQ5QTZ6IN88US=> MVjTRW5ITVJ?
DB NGXqV2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHBOZQzUUN3ME2wMlUxODJzIN88US=> NHnJV4tUSU6JRWK=
KNS-62 NVnIPYZIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnzRo57UUN3ME2wMlUxPTZ6IN88US=> NG\VXXFUSU6JRWK=
NCI-H460 NXfmOW1rT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYT3PZZzUUN3ME2wMlUxPTl5IN88US=> MmjtV2FPT0WU
MDA-MB-361 M2TTSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnVTWM2OD1yLkWwPFch|ryP M37BXXNCVkeHUh?=
DOK MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTBwNUGzN|Mh|ryP NGjuPFBUSU6JRWK=
CAL-39 Mk[4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnu[ZNyUUN3ME2wMlUzOjZ6IN88US=> NU\re412W0GQR1XS
HT-1080 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTBwNUK1OFMh|ryP NX;nVJVOW0GQR1XS
GR-ST MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17sUWlEPTB;MD61N|AyPSEQvF2= M2rkZ3NCVkeHUh?=
J-RT3-T3-5 M4W5XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXoWWNLUUN3ME2wMlU{OTl3IN88US=> MkHYV2FPT0WU
NCI-H1793 NIHiSopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTBwNUO0OFch|ryP M1fTenNCVkeHUh?=
NCI-H1355 NHTlOXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDCeVJKSzVyPUCuOVM5PzhizszN MnroV2FPT0WU
YH-13 NX\vZoRWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TzO2lEPTB;MD61OFk{QCEQvF2= MXfTRW5ITVJ?
LOXIMVI NELob2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M336UmlEPTB;MD61OVEzOyEQvF2= MX3TRW5ITVJ?
ES1 M3zORWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLrWpB6UUN3ME2wMlU2PTF6IN88US=> MWrTRW5ITVJ?
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BT-12 NH[zO5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTJ2Lkegcm0> NGG0[JczOTN|N{[3PS=>
CHLA-266 MoC3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vnRWlEPTB;MT6xJI5O NX\NbItYOjF|M{e2O|k>
TC-71 NWDncI84T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWS3Z2x6UUN3ME20Ok42KG6P MlnsNlE{Ozd4N{m=
CHLA-9 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF[5bpBKSzVyPUG1MlMhdk1? M2qzd|IyOzN5Nke5
CHLA-10 M17GO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\3TWM2OD1|Lkmgcm0> M2LRW|IyOzN5Nke5
CHLA-258 NX3hepVMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HtUmlEPTB;MUCuOEBvVQ>? NVXzfnZPOjF|M{e2O|k>
GBM2 M3TYZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjITWM2OD12MD63JI5O NGjVPYYzOTN|N{[3PS=>
NB-1643 NELZPJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLXTWM2OD1|Mz64JI5O MYWyNVM{PzZ5OR?=
NB-EBc1 NFL1bFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4P4cWlEPTB;MkeuNUBvVQ>? Ml60NlE{Ozd4N{m=
CHLA-90 NIjCXWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\FSVZKSzVyPUO0MlUhdk1? MVmyNVM{PzZ5OR?=
CHLA-136 NUnW[mV7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzZXW5vUUN3ME2xOlIvPiCwTR?= M2HrcFIyOzN5Nke5
NALM-6 M3q0bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rlSWlEPTB;M{KuPUBvVQ>? Ml;YNlE{Ozd4N{m=
COG-LL-317 NEfhbXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1P3T2lEPTB;MT6zJI5O M4fXblIyOzN5Nke5
RS4;11 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDibJRIUUN3ME2zOUBvVQ>? NF\Qc|gzOTN|N{[3PS=>
MOLT-4 M3PY[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF20U4RKSzVyPUiuOkBvVQ>? M4fKNVIyOzN5Nke5
CCRF-CEM MlHpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13JVGlEPTB;ND6xJI5O NWX5ZnhwOjF|M{e2O|k>
Kasumi-1 MlvZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTFwNDDuUS=> NV7jOGlSOjF|M{e2O|k>
Karpas-299 NV7CdY5{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHyOVY6UUN3ME2yNU44KG6P M2nBNVIyOzN5Nke5
Ramos-RA1 NVzw[5h1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\oTmlEPTB;OD6yJI5O M{\DSlIyOzN5Nke5
H838 NGTRO2RHfW6ldHnvckBCe3OjeR?= MXuxJO69VQ>? Mn;6OFghcA>? NXPIdXlScW6mdXPld{Bk\WyuIHH1eI9xcGGpeR?= MnTBNlA{PjRzMUO=
H838 NF3NXYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnFOXJbOC1|IN88US=> NGHoT284OiCq MmDubY5lfWOnczDndo94fGhiaX7obYJqfGmxbjDhcoQh[XW2b4DoZYd6 Mn;wNlAxOjh6NUS=
A549  NIHrcFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HuSFAuOyEQvF2= MU[3NkBp NXn2O5gycW6mdXPld{Boem:5dHigbY5pcWKrdHnvckBidmRiYYX0c5Bp[We7 NFrwfo8zODB{OEi1OC=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-mTOR / p-AKT / p-4EBP1 / p-P70S6K / p-PRAS40; 

PubMed: 24457069     


Western blots of 70% confluent TamR (A) and MCF7-X (B) cells treated for 15 minutes to 24 hours with AZD8055 (0 to 100 nM). Blots were probed with phospho- and total antibodies for mTORC1 and two signalling pathways. In both cell lines mTORC1 and mTORC2 s䲧疝Ỵ疞㧀疜膉痘 瘿삨ՂᾰƌՂĀ 㺣痖帉痖Ѐ瑖堘𢡄빢᎒ՂĀ鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙

p-EGFR / EGFR; 

PubMed: 25654224     


PANC-1 cells were treated with AZD8055 for the indicated hours and EGFR (T/P), AKT (T/P) and ribosomal protein S6 (S6) (T/P) proteins were examined by western-blot;

p-FOXO1 / FOXO1 / p-FOXO3a / FOXO3a ; 

PubMed: 25654224     


PANC-1 cells were transfected with FoxO1/FoxO3a siRNAs and treated with AZD8055 for 1 h, then AKT (T/P), FoxO1 (T/P), FoxO3a (T/P) and EGFR (T/P) proteins were examined by western-blot.

24457069 25654224
Immunofluorescence
p-4EBP1 / EIF4E / mTOR; 

PubMed: 24600487     


(C) Hoechst 33258 staining of Hep-2 cells after treatment with AZD8055 for 24 hours were shown. The cells were fixed and immunereacted with anti-mTOR antibody followed by incubation with Alexa 488-labeled secondary antibody (C-F). Images were taken by a c䲧疝Ỵ疞㧀疜膉痘 瘿삨ՂᾰƌՂĀ 㺣痖帉痖Ѐ瑖堘𢡄빢᎒ՂĀ鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤瘯Ɖ�෋䐺痖暼瘿�෋ᾰƌ �෋à㺣痖�෋€𢡄�෋€䀷痗�෋౴�෋㵶痗�෋뺖᎒泌Itemセ᎒Count﫨呂�෋猴፲�෋፲씢痗猸፲髸莤䥷堙᎒セ᎒�堞ﻮ᎒፲露𢡄堚،齃礤v�堞ﻮ᎒猢Wセ᎒䨼Ą鹿齃殺獸W戀醙玛W戀ⶰ໯齃礤v 玚W玢Wⶰ໯﫰礌vtЉᔈැ鲬౴᥊疜犈፲Eo狜፲艘ᎂ艘ᎂ⩈̎䥠̌씢痗狠፲붖᎒i變ﱘ﫰﬐먙堘붖᎒狠፲i變ﱘ﫰먰堘ﱘ붖᎒�堞봆᎒릎堘붖᎒i꣩쯟巰痗ꣵ쯟巰痗Љ镴౴￿￿嶴痗Љ镨౴ᔈැ竗ᔈැ屷痗W竗尊痗

LC3B / p62 ; 

PubMed: 30337536     


Immunofluorescence staining of U87 and U251 GICs, which treated by DMSO, AZD8055 (0.3 μM) and rapamycin (3 μM). The nuclei were stained with DAPI and the antibody against LC3B and p62. Images were captured by laser confocal microscope ( × 400), scale bar 䲧疝Ỵ疞

24600487 30337536
Growth inhibition assay
Cell viability ; 

PubMed: 29263324     


Growth for the indicated cell lines was assessed after 72 h of treatment with AZD8055 (0–250 nM). Results are expressed as a percentage of cell number relative to the DMSO-treated control cells a.

29263324
体内研究 AZD8055 按2.5/10 mg/kg剂量作用于U87MG和A549移植瘤抑制pS6和pAKT,导致肿瘤生长受抑制。AZD8055按10/20 mg/kg剂量处理多种移植瘤包括U87MG, BT474c, A549, Calu-3, LoVo, SW620, PC3和MES-SA时,显示出明显的抗癌活性。[1] AZD8055诱导肿瘤体积下降约40%, 伴随着AKT, S6K,和SGK蛋白激酶磷酸化的切除。用AZD8055 (5mg/kg, 每天2次) 和SAHA (100 mg/kg/每天)处理PTEN+/−LKB1+/hypo 移植瘤,导致肿瘤生长全部受抑制,且对鼠mTORC1和mTORC2信号抑制没有副作用。[4]

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

抑制mTOR的细胞为基础的测定实验:

通过高通量筛选细胞检测法,使用MDA-MB-468细胞,测定mTORC1 和mTORC2活性。用增加浓度的AZD8055处理细胞2小时。温育到最后时,细胞进行固定,冲洗,用p-Akt(S473)抗体和p-S6(S235/236)抗体探测。用激光扫描仪检测磷酸化水平。
细胞实验:[1]
- 合并
  • Cell lines: U87MG, A549,和H838 细胞
  • Concentrations: 溶解在DMSO中,作为10 mM 储备液, 0.001-1.0 μM
  • Incubation Time: 72到96小时
  • Method: 用AZD8055处理细胞72到96小时, 用0.03 mg/mL Hoechst 33342染色细胞核,用1 μg/mL 吖啶橙染色酸性小囊泡染色。通过ArrayScan II平台在450和536纳米处获得图像,测量酸性小囊泡的百分数和细胞数量。进行LC3测评,用10 μg/mL e64d/抑肽素处理细胞30 到90分钟,然后和AZD8055温育。细胞溶解在冰上,通过免疫印迹法分析。
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: U87MG, BT474c, A549, Calu-3, LoVo, SW620, PC3 and MES-SA U87-MG和A549细胞建立在无病原体,雌性裸鼠体内(nu/nu:Alpk)。
  • Dosages: 2.5-20 mg/kg
  • Administration: 口服饲喂,每天1到2次。
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 50 mg/mL warmed (107.4 mM)
Ethanol 3 mg/mL (6.44 mM)
Water Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
4% DMSO+30% PEG 300+ddH2O
5mg/mL

* 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 465.54
化学式

C25H31N5O4

CAS号 1009298-09-2
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、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

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

  • 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

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。

  • * 必填项

mTOR Signaling Pathway Map

mTOR Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID