AZD8055

目录号：S1555

AZD8055 Chemical Structure

Molecular Weight(MW): 465.54

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）。Phase 1。

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客户购买Selleck的此次产品后发表的文献40篇：

客户使用该产品的8个实验数据：

  • PC3-LN4 cells were treated with GSK690693 (5 uM) alone, or in combination with PP242 (2 uM) or AZD8055 (1 uM) for 24 h, and immunoblotting performed.

    Cancer Res 2013 73(11), 3402-11. AZD8055 purchased from Selleck.

    mTOR kinase inhibitor AZD8055 activates PI3K accompanied with induction of expression of EGFR, HER2, HER3 and IRS1. Serum-deprived CHO-EGFP-AKT cells were incubated with 50 nM AZD8055 for 24 hr. The EGFP signal was detected using confocal microscopy. The white arrows indicate EGFP-AKT located on cellular membrane.

    Int J Cancer 2014 135(10), 2462-74. AZD8055 purchased from Selleck.

  • HUVEC were treated with either RAD001 or AZD8055 before PA treatment. p53, GPX1, p53 acetylation, and subcellular PTEN were analyzed with corresponding antibodies. The blot is a representative of the results of three experiments. Values (mean盨D) are expressed as fold over untreated control. *p<0.05 versus their corresponding control groups in the one-way ANOVA.

    Antioxid Redox Signal 2014 20(9), 1382-95. AZD8055 purchased from Selleck.

    CSCs+24/44/ESA at 5,000 cells per well with stem cell culture media in triplicate in an ultra-low adhesion plate were treated with 5 umol/L BMS-777607, 1 umol/L AZD8055 alone, or in their different combinations. Cells were cultured for 72 hours. Cell viability was determined by the MTS assay. Percentages of polyploid cells were determined by counting 300 cells from two different regions. Results shown here were from one of two experiments with similar results.

    Mol Cancer Ther 2014 13(1), 37-48. AZD8055 purchased from Selleck.

  • mTOR, P70S6K1, 4E-BP1 and PCNA activation in the basilar artery of SAH. Top, Western blotting bands of antibodies, bottom, density of the protein band from each group. A, mTOR activation in the basilar artery demonstrated an elevated expression of mTOR on day 7 following SAH in SAH and SAH+DMSO animals. The mTOR inhibitors, Rapamycin and AZD8055 reduced the enhanced expression of mTOR (pb0.05, ANOVA). B. P70S6K1 activation. C. 4E-BP1 activation. D. PCNA activation. Rapamycin and AZD8055 significantly decreased the expression of P70S6K1, 4E-BP1 and PCNA compared with the SAH and SAH+DMSO (pb0.05, respectively; ANOVA). There was no significant difference between the two inhibitors in mTOR, P70S6K1, 4E-BP1 and PCNA expression.

    Exp Neurol 2012 233, 799-806. AZD8055 purchased from Selleck.

    Induction of TCTP expression through 5-FU or oxaliplatin is inhibited by mTOR kinase inhibitors. HCT116 cells were treated for 48 h with 5-FU or oxaliplatin at the indicated concentrations. Where indicated, AZD 8055 (100 nM) or PP242 (1 μM) were added. TCTP levels were assessed by western blotting; signals were quantified and normalised against α-tubulin as a loading control. As a readout of mTOR activity, phosphorylation of the ribosomal protein S6 at Ser 240/244 was assessed using a phospho-specific antibody. a. Representative western blots demonstrating the alteration of the levels of TCTP protein and of phospho-ribosomal protein S6, respectively, in relation to the drug concentration.

    Cell Commun Signal, 2017, 15(1):9. AZD8055 purchased from Selleck.

  • (A) HCT116 or MDA-MB-468 cells were treated with 500 nM AZD8055 for the indicated times. Cell lysates were immunoblotted with the indicated antibodies. (B) HCT116 or MDA-MB-468 cells were treated with 50 nM rapamycin. 500 nM AZD8055, 1 uM MK2206 or dimethyl sulfoxide (DMSO) as control for 12 h. Cell lysates were immunoblotted with the indicated antibodies.

    Oncotarget 2014 5(15), 6015-27. AZD8055 purchased from Selleck.

    After starved in serum-free medium for 24h , A549 cells incubated with the indicated concentrations of AZD8055 for 3h , followed by 20-minute stimolation of 100ng/ml EGF

     
     

     

    Dr. Zhang of Tianjin Medical University. AZD8055 purchased from Selleck.

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）。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 NHPhN5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPDVYlKSzVyPUCuNFI{OzFizszN MkfyV2FPT0WU
NCI-H720 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoH2TWM2OD1yLkCyPVM5KM7:TR?= NF7G[2FUSU6JRWK=
KARPAS-45 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4T3SmlEPTB;MD6wN|M4OSEQvF2= M2TPVXNCVkeHUh?=
EW-3 M1;YUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTBwMESwOVYh|ryP NVLNeVl6W0GQR1XS
SBC-1 MmfCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHUTWM2OD1yLkC0OVgyKM7:TR?= NW\ZcZE2W0GQR1XS
NCI-H209 NEjWSJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXn0[FQxUUN3ME2wMlA2PDV|IN88US=> MnOxV2FPT0WU
EoL-1-cell NX[weXF6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Moe4TWM2OD1yLkC2OVY6KM7:TR?= NYHlOlVtW0GQR1XS
H9 MlPVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjydGNKSzVyPUCuNFY3QTJizszN Mn7VV2FPT0WU
AN3-CA NH[2fmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTK[mY5UUN3ME2wMlA4QTVzIN88US=> MnP2V2FPT0WU
HH M2jhUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPaTWM2OD1yLkC4NFA6KM7:TR?= M1GzUXNCVkeHUh?=
KU812 M3PW[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7ke2hKSzVyPUCuNFgxPDNizszN NHn1T5VUSU6JRWK=
DU-4475 NVr4UIh[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTBwMEiwOFch|ryP NVrIN2xkW0GQR1XS
CTV-1 M2LNbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{L0[2lEPTB;MD6wPFY1OSEQvF2= M{HkcXNCVkeHUh?=
BV-173 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTBwMEmwOlEh|ryP MoDnV2FPT0WU
ES5 Mo\NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTTTWM2OD1yLkC5N|Uh|ryP NETicmRUSU6JRWK=
G-402 NHTnWG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Moe3TWM2OD1yLkC5PVgh|ryP NUnJSox7W0GQR1XS
MV-4-11 NXTpeHFLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7wdlVKSzVyPUCuNVA{PDdizszN MkD6V2FPT0WU
NB69 MoDWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXz3bFlTUUN3ME2wMlE{PSEQvF2= MmrZV2FPT0WU
EGI-1 NUTTdYl{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLtfGNqUUN3ME2wMlE{PTNzIN88US=> NEPyU29USU6JRWK=
EW-18 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHn4b3lKSzVyPUCuNVQxPzNizszN M17UN3NCVkeHUh?=
ME-180 NYLpc2ZVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn74TWM2OD1yLkG0OlgyKM7:TR?= M4rOc3NCVkeHUh?=
D-283MED NXL0V49QT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTBwMUS3NlMh|ryP Mmi1V2FPT0WU
NB14 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTBwMU[0OFch|ryP MX7TRW5ITVJ?
Ramos-2G6-4C10 NVvkc4NJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHkdJZKSzVyPUCuNVY6QDNizszN NHraN|BUSU6JRWK=
NBsusSR MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2K2T2lEPTB;MD6xO|AyQSEQvF2= M{DyS3NCVkeHUh?=
LAMA-84 NXzI[WNbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTBwMUiwN|Ih|ryP NIf6VotUSU6JRWK=
NCI-H1581 NGL4dJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnxWYpKSzVyPUCuNVg6PjZizszN MkfPV2FPT0WU
A204 M172bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTBwMUi5O{DPxE1? MVXTRW5ITVJ?
A549 MlP2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TaUGlEPTB;MD6xPVU2KM7:TR?= MnPWV2FPT0WU
CAL-51 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkK2TWM2OD1yLkG5OlUyKM7:TR?= M3LB[nNCVkeHUh?=
NKM-1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTBwMkCwNlkh|ryP MmrXV2FPT0WU
LoVo NHK2Z4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkX5TWM2OD1yLkKwNlAzKM7:TR?= Ml74V2FPT0WU
HAL-01 M1jJPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXPTWM2OD1yLkKwNlk4KM7:TR?= MWnTRW5ITVJ?
HCC2218 MmLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTTOWl6UUN3ME2wMlIxPjh6IN88US=> M3PMN3NCVkeHUh?=
BEN M4H5b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PP[mlEPTB;MD6yNVI6OyEQvF2= MVvTRW5ITVJ?
LC-2-ad NGPUb4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2T1UmlEPTB;MD6yNlA5PCEQvF2= NXL5VI1lW0GQR1XS
LXF-289 M1HWN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\QcmZHUUN3ME2wMlI2ODRzIN88US=> NUiwcI5WW0GQR1XS
HGC-27 MnjxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrvW3ZQUUN3ME2wMlI3PDF2IN88US=> MUTTRW5ITVJ?
LK-2 M{KxeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\iTmlEPTB;MD6yOlgzPCEQvF2= NF;YPIxUSU6JRWK=
CTB-1 NW\IZlB4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrtTWM2OD1yLkK3NlE2KM7:TR?= MYTTRW5ITVJ?
697 NHq2SmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYr2XVBvUUN3ME2wMlI4OzZ5IN88US=> M2fpSnNCVkeHUh?=
ES7 M2qyXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3Hqd2lEPTB;MD6yO|M5OyEQvF2= Mm[0V2FPT0WU
MG-63 NVvWVpdXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nscWlEPTB;MD6yO|QxPyEQvF2= MljMV2FPT0WU
T47D MnfLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrWTWM2OD1yLkK3OFc2KM7:TR?= NHvlRYJUSU6JRWK=
RPMI-8226 NXi5XlRxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTBwMki1PFkh|ryP M13rZ3NCVkeHUh?=
NCI-H292 NIDSTIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\tc29KSzVyPUCuNlkyPjRizszN MV3TRW5ITVJ?
HT M2PCRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGj4VnZKSzVyPUCuNlk{QCEQvF2= M{nl[nNCVkeHUh?=
A3-KAW MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmn0TWM2OD1yLkK5O|Qh|ryP MYHTRW5ITVJ?
LB2241-RCC Mk\1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTBwM{CxPVgh|ryP MmDGV2FPT0WU
BB65-RCC M37rWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTRN2JtUUN3ME2wMlMxQDB3IN88US=> NW\tPI1kW0GQR1XS
G-401 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrD[nNKSzVyPUCuN|A6QDZizszN M3nqSHNCVkeHUh?=
TYK-nu NUn5WHoxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH71T29KSzVyPUCuN|E5PjRizszN MlPmV2FPT0WU
NCI-SNU-1 M3LucGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknaTWM2OD1yLkOyN|MyKM7:TR?= MlTSV2FPT0WU
CHL-1 NU\IenA1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPJZVVLUUN3ME2wMlMzPzB|IN88US=> Mlz4V2FPT0WU
P30-OHK MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;iSmFsUUN3ME2wMlMzPzB3IN88US=> Mn3nV2FPT0WU
PA-1 NITUdlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4K2dGlEPTB;MD6zN|YyQSEQvF2= MoDEV2FPT0WU
LB1047-RCC NWPIflBFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vVdGlEPTB;MD6zOFA1PyEQvF2= M3nQcHNCVkeHUh?=
EM-2 NVnJSGpRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPBbmJMUUN3ME2wMlM1OTh6IN88US=> NYXn[okzW0GQR1XS
VA-ES-BJ M3XoVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTBwM{SyOlgh|ryP NYDDOI05W0GQR1XS
NCI-H520 MnjHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXj5XmREUUN3ME2wMlM1QDN2IN88US=> MmjWV2FPT0WU
ECC10 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HURmlEPTB;MD6zOVA{PSEQvF2= M2DaUnNCVkeHUh?=
LNCaP-Clone-FGC NFi4[VZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoKwTWM2OD1yLkO1N|E1KM7:TR?= NWrUTIFwW0GQR1XS
ES8 MojhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XMN2lEPTB;MD6zOlU2OyEQvF2= NFTQWJdUSU6JRWK=
HuO-3N1 MmXlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHT1XYdKSzVyPUCuN|g{PzlizszN M4LsNHNCVkeHUh?=
L-363 MkXJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTBwM{mwNlYh|ryP NIHG[mlUSU6JRWK=
SK-LU-1 Mn3FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLuSJBKSzVyPUCuN|kzODhizszN MmXjV2FPT0WU
MCF7 Mof1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTBwNEC1N{DPxE1? MXXTRW5ITVJ?
HuO9 M4[4e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTBwNEC2Olch|ryP NE\pfY5USU6JRWK=
BHT-101 MnLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTBwNEC3PFch|ryP NXfieHlTW0GQR1XS
MZ2-MEL NUfI[lBmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEP4ZWtKSzVyPUCuOFA5QDJizszN MlXhV2FPT0WU
NOS-1 NXXPU5FyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHqyPXpKSzVyPUCuOFExPzRizszN MonUV2FPT0WU
NEC8 M2TiSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjqd3lKSzVyPUCuOFE3QTVizszN NVnMSo1wW0GQR1XS
COR-L88 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVq5cFlqUUN3ME2wMlQzOjZ5IN88US=> NFfQUXVUSU6JRWK=
MFM-223 NGTGbohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkL4TWM2OD1yLkSyOlE4KM7:TR?= MXvTRW5ITVJ?
HSC-3 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHh[3RPUUN3ME2wMlQzQTB6IN88US=> NVPI[WV1W0GQR1XS
OVCAR-5 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{G2XmlEPTB;MD60Nlk{OyEQvF2= NEfqfWhUSU6JRWK=
MFE-280 M3zsOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTBwNEOwN|Ih|ryP MlH0V2FPT0WU
KP-N-YS NGPadYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTBwNEOwO{DPxE1? NGj6c3FUSU6JRWK=
EPLC-272H MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmO1TWM2OD1yLkSzNFc4KM7:TR?= Mk[wV2FPT0WU
KE-37 NHLEOnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE[0OWdKSzVyPUCuOFMzPDdizszN M37ySHNCVkeHUh?=
HuH-7 NYGzUGxIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\NeZM2UUN3ME2wMlQ{Ozd{IN88US=> NUjiVoY{W0GQR1XS
CHP-212 NHziN2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnv6TWM2OD1yLkSzOlk4KM7:TR?= NHS0[npUSU6JRWK=
SK-MES-1 MlHXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfzTWM2OD1yLkSzPFQ5KM7:TR?= NV70SHQ6W0GQR1XS
SJSA-1 Mn7VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NESxfXZKSzVyPUCuOFQ2PTRizszN MnjJV2FPT0WU
QIMR-WIL MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXSTWM2OD1yLkS1NVUh|ryP NEPkRnVUSU6JRWK=
ES4 NEfN[4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LFfGlEPTB;MD60OVM{PiEQvF2= NF\qc3JUSU6JRWK=
TI-73 M2XzU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHr2PHpKSzVyPUCuOFU3QDZizszN NVyxR|dLW0GQR1XS
COLO-684 Mk\rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\nZ2lEPTB;MD60OVczPiEQvF2= M4LqUHNCVkeHUh?=
GCIY MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTBwNEW3OVQh|ryP MWHTRW5ITVJ?
JVM-3 NEjq[m9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTBwNE[yPVIh|ryP M1K0OHNCVkeHUh?=
MPP-89 Ml\tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTBwNE[5OFch|ryP NF;HUXVUSU6JRWK=
M14 M4jNO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrnRYpKSzVyPUCuOFcyPyEQvF2= M37QfnNCVkeHUh?=
SW962 MnfXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfHXlJKSzVyPUCuOFcyQSEQvF2= M2\GWHNCVkeHUh?=
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NCI-H1573 NEe5O2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rUWWlEPTB;MD65NFIzQSEQvF2= MWPTRW5ITVJ?
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RXF393 NYrVW2xUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTBwOUK4PVch|ryP MoX5V2FPT0WU
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DMS-114 NGDYZ|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYq2RYpJUUN3ME2wMlk{Pjd5IN88US=> NUiw[5BNW0GQR1XS
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ACN MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHj2ZpRKSzVyPUCuPVQzPzdizszN NVy0U4M5W0GQR1XS
SNU-449 M1TBTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlq0TWM2OD1yLkm1PVI1KM7:TR?= MXLTRW5ITVJ?
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SW13 NEDnTlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHuVXRWUUN3ME2wMlk5Ozl{IN88US=> MUDTRW5ITVJ?
T98G NEnBfHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTFwMEGzOlQh|ryP MnTNV2FPT0WU
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NCI-H2228 NHf6[49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWq1UodJUUN3ME2xMlI4OTZ5IN88US=> MlvKV2FPT0WU
LN-405 MmrZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVS2S|hnUUN3ME2xMlI5ODJzIN88US=> MYXTRW5ITVJ?
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COR-L23 MofpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzve|VZUUN3ME2xMlM1QDR3IN88US=> NV;LXWlEW0GQR1XS
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CHP-134 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYWwcYNbUUN3ME2xMlM4QDR2IN88US=> NI\O[2ZUSU6JRWK=
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LCLC-97TM1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfhUmx3UUN3ME2xMlQyODR4IN88US=> MY\TRW5ITVJ?
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NCI-H661 M{fFV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXtTWM2OD1zLkS0O|c2KM7:TR?= MmDIV2FPT0WU
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NCI-H1299 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnVd5J[UUN3ME2xMlUxODh4IN88US=> NUP4dph5W0GQR1XS
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NCI-H23 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7ub3VkUUN3ME2xMlU2PzF2IN88US=> M2XaUHNCVkeHUh?=
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KYSE-270 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTFwNUe0NlMh|ryP MmHnV2FPT0WU
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NCI-H69 NYLkSG9iT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUm3V4Q6UUN3ME2xMlY4OzR|IN88US=> NWnOZYFvW0GQR1XS
NCI-H2126 NH;u[ZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;SUZgzUUN3ME2xMlY4Pzl5IN88US=> NV3p[mVJW0GQR1XS
RPMI-2650 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTFwNkizNVch|ryP M1zr[3NCVkeHUh?=
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LCLC-103H NVLrflhXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml71TWM2OD1|LkKzPFk1KM7:TR?= M4\Ne3NCVkeHUh?=
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UACC-257 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\GTWM2OD1|LkS2OFMyKM7:TR?= MYPTRW5ITVJ?
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NCI-H1650 NEH3W49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljTTWM2OD14LkewOVIzKM7:TR?= M2nt[nNCVkeHUh?=
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RMG2 MnjqRZBweHSxc3nzJGF{e2G7 NXzXO2Y5OS1zMECwJI5O M2DxR|czKGh? NEnWRohHSlN? NHvRfJdqdmirYnn0d{B1cGViY3XscEB3cWGkaXzpeJkh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> NHe0dJgzOzZzNU[zNS=>
HAC2 M{f4SWFxd3C2b4Ppd{BCe3OjeR?= NGDoU2oyNTFyMECgcm0> MoHnO|IhcA>? M3OzUGZDWw>? M{fPXIlvcGmkaYTzJJRp\SClZXzsJJZq[WKrbHn0fUBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NFrEZVMzOzZzNU[zNS=>
HT-29 NYLXNlBYSXCxcITvd4l{KEG|c3H5 MW[xJO69VQ>? NYW4bYsxPzJiaB?= MWTheJRmdnWjdHXzJFUuTlVvaX7keYNm\CClZXzsJIRm[XSq M{XRbVIyQTR7MUKx
DLD1 MV7BdI9xfG:|aYOgRZN{[Xl? M{LtdVEh|ryP MYK3NkBp NG\EU4tifHSnboXheIV{KDVvRmWtbY5lfWOnZDDj[YxtKGSnYYTo MWqyNVk1QTF{MR?=
HT-29 MUXGeY5kfGmxbjDBd5NigQ>? M1XrfFEh|ryP MlnrO|IhcA>? NIP3[lJqdmS3Y3XzJIF2fG:yaHHnfUB1dyClb37m[ZIh[3m2b4Dyc5Rm[3Srb36= NWnGNVhWOjF7NEmxNlE>
DLD1 MnrxSpVv[3Srb36gRZN{[Xl? NVjUe2lPOSEQvF2= NHPRWYg4OiCq M4nqNIlv\HWlZYOgZZV1d3CqYXf5JJRwKGOxbn\ldkBkgXSxcILveIVkfGmxbh?= MXqyNVk1QTF{MR?=
Rh41 M1i0XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTNyLkegcm0> MnHhNlE{Ozd4N{m=
Rh18 NF:1b2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXUWnliUUN3ME20NU41KG6P M3u2TVIyOzN5Nke5
Rh30 M4PoTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYe5cJdKUUN3ME2xOEBvVQ>? M{j0V|IyOzN5Nke5
BT-12 M3\Ubmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HhOGlEPTB;MkSuO{BvVQ>? M1PZe|IyOzN5Nke5
CHLA-266 M2LqW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzwTWM2OD1zLkGgcm0> MmjjNlE{Ozd4N{m=
TC-71 NV70T49RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFvQXY1KSzVyPUS2MlUhdk1? NUT2cFF7OjF|M{e2O|k>
CHLA-9 M1u3c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LrSGlEPTB;MUWuN{BvVQ>? NYPZS4ZOOjF|M{e2O|k>
CHLA-10 NVn1NW1ST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDXTWM2OD1|Lkmgcm0> NWDHSYV1OjF|M{e2O|k>
CHLA-258 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHFco5KSzVyPUGwMlQhdk1? Ml\zNlE{Ozd4N{m=
GBM2 NEDDU|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nRSWlEPTB;NECuO{BvVQ>? M1jGZVIyOzN5Nke5
NB-1643 M3vUXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDNTWM2OD1|Mz64JI5O M4S0[VIyOzN5Nke5
NB-EBc1 NFHGe25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDZTWM2OD1{Nz6xJI5O NWnkVlVDOjF|M{e2O|k>
CHLA-90 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTN2LkWgcm0> MmPtNlE{Ozd4N{m=
CHLA-136 NFvTXnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEftU5lKSzVyPUG2Nk43KG6P M1XCRlIyOzN5Nke5
NALM-6 M{fxdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjqfJp7UUN3ME2zNk46KG6P MY[yNVM{PzZ5OR?=
COG-LL-317 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3nvZmlEPTB;MT6zJI5O NGGzOFEzOTN|N{[3PS=>
RS4;11 NEL3WHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTN3IH7N Ml[5NlE{Ozd4N{m=
MOLT-4 M{SxbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XOV2lEPTB;OD62JI5O NVTCN4d2OjF|M{e2O|k>
CCRF-CEM MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7yTWM2OD12LkGgcm0> NVu2TmszOjF|M{e2O|k>
Kasumi-1 MlLuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWn3fmhyUUN3ME2xMlQhdk1? M1j0XFIyOzN5Nke5
Karpas-299 NXSwT|Z4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XDPWlEPTB;MkGuO{BvVQ>? NIr6NGozOTN|N{[3PS=>
Ramos-RA1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{O0WGlEPTB;OD6yJI5O M2nUWlIyOzN5Nke5
H838 MWjGeY5kfGmxbjDBd5NigQ>? MYOxJO69VQ>? MoDOOFghcA>? M335NIlv\HWlZYOgZ4VtdCCjdYTvdIhi\3l? MoTzNlA{PjRzMUO=
H838 M3Padmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjrbVZIOC1|IN88US=> MlTxO|IhcA>? MUjpcoR2[2W|IHfyc5d1cCCrbnjpZol1cW:wIHHu[EBifXSxcHjh[5k> NFTuTGkzODB{OEi1OC=>
A549  NV7me|U2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;5NE0{KM7:TR?= NWj1THBxPzJiaB?= NUfx[4YzcW6mdXPld{Boem:5dHigbY5pcWKrdHnvckBidmRiYYX0c5Bp[We7 M2\aVVIxODJ6OEW0

... Click to View More Cell Line Experimental Data
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]
+ 展开

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]
+ 展开
  • 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]
+ 展开
  • 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)。
  • Formulation: 溶解在captisol中 (CyDex, pH 3.0)，稀释到最终captisol浓度为30% (w/v)。
  • 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
稳定性 powder
in solvent
别名 N/A

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 (g) = 浓度 (mol/L) x 体积 (L) 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

临床试验信息

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01316809 Completed Glioblastoma Multiforme|Anaplastic Astrocytoma|Anaplastic Oligodendroglioma|Malignant Glioma|Brainstem Glioma National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) March 4 2011 Phase 1
NCT00999882 Completed Cancer|Advanced Hepatocellular Carcinoma AstraZeneca October 2009 Phase 1
NCT00973076 Completed Cancer|Solid Tumors|Advanced Solid Malignancies AstraZeneca August 2009 Phase 1
NCT00731263 Completed Solid Tumors AstraZeneca July 2008 Phase 1
NCT01194193 Withdrawn Cancer|Advanced Solid Tumours|Lymphomas AstraZeneca null 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。

  • * 必填项
Selleck产品目录册

mTOR Signaling Pathway Map

mTOR Inhibitors with Unique Features

相关mTOR产品

  • MHY1485 New

    MHY1485是一种有效的，细胞渗透性 mTOR 激动剂，也能有效抑制 autophagy。

  • CHIR-99021 (CT99021) New

    CHIR-99021 (CT99021)是一种GSK-3α和GSK-3β抑制剂， IC50分别为10 nM and 6.7 nM。CHIR99201对CDKs没有交叉反应性，对GSK-3β的选择性是对CDKs选择性的350倍。

  • Dorsomorphin (Compound C) New

    Dorsomorphin (Compound C)是一种有效的，可逆选择性 AMPK 抑制剂，无细胞试验中 Ki 为 109 nM，对几个结构相关的激酶，包括ZAPK，SYK，PKCθ，PKA，和 JAK3没有显著的抑制作用。 也会抑制 I型 BMP receptor 活性。

  • Rapamycin (Sirolimus)

    Rapamycin (Sirolimus)是一种特定的 mTOR 抑制剂，在 HEK293细胞中，IC50 为 ~0.1 nM。

  • Everolimus (RAD001)

    Everolimus (RAD001)是一种mTOR抑制剂，作用于FKBP12，在无细胞试验中IC50为1.6-2.4 nM。

  • Torin 1

    Torin 1是一种有效的mTORC1/2抑制剂，在无细胞试验中IC50为2 nM/10 nM；作用于mTOR比作用于PI3K选择性高1000倍。

  • Temsirolimus (CCI-779, NSC 683864)

    Temsirolimus (CCI-779, NSC 683864)是一种特定的mTOR抑制剂，在无细胞试验中IC50为1.76 μM。

  • Sapanisertib (INK 128, MLN0128,TAK-228)

    Sapanisertib (INK 128, MLN0128) 是一种有效的，选择性mTOR抑制剂，在无细胞试验中IC50为1 nM；对I型PI3K亚型的作用效果低200倍以上，与Rapamycin相比，优先抑制mTORC1/2，且对促侵袭基因敏感。Phase 1。

  • Tacrolimus (FK506)

    Tacrolimus (FK506) 是一种23元大环内酯物，通过结合到抑免蛋白FKBP12 (FK506 结合蛋白)产生新的复合物，从而降低T细胞中肽酰脯氨酰异构酶活性。

  • KU-0063794

    KU-0063794是一种有效的，高度特异性的，作用于mTORC1和mTORC2的双重mTOR抑制剂，在无细胞试验中IC50约为~10 nM；对PI3Ks没有作用。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID