AZD8055

For research use only.

Catalog No.S1555

198 publications

AZD8055 Chemical Structure

CAS No. 1009298-09-2

AZD8055 is a novel ATP-competitive mTOR inhibitor with IC50 of 0.8 nM in MDA-MB-468 cells with excellent selectivity (∼1,000-fold) against PI3K isoforms and ATM/DNA-PK. AZD8055 induces caspase-dependent apoptosis and also induces autophagy. Phase 1.

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Selleck's AZD8055 has been cited by 198 publications

Purity & Quality Control

Choose Selective mTOR Inhibitors

Biological Activity

Description AZD8055 is a novel ATP-competitive mTOR inhibitor with IC50 of 0.8 nM in MDA-MB-468 cells with excellent selectivity (∼1,000-fold) against PI3K isoforms and ATM/DNA-PK. AZD8055 induces caspase-dependent apoptosis and also induces autophagy. Phase 1.
Features First drug to inhibit both types of mTOR protein.
Targets
mTOR (truncated) [1]
(MDA-MB-468 cells)
mTOR (full length) [1]
(MDA-MB-468 cells)
0.13 nM 0.8 nM
In vitro

AZD8055 shows low activity (∼1,000-fold) against all PI3K isoforms (α, β, γ, δ) and other members of the PI3K-like kinase family (ATM and DNA-PK). AZD8055 inhibits the phosphorylation of mTORC1 (p70S6K and 4E-BP1) as well as phosphorylation of the mTORC2 (Akt) and downstream proteins. The rapamycin-resistant T37/46 phosphorylation sites on 4E-BP1 can be fully inhibited by AZD8055, resulting in significant inhibition of cap-dependent translation. AZD8055 potently inhibits proliferation in U87MG, A549 and H838 cells with IC50 of 53, 50 and 20 nM, respectively. AZD8055 also induces autophagy and increased LC3-II levels in H838 and A549 cells. [1] AZD8055 decreases AML blast cell proliferation and cell cycle progression, reduces the clonogenic growth of leukemic progenitors and induces caspase-dependent apoptosis in leukemic cells but not in normal immature CD34+ cells. [2] AZD8055 indicates inhibitory against the pediatric preclinical testing program (PPTP) cell lines with IC50 of 24.7 nM and induces significant differences in EFS distribution. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
LU-139 M4HXSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTBwMEKzN|Eh|ryP MoTQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVgxOTJyND:nQnNCVkeHUkyvZV4>
NCI-H720 NVPPO2lUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFuyeVJKSzVyPUCuNFI6OzhizszN Mn\XQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVgxOTJyND:nQnNCVkeHUkyvZV4>
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EW-3 MmfWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfxZVl[UUN3ME2wMlA1ODV4IN88US=> MlvkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVgxOTJyND:nQnNCVkeHUkyvZV4>
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LB2241-RCC NULEVFZHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXm3[otjUUN3ME2wMlMxOTl6IN88US=> NW\QUZU5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOThyMUKwOE8oRlODTlfFVlww[T5?
BB65-RCC MoDES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2SzbWlEPTB;MD6zNFgxPSEQvF2= M3HQflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5ODF{MESvK|5USU6JRWK8M4E,
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TYK-nu MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH:3[HBKSzVyPUCuN|E5PjRizszN MnO2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVgxOTJyND:nQnNCVkeHUkyvZV4>
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HSC-3 MoDtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4Py[WlEPTB;MD60NlkxQCEQvF2= NGm4R4E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDBzMkC0M{c,W0GQR1XSQE9iRg>?
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TI-73 M2LxZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fWemlEPTB;MD60OVY5PiEQvF2= NIHqPIw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDBzMkC0M{c,W0GQR1XSQE9iRg>?
COLO-684 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLCZZJPUUN3ME2wMlQ2PzJ4IN88US=> NWLScYV2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOThyMUKwOE8oRlODTlfFVlww[T5?
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TE-9 NV\tVHhNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjPVWllUUN3ME2xO{42OTZ4IN88US=> NVjlfpBjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOThyMUKwOE8oRlODTlfFVlww[T5?
TE-10 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXwSoxKSzVyPUG5MlA3ODdizszN MmTiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVgxOTJyND:nQnNCVkeHUkyvZV4>
COLO-824 MnfQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml6zTWM2OD1{MD65Nlc3KM7:TR?= Mn2zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVgxOTJyND:nQnNCVkeHUkyvZV4>
HuP-T3 NESxRotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\yTWM2OD1{MT6wO|Q5KM7:TR?= NFvGe2I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDBzMkC0M{c,W0GQR1XSQE9iRg>?
KALS-1 MkTtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1[xcGlEPTB;MkGuNVc2KM7:TR?= NGHrO5M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDBzMkC0M{c,W0GQR1XSQE9iRg>?
L-428 NV\k[pdQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{O3[2lEPTB;MkGuOFAyPiEQvF2= MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFAyOjB2Lze+V2FPT0WUPD;hQi=>
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DoTc2-4510 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnnc|BwUUN3ME2yN{45PDd3IN88US=> MkTrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVgxOTJyND:nQnNCVkeHUkyvZV4>
ABC-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTJ4Lke5OVch|ryP MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFAyOjB2Lze+V2FPT0WUPD;hQi=>
MHH-NB-11 NV7N[5lCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHkUpBLUUN3ME2zN{4{PDZ2IN88US=> NX;aWXJ5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOThyMUKwOE8oRlODTlfFVlww[T5?
SW1463 M3nGSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3sSYQ3UUN3ME2zN{46QDNizszN M2DzTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5ODF{MESvK|5USU6JRWK8M4E,
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NB12 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU[5eYNSUUN3ME2zPU41PjV3IN88US=> NELDRpk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDBzMkC0M{c,W0GQR1XSQE9iRg>?
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H1048 NV\4O41iSXCxcITvd4l{KEG|c3H5 NHThR4M2ODBibl2= MlO0O|IhcA>? NXTmfY1KdmijbnPld{BCSlRvMk[z5qCUcW6mdXPl[EBieG:ydH;zbZM> NHzSNFA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUezO|U1Oid-MkW3N|c2PDJ:L3G+
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MOLM13 MnzLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXEemRHOC5{IN88US=> NH\kWHI1QCCq NWfzfGVZ\W6qYX7j[ZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDpcoR2[2WmIHL5JJNmdHWvZYTpcolj MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd|OUO5N{c,OjR5M{mzPVM9N2F-
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MCF7-X  NH6yelhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTxTWM2OD1{NDDuUS=> NFW2WI89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NES1O|A3QSd-MkS0OVcxPjl:L3G+
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Huh7  MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLvS4wyPS1zMECgcm0> MUmwMVI1KGh? MVXEUXNQ NFS3RnFqdmO{ZXHz[ZMh[2WubDDk[YF1cCCrbjDhJINwdmOnboTyZZRqd25vIHHu[EB1cW2nLXTldIVv\GWwdDDtZY5v\XJ? MljGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR{OUezNFAoRjJ2Mkm3N|AxRC:jPh?=
Hep3B  MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HER|UuOTByIH7N M3ns[FAuOjRiaB?= Moe0SG1UVw>? MmXsbY5kemWjc3XzJINmdGxiZHXheIghcW5iYTDjc45k\W62cnH0bY9vNSCjbnSgeIlu\S2mZYDlcoRmdnRibXHucoVz NYPhW|VHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyPVc{ODBpPkK0Nlk4OzByPD;hQi=>
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SCC-9 MmmzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFrTcWoxNjBzLUGg{txO NV;pSZJFOTJvOU[gbC=> M{m5O4lv[3KnYYPld{Bk\WyuIHTlZZRpKGmwIHGgZ49v[2WwdILheIlwdi1iYX7kJJRqdWVvZHXw[Y5l\W62IH3hco5meg>? MlvnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzMEO3OFkoRjJ2MUCzO|Q6RC:jPh?=
Hep-2 NULqZpZKTnWwY4Tpc44hSXO|YYm= NVvudHN7OC5zL{CuOUDPxE1? MmTTNlQhcA>? M2W1[4Jtd2OtczDtWG9TSzFiYX7kJI1VV1KFMjDhZ5RqfmG2aX;u M4jmNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MUCzO|Q6Lz5{NEGwN|c1QTxxYU6=
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PANC-1 MVjBdI9xfG:|aYOgRZN{[Xl? NV;hemdqPTByIH7N NWXMV|M3PDhiaB?= NH;xOnJ{\W6|aYTpfoV{KHCjbnPy[YF1cWNiY3HuZ4VzKGOnbHzzJJRwKHKjZHnveIhmemGyeR?= M4rpclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OEi2Nlk1Lz5{M{i4OlI6PDxxYU6=
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HT-29 NE\BUYdCeG:ydH;zbZMhSXO|YYm= NISzd5AyKM7:TR?= NGHjOYY4OiCq MXrheJRmdnWjdHXzJFUuTlVvaX7keYNm\CClZXzsJIRm[XSq MmnYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7NEmxNlEoRjJzOUS5NVIyRC:jPh?=
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HT-29 M33USWZ2dmO2aX;uJGF{e2G7 M1jwdVEh|ryP NGr0NVY4OiCq NEjucplqdmS3Y3XzJIF2fG:yaHHnfUB1dyClb37m[ZIh[3m2b4Dyc5Rm[3Srb36= MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTl2OUGyNUc,OjF7NEmxNlE9N2F-
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CHLA-266 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4[yWmlEPTB;MT6xJI5O NFvvRm09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUOzO|Y4QSd-MkGzN|c3Pzl:L3G+
TC-71 Ml\OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;BW5BRUUN3ME20Ok42KG6P NHn2W5I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUOzO|Y4QSd-MkGzN|c3Pzl:L3G+
CHLA-9 M3XrPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HESGlEPTB;MUWuN{BvVQ>? NEflOok9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUOzO|Y4QSd-MkGzN|c3Pzl:L3G+
CHLA-10 NX31Z4d[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfKfVN[UUN3ME2zMlkhdk1? Mk\uQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|M{e2O|koRjJzM{O3Olc6RC:jPh?=
CHLA-258 NFjFXHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXCTWM2OD1zMD60JI5O NGLVb|A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUOzO|Y4QSd-MkGzN|c3Pzl:L3G+
GBM2 Mmf0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzNTWM2OD12MD63JI5O NFHCUHg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUOzO|Y4QSd-MkGzN|c3Pzl:L3G+
NB-1643 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\3VmNbUUN3ME2zN{45KG6P M3zIcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{O3Olc6Lz5{MUOzO|Y4QTxxYU6=
NB-EBc1 M4G2O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjtTXNiUUN3ME2yO{4yKG6P NHHPcJc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUOzO|Y4QSd-MkGzN|c3Pzl:L3G+
CHLA-90 NFS2Tm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\6TWM2OD1|ND61JI5O MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN|N{[3PUc,OjF|M{e2O|k9N2F-
CHLA-136 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LjR2lEPTB;MU[yMlYhdk1? M3;uWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{O3Olc6Lz5{MUOzO|Y4QTxxYU6=
NALM-6 NYTPR4l4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHTTWM2OD1|Mj65JI5O NYnKRVVORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzN|c3PzlpPkKxN|M4Pjd7PD;hQi=>
COG-LL-317 NEjZcXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHHO4RKUUN3ME2xMlMhdk1? MkHpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|M{e2O|koRjJzM{O3Olc6RC:jPh?=
RS4;11 M1nYWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LZc2lEPTB;M{Wgcm0> M3:wcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{O3Olc6Lz5{MUOzO|Y4QTxxYU6=
MOLT-4 NFjO[YdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRThwNjDuUS=> MlGyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|M{e2O|koRjJzM{O3Olc6RC:jPh?=
CCRF-CEM NXLjU2FOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHFTWM2OD12LkGgcm0> NWLjXJYyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzN|c3PzlpPkKxN|M4Pjd7PD;hQi=>
Kasumi-1 M1[zb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXWOnRKSzVyPUGuOEBvVQ>? MkPuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|M{e2O|koRjJzM{O3Olc6RC:jPh?=
Karpas-299 MnHGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTJzLkegcm0> NFK5d|c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUOzO|Y4QSd-MkGzN|c3Pzl:L3G+
Ramos-RA1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPWTWM2OD16LkKgcm0> MmT1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|M{e2O|koRjJzM{O3Olc6RC:jPh?=
H838 NWrKUpRJTnWwY4Tpc44hSXO|YYm= NGHZRpIyKM7:TR?= M2TyWVQ5KGh? MVvpcoR2[2W|IHPlcIwh[XW2b4DoZYd6 NHTDRXU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEO2OFEyOyd-MkCzOlQyOTN:L3G+
H838 NEjRelFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFj5NoQxNTNizszN NXfJdW1oPzJiaB?= NXm1d|VMcW6mdXPld{Boem:5dHigbY5pcWKrdHnvckBidmRiYYX0c5Bp[We7 NE\nN5I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MECyPFg2PCd-MkCwNlg5PTR:L3G+
A549  NY\NZW9MT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\6NE0{KM7:TR?= MlTFO|IhcA>? M1zTNYlv\HWlZYOg[5Jwf3SqIHnubIljcXSrb36gZY5lKGG3dH;wbIFogQ>? NHXqU2Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MECyPFg2PCd-MkCwNlg5PTR:L3G+

... 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
In vivo AZD8055 inhibits the pS6 and pAkt in U87MG and A549 xenografts at 2.5/10 mg/kg, which leads to tumor growth inhibition. AZD8055 shows significant antitumor activity in many xenografts, including U87MG, BT474c, A549, Calu-3, LoVo, SW620, PC3 and MES-SA at a dose of 10/20 mg/kg. [1] AZD8055 induces ~40% reduction in tumour volume, accompanied by ablation of phosphorylation of Akt, S6K and SGK protein kinases. Administration of AZD8055 (5mg/kg, Bid) and SAHA (100 mg/kg/d) results in complete tumor growth inhibition in PTEN+/−LKB1+/hypo xenografts without side effects on mice by inhibition of mTORC1 and mTORC2 signaling. [4]

Protocol

Kinase Assay:[1]
- Collapse

Cell-based determinations of mTOR inhibition:

A high-throughput screening cell-based assay is developed using MDA-MB-468 cells to detect mTORC1 and mTORC2 activity. Cells are exposed for 2 hours to increasing concentrations of AZD8055. At the end of the incubation period, cells are fixed, washed, and probed with antibodies against S473 pAkt or against S235/236 phosphorylated S6 (pS6). Levels of phosphorylation are assessed using an Acumen laser scanning cytometer.
Cell Research:[1]
- Collapse
  • Cell lines: U87MG, A549 and H838 cells
  • Concentrations: 1 nM - 1 μM
  • Incubation Time: 72 to 96 hours
  • Method: Cells are exposed to AZD8055 for 72 to 96 hours and stained for cell nuclei (0.03 mg/mL Hoechst 33342) and acidic vesicles (1 μg/mL acridine orange). Images are captured at 450 and 536 nm on an ArrayScan II platform, and the percentage of acidic vesicles and the number of cells are quantified. For LC3 assessment, cells are exposed to e64d/pepstatin (10 μg/mL) for 30 to 90 min before incubation with AZD8055. Cells are lysed on ice and analyzed by immunoblotting.
    (Only for Reference)
Animal Research:[1]
- Collapse
  • Animal Models: U87MG, BT474c, A549, Calu-3, LoVo, SW620, PC3 and MES-SA U87-MG and A549 are established in pathogen-free, female nude mice (nu/nu:Alpk).
  • Dosages: 2.5-20 mg/kg
  • Administration: Oral gavage once or twice daily
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 50 mg/mL warmed (107.4 mM)
Ethanol 3 mg/mL (6.44 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
4% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.
5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 465.54
Formula

C25H31N5O4

CAS No. 1009298-09-2
Storage powder
in solvent
Synonyms N/A
Smiles CC1COCCN1C2=NC(=NC3=C2C=CC(=N3)C4=CC(=C(C=C4)OC)CO)N5CCOCC5C

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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Mass Concentration Volume Molecular Weight

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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