MK-2206 2HCl

For research use only.

Catalog No.S1078

1308 publications

MK-2206 2HCl Chemical Structure

CAS No. 1032350-13-2

MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM in cell-free assays, respectively; no inhibitory activities against 250 other protein kinases observed. MK-2206 2HCl induces autophagy and apoptosis in cancer cells. Phase 2.

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Selleck's MK-2206 2HCl has been cited by 1308 publications

Purity & Quality Control

Choose Selective Akt Inhibitors

Biological Activity

Description MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM in cell-free assays, respectively; no inhibitory activities against 250 other protein kinases observed. MK-2206 2HCl induces autophagy and apoptosis in cancer cells. Phase 2.
Features The first allosteric small molecule inhibitor of Akt to enter clinical development.
Targets
Akt1 [1]
(Cell-free assay)
Akt2 [1]
(Cell-free assay)
Akt3 [1]
(Cell-free assay)
8 nM 12 nM 65 nM
In vitro

MK-2206 is an allosteric inhibitor and is activated by the pleckstrin homology domain. MK-2206 inhibits auto-phosphorylation of both Akt T308 and S473. MK-2206 also prevents Akt-mediated phosphorylation of downstream signaling molecules, including TSC2, PRAS40 and ribosomal S6 proteins. [1] MK-2206 inhibits Ras wild-type (WT) cell lines (A431, HCC827, and NCI-H292) more potently when compared to Ras-mutant cell lines (NCI-H358, NCI-H23, NCI-H1299, and Calu-6). MK-2206 also shows synergistic responses in combination with cytotoxic agents such as erlotinib or lapatinib in lung NCI-H460 or ovarian A2780 tumor cells. [2] MK-2206 or siRNA-mediated Akt inhibition strongly activates autophagy in human glioma cells. However, eukaryotic elongation factor-2 (eEF-2) silencing suppresses MK-2206-induced-autophagy, with a promotion of apoptotic cell death. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-H69 M3TpPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrNS|BqUUN3ME20OFEvODh|IN88US=> NVXNdXk1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
HCC38 NHfXSJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWe3VXc4UUN3ME20NFEvPTl|IN88US=> NWTET5dZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
NCI-H2052 NFPm[WdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTN7OD60O|Ih|ryP NH\lZVc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
NB17 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4D6fWlEPTB;M{myMlU6PiEQvF2= M3\DWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
SBC-5 M3ftdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLLTWM2OD1|OE[uPVg2KM7:TR?= NFTTVY89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
K-562 M1HN[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\GfmlEPTB;M{izMlM3KM7:TR?= NHz1fIQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
T84 NFfKSJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2Xte2lEPTB;M{e0MlcyOiEQvF2= MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
LU-135 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTN4Nz6wN|Uh|ryP M3S4R|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
TE-9 NHfCdZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTN4Mz61PFkh|ryP M4L3O|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
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BE-13 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLucFN7UUN3ME2zOFQvOTZ5IN88US=> NYi0cox1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
NCI-H1993 M1:1Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\IW4RKSzVyPUO0Nk4{PjVizszN MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
MOLT-13 NHnOXlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzSTG5KSzVyPUO0Nk4{OjZizszN MoLXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
NCI-H630 MmTkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrVTWM2OD1|M{KuNlk1KM7:TR?= NXKyUnlJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
KP-N-YN NWmzPVAzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPWTWM2OD1|NEGuNVI{KM7:TR?= NYjXb3NmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
C3A NVP2WIlYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEC3cI9KSzVyPUOxNU45ODJizszN MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
HEL NW[3dmo4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPSbW1KSzVyPUOwPU46QDNizszN NUXrXoZORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
NCI-H810 Mn:yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nycGlEPTB;M{GwMlU4KM7:TR?= M2HTeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
LU-65 MlPYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvITWM2OD1|MESuN|Ih|ryP M4G1XlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
L-428 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIH0c2ZKSzVyPUK5O{43OTZizszN NGTwXYU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
FADU NF25T4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTJ7Nz61NUDPxE1? MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
IGR-1 MoXZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTLWIFKSzVyPUK5OU43PTlizszN NHfvSHc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
HDLM-2 M2HZemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\UXFlKSzVyPUK5OE41ODlizszN NVvXWGVyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
C8166 MmPQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkT0TWM2OD1{N{iuOVA3KM7:TR?= M3qz[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
TGBC11TKB Ml[4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzFNlhKSzVyPUK3PE4yPzhizszN NITtfXA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
RERF-LC-MS M1nsNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3wdZhKSzVyPUK3Ok4xODdizszN Ml\qQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
COLO-680N NXnS[IYyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M364eWlEPTB;MkeyMlUzPyEQvF2= MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
NB6 MljES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnPTWM2OD1{N{CuNUDPxE1? MlHEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
GAK M3y2WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHZOo9sUUN3ME2yOVMvODB{IN88US=> NXPrbVRFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
RPMI-8866 MlXDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPrTWM2OD1{NEmuNlch|ryP MmDzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
NCI-H2347 NG[yW|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXBTWM2OD1{NEeuO|E{KM7:TR?= NFu0bms9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
LS-1034 M2\L[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrzTldKSzVyPUK0Ok4zPjZizszN MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
SH-4 M2XFSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmq4TWM2OD1{NE[uNFkh|ryP MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
CCRF-CEM NHTVS5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPQSWk{UUN3ME2yOFMvPzl3IN88US=> MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
C2BBe1 NFjvc2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rRR2lEPTB;MkOxMlkxPSEQvF2= NEnrRZk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
COLO-320-HSR MmfTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHu2UZpKSzVyPUKxOk4yOjVizszN NIntUoo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
KNS-42 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTJzNj61O|Qh|ryP M2HRNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
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DBTRG-05MG M{W4eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33RTmlEPTB;MkC3MlkxQSEQvF2= MlrPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
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HuCCT1 MkTsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHxfINuUUN3ME2yNFQvOjB6IN88US=> MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
NCI-H650 NF7CNJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXvTmZNUUN3ME2yNFIvOTB|IN88US=> NEPqZ4Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
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SBC-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITaSGdKSzVyPUCuOFQxOzVizszN M{HwPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
EFM-19 NXvuZZhZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPrTWM2OD1yLkS0NFEh|ryP MlHxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
H9 NEDSUpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonXTWM2OD1yLkO4PFg{KM7:TR?= MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
NCI-H720 NFOxW|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTBwM{e2O|kh|ryP NUXqXnlvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
KARPAS-45 M4C0SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTBwM{ezNlEh|ryP MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
RS4-11 NY\lNGJLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHuSI1JUUN3ME2wMlM1PjFizszN NXrvWnZURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
ES5 NVf1copMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fUT2lEPTB;MD6zOFQ2PSEQvF2= NX;QV|dFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
MOLT-16 MlvvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTEfpJKSzVyPUCuN|A{OiEQvF2= M3;2bVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
HH MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvId2lKSzVyPUCuN|AzQDNizszN NHvUTmo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
T47D NG[2UmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrqRXRKSzVyPUCuNlgzPSEQvF2= M2H3bVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
AsPC-1 NYDvN5B[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIToOo5KSzVyPUCuNlIyOjJizszN MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
MDA-MB-175-VII M4iwdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoH4TWM2OD1yLkGzO|M5KM7:TR?= NVXZPVBlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
P12-ICHIKAWA M{XDdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnOTWM2OD1yLkGxOlIh|ryP NGC4PWw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
NEC8 NVrwPVUyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTBwMEm2OVEh|ryP M{XGelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
HONE-1 Ml\SSpVv[3Srb36gRZN{[Xl? NI\lW5kyOCEQvF2= MWi0PEBp NX;TWHZtTE2VTx?= NFn2SFNKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0JIF1KEdz NV7MVFV2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzN|Y6OjVpPkK1N|M3QTJ3PD;hQi=>
CNE-2 NHHhelhHfW6ldHnvckBCe3OjeR?= M37lTFExKM7:TR?= M2LyRlQ5KGh? MmToSG1UVw>? NX2yb|VpUW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeEBifCCJMR?= M1O3VlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{O2PVI2Lz5{NUOzOlkzPTxxYU6=
HONE-1 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY[wZndwOTBizszN NWnncFZoQTZiaB?= NWLxXnpCTE2VTx?= M{Dz[2lEPTB;Mz6zO{DPxE1? NH3tV4c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOzOlkzPSd-MkWzN|Y6OjV:L3G+
SUNE-1 NXPWTpVXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF[zbHQyOCEQvF2= MVK5OkBp MXjEUXNQ MYfJR|UxRTBwNUKg{txO M1zqUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{O2PVI2Lz5{NUOzOlkzPTxxYU6=
CNE-2 M{nFTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XveVExKM7:TR?= NFP5NGw6PiCq NUG2fGhDTE2VTx?= MoPYTWM2OD12LkWzJO69VQ>? MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN|NkmyOUc,OjV|M{[5NlU9N2F-
CNE-1 NXPObJd{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGC5OIgyOCEQvF2= NHrVTIw6PiCq MWnEUXNQ NFPPNnlKSzVyPUKuPVYh|ryP MoTFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|M{[5NlUoRjJ3M{O2PVI2RC:jPh?=
GEO NXzjVYhrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLMbHV4PTByIH7N NUH1[IZMPzJiaB?= M2rMNmROW09? M1vydmlvcGmkaYTzJINmdGxiZ4Lve5Rp MoT0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3OEGyN|EoRjJ2NUixNlMyRC:jPh?=
HepG2 cell M4X2d2Fxd3C2b4Ppd{BCe3OjeR?= MnKyNlAh|ryP M1PQVlI1KGh? MUHEUXNQ NV[0SJNKUW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= NH3RbII9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e5O|MyQSd-MkO3PVc{OTl:L3G+
HepG2 cell NF;zRo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2ixdVMxKM7:TR?= MW[yOEBp MkTmSG1UVw>? NFzvSYZKdmirYnn0d{Bk\WyuIHfyc5d1cA>? MoqzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5OUezNVkoRjJ|N{m3N|E6RC:jPh?=
HepG2 cell NILGbFRMcW6jc3WgRZN{[Xl? M3juZ|IxKM7:TR?= NVjzflU1OjRiaB?= MX7EUXNQ MojUSI94dnKnZ4XsZZRmeyC2aHWgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXA>? MnviQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5OUezNVkoRjJ|N{m3N|E6RC:jPh?=
CEM-S Mn7BSpVv[3Srb36gRZN{[Xl? MX605qCK|ryP NIfweXc1KGh? MV\EUXNQ NYftZmtrUW6lcnXhd4V{KHSqZTDhcY92dnRib3[gZ4xm[X[nZDDMR|VCN0JuIHGge4VtdC2nc4ThZoxqe2inZDDheZRweGijZ4mgcYFzc2W{ NEO2Npc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[xOFI1Oyd-MkK2NVQzPDN:L3G+
CEM-R M3rwTGZ2dmO2aX;uJGF{e2G7 MVK05qCK|ryP NIPSXWc1KGh? NV3SfHQ2TE2VTx?= Mmr5TY5kemWjc3XzJJRp\SCjbX;1cpQhd2ZiY3zlZZZm\CCOQ{TBM2ItKGFid3XscE1me3SjYnzpd4hm\CCjdYTvdIhi\3libXHyb4Vz M{H4O|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkG0NlQ{Lz5{Mk[xOFI1OzxxYU6=
MOLT-4 MlviSpVv[3Srb36gRZN{[Xl? MlLSOQKBkc7:TR?= MX20JIg> MXzEUXNQ MWLJcoNz\WG|ZYOgeIhmKGGvb4XueEBw\iClbHXheoVlKEyFM1GvRkwh[SC5ZXzsMYV{fGGkbHnzbIVlKGG3dH;wbIFogSCvYYLr[ZI> M3H5OVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkG0NlQ{Lz5{Mk[xOFI1OzxxYU6=
MOLT-4 NY[1VnFZTnWwY4Tpc44hSXO|YYm= MWCxNEDPxE1? M2KySFI1KGh? NG[2WnBFVVOR MWfCcI9kc3NiY3XscJMhcW5idHjlJGcxN0dzIIDoZZNmKG:oIITo[UBk\WyuIHP5Z4xm NFPh[Xg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[xOFI1Oyd-MkK2NVQzPDN:L3G+
CEM-S M12xZ2N6fG:2b4jpZ{BCe3OjeR?= MXqxNEDPxE1? M1TVRlQ5KGh? MUXEUXNQ M{LWNmlEPTB;NT6x5qCK|ryP MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZzNEK0N{c,OjJ4MUSyOFM9N2F-
CEM-R MlT3R5l1d3SxeHnjJGF{e2G7 MlewNVAh|ryP MlHMOFghcA>? MV\EUXNQ MUPJR|UxRTNwM,MAje69VQ>? NGDBbXQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[xOFI1Oyd-MkK2NVQzPDN:L3G+
MOLT-4 NVTYS2dOS3m2b4TvfIlkKEG|c3H5 M{CxflExKM7:TR?= NWf5O|A2PDhiaB?= NGLDVYhFVVOR MYDJR|UxRTFwN,MAje69VQ>? NXzSb4VMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2NVQzPDNpPkKyOlE1OjR|PD;hQi=>
HC11 NF7oeIJHfW6ldHnvckBCe3OjeR?= MmPMNVAh|ryP M{CycVI1KGh? MoLtSG1UVw>? NGP1Z|NKdmirYnn0d{DPui2lYYPlbY4h[W6mIFHEVnAhe3mwdHjld4l{ NW\BTFZNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK0NlY3OjFpPkKyOFI3PjJzPD;hQi=>
T98G NIPyTJZCeG:ydH;zbZMhSXO|YYm= NXyzOWpoOC53IN88US=> MXO2NEBp MkToSG1UVw>? MnX3RZVodWWwdIOgZZBweHSxZ3XubYMh\W[oZXP0d{Bw\iCpZX\peIlvcWJ? MoDiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJyNUe5NVQoRjJ{MEW3PVE1RC:jPh?=
TAD2 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\NNVAxOCEQvF2= NYTrTYFpPSCm MUPEUXNQ M1jZUGlEPTB-MUCwNEDPxE1? NUjI[ZlGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGyPFkzPjdpPkKxNlg6OjZ5PD;hQi=>
LN229 MmXHRZBweHSxc3nzJGF{e2G7 NV7IeIN2OC53IN88US=> MnfoOlAhcA>? NIm3bY9FVVOR NF[4V2lCfWevZX70d{BieG:ydH;n[Y5q[yCnZn\lZ5R{KG:oIHfl[ol1cW6rYh?= NGD3WXc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkC1O|kyPCd-MkKwOVc6OTR:L3G+
WRO M1vRWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPyNVAxOCEQvF2= NHPI[pQ2KGR? MYPEUXNQ MU\JR|UxRjFyMECg{txO M{HHb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzMki5NlY4Lz5{MUK4PVI3PzxxYU6=
SW1736 NF;HXoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fFXFExOCEQvF2= MYK1JIQ> MnOySG1UVw>? NFjBOXlKSzVyPUS3MlU3KM7:TR?= MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTJ6OUK2O{c,OjF{OEmyOlc9N2F-
KAT18 NWHjOXZZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE[zUZQ{KM7:TR?= NWf0RY5kPSCm M{LQfmROW09? MXvJR|UxRTRwNkKg{txO M3;uZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzMki5NlY4Lz5{MUK4PVI3PzxxYU6=
Hth74 NHm4dHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7IZYo{KM7:TR?= Ml3vOUBl Mke4SG1UVw>? M3;1dmlEPTB;Mj6xPUDPxE1? NInhem89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUK4PVI3Pyd-MkGyPFkzPjd:L3G+
TPC1 cells harbored RET/PTC1 rearrangement NGnmd2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3vN{DPxE1? M3iz[lUh\A>? MmTwSG1UVw>? M4CzeGlEPTB;MD61PUDPxE1? M4LnSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzMki5NlY4Lz5{MUK4PVI3PzxxYU6=
Hth7 cells harbored NRAS (Q61R+/−) Mkj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\p[lA{KM7:TR?= Mke1OUBl NI\zc4RFVVOR MnryTWM2OD12LkWg{txO M1HZXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzMki5NlY4Lz5{MUK4PVI3PzxxYU6=
C643 cells harbored HRAS (G13R+/−) MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TrR|Mh|ryP MnL0OUBl M3zPdmROW09? MlfvTWM2OD1yLkK3JO69VQ>? MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTJ6OUK2O{c,OjF{OEmyOlc9N2F-
FTC133 cells harbored PTEN (allele deletion and R130+) M1u0Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1iyVFMh|ryP NEfue|k2KGR? MV;EUXNQ Mme1TWM2OD1yLkG4JO69VQ>? NGrKSpQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUK4PVI3Pyd-MkGyPFkzPjd:L3G+
K1 cells harbored PIK3CA (E542K+/+) NVTOVYV[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HuXFMh|ryP Mk\GOUBl MoHvSG1UVw>? M1PSN2lEPTB;MD61NkDPxE1? MlSwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF{OEmyOlcoRjJzMki5NlY4RC:jPh?=
OCUT1 cells harbored PIK3CA (H1047R+/+) NVLyXWdZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWizJO69VQ>? M4DHWFUh\A>? M3PtZ2ROW09? NWf6cIt2UUN3ME2wMlE1KM7:TR?= M2PwW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzMki5NlY4Lz5{MUK4PVI3PzxxYU6=
Sk-Hep1 M3rwVmN6fG:2b4jpZ{BCe3OjeR?= M1XCXlExKM7:TR?= NYfYOoV[OjRiaB?= NW\rbnZuTE2VTx?= M3jEdXNmdnOrdHn6[ZMhemW|aYP0ZY51KGOnbHzzJJRwKHSqZTDjfZRwfG:6aXOg[YZn\WO2IH;mJJNwemGoZX7pZi=> MoDIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF{MEW5NlUoRjJzMkC1PVI2RC:jPh?=
HepG2 Ml[0R5l1d3SxeHnjJGF{e2G7 NXHON3E5OTBizszN MnL0NlQhcA>? MmDYSG1UVw>? NHnsVnZU\W6|aYTpfoV{KHKnc3nzeIFvfCClZXzsd{B1dyC2aHWgZ5l1d3SxeHnjJIVn\mWldDDv[kB{d3KjZnXubYI> Mo[zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF{MEW5NlUoRjJzMkC1PVI2RC:jPh?=
A431 Mlr5T4lv[XOnIFHzd4F6 MV:1JO69VQ>? NVnZV5JTPSCq M3rkXGROW09? NHrXcodUfXCycnXzd4V{KHSqZTDzbYdv[Wyrbnegc4YhSWu2IHHu[EBGemt? M3TiPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNUexNFY6Lz5{MEW3NVA3QTxxYU6=
NCI-H292 M3frPWN6fG:2b4jpZ{BCe3OjeR?= MVGzJO69VQ>? NXv0dnRKPzJiaB?= NHfqR49FVVOR NVG0TJZHUW6qaXLpeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36= NEK5elI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEW3NVA3QSd-MkC1O|ExPjl:L3G+
HeLa M4TTR2Z2dmO2aX;uJIF{e2G7 M370SVEhcA>? NXPrTnE1UUN3MDC9JFAvODJ{ODFOwG0> NFLYU4U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUGwNFc{Oyd-MkmxNFA4OzN:L3G+
NCI-H460 M1XBfmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnHvO|IhcA>? NVL2ZW86UUN3MDC9JFUvPCEQvF2= MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyMEi2Nkc,OjR7MEC4OlI9N2F-
HCT116 MVrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NW\t[XllPzJiaB?= M{\q[2lEPTBiPTC3MlUh|ryP M{jxZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUCwPFYzLz5{NEmwNFg3OjxxYU6=
A673 NVPjeZdOTnWwY4Tpc44h[XO|YYm= MYjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>? NEHwbIc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
DAOY M36wUWZ2dmO2aX;uJIF{e2G7 NEO1V|NyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiRFHPXUBk\Wyucx?= MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Saos-2 NFnCVZNHfW6ldHnvckBie3OjeR?= M3Pt[pFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVYX;zMVIh[2WubIO= M1HlfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
BT-37 MVjGeY5kfGmxbjDhd5NigQ>? MkKwdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUO3JINmdGy| MnnQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
RD M4W0eGZ2dmO2aX;uJIF{e2G7 NXLaXZg2eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLEJINmdGy| MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-SH MXvGeY5kfGmxbjDhd5NigQ>? MkjadWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tV2gh[2WubIO= MnL5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
BT-12 NIjuSI5HfW6ldHnvckBie3OjeR?= MnrOdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUGyJINmdGy| NYHTXm5QRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
MG 63 (6-TG R) MnznSpVv[3Srb36gZZN{[Xl? MXLxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN? NWnDUHJ2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB1643 MmfTSpVv[3Srb36gZZN{[Xl? MoHKdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6EMU[0N{Bk\Wyucx?= MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
OHS-50 M1frfGZ2dmO2aX;uJIF{e2G7 MVPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhV0iVLUWwJINmdGy| MmHSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh41 NGDIWHpHfW6ldHnvckBie3OjeR?= NUTV[3g1eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLoOFEh[2WubIO= Mn[5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh30 NUHFdYtUTnWwY4Tpc44h[XO|YYm= NYTvVZRieUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLoN|Ah[2WubIO= NVu2fotDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SJ-GBM2 MVTGeY5kfGmxbjDhd5NigQ>? MlzmdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOMLVfCUVIh[2WubIO= MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-MC M2S2R2Z2dmO2aX;uJIF{e2G7 M4DjNZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMW1EKGOnbHzz MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
NB-EBc1 NGrsT5NHfW6ldHnvckBie3OjeR?= NFe0eIhyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKtSWJkOSClZXzsdy=> MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
LAN-5 Ml;PSpVv[3Srb36gZZN{[Xl? NYPZS4s3eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFzBUk02KGOnbHzz NFW1SoY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh18 MWPGeY5kfGmxbjDhd5NigQ>? NGnrWIlyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUnixPEBk\Wyucx?= MlPMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-AKT(T308) / p-AKT(S473) / pGSK3β(S9) / pFOXO1 / pPRAS(T246) / pBAD / pS6K(T389) / p4E-BP1; 

PubMed: 22932669     


ZR75-1 cells were treated with MK-2206 150 nmol/L and collected after indicated hours. Akt signaling was assessed by Western blotting. 

22932669
Growth inhibition assay
Cell viability; 

PubMed: 24665203     


(A) MK-2206 reduced the viability of anaplastic thyroid carcinoma (ATC) cells. CAL62 and KAT4 cells were treated with MK-2206 for 72 hours, followed by measurement with a cell viability assay. (B) In vitro cell viability assay of combination with MK-2206 and tyrphostin AG 1296 in KAT4 cells. 

24665203
Immunofluorescence
LC3; 

PubMed: 24490764     


Immunofluorescence staining of LC3A (green) and DAPI (blue) in M368 cells following treatment with either MK-2206, Carboplatin and Paclitaxel or the combination of all three agents for 72h.

CFTR/LC3; 

PubMed: 28794469     


Co-localisation of CFTR (red- 549nm) and LC3 (green- 488nm) in ΔF508 CFBE41o- cells treated with MK-2206 and a negative control CFBE41o- cells at 37 ℃. Nuclei were stained with DAPI (blue- 358nm). Scale bar is 10 µm.

HMGA2; 

PubMed: 24476133     


Immunofluorescent staining for HMGA2 of leiomyoma cells in control and MK-2206-treated cells was done. Cells were costained with DAPI. Immunointensity of HMGA2 expression was measured and calculated. *, P < .05; **, P < .01; ***, P < .001.

24490764 28794469 24476133
ELISA
VEGFA; 

PubMed: 29449553     


VEGF-A protein expression of conditioned medium was determined by ELISA in cervical cancer cells. The results were analyzed using one-way ANOVA. Column, mean (n = 3); bars, SD. **P < 0.01, compared with control. ##P < 0.01, compared with NF90.

29449553
In vivo MK-2206 shows 60% TGI and inhibits more than 70 % of phospho-Akt1/2 (T308 and S473) in A2780 ovarian cancer xenografts at a dose of 240 mg/kg. [1] MK-2206 exhibits significant antitumor activity in NCI-H292 xenograft in combination with erlotinib or lapatinib. [2]

Protocol

Kinase Assay:

[4]

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Akt kinases assay:

Akt kinases are assayed by a GSK-derived biotinylated peptide substrate. The extent of peptide phosphorylation is determined by Homogeneous Time Resolved Fluorescence (HTRF) using a lanthanide chelate (Lance)-coupled monoclonal antibody specific for the phosphopeptide in combination with a streptavidin-linked allophycocyanin (SA-APC) fluorophore which will bind to the biotin moiety on the peptide. When the Lance and APC are in proximity, a non-radiative energy transfer takes place from the Lance to the APC, followed by emission of light from APC at 655 nm. Working Solution: 100X protease inhibitor cocktail (PIC): 1mg/mL benzamidine, 0.5 mg/mL pepstatin, 0.5 mg/mL leupeptin, 0.5 mg/mL aprotinin; 10X assay buffer: 500 mM HEPES, pH7.5, 1% PEG, 16.6 mM EDTA, 1 mM EGTA, 1% BSA, 20 mM 9-glycerol phosphate; Quench buffer 50 mM HEPES pH 7.3, 16.6 mM EDTA, 0.1% BSA, 0.1% Triton X-100, 0.17 nM labeled monoclonal antibody, 0.0067 mg/mL SA-APC; ATP/MgCl2 working solution: 1X Assay buffer, 1 mM DTT, 1X PIC, 5% glycerol, active Akt; Peptide working solution: 1X Assay buffer, 1 mM DTT, 1X PIC, 5% glycerol, 2 TM GSK biotinylated peptide. The reaction is assembled by adding 16 µL of ATP/MgCl2 working solution to the appropriate wells. MK-2206 or vehicle (1.0 µL) is added followed by 10 µL of peptide working solution. The reaction is started by adding 13 μL of the enzyme working solution and mixing. The reaction is allowed to proceed for 50 min and then stopped by the addition of 60 µL HTRF quench buffer. The stopped reactions are incubated at room temperature for at least 30 min and then read in the instrument.
Cell Research:

[2]

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  • Cell lines: A431, HCC827, NCI-H292, NCI-H358, NCI-H23, NCI-H1299, Calu-6 and NCI-H460 cells
  • Concentrations: 0, 0.3, 1 and 3 μM
  • Incubation Time: 72 or 96 hours
  • Method:

    MK-2206 is dissolved in DMSO as a stock solution and diluted by culture media before use. Cells are seeded at a density of 2-3 × 103 in 96-well plates and incubated for 24 hours. Then MK-2206 (0, 0.3, 1 and 3 μM) is added to the cells. Cell proliferation is determined after 72 or 96 hours.


    (Only for Reference)
Animal Research:

[2]

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  • Animal Models: SK-OV-3, NCI-H292, HCC70, PC-3, and NCI-H460 models in male CD1-nude mice
  • Dosages: 120 mg/kg
  • Administration: Orally administered
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 14 mg/mL (29.14 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+40% PEG 300+5%Tween80+ 50%H2O
For best results, use promptly after mixing.
0.625 mg/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 480.39
Formula

C25H21N5O.2HCl

CAS No. 1032350-13-2
Storage powder
in solvent
Synonyms N/A
Smiles C1CC(C1)(C2=CC=C(C=C2)C3=C(C=C4C(=N3)C=CN5C4=NNC5=O)C6=CC=CC=C6)N.Cl.Cl

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% DMSO % % Tween 80 % ddH2O
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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.

Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01480154 Active not recruiting Drug: Akt Inhibitor MK2206|Drug: Hydroxychloroquine Advanced Malignant Solid Neoplasm|Stage III Cutaneous Melanoma AJCC v7|Stage III Prostate Cancer AJCC v7|Stage III Renal Cell Cancer AJCC v7|Stage IIIA Cutaneous Melanoma AJCC v7|Stage IIIB Cutaneous Melanoma AJCC v7|Stage IIIC Cutaneous Melanoma AJCC v7|Stage IV Cutaneous Melanoma AJCC v6 and v7|Stage IV Prostate Cancer AJCC v7|Stage IV Renal Cell Cancer AJCC v7 National Cancer Institute (NCI) November 23 2011 Phase 1
NCT01466868 Terminated Drug: MK2206 Diffuse Large B Cell Lymphoma Centre Leon Berard|National Cancer Institute France November 2011 Phase 2

Tech Support

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

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    What is your recommendation for preparing the solution and how would you deliver it to the mice (i.p. or gavage)?

  • Answer:

    You can resuspend MK-2206 in 15% Captisol at up to 17mg/ml. It's a suspension and is for oral gavage use only.

  • Question 2:

    I would want to know if MK-2206 could cross the blood brain barrier?

  • Answer:

    MK-2206 can cross BBB based on the following reference: https://clinicaltrials.gov/ct2/show/NCT01249105.

Akt Signaling Pathway Map

Akt Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID