MK-2206 2HCl

Catalog No.S1078

For research use only.

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.

MK-2206 2HCl Chemical Structure

CAS No. 1032350-13-2

Selleck's MK-2206 2HCl has been cited by 1540 publications

Purity & Quality Control

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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 NHy3Nm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW[0d|RXUUN3ME20OFEvODh|IN88US=> M3XNSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
HCC38 NYXwUm5{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTRyMT61PVMh|ryP MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
NCI-H2052 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTN7OD60O|Ih|ryP NHvMZmo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
NB17 NVrZSYt5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTN7Mj61PVYh|ryP MmfEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
SBC-5 NGfUbYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\STWM2OD1|OE[uPVg2KM7:TR?= MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
K-562 NXPyTJlqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\pOGlEPTB;M{izMlM3KM7:TR?= M1;4SlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
T84 M4mxVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2f1dmlEPTB;M{e0MlcyOiEQvF2= NXL6flUyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
LU-135 M4LucWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljETWM2OD1|NkeuNFM2KM7:TR?= NYTvXINWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
TE-9 NU\hfY9[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWGxTJc4UUN3ME2zOlMvPTh7IN88US=> MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
IST-SL1 MmHjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DP[GlEPTB;M{S3MlQxOSEQvF2= M3LsOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
BE-13 NFzHT4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\GWm5KSzVyPUO0OE4yPjdizszN MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
NCI-H1993 NGHF[lRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHuxO4ZKSzVyPUO0Nk4{PjVizszN NF20NJE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
MOLT-13 MnjjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnuzTWM2OD1|NEKuN|I3KM7:TR?= NEnKRYQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
NCI-H630 NI\VcYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;LVWlEPTB;M{OyMlI6PCEQvF2= NEP5Vm89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
KP-N-YN NEe0VXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTN2MT6xNlMh|ryP NETDV5o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
C3A NUj3epFlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXNfGFKSzVyPUOxNU45ODJizszN NInXemE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
HEL Ml7zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHTUFFKSzVyPUOwPU46QDNizszN NGKxdYk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
NCI-H810 NUfFOlR4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;zXmlEPTB;M{GwMlU4KM7:TR?= M1TUfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
LU-65 NGG4[oVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjSR5AzUUN3ME2zNFQvOzJizszN MmP6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
L-428 M2C0WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTJ7Nz62NVYh|ryP MnyzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
FADU NGnH[Y1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTlUoFyUUN3ME2yPVcvPTFizszN M3rzVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
IGR-1 MoXES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\EN2lEPTB;Mkm1MlY2QSEQvF2= MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
HDLM-2 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfPVoRKSzVyPUK5OE41ODlizszN NIG0UGU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
C8166 Mn\HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TsO2lEPTB;Mke4MlUxPiEQvF2= MnjRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
TGBC11TKB NUnFN2V3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nYc2lEPTB;Mke4MlE4QCEQvF2= NYW5WW5CRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
RERF-LC-MS MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1OzdWlEPTB;Mke2MlAxPyEQvF2= MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
COLO-680N MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzLbmxiUUN3ME2yO|IvPTJ5IN88US=> NYrSfINuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
NB6 NID2enJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHLTWM2OD1{N{CuNUDPxE1? NIXGSFE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
GAK MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlKwTWM2OD1{NUOuNFAzKM7:TR?= MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
RPMI-8866 MorVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTJ2OT6yO{DPxE1? NVXpd49MRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
NCI-H2347 NG\1e2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWm4do0zUUN3ME2yOFcvPzF|IN88US=> NE\mbJk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
LS-1034 NXzBdG5zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2OxZWlEPTB;MkS2MlI3PiEQvF2= M3rRN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
SH-4 M{W0c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;pTWM2OD1{NE[uNFkh|ryP NXHLNmtMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
CCRF-CEM NF;kUYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTJ2Mz63PVUh|ryP MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
C2BBe1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4n5NGlEPTB;MkOxMlkxPSEQvF2= MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
COLO-320-HSR MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXToTIh1UUN3ME2yNVYvOTJ3IN88US=> M17Cd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
KNS-42 NWLNPGpET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnhVnk6UUN3ME2yNVYvPTd2IN88US=> M2OxOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
RCM-1 MkXCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH34V2hKSzVyPUKxOE44PjJizszN MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
DBTRG-05MG MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvBSoR{UUN3ME2yNFcvQTB7IN88US=> M2nqR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
SW982 NYfJNZMxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTJyNz65OFgh|ryP NYHhUJJkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
SW1116 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjL[|N7UUN3ME2yNFcvODd5IN88US=> MljvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
HuCCT1 M1HoZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTJyND6yNFgh|ryP NHTZeWg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
NCI-H650 NYjpd5pFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXzTWM2OD1{MEKuNVA{KM7:TR?= NHf4OpA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
COLO-678 NV\RNVJxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7EN4NDUUN3ME2yNFEvPDVizszN MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
HT-29 MnPRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHxTG5KSzVyPUKwNU4zOTJizszN NUTIU4RDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
SCC-9 MnPBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3keVZKSzVyPUG5NUDPxE1? Mk\MQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
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GR-ST NG\FbYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PtXWlEPTB;Mz6wOFYyOSEQvF2= Mlq0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
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RPMI-8226 Mn31S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fIe2lEPTB;Mj62Nlk2OyEQvF2= M1jNVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
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SBC-1 MmnVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnUdlEyUUN3ME2wMlQ1ODN3IN88US=> M4LCNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
EFM-19 NFrVR5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEezOYRKSzVyPUCuOFQxOSEQvF2= NH;2W289[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
H9 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4riemlEPTB;MD6zPFg5OyEQvF2= NWfyUFh2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
NCI-H720 NYrvSGhMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEm3WmpKSzVyPUCuN|c3PzlizszN MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
KARPAS-45 NXS2TndzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTBwM{ezNlEh|ryP MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
RS4-11 MmD5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPRTWM2OD1yLkO0OlEh|ryP MljnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
ES5 MnHuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\XPFlKSzVyPUCuN|Q1PTVizszN NV\Wb4h{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
MOLT-16 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\He4ZzUUN3ME2wMlMxOzJizszN NX6yfWtLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
HH M{Dqemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjZbI5KSzVyPUCuN|AzQDNizszN M3:5NVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
T47D MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnRZllKSzVyPUCuNlgzPSEQvF2= M4D3eVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
AsPC-1 NYjYc49jT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTBwMkKxNlIh|ryP MnezQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
MDA-MB-175-VII MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3WxfWlEPTB;MD6xN|c{QCEQvF2= MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
P12-ICHIKAWA M2PvTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\6elNWUUN3ME2wMlEyPjJizszN MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
NEC8 NHzWPWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfIR3RwUUN3ME2wMlA6PjVzIN88US=> NIfTR2g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
HONE-1 M1;rV2Z2dmO2aX;uJGF{e2G7 MmPoNVAh|ryP MknjOFghcA>? NEHrPZVFVVOR MkLGTY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dDDheEBIOQ>? NULBXIJRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzN|Y6OjVpPkK1N|M3QTJ3PD;hQi=>
CNE-2 Mo\aSpVv[3Srb36gRZN{[Xl? NFGyO4gyOCEQvF2= MkXWOFghcA>? NGXPZWNFVVOR NIDYb|dKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0JIF1KEdz NHvUXI49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOzOlkzPSd-MkWzN|Y6OjV:L3G+
HONE-1 M4rNN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYKxNEDPxE1? M3TtVFk3KGh? NX7pepdFTE2VTx?= NV\oSmNuUUN3ME2zMlM4KM7:TR?= MoDtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|M{[5NlUoRjJ3M{O2PVI2RC:jPh?=
SUNE-1 MnvTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXOXW1ZOTBizszN NXLrVY9tQTZiaB?= MkXJSG1UVw>? MYnJR|UxRTBwNUKg{txO NX\JZYxwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzN|Y6OjVpPkK1N|M3QTJ3PD;hQi=>
CNE-2 NVLXVoVLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37ud|ExKM7:TR?= MUe5OkBp NF2wdpBFVVOR NXfub2ZOUUN3ME20MlU{KM7:TR?= MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN|NkmyOUc,OjV|M{[5NlU9N2F-
CNE-1 M4Tl[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfzSpc2OTBizszN NGfsUlk6PiCq MlnOSG1UVw>? NWXUPZhYUUN3ME2yMlk3KM7:TR?= MlXFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|M{[5NlUoRjJ3M{O2PVI2RC:jPh?=
GEO M2XmTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUC1NFAhdk1? MWG3NkBp MUTEUXNQ M37xfmlvcGmkaYTzJINmdGxiZ4Lve5Rp MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV6MUKzNUc,OjR3OEGyN|E9N2F-
HepG2 cell M3nzOGFxd3C2b4Ppd{BCe3OjeR?= MnvhNlAh|ryP MYOyOEBp M3TVcmROW09? MWDJcoR2[2W|IHPlcIwh[XCxcITvd4l{ NFzYbIs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e5O|MyQSd-MkO3PVc{OTl:L3G+
HepG2 cell MmLxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1yxOVMxKM7:TR?= NV;hfJg6OjRiaB?= NEXBTGlFVVOR NE\M[WlKdmirYnn0d{Bk\WyuIHfyc5d1cA>? MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd7N{OxPUc,OjN5OUezNVk9N2F-
HepG2 cell NVP3ZW1HU2mwYYPlJGF{e2G7 MXyyNEDPxE1? NU\OWppXOjRiaB?= NXPUdVRXTE2VTx?= NGfremVFd3ewcnXneYxifGW|IITo[UBxcG:|cHjvdplt[XSrb36gc4YhSUuW NVTRcmgxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3PVc{OTlpPkKzO|k4OzF7PD;hQi=>
CEM-S M{\n[GZ2dmO2aX;uJGF{e2G7 M4HoRlTjiIoQvF2= MWS0JIg> NFLsV2VFVVOR NUT4T5d5UW6lcnXhd4V{KHSqZTDhcY92dnRib3[gZ4xm[X[nZDDMR|VCN0JuIHGge4VtdC2nc4ThZoxqe2inZDDheZRweGijZ4mgcYFzc2W{ NWjETlZjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2NVQzPDNpPkKyOlE1OjR|PD;hQi=>
CEM-R M2nhcmZ2dmO2aX;uJGF{e2G7 M4TGPFTjiIoQvF2= M133UVQhcA>? M2XSb2ROW09? NUPVV2tVUW6lcnXhd4V{KHSqZTDhcY92dnRib3[gZ4xm[X[nZDDMR|RCN0JuIHGge4VtdC2nc4ThZoxqe2inZDDheZRweGijZ4mgcYFzc2W{ M4ezNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkG0NlQ{Lz5{Mk[xOFI1OzxxYU6=
MOLT-4 NHPkXnJHfW6ldHnvckBCe3OjeR?= MofUOQKBkc7:TR?= M3Ljd|QhcA>? NELGd5ZFVVOR M1\qZWlv[3KnYYPld{B1cGViYX3veY51KG:oIHPs[YF3\WRiTFOzRU9DNCCjIIflcIwu\XO2YXLsbZNp\WRiYYX0c5Bp[We7IH3hdotmeg>? NU\KN5J5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2NVQzPDNpPkKyOlE1OjR|PD;hQi=>
MOLT-4 MnroSpVv[3Srb36gRZN{[Xl? NWHwfIt3OTBizszN NF7ZbpIzPCCq NWnMe2MzTE2VTx?= M4\LZmJtd2OtczDj[YxteyCrbjD0bIUhTzBxR{GgdIhie2Vib3[geIhmKGOnbHygZ5lkdGV? MoqxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4MUSyOFMoRjJ{NkG0NlQ{RC:jPh?=
CEM-S MVXDfZRwfG:6aXOgRZN{[Xl? MmPiNVAh|ryP MUm0PEBp MljnSG1UVw>? M1K5WWlEPTB;NT6x5qCK|ryP NEP2U2k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[xOFI1Oyd-MkK2NVQzPDN:L3G+
CEM-R MWXDfZRwfG:6aXOgRZN{[Xl? M2HlU|ExKM7:TR?= M3S0OFQ5KGh? NIXXclNFVVOR MUTJR|UxRTNwM,MAje69VQ>? NGPIbGc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[xOFI1Oyd-MkK2NVQzPDN:L3G+
MOLT-4 NV:5XnJ7S3m2b4TvfIlkKEG|c3H5 MojWNVAh|ryP MoTEOFghcA>? Mlr2SG1UVw>? M1jySGlEPTB;MT635qCK|ryP NWXtSI1xRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2NVQzPDNpPkKyOlE1OjR|PD;hQi=>
HC11 M1nTcWZ2dmO2aX;uJGF{e2G7 M1rSd|ExKM7:TR?= NUfZXm9iOjRiaB?= MoT6SG1UVw>? MlnFTY5pcWKrdIOg{tIu[2G|ZXnuJIFv\CCDRGLQJJN6dnSqZYPpdy=> MoKxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ2Mk[2NlEoRjJ{NEK2OlIyRC:jPh?=
T98G MoG3RZBweHSxc3nzJGF{e2G7 NILxZoExNjVizszN NUHYS4hXPjBiaB?= NWDOZZdqTE2VTx?= Ml33RZVodWWwdIOgZZBweHSxZ3XubYMh\W[oZXP0d{Bw\iCpZX\peIlvcWJ? NVP0Xmc5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKwOVc6OTRpPkKyNFU4QTF2PD;hQi=>
TAD2 M1XMZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml23NVAxOCEQvF2= NEe0RYw2KGR? NXz2XJBNTE2VTx?= NFfHU3NKSzVyPkGwNFAh|ryP M1fSNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzMki5NlY4Lz5{MUK4PVI3PzxxYU6=
LN229 MnrRRZBweHSxc3nzJGF{e2G7 NIXWVW8xNjVizszN NUe0[XRwPjBiaB?= M4O3cmROW09? Mo\qRZVodWWwdIOgZZBweHSxZ3XubYMh\W[oZXP0d{Bw\iCpZX\peIlvcWJ? NHewVFI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkC1O|kyPCd-MkKwOVc6OTR:L3G+
WRO NIjF[|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfWNmpPOTByMDFOwG0> NYjVV45wPSCm M4fHUGROW09? NH7YZYNKSzVyPkGwNFAh|ryP NVLBRmZ3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGyPFkzPjdpPkKxNlg6OjZ5PD;hQi=>
SW1736 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTYOpFPOTByIN88US=> M2HJPFUh\A>? MXHEUXNQ NU\6ellRUUN3ME20O{42PiEQvF2= MnTTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF{OEmyOlcoRjJzMki5NlY4RC:jPh?=
KAT18 NXzv[mdwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkSzN{DPxE1? MoflOUBl NWG2dm8yTE2VTx?= Ml7STWM2OD12Lk[yJO69VQ>? Mn;wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF{OEmyOlcoRjJzMki5NlY4RC:jPh?=
Hth74 NF7vZoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jKOVMh|ryP MYW1JIQ> MVfEUXNQ M4TyfmlEPTB;Mj6xPUDPxE1? NFnLcIw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUK4PVI3Pyd-MkGyPFkzPjd:L3G+
TPC1 cells harbored RET/PTC1 rearrangement MmS1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV6zJO69VQ>? NYrBXGhvPSCm NWrKOXBpTE2VTx?= MUTJR|UxRTBwNUmg{txO NIqxSVk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUK4PVI3Pyd-MkGyPFkzPjd:L3G+
Hth7 cells harbored NRAS (Q61R+/−) MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYmzJO69VQ>? MnHiOUBl M{LkUWROW09? NWfrVGJxUUN3ME20MlUh|ryP MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTJ6OUK2O{c,OjF{OEmyOlc9N2F-
C643 cells harbored HRAS (G13R+/−) NVuxXopRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1m0eFMh|ryP M1G4dVUh\A>? MUXEUXNQ NEXvZ3pKSzVyPUCuNlch|ryP NIPL[lI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUK4PVI3Pyd-MkGyPFkzPjd:L3G+
FTC133 cells harbored PTEN (allele deletion and R130+) M1TU[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWmzJO69VQ>? MoDVOUBl M{[0WWROW09? NVy1R3FJUUN3ME2wMlE5KM7:TR?= M3P4dVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzMki5NlY4Lz5{MUK4PVI3PzxxYU6=
K1 cells harbored PIK3CA (E542K+/+) MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWSzJO69VQ>? M1LteFUh\A>? MkWzSG1UVw>? NXO1NHlzUUN3ME2wMlUzKM7:TR?= MkXRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF{OEmyOlcoRjJzMki5NlY4RC:jPh?=
OCUT1 cells harbored PIK3CA (H1047R+/+) MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NES0NXI{KM7:TR?= MU[1JIQ> Mkn5SG1UVw>? NFK0TmpKSzVyPUCuNVQh|ryP MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTJ6OUK2O{c,OjF{OEmyOlc9N2F-
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BT-12 M1[1fmZ2dmO2aX;uJIF{e2G7 NXXm[VBueUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFLUMVEzKGOnbHzz MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
MG 63 (6-TG R) NVT4VW1[TnWwY4Tpc44h[XO|YYm= NYjVdFZweUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF3HJFY{KCh4LWTHJHIqKGOnbHzz NXT6OYJKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB1643 M2DxfmZ2dmO2aX;uJIF{e2G7 NXfOSI9[eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CNVY1OyClZXzsdy=> MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
OHS-50 NIPKOIJHfW6ldHnvckBie3OjeR?= MVnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhV0iVLUWwJINmdGy| MkHYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh41 MlfJSpVv[3Srb36gZZN{[Xl? NUn4[4hweUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLoOFEh[2WubIO= NXPJdWhORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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SJ-GBM2 M4nlPWZ2dmO2aX;uJIF{e2G7 M1XLV5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSj3HRm0zKGOnbHzz NGXwNlU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-MC NEfHdI5HfW6ldHnvckBie3OjeR?= NFuxUlJyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1OSyClZXzsdy=> NIO1NY09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB-EBc1 MXfGeY5kfGmxbjDhd5NigQ>? NYPJZXlveUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CMWVD[zFiY3XscJM> NWS0RlNzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
LAN-5 MXTGeY5kfGmxbjDhd5NigQ>? MVzxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVEGQLUWgZ4VtdHN? NVvnd4JkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh18 MV\GeY5kfGmxbjDhd5NigQ>? Ml7WdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqMUigZ4VtdHN? M3O5U|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Assay
Methods Test Index PMID
Western blot p-AKT(T308) / p-AKT(S473) / pGSK3β(S9) / pFOXO1 / pPRAS(T246) / pBAD / pS6K(T389) / p4E-BP1 22932669
Growth inhibition assay Cell viability 24665203
Immunofluorescence LC3 ; CFTR/LC3 ; HMGA2 24490764 28794469 24476133
ELISA VEGFA 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 (from reference)

Kinase Assay:

[4]

  • 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]

  • 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.

Animal Research:

[2]

  • 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

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

Chemical Information

Molecular Weight 480.39
Formula

C25H21N5O.2HCl

CAS No. 1032350-13-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CC(C1)(C2=CC=C(C=C2)C3=C(C=C4C(=N3)C=CN5C4=NNC5=O)C6=CC=CC=C6)N.Cl.Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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

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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.

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