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 1480 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 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnu3TWM2OD12NEGuNFg{KM7:TR?= M3i3OFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
HCC38 NGjHPIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XrcmlEPTB;NECxMlU6OyEQvF2= NEHaPGU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
NCI-H2052 M{DaNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHxeo4{UUN3ME2zPVgvPDd{IN88US=> M{PLelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
NB17 M{mzR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\RXZVKSzVyPUO5Nk42QTZizszN NGjRZpE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
SBC-5 M{LhUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlT2TWM2OD1|OE[uPVg2KM7:TR?= MkfBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
K-562 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTN6Mz6zOkDPxE1? MoTuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
T84 NXrqV4hqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDsZVNKSzVyPUO3OE44OTJizszN MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
LU-135 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDueYxKSzVyPUO2O{4xOzVizszN NHHrRpM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
TE-9 NWTN[nk1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTN4Mz61PFkh|ryP MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
IST-SL1 MoHaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XHc2lEPTB;M{S3MlQxOSEQvF2= NWfCWFV3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
BE-13 Mo[0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjhPFF3UUN3ME2zOFQvOTZ5IN88US=> NHrafIg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
NCI-H1993 MmrPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTsTWM2OD1|NEKuN|Y2KM7:TR?= NHW0WG49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
MOLT-13 M3TPS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTN2Mj6zNlYh|ryP M1XyXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
NCI-H630 NUXpVoE1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTN|Mj6yPVQh|ryP NVjt[GJORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
KP-N-YN M1TNTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTN2MT6xNlMh|ryP MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
C3A MnnsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFfwTHJKSzVyPUOxNU45ODJizszN NH;3O2Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
HEL NUnOdG1nT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1v2dGlEPTB;M{C5Mlk5OyEQvF2= MmnLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
NCI-H810 M3PFWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVe4SnM{UUN3ME2zNVAvPTdizszN Mo\SQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
LU-65 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzPb2pEUUN3ME2zNFQvOzJizszN M1K1eVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
L-428 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGOzSJNKSzVyPUK5O{43OTZizszN NHLaT5M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
FADU NUDBPYZYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTJ7Nz61NUDPxE1? NYrabJR2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
IGR-1 M1j5R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHpTWM2OD1{OUWuOlU6KM7:TR?= M1fxPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
HDLM-2 M3nvUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInpbIlKSzVyPUK5OE41ODlizszN NYTvc4lkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
C8166 NUjKc4ROT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTJ5OD61NFYh|ryP NV31c|R4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
TGBC11TKB NXnSZ4xET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HRemlEPTB;Mke4MlE4QCEQvF2= MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
RERF-LC-MS MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlS4TWM2OD1{N{[uNFA4KM7:TR?= MlrpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
COLO-680N M4XUPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTJ5Mj61Nlch|ryP MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
NB6 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHSV29PUUN3ME2yO|AvOSEQvF2= NV;R[3lMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
GAK NYPEUJpUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTJ3Mz6wNFIh|ryP MnXpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
RPMI-8866 MnLSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3z2UGlEPTB;MkS5MlI4KM7:TR?= NH;xWoE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
NCI-H2347 NUfVOWRiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rNT2lEPTB;MkS3MlcyOyEQvF2= M1LFXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
LS-1034 NF7GbFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTJ2Nj6yOlYh|ryP NHLjOFE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
SH-4 MoHsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTJ2Nj6wPUDPxE1? NXflOWhVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
CCRF-CEM NEG5b|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml31TWM2OD1{NEOuO|k2KM7:TR?= NUC4T2pZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
C2BBe1 NFvBcVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHwU5JKSzVyPUKzNU46ODVizszN M1;rT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
COLO-320-HSR NXHYOHJ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTJzNj6xNlUh|ryP NVn3[nRZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
KNS-42 MnP1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vTSGlEPTB;MkG2MlU4PCEQvF2= MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
RCM-1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTJzND63OlIh|ryP MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
DBTRG-05MG MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TlWmlEPTB;MkC3MlkxQSEQvF2= Mm\0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
SW982 NYPTdnp[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXm1flE4UUN3ME2yNFcvQTR6IN88US=> NETpXIs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
SW1116 NEP1b3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIP6VG5KSzVyPUKwO{4xPzdizszN M4\rfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
HuCCT1 M2Todmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWW5ZmNnUUN3ME2yNFQvOjB6IN88US=> NFLWVYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
NCI-H650 Mkj5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTJyMj6xNFMh|ryP MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
COLO-678 NGDUOIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;KR2lEPTB;MkCxMlQ2KM7:TR?= M17RXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
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NCI-H720 NH3KeIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{[3fWlEPTB;MD6zO|Y4QSEQvF2= NVnIWGl4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
KARPAS-45 NWK5SY5qT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLSTWM2OD1yLkO3N|IyKM7:TR?= M1z1OVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
RS4-11 NYnWSm5zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTBwM{S2NUDPxE1? MmLiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
ES5 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\HTosxUUN3ME2wMlM1PDV3IN88US=> MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
MOLT-16 M4HyU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTBwM{CzNkDPxE1? MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
HH MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\Lb4drUUN3ME2wMlMxOjh|IN88US=> M4GxTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
T47D NWK5bWlrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTBwMkiyOUDPxE1? MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
AsPC-1 M37GZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTBwMkKxNlIh|ryP M1[1NlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
MDA-MB-175-VII NETi[XJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnz[pZxUUN3ME2wMlE{PzN6IN88US=> NYDXbYlmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
P12-ICHIKAWA M4exfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGWxdY9KSzVyPUCuNVE3OiEQvF2= NVjSUG9IRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
NEC8 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVv4c3RrUUN3ME2wMlA6PjVzIN88US=> M4DWO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
HONE-1 MnLGSpVv[3Srb36gRZN{[Xl? NYTxZm1lOTBizszN M3nnelQ5KGh? M1TYR2ROW09? NETUdXhKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0JIF1KEdz M3vPPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{O2PVI2Lz5{NUOzOlkzPTxxYU6=
CNE-2 M33XU2Z2dmO2aX;uJGF{e2G7 MYOxNEDPxE1? NUT2cnVGPDhiaB?= NFTBWotFVVOR NHf5NlJKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0JIF1KEdz MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN|NkmyOUc,OjV|M{[5NlU9N2F-
HONE-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjnRXZWOTBizszN M{LhU|k3KGh? MYXEUXNQ Mnj1TWM2OD1|LkO3JO69VQ>? NF\6flg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOzOlkzPSd-MkWzN|Y6OjV:L3G+
SUNE-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPVT41SOTBizszN MoPCPVYhcA>? NGjVZZhFVVOR MXPJR|UxRTBwNUKg{txO MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN|NkmyOUc,OjV|M{[5NlU9N2F-
CNE-2 M{LV[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXvdlFqOTBizszN NWPTUmtvQTZiaB?= MX3EUXNQ M4rBZmlEPTB;ND61N{DPxE1? M3;kbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{O2PVI2Lz5{NUOzOlkzPTxxYU6=
CNE-1 MoK2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PuclExKM7:TR?= MYS5OkBp MYLEUXNQ NHPnVGFKSzVyPUKuPVYh|ryP NWfEWJA6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzN|Y6OjVpPkK1N|M3QTJ3PD;hQi=>
GEO MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjndpN5PTByIH7N MoHoO|IhcA>? M1XrT2ROW09? MWfJcohq[mm2czDj[YxtKGe{b4f0bC=> NULQXGZ{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1PFEzOzFpPkK0OVgyOjNzPD;hQi=>
HepG2 cell MVzBdI9xfG:|aYOgRZN{[Xl? M1P0V|IxKM7:TR?= NY\MOoRzOjRiaB?= NEHpPWlFVVOR M{Luc2lv\HWlZYOgZ4VtdCCjcH;weI9{cXN? MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd7N{OxPUc,OjN5OUezNVk9N2F-
HepG2 cell NUjNOHJuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37PNVMxKM7:TR?= M1vhNVI1KGh? NFrk[YNFVVOR NUfjd|JjUW6qaXLpeJMh[2WubDDndo94fGh? NVLyeJd5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3PVc{OTlpPkKzO|k4OzF7PD;hQi=>
HepG2 cell NF31TlBMcW6jc3WgRZN{[Xl? MVeyNEDPxE1? MnOzNlQhcA>? NIXCU2xFVVOR Mn7vSI94dnKnZ4XsZZRmeyC2aHWgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXA>? NV;heZlERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3PVc{OTlpPkKzO|k4OzF7PD;hQi=>
CEM-S MXHGeY5kfGmxbjDBd5NigQ>? MUm05qCK|ryP NUL5Xmt3PCCq NYnOd3JVTE2VTx?= NWLkUWdZUW6lcnXhd4V{KHSqZTDhcY92dnRib3[gZ4xm[X[nZDDMR|VCN0JuIHGge4VtdC2nc4ThZoxqe2inZDDheZRweGijZ4mgcYFzc2W{ MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZzNEK0N{c,OjJ4MUSyOFM9N2F-
CEM-R NGHFfoZHfW6ldHnvckBCe3OjeR?= MoT6OQKBkc7:TR?= NXy4fXRuPCCq NW[3S49pTE2VTx?= NVzrXXNVUW6lcnXhd4V{KHSqZTDhcY92dnRib3[gZ4xm[X[nZDDMR|RCN0JuIHGge4VtdC2nc4ThZoxqe2inZDDheZRweGijZ4mgcYFzc2W{ NW\icYVXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2NVQzPDNpPkKyOlE1OjR|PD;hQi=>
MOLT-4 NH\Vb3dHfW6ldHnvckBCe3OjeR?= NXLnUnd4POLCid88US=> NF3ESms1KGh? MkTsSG1UVw>? MXrJcoNz\WG|ZYOgeIhmKGGvb4XueEBw\iClbHXheoVlKEyFM1GvRkwh[SC5ZXzsMYV{fGGkbHnzbIVlKGG3dH;wbIFogSCvYYLr[ZI> MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZzNEK0N{c,OjJ4MUSyOFM9N2F-
MOLT-4 MX\GeY5kfGmxbjDBd5NigQ>? NXXNTHViOTBizszN NHPBd5czPCCq NGf0VnFFVVOR MmnjRoxw[2u|IHPlcIx{KGmwIITo[UBIOC:JMTDwbIF{\SCxZjD0bIUh[2WubDDjfYNt\Q>? M2D2c|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkG0NlQ{Lz5{Mk[xOFI1OzxxYU6=
CEM-S M2LxNWN6fG:2b4jpZ{BCe3OjeR?= MVyxNEDPxE1? NYmxXmF1PDhiaB?= MnH3SG1UVw>? MUTJR|UxRTVwMfMAje69VQ>? MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZzNEK0N{c,OjJ4MUSyOFM9N2F-
CEM-R NVWzVmliS3m2b4TvfIlkKEG|c3H5 NF;ubmsyOCEQvF2= M4TsNVQ5KGh? NIPNUIpFVVOR MlrrTWM2OD1|LkRihKnPxE1? M2rmSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkG0NlQ{Lz5{Mk[xOFI1OzxxYU6=
MOLT-4 NV;ubWpJS3m2b4TvfIlkKEG|c3H5 NXHLTndNOTBizszN M3LiTlQ5KGh? M1i0R2ROW09? NGO1boxKSzVyPUGuO-KBkc7:TR?= NEm0TZU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[xOFI1Oyd-MkK2NVQzPDN:L3G+
HC11 NIjjXWJHfW6ldHnvckBCe3OjeR?= MnH6NVAh|ryP M2DGTVI1KGh? NGL3fWlFVVOR Ml;5TY5pcWKrdIOg{tIu[2G|ZXnuJIFv\CCDRGLQJJN6dnSqZYPpdy=> M2\zflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NEK2OlIyLz5{MkSyOlYzOTxxYU6=
T98G MVHBdI9xfG:|aYOgRZN{[Xl? NFXjO5UxNjVizszN Mn\JOlAhcA>? M2nHT2ROW09? NXXndpJoSXWpbXXueJMh[XCxcITv[4VvcWNiZX\m[YN1eyCxZjDn[YZqfGmwaXK= MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjB3N{mxOEc,OjJyNUe5NVQ9N2F-
TAD2 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLqepoyODByIN88US=> MlewOUBl NVX3ZYJCTE2VTx?= MUXJR|UxRjFyMECg{txO M1vDNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzMki5NlY4Lz5{MUK4PVI3PzxxYU6=
LN229 NE\1bXJCeG:ydH;zbZMhSXO|YYm= NFPo[HIxNjVizszN M{jRd|YxKGh? NYP6cGNyTE2VTx?= NEO0ZmlCfWevZX70d{BieG:ydH;n[Y5q[yCnZn\lZ5R{KG:oIHfl[ol1cW6rYh?= MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjB3N{mxOEc,OjJyNUe5NVQ9N2F-
WRO MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV2xNFAxKM7:TR?= NWLQUGxvPSCm NE\vT2NFVVOR NFv0XXNKSzVyPkGwNFAh|ryP NGS5fYo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUK4PVI3Pyd-MkGyPFkzPjd:L3G+
SW1736 Mmj3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrSO3U{OTByIN88US=> M4L4XFUh\A>? NHfmNlJFVVOR M{PhdGlEPTB;NEeuOVYh|ryP NF;BenY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUK4PVI3Pyd-MkGyPFkzPjd:L3G+
KAT18 NYDqfZhST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn[3N{DPxE1? NIXQR3M2KGR? M1TyN2ROW09? MojkTWM2OD12Lk[yJO69VQ>? M2TuS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzMki5NlY4Lz5{MUK4PVI3PzxxYU6=
Hth74 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXuzJO69VQ>? MVm1JIQ> MXzEUXNQ MlTXTWM2OD1{LkG5JO69VQ>? NV\CXldsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGyPFkzPjdpPkKxNlg6OjZ5PD;hQi=>
TPC1 cells harbored RET/PTC1 rearrangement MliyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXUSVA{KM7:TR?= MVG1JIQ> NYLuWoVMTE2VTx?= NIPKZmJKSzVyPUCuOVkh|ryP NHTNXFg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUK4PVI3Pyd-MkGyPFkzPjd:L3G+
Hth7 cells harbored NRAS (Q61R+/−) MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrXPGc{KM7:TR?= NHfXNpY2KGR? NEjKWXJFVVOR NIjQW2FKSzVyPUSuOUDPxE1? MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTJ6OUK2O{c,OjF{OEmyOlc9N2F-
C643 cells harbored HRAS (G13R+/−) Mkm1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETEfmk{KM7:TR?= M{\DT|Uh\A>? MXrEUXNQ MmH2TWM2OD1yLkK3JO69VQ>? NX\hTZRpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGyPFkzPjdpPkKxNlg6OjZ5PD;hQi=>
FTC133 cells harbored PTEN (allele deletion and R130+) MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInRbHQ{KM7:TR?= MYO1JIQ> NXHWUmIyTE2VTx?= NHjyTHhKSzVyPUCuNVgh|ryP M3X1fFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzMki5NlY4Lz5{MUK4PVI3PzxxYU6=
K1 cells harbored PIK3CA (E542K+/+) NY[2Tlc1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;sbVMh|ryP MnW4OUBl NES4U|FFVVOR NFfhdmxKSzVyPUCuOVIh|ryP MonjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF{OEmyOlcoRjJzMki5NlY4RC:jPh?=
OCUT1 cells harbored PIK3CA (H1047R+/+) MkDUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPNS4c5OyEQvF2= MVK1JIQ> NV7KV2c5TE2VTx?= NGS4XplKSzVyPUCuNVQh|ryP NF;kdGI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUK4PVI3Pyd-MkGyPFkzPjd:L3G+
Sk-Hep1 M3;EUGN6fG:2b4jpZ{BCe3OjeR?= MlHCNVAh|ryP NGjhSYIzPCCq NUfN[41nTE2VTx?= NXP3VIRbW2Wwc3n0bZpmeyC{ZYPpd5RidnRiY3XscJMhfG9idHjlJIN6fG:2b4jpZ{Bm\m[nY4Sgc4Yhe2:{YX\lcolj NH\IPGc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUKwOVkzPSd-MkGyNFU6OjV:L3G+
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HeLa MYDGeY5kfGmxbjDhd5NigQ>? M36wblEhcA>? NH;QRlZKSzVyIE2gNE4xOjJ6IN88US=> NEX0N3I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUGwNFc{Oyd-MkmxNFA4OzN:L3G+
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MG 63 (6-TG R) MlPHSpVv[3Srb36gZZN{[Xl? NGH1e4xyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTVegOlMhMDZvVFegVkkh[2WubIO= MoO1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
NB1643 MXvGeY5kfGmxbjDhd5NigQ>? M1riSZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQkG2OFMh[2WubIO= NEXKOGM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
OHS-50 NVnKTWtFTnWwY4Tpc44h[XO|YYm= M3vmcJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCRSGOtOVAh[2WubIO= Mln3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh41 M{P5VmZ2dmO2aX;uJIF{e2G7 M{DVNZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCUaESxJINmdGy| NUTaNml2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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SJ-GBM2 M4jRemZ2dmO2aX;uJIF{e2G7 MorQdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOMLVfCUVIh[2WubIO= NXTjOlY2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC M2GwNGZ2dmO2aX;uJIF{e2G7 NYDIXY04eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM> M1HwbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB-EBc1 NHPkOWFHfW6ldHnvckBie3OjeR?= M3jXPJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQj3FRoMyKGOnbHzz M{jUdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
LAN-5 NGizSIFHfW6ldHnvckBie3OjeR?= M1vSRpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCOQV6tOUBk\Wyucx?= MlnzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh18 NEO4dm9HfW6ldHnvckBie3OjeR?= Mnj2dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqMUigZ4VtdHN? M{ThTFxiKHSjcnfleF0oZ2KuYX7rK{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.

  • (Only for Reference)
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
  • (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 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 2021-09-06)

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.

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