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 1585 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 NFT4NlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jOW2lEPTB;NESxMlA5OyEQvF2= M3n4bVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
HCC38 NWC0cmRpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2n4UmlEPTB;NECxMlU6OyEQvF2= Mnj2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
NCI-H2052 MlPoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHG4W29KSzVyPUO5PE41PzJizszN M1;SZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
NB17 NWTlUZR6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTN7Mj61PVYh|ryP M3XPS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
SBC-5 NXzwd3pnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2f3NmlEPTB;M{i2Mlk5PSEQvF2= NYPkUGhSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
K-562 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWiyPHg6UUN3ME2zPFMvOzZizszN NVvGNWxIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
T84 NXfHXmlmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPWTWM2OD1|N{SuO|EzKM7:TR?= MoDWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
LU-135 NFPI[mhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfRTWM2OD1|NkeuNFM2KM7:TR?= NXjtV29mRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
TE-9 NYHXNnczT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mle1TWM2OD1|NkOuOVg6KM7:TR?= NGfldZQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
IST-SL1 M4fxdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7Mb45TUUN3ME2zOFcvPDBzIN88US=> M4SxNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
BE-13 M4TI[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3OwVWlEPTB;M{S0MlE3PyEQvF2= NFm3e4k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
NCI-H1993 NX\HbXRpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnyOYpKSzVyPUO0Nk4{PjVizszN NILlXJM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
MOLT-13 M2i3cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fwVGlEPTB;M{SyMlMzPiEQvF2= MmHiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
NCI-H630 MlzSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTwTWM2OD1|M{KuNlk1KM7:TR?= NVnvXIlxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
KP-N-YN MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fCUWlEPTB;M{SxMlEzOyEQvF2= M3T6PVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
C3A MkHhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXMOJZnUUN3ME2zNVEvQDB{IN88US=> MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
HEL M2\F[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3:1O2lEPTB;M{C5Mlk5OyEQvF2= NF:wUpo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
NCI-H810 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTNzMD61O{DPxE1? NU\WNWlsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
LU-65 Mo\DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGn4O4NKSzVyPUOwOE4{OiEQvF2= NGnjeYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
L-428 M1\zeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPVTWM2OD1{OUeuOlE3KM7:TR?= MoHwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
FADU NEPkOoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlSxTWM2OD1{OUeuOVEh|ryP NIfJRYQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
IGR-1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYL3SFA1UUN3ME2yPVUvPjV7IN88US=> M3PQO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
HDLM-2 M2naXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEGyUndKSzVyPUK5OE41ODlizszN NGHl[YQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
C8166 NUXo[JFjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jtZWlEPTB;Mke4MlUxPiEQvF2= NVzIXotNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
TGBC11TKB MnL2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3xT|hKSzVyPUK3PE4yPzhizszN MkC4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
RERF-LC-MS MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4Poe2lEPTB;Mke2MlAxPyEQvF2= NU\5XJI2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
COLO-680N M4HVNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLsTWM2OD1{N{KuOVI4KM7:TR?= MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
NB6 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TTO2lEPTB;MkewMlEh|ryP M4PZ[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
GAK MoHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17LNmlEPTB;MkWzMlAxOiEQvF2= MlTYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
RPMI-8866 M4jiUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTJ2OT6yO{DPxE1? MkL4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
NCI-H2347 NEDzN5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvVO|E3UUN3ME2yOFcvPzF|IN88US=> M4\2cFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
LS-1034 M1n1XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDiTWM2OD1{NE[uNlY3KM7:TR?= MoDEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
SH-4 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\lRmlEPTB;MkS2MlA6KM7:TR?= NILHPJI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
CCRF-CEM M2\UWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTuTWM2OD1{NEOuO|k2KM7:TR?= M1H3eFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
C2BBe1 M4jrd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nweWlEPTB;MkOxMlkxPSEQvF2= M134ZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
COLO-320-HSR MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPaNnBnUUN3ME2yNVYvOTJ3IN88US=> NFrIUpQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
KNS-42 Mly3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlr0TWM2OD1{MU[uOVc1KM7:TR?= M2r5NVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
RCM-1 MlnkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnjGTWM2OD1{MUSuO|YzKM7:TR?= MlKzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
DBTRG-05MG MnPpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTJyNz65NFkh|ryP NUeyNog3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
SW982 Mo\US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTJyNz65OFgh|ryP NFLvZoQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
SW1116 M4HnXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTJyNz6wO|ch|ryP NVf0UGRmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
HuCCT1 M3XxVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPm[IhKSzVyPUKwOE4zODhizszN MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
NCI-H650 MlPBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HDU2lEPTB;MkCyMlExOyEQvF2= MmP6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
COLO-678 NX7WcpRPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTJyMT60OUDPxE1? MmrLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
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SCC-9 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTYTWM2OD1zOUGg{txO NIDHRmU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
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NCI-H1304 NVjENJA6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;rOGY5UUN3ME2xOVQvPjl2IN88US=> MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
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EFM-19 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH[xcFVKSzVyPUCuOFQxOSEQvF2= M{\Jc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
H9 Mlz5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrUTWM2OD1yLkO4PFg{KM7:TR?= MoPKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
NCI-H720 NELrSWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHpOWkxUUN3ME2wMlM4Pjd7IN88US=> NYfySnJVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
KARPAS-45 MknyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M125RWlEPTB;MD6zO|MzOSEQvF2= MoLwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
RS4-11 NUPBbHhbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1fsUGlEPTB;MD6zOFYyKM7:TR?= NYTZco9IRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
ES5 NFW5O2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlS3TWM2OD1yLkO0OFU2KM7:TR?= NGrpUpE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
MOLT-16 NHPkVGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vP[WlEPTB;MD6zNFMzKM7:TR?= NXrHXXFQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
HH M{jNU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljPTWM2OD1yLkOwNlg{KM7:TR?= Mo\yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
T47D M3j4bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTBwMkiyOUDPxE1? NWS3PY1{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
AsPC-1 M{DMSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTBwMkKxNlIh|ryP NX2xPW53RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
MDA-MB-175-VII NEewOpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfUdGJKSzVyPUCuNVM4OzhizszN NV\Lb4k3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
P12-ICHIKAWA NEL2fnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlr6TWM2OD1yLkGxOlIh|ryP NG\xcI89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
NEC8 NVfGe25PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkKyTWM2OD1yLkC5OlUyKM7:TR?= NGP0b|Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
HONE-1 NIDHOFNHfW6ldHnvckBCe3OjeR?= MnqyNVAh|ryP NFXkWVM1QCCq MmjFSG1UVw>? MUTJcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2IHH0JGcy NX\Nd49yRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzN|Y6OjVpPkK1N|M3QTJ3PD;hQi=>
CNE-2 NEfWTmNHfW6ldHnvckBCe3OjeR?= NXPjUVhTOTBizszN MVu0PEBp NXHTeIdVTE2VTx?= M3;EPGlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4SgZZQhTzF? M1PobFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{O2PVI2Lz5{NUOzOlkzPTxxYU6=
HONE-1 MnPyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYWxNEDPxE1? MXe5OkBp MkPySG1UVw>? NHv6OVlKSzVyPUOuN|ch|ryP MoK1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|M{[5NlUoRjJ3M{O2PVI2RC:jPh?=
SUNE-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUOxNEDPxE1? NUfBUHNDQTZiaB?= NY[0dIdLTE2VTx?= M3j0XGlEPTB;MD61NkDPxE1? MnHlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|M{[5NlUoRjJ3M{O2PVI2RC:jPh?=
CNE-2 NGXBeWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlziNVAh|ryP Mlu5PVYhcA>? NWPHelVMTE2VTx?= MX;JR|UxRTRwNUOg{txO NWjZZYxPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzN|Y6OjVpPkK1N|M3QTJ3PD;hQi=>
CNE-1 M{C5Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXWxNEDPxE1? M1PlbFk3KGh? NUPO[YpMTE2VTx?= M1\tOWlEPTB;Mj65OkDPxE1? MmDVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|M{[5NlUoRjJ3M{O2PVI2RC:jPh?=
GEO NYjzTYZrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVziVVBFPTByIH7N NH;yUVM4OiCq NWnXeIJ5TE2VTx?= M4qy[mlvcGmkaYTzJINmdGxiZ4Lve5Rp MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV6MUKzNUc,OjR3OEGyN|E9N2F-
HepG2 cell MoHHRZBweHSxc3nzJGF{e2G7 NU\jT5F3OjBizszN M4P1ZVI1KGh? MojiSG1UVw>? NHXje2tKdmS3Y3XzJINmdGxiYYDvdJRwe2m| NHfvZnY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e5O|MyQSd-MkO3PVc{OTl:L3G+
HepG2 cell MmLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGra[GE{OCEQvF2= NFrVb|gzPCCq MXvEUXNQ NWG5dFBLUW6qaXLpeJMh[2WubDDndo94fGh? M{e1PVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{m3N|E6Lz5{M{e5O|MyQTxxYU6=
HepG2 cell MlWwT4lv[XOnIFHzd4F6 NFjRUmMzOCEQvF2= NWToSI5sOjRiaB?= M17yeWROW09? MnzySI94dnKnZ4XsZZRmeyC2aHWgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXA>? MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd7N{OxPUc,OjN5OUezNVk9N2F-
CEM-S MmnZSpVv[3Srb36gRZN{[Xl? MkPtOQKBkc7:TR?= M1jBb|QhcA>? NFPNW3lFVVOR MmWxTY5kemWjc3XzJJRp\SCjbX;1cpQhd2ZiY3zlZZZm\CCOQ{XBM2ItKGFid3XscE1me3SjYnzpd4hm\CCjdYTvdIhi\3libXHyb4Vz MoeyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4MUSyOFMoRjJ{NkG0NlQ{RC:jPh?=
CEM-R MljISpVv[3Srb36gRZN{[Xl? MlrIOQKBkc7:TR?= Mne5OEBp Mmm4SG1UVw>? NILyRppKdmO{ZXHz[ZMhfGinIHHtc5VvfCCxZjDjcIVifmWmIFzDOGEwSixiYTD3[YxtNWW|dHHicIl{cGWmIHH1eI9xcGGpeTDtZZJs\XJ? M3Hsd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkG0NlQ{Lz5{Mk[xOFI1OzxxYU6=
MOLT-4 NHr0TIxHfW6ldHnvckBCe3OjeR?= Ml7yOQKBkc7:TR?= NFW2Voc1KGh? NGHwcYNFVVOR M1r4Xmlv[3KnYYPld{B1cGViYX3veY51KG:oIHPs[YF3\WRiTFOzRU9DNCCjIIflcIwu\XO2YXLsbZNp\WRiYYX0c5Bp[We7IH3hdotmeg>? MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZzNEK0N{c,OjJ4MUSyOFM9N2F-
MOLT-4 NY[ycZdPTnWwY4Tpc44hSXO|YYm= NX[wZYJFOTBizszN MojFNlQhcA>? MUXEUXNQ MkDVRoxw[2u|IHPlcIx{KGmwIITo[UBIOC:JMTDwbIF{\SCxZjD0bIUh[2WubDDjfYNt\Q>? M1zjclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkG0NlQ{Lz5{Mk[xOFI1OzxxYU6=
CEM-S MnrKR5l1d3SxeHnjJGF{e2G7 M2LubVExKM7:TR?= NVvsTmdCPDhiaB?= NYfOdVh3TE2VTx?= M{DXcWlEPTB;NT6x5qCK|ryP NHzScm89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[xOFI1Oyd-MkK2NVQzPDN:L3G+
CEM-R MUfDfZRwfG:6aXOgRZN{[Xl? NX\pbmpMOTBizszN MoO2OFghcA>? MmrYSG1UVw>? NHO0OmZKSzVyPUOuN-KBkc7:TR?= NX:yPGxkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2NVQzPDNpPkKyOlE1OjR|PD;hQi=>
MOLT-4 MlXiR5l1d3SxeHnjJGF{e2G7 NHzpWWIyOCEQvF2= M1XqT|Q5KGh? M1XI[2ROW09? NGjoV|FKSzVyPUGuO-KBkc7:TR?= NFn6bVc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[xOFI1Oyd-MkK2NVQzPDN:L3G+
HC11 MV\GeY5kfGmxbjDBd5NigQ>? NELNd2wyOCEQvF2= Ml31NlQhcA>? MnvPSG1UVw>? NVXobVl2UW6qaXLpeJMh|rJvY3Hz[YlvKGGwZDDBSHJRKHO7boTo[ZNqew>? MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjR{Nk[yNUc,OjJ2Mk[2NlE9N2F-
T98G NIDub41CeG:ydH;zbZMhSXO|YYm= M1;xNVAvPSEQvF2= MVS2NEBp NIXXepdFVVOR NUTCU4NlSXWpbXXueJMh[XCxcITv[4VvcWNiZX\m[YN1eyCxZjDn[YZqfGmwaXK= MoDaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJyNUe5NVQoRjJ{MEW3PVE1RC:jPh?=
TAD2 NEPLd3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7GVJUyODByIN88US=> MYm1JIQ> MknrSG1UVw>? MnvWTWM2OD5zMECwJO69VQ>? MonXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF{OEmyOlcoRjJzMki5NlY4RC:jPh?=
LN229 NXi1UGRwSXCxcITvd4l{KEG|c3H5 NG\aOGYxNjVizszN MnrqOlAhcA>? NXvMOoY6TE2VTx?= MnzWRZVodWWwdIOgZZBweHSxZ3XubYMh\W[oZXP0d{Bw\iCpZX\peIlvcWJ? Mn3GQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJyNUe5NVQoRjJ{MEW3PVE1RC:jPh?=
WRO NELl[npIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XHPVExODBizszN NWL4[IJuPSCm M1ToSmROW09? MkHxTWM2OD5zMECwJO69VQ>? M1nn[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzMki5NlY4Lz5{MUK4PVI3PzxxYU6=
SW1736 NHTydYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXFT3QyODBizszN M4P4WVUh\A>? MXTEUXNQ MXvJR|UxRTR5LkW2JO69VQ>? NUWxTWtSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGyPFkzPjdpPkKxNlg6OjZ5PD;hQi=>
KAT18 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrpV4loOyEQvF2= NVTheodPPSCm MmXjSG1UVw>? NVnLVG5DUUN3ME20MlYzKM7:TR?= NX3xPYk6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGyPFkzPjdpPkKxNlg6OjZ5PD;hQi=>
Hth74 NGLDTZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmS2N{DPxE1? NGXwZnc2KGR? MXTEUXNQ NHLhN3VKSzVyPUKuNVkh|ryP NFGyeG49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUK4PVI3Pyd-MkGyPFkzPjd:L3G+
TPC1 cells harbored RET/PTC1 rearrangement NHHTW|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYSzJO69VQ>? MVG1JIQ> M1rQNmROW09? NG\odHdKSzVyPUCuOVkh|ryP M1rreVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzMki5NlY4Lz5{MUK4PVI3PzxxYU6=
Hth7 cells harbored NRAS (Q61R+/−) M3;N[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknTN{DPxE1? NG[5em42KGR? MUHEUXNQ MWDJR|UxRTRwNTFOwG0> NWTpUpU{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGyPFkzPjdpPkKxNlg6OjZ5PD;hQi=>
C643 cells harbored HRAS (G13R+/−) NHPFUpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPUVpg{KM7:TR?= NFfobIk2KGR? NWDQPG54TE2VTx?= NFn2fm5KSzVyPUCuNlch|ryP MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTJ6OUK2O{c,OjF{OEmyOlc9N2F-
FTC133 cells harbored PTEN (allele deletion and R130+) NYXVS4dRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXv4VWhnOyEQvF2= NHfrOWw2KGR? M2XScGROW09? MYHJR|UxRTBwMUig{txO NETPWIM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUK4PVI3Pyd-MkGyPFkzPjd:L3G+
K1 cells harbored PIK3CA (E542K+/+) NHrPbGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW[zJO69VQ>? M3zkNFUh\A>? MYrEUXNQ NYTENmF5UUN3ME2wMlUzKM7:TR?= NHTaVXo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUK4PVI3Pyd-MkGyPFkzPjd:L3G+
OCUT1 cells harbored PIK3CA (H1047R+/+) M{H6emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13VcFMh|ryP Ml7pOUBl MV7EUXNQ NVfBN29ZUUN3ME2wMlE1KM7:TR?= MnTKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF{OEmyOlcoRjJzMki5NlY4RC:jPh?=
Sk-Hep1 MUjDfZRwfG:6aXOgRZN{[Xl? MYCxNEDPxE1? NID2ZnkzPCCq NYi3UVJETE2VTx?= NVj4NXFnW2Wwc3n0bZpmeyC{ZYPpd5RidnRiY3XscJMhfG9idHjlJIN6fG:2b4jpZ{Bm\m[nY4Sgc4Yhe2:{YX\lcolj MofLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF{MEW5NlUoRjJzMkC1PVI2RC:jPh?=
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NCI-H292 M2HYTWN6fG:2b4jpZ{BCe3OjeR?= M4jHWFMh|ryP MVW3NkBp MmXSSG1UVw>? MoX6TY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25? Mm\rQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB3N{GwOlkoRjJyNUexNFY6RC:jPh?=
HeLa NV:xcmJbTnWwY4Tpc44h[XO|YYm= NGnFeXQyKGh? MmTqTWM2OCB;IECuNFIzQCEQvF2= MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTFyMEezN{c,OjlzMEC3N|M9N2F-
NCI-H460 M1L3[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYjBU|NKPzJiaB?= MlXOTWM2OCB;IEWuOEDPxE1? NXz2SI5IRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA5PjJpPkK0PVAxQDZ{PD;hQi=>
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Saos-2 NWH6W3hlTnWwY4Tpc44h[XO|YYm= M13Oc5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVYX;zMVIh[2WubIO= M{fs[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
BT-37 NV25W3d5TnWwY4Tpc44h[XO|YYm= NHv0NW5yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQmStN|ch[2WubIO= MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
RD NVjJRldvTnWwY4Tpc44h[XO|YYm= NEK1cVVyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUlSgZ4VtdHN? M1jSV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-SH NF3pbXZHfW6ldHnvckBie3OjeR?= MYnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3TTEBk\Wyucx?= MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
BT-12 NIH3[XdHfW6ldHnvckBie3OjeR?= MkHtdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUGyJINmdGy| MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
MG 63 (6-TG R) M4HCNmZ2dmO2aX;uJIF{e2G7 NI\VcoRyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTVegOlMhMDZvVFegVkkh[2WubIO= M3H3VVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB1643 NGjnSJRHfW6ldHnvckBie3OjeR?= NWG2dZdxeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CNVY1OyClZXzsdy=> M1n3bVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
OHS-50 MkW0SpVv[3Srb36gZZN{[Xl? Ml[zdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE:KUz21NEBk\Wyucx?= MofUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh41 MnrCSpVv[3Srb36gZZN{[Xl? NFzpXY5yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUni0NUBk\Wyucx?= NXTtdHB2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh30 NYPrUJlyTnWwY4Tpc44h[XO|YYm= Mo\idWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqM{CgZ4VtdHN? NG\2b2o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SJ-GBM2 NW\BfmVxTnWwY4Tpc44h[XO|YYm= Mle2dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOMLVfCUVIh[2WubIO= MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-MC MljFSpVv[3Srb36gZZN{[Xl? NVfUSmxueUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM> NWLRZ2ZzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB-EBc1 MlLzSpVv[3Srb36gZZN{[Xl? NVfJO201eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CMWVD[zFiY3XscJM> NVLh[3RPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
LAN-5 MVfGeY5kfGmxbjDhd5NigQ>? M1vCd5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCOQV6tOUBk\Wyucx?= NVi3NJFKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh18 M3HBd2Z2dmO2aX;uJIF{e2G7 MX3xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmhzODDj[Yxtew>? Mor3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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 HMGA2 ; CFTR/LC3 ; LC3 24476133 28794469 24490764
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

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 2022-08-01)

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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