MK-2206 2HCl

For research use only.

Catalog No.S1078

1218 publications

MK-2206 2HCl Chemical Structure

CAS No. 1032350-13-2

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

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Selleck's MK-2206 2HCl has been cited by 1218 publications

Purity & Quality Control

Choose Selective Akt Inhibitors

Biological Activity

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

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

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-H69 M{nx[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnSenp1UUN3ME20OFEvODh|IN88US=> MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
HCC38 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDYeZFKSzVyPUSwNU42QTNizszN M2DMdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
NCI-H2052 M2CzW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoL3TWM2OD1|OUiuOFczKM7:TR?= NGrzXoY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
NB17 M1PGUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmf1TWM2OD1|OUKuOVk3KM7:TR?= NFHpU449[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
SBC-5 M2fGNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LKeGlEPTB;M{i2Mlk5PSEQvF2= M{G5SVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
K-562 M3zYPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTN6Mz6zOkDPxE1? MlTwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
T84 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTN5ND63NVIh|ryP MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
LU-135 NGjMOnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\KUopKSzVyPUO2O{4xOzVizszN MmHZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
TE-9 NXHmVZF7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDWTWM2OD1|NkOuOVg6KM7:TR?= Mke1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
IST-SL1 NUf2N4NuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPENm1KSzVyPUO0O{41ODFizszN M37QRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
BE-13 NEPOUYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHqV2pKSzVyPUO0OE4yPjdizszN NHG2coE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
NCI-H1993 NHHBNGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPWTWM2OD1|NEKuN|Y2KM7:TR?= MoDiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
MOLT-13 M2HjbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXzTWM2OD1|NEKuN|I3KM7:TR?= M1n5dFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
NCI-H630 M3\xSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1Pqe2lEPTB;M{OyMlI6PCEQvF2= M33qelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
KP-N-YN NX;uZ4Q2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTN2MT6xNlMh|ryP M1z5PVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
C3A M1zN[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnyOY8{UUN3ME2zNVEvQDB{IN88US=> NGL1cJk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
HEL MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlL3TWM2OD1|MEmuPVg{KM7:TR?= MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
NCI-H810 M2HGS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjqPHJKSzVyPUOxNE42PyEQvF2= NILqR4Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
LU-65 NX\ydmF1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1v6[GlEPTB;M{C0MlMzKM7:TR?= MljvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
L-428 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1K4TWlEPTB;Mkm3MlYyPiEQvF2= MojPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
FADU NYn4c|RET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvnR5FKSzVyPUK5O{42OSEQvF2= M3jRN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
IGR-1 NHLGc3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTJ7NT62OVkh|ryP M17uc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
HDLM-2 M2HZTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\aTWM2OD1{OUSuOFA6KM7:TR?= MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
C8166 M3G4b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzt[W1KSzVyPUK3PE42ODZizszN MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
TGBC11TKB NF7yZWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLtTWM2OD1{N{iuNVc5KM7:TR?= M1;UdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
RERF-LC-MS M3vqUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfFRpVKSzVyPUK3Ok4xODdizszN MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
COLO-680N M2jyeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PYUWlEPTB;MkeyMlUzPyEQvF2= NHTBUYk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
NB6 M3HSPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGD4UpdKSzVyPUK3NE4yKM7:TR?= M{HmUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
GAK MmniS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTJ3Mz6wNFIh|ryP NVzPcFJ1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
RPMI-8866 NHXrdlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fVU2lEPTB;MkS5MlI4KM7:TR?= MlL2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
NCI-H2347 MmC4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\5VGlEPTB;MkS3MlcyOyEQvF2= NY[2d40zRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
LS-1034 NUj5SJBqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37DXGlEPTB;MkS2MlI3PiEQvF2= NEK5SYw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
SH-4 NFrK[JNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoOyTWM2OD1{NE[uNFkh|ryP NX;3eWRVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
CCRF-CEM NHTIPWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\ZUoZGUUN3ME2yOFMvPzl3IN88US=> NITSSoQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
C2BBe1 Ml3aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrHR|NiUUN3ME2yN|EvQTB3IN88US=> NUXseZg1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
COLO-320-HSR NEDMdI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\mTWM2OD1{MU[uNVI2KM7:TR?= MlnqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
KNS-42 NHW0XGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXQTWM2OD1{MU[uOVc1KM7:TR?= MmLJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
RCM-1 M3zKc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vCW2lEPTB;MkG0Mlc3OiEQvF2= NGjPV|Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
DBTRG-05MG MmTFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37aVGlEPTB;MkC3MlkxQSEQvF2= Ml3sQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
SW982 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLwTWM2OD1{MEeuPVQ5KM7:TR?= M3e0bVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
SW1116 NEDndWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\qTG1yUUN3ME2yNFcvODd5IN88US=> MmflQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
HuCCT1 NIrUemhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHhTWM2OD1{MESuNlA5KM7:TR?= MkPjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
NCI-H650 M1rtd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjrfnlKSzVyPUKwNk4yODNizszN MnnlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
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BALL-1 NUPCcItGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTF{Nj6yN{DPxE1? MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
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A4-Fuk MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfjfYFrUUN3ME2wMlQ3QDZ6IN88US=> Ml;NQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
SBC-1 NVHveGJPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTXb5RKSzVyPUCuOFQxOzVizszN M1LNclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
EFM-19 NFr0OVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTBwNESwNUDPxE1? M{D0T|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
H9 MkiyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHn4OY1KSzVyPUCuN|g5QDNizszN M4fublxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
NCI-H720 NVix[pd3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jNV2lEPTB;MD6zO|Y4QSEQvF2= MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
KARPAS-45 MoHZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHuTWM2OD1yLkO3N|IyKM7:TR?= NVHHZ3poRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
RS4-11 M4TCcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPOdVRiUUN3ME2wMlM1PjFizszN NYjPeFVMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
ES5 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTmU5RKSzVyPUCuN|Q1PTVizszN NGO1fIM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
MOLT-16 MmDIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTBwM{CzNkDPxE1? M1XZSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
HH MoLOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonKTWM2OD1yLkOwNlg{KM7:TR?= NIfYfmo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
T47D NFLmV2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDUTWM2OD1yLkK4NlUh|ryP NYnFcHU3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB5OUG3OU8oRlODTlfFVlww[T5?
AsPC-1 NVLuPWdWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnZSFFrUUN3ME2wMlIzOTJ{IN88US=> NIr5bZk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd7MUe1M{c,W0GQR1XSQE9iRg>?
MDA-MB-175-VII MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;DTWM2OD1yLkGzO|M5KM7:TR?= M{f0TVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExPzlzN{WvK|5USU6JRWK8M4E,
P12-ICHIKAWA MnLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTBwMUG2NkDPxE1? MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFc6OTd3Lze+V2FPT0WUPD;hQi=>
NEC8 MnvpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHNfmtKSzVyPUCuNFk3PTFizszN MmnyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA4QTF5NT:nQnNCVkeHUkyvZV4>
HONE-1 NV3XNGJtTnWwY4Tpc44hSXO|YYm= M13vZ|ExKM7:TR?= NYLDXIpoPDhiaB?= MlvsSG1UVw>? MXXJcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2IHH0JGcy MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN|NkmyOUc,OjV|M{[5NlU9N2F-
CNE-2 M{PWSWZ2dmO2aX;uJGF{e2G7 MYKxNEDPxE1? M4jQblQ5KGh? M4HFXmROW09? M33XN2lv\HWlZYOgZ4VtdCCleXPs[UBienKnc4SgZZQhTzF? MnLpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|M{[5NlUoRjJ3M{O2PVI2RC:jPh?=
HONE-1 NE\EcItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVOxNEDPxE1? NH:wcY46PiCq M1rlXmROW09? MlnOTWM2OD1|LkO3JO69VQ>? MoD0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|M{[5NlUoRjJ3M{O2PVI2RC:jPh?=
SUNE-1 M4HjOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLxNVAh|ryP MVS5OkBp M1fqW2ROW09? NFHWWmVKSzVyPUCuOVIh|ryP NU\0UGVoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzN|Y6OjVpPkK1N|M3QTJ3PD;hQi=>
CNE-2 M3vETWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvDOJcyOCEQvF2= MYS5OkBp M4fhUGROW09? NYS4dHdWUUN3ME20MlU{KM7:TR?= MnLNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|M{[5NlUoRjJ3M{O2PVI2RC:jPh?=
CNE-1 MkXzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DQflExKM7:TR?= NGfxVFU6PiCq MXvEUXNQ MY\JR|UxRTJwOU[g{txO NX\LdW5bRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzN|Y6OjVpPkK1N|M3QTJ3PD;hQi=>
GEO M2L3cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkW0OVAxKG6P MWi3NkBp NFvuO|dFVVOR NFzLU5FKdmirYnn0d{Bk\WyuIHfyc5d1cA>? NEDPSo49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW4NVI{OSd-MkS1PFEzOzF:L3G+
HepG2 cell NFfwW2pCeG:ydH;zbZMhSXO|YYm= NVv6VmNHOjBizszN NVLVOVJQOjRiaB?= M3LFVmROW09? NGj5UVFKdmS3Y3XzJINmdGxiYYDvdJRwe2m| M2XmSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{m3N|E6Lz5{M{e5O|MyQTxxYU6=
HepG2 cell MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mon6N|Ah|ryP MmjQNlQhcA>? NFvMSlFFVVOR MVHJcohq[mm2czDj[YxtKGe{b4f0bC=> MonDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5OUezNVkoRjJ|N{m3N|E6RC:jPh?=
HepG2 cell MmmwT4lv[XOnIFHzd4F6 NU\0VVBVOjBizszN MWCyOEBp M{\EZmROW09? M1HkcmRwf26{ZXf1cIF1\XNidHjlJJBpd3OyaH;yfYxifGmxbjDv[kBCU1R? Mn:3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5OUezNVkoRjJ|N{m3N|E6RC:jPh?=
CEM-S NX3jTng6TnWwY4Tpc44hSXO|YYm= NFTWc4g16oDLzszN MlTvOEBp NVvWe|J6TE2VTx?= M2HLUWlv[3KnYYPld{B1cGViYX3veY51KG:oIHPs[YF3\WRiTFO1RU9DNCCjIIflcIwu\XO2YXLsbZNp\WRiYYX0c5Bp[We7IH3hdotmeg>? M4i2NVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkG0NlQ{Lz5{Mk[xOFI1OzxxYU6=
CEM-R MlrySpVv[3Srb36gRZN{[Xl? M33LUFTjiIoQvF2= MmrGOEBp NInsXVlFVVOR NWizZo1GUW6lcnXhd4V{KHSqZTDhcY92dnRib3[gZ4xm[X[nZDDMR|RCN0JuIHGge4VtdC2nc4ThZoxqe2inZDDheZRweGijZ4mgcYFzc2W{ MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZzNEK0N{c,OjJ4MUSyOFM9N2F-
MOLT-4 MmWxSpVv[3Srb36gRZN{[Xl? M33oWFTjiIoQvF2= M1\GUlQhcA>? Mn2xSG1UVw>? NF\LSlRKdmO{ZXHz[ZMhfGinIHHtc5VvfCCxZjDjcIVifmWmIFzDN2EwSixiYTD3[YxtNWW|dHHicIl{cGWmIHH1eI9xcGGpeTDtZZJs\XJ? M3PXWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkG0NlQ{Lz5{Mk[xOFI1OzxxYU6=
MOLT-4 NXOybVlyTnWwY4Tpc44hSXO|YYm= NIfFXm0yOCEQvF2= NH;FS|MzPCCq MUnEUXNQ NGq3dpNDdG:la4OgZ4VtdHNiaX6geIhmKEdyL1exJJBp[XOnIH;mJJRp\SClZXzsJIN6[2yn M1[1WVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkG0NlQ{Lz5{Mk[xOFI1OzxxYU6=
CEM-S M2T1c2N6fG:2b4jpZ{BCe3OjeR?= MVmxNEDPxE1? MYq0PEBp M3ywW2ROW09? NGmwcoRKSzVyPUWuNgKBkc7:TR?= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZzNEK0N{c,OjJ4MUSyOFM9N2F-
CEM-R MX\DfZRwfG:6aXOgRZN{[Xl? NWjj[5JrOTBizszN MVW0PEBp MoThSG1UVw>? M3K0V2lEPTB;Mz6z5qCK|ryP NEHPe5U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[xOFI1Oyd-MkK2NVQzPDN:L3G+
MOLT-4 NWjSWItWS3m2b4TvfIlkKEG|c3H5 MWKxNEDPxE1? M2O5OVQ5KGh? NFfYcHpFVVOR NU\YeIFGUUN3ME2xMlfjiIoQvF2= NYPyS5FvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2NVQzPDNpPkKyOlE1OjR|PD;hQi=>
HC11 M1vreGZ2dmO2aX;uJGF{e2G7 MYCxNEDPxE1? NESycZgzPCCq M3HBOmROW09? MYjJcohq[mm2czFOtk1k[XOnaX6gZY5lKEGGUmCgd5lvfGinc3nz MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjR{Nk[yNUc,OjJ2Mk[2NlE9N2F-
T98G NW\GdpNvSXCxcITvd4l{KEG|c3H5 M1LVXFAvPSEQvF2= Moi2OlAhcA>? MUPEUXNQ Mk\jRZVodWWwdIOgZZBweHSxZ3XubYMh\W[oZXP0d{Bw\iCpZX\peIlvcWJ? NYH1[4U6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKwOVc6OTRpPkKyNFU4QTF2PD;hQi=>
TAD2 M4LBVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonqNVAxOCEQvF2= M3;rWFUh\A>? NHzzVIdFVVOR NHTC[GpKSzVyPkGwNFAh|ryP MoXMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF{OEmyOlcoRjJzMki5NlY4RC:jPh?=
LN229 NVPsUZNnSXCxcITvd4l{KEG|c3H5 NWD0[5RSOC53IN88US=> MYq2NEBp NIX4eoZFVVOR M3zwbmF2\22nboTzJIFxd3C2b3flcolkKGWoZnXjeJMhd2ZiZ3XmbZRqdmmk MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjB3N{mxOEc,OjJyNUe5NVQ9N2F-
WRO MkLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELEcZYyODByIN88US=> NGHTRnI2KGR? NUTUU2VsTE2VTx?= NWjXe2JEUUN3ME6xNFAxKM7:TR?= M4rMSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzMki5NlY4Lz5{MUK4PVI3PzxxYU6=
SW1736 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV[xNFAh|ryP MVq1JIQ> MX7EUXNQ MkfkTWM2OD12Nz61OkDPxE1? NWT6eGpZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGyPFkzPjdpPkKxNlg6OjZ5PD;hQi=>
KAT18 NIPjR4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXGzJO69VQ>? NULUeoJUPSCm M{XDWWROW09? M4TGNWlEPTB;ND62NkDPxE1? NEGxOVU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUK4PVI3Pyd-MkGyPFkzPjd:L3G+
Hth74 MkDsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzSdmE{KM7:TR?= M4XnUVUh\A>? NFHjPJBFVVOR M1nueGlEPTB;Mj6xPUDPxE1? MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTJ6OUK2O{c,OjF{OEmyOlc9N2F-
TPC1 cells harbored RET/PTC1 rearrangement MlnaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HjV|Mh|ryP NEnZZm42KGR? M1jXc2ROW09? NVfuSmdYUUN3ME2wMlU6KM7:TR?= MmrsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF{OEmyOlcoRjJzMki5NlY4RC:jPh?=
Hth7 cells harbored NRAS (Q61R+/−) MofzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4D0elMh|ryP MofJOUBl MXvEUXNQ MlPkTWM2OD12LkWg{txO M3r0RVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzMki5NlY4Lz5{MUK4PVI3PzxxYU6=
C643 cells harbored HRAS (G13R+/−) MlraS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XqOlMh|ryP M2nYVVUh\A>? NHf3ZmNFVVOR NF\HNmtKSzVyPUCuNlch|ryP MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTJ6OUK2O{c,OjF{OEmyOlc9N2F-
FTC133 cells harbored PTEN (allele deletion and R130+) MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mkm2N{DPxE1? MmnJOUBl MWHEUXNQ M2POTmlEPTB;MD6xPEDPxE1? Mly1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF{OEmyOlcoRjJzMki5NlY4RC:jPh?=
K1 cells harbored PIK3CA (E542K+/+) MkTvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI[5dXA{KM7:TR?= Ml\sOUBl NV7zbGp{TE2VTx?= MXvJR|UxRTBwNUKg{txO MkHFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF{OEmyOlcoRjJzMki5NlY4RC:jPh?=
OCUT1 cells harbored PIK3CA (H1047R+/+) M2rx[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXKzJO69VQ>? NYLHfXpjPSCm MVLEUXNQ MYjJR|UxRTBwMUSg{txO MmXLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF{OEmyOlcoRjJzMki5NlY4RC:jPh?=
Sk-Hep1 M2P5[mN6fG:2b4jpZ{BCe3OjeR?= MoPsNVAh|ryP MUCyOEBp MYHEUXNQ NH3QfXFU\W6|aYTpfoV{KHKnc3nzeIFvfCClZXzsd{B1dyC2aHWgZ5l1d3SxeHnjJIVn\mWldDDv[kB{d3KjZnXubYI> NHHHSlk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUKwOVkzPSd-MkGyNFU6OjV:L3G+
HepG2 MU\DfZRwfG:6aXOgRZN{[Xl? M3XlWVExKM7:TR?= NF\DOIczPCCq MWfEUXNQ NFfxNHhU\W6|aYTpfoV{KHKnc3nzeIFvfCClZXzsd{B1dyC2aHWgZ5l1d3SxeHnjJIVn\mWldDDv[kB{d3KjZnXubYI> NFz2Slk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUKwOVkzPSd-MkGyNFU6OjV:L3G+
A431 Ml3xT4lv[XOnIFHzd4F6 MYq1JO69VQ>? NXjvZ2VOPSCq NGLvbZhFVVOR MnjxV5VxeHKnc4Pld{B1cGVic3nncoFtcW6pIH;mJGFsfCCjbnSgSZJs NIXXO2Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEW3NVA3QSd-MkC1O|ExPjl:L3G+
NCI-H292 M4fueGN6fG:2b4jpZ{BCe3OjeR?= NUTmRmRQOyEQvF2= MWm3NkBp M4nvc2ROW09? NHjDO|dKdmirYnn0bY9vKG:oIHPlcIwheHKxbHnm[ZJifGmxbh?= MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODV5MUC2PUc,OjB3N{GwOlk9N2F-
HeLa NUS3W|F3TnWwY4Tpc44h[XO|YYm= MnvJNUBp NGO5bYNKSzVyIE2gNE4xOjJ6IN88US=> NV34N5NKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxNFA4OzNpPkK5NVAxPzN|PD;hQi=>
NCI-H460 M2jiSWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIXTOFI4OiCq NGCwRZJKSzVyIE2gOU41KM7:TR?= NH22TIE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwNFg3Oid-MkS5NFA5PjJ:L3G+
HCT116 MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVHKU3BMPzJiaB?= NWjpdFNHUUN3MDC9JFcvPSEQvF2= NYm2enV5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA5PjJpPkK0PVAxQDZ{PD;hQi=>
A673 NIKwVVRHfW6ldHnvckBie3OjeR?= NVXmOIhQeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFG2O|Mh[2WubIO= NFnkR|k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
DAOY MlTvSpVv[3Srb36gZZN{[Xl? MoTsdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKESDT2mgZ4VtdHN? MnP0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Saos-2 MU\GeY5kfGmxbjDhd5NigQ>? MojsdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOjb4OtNkBk\Wyucx?= NXrreFRZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
BT-37 M3q3ZmZ2dmO2aX;uJIF{e2G7 NFXke|lyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQmStN|ch[2WubIO= Mli3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
RD MX7GeY5kfGmxbjDhd5NigQ>? NFXqWoZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUlSgZ4VtdHN? NYfZNpJORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-SH M3XueWZ2dmO2aX;uJIF{e2G7 NVTtRpZzeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uW0hiY3XscJM> NVXQNJhuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
BT-12 MUjGeY5kfGmxbjDhd5NigQ>? NFvjTYxyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQmStNVIh[2WubIO= NVn0[GdqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
MG 63 (6-TG R) MoSySpVv[3Srb36gZZN{[Xl? MX7xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN? NX3O[5VIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB1643 NWTQc254TnWwY4Tpc44h[XO|YYm= NUPHOmQ5eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CNVY1OyClZXzsdy=> NEDoOXk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
OHS-50 NILsUotHfW6ldHnvckBie3OjeR?= NFjaNIVyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiT1jTMVUxKGOnbHzz NInGcY09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh41 MkjJSpVv[3Srb36gZZN{[Xl? MU\xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmh2MTDj[Yxtew>? Ml;oQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh30 NV;kUG1WTnWwY4Tpc44h[XO|YYm= MlTZdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqM{CgZ4VtdHN? M2jLSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SJ-GBM2 MlftSpVv[3Srb36gZZN{[Xl? NGP1ZVFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1qtS2JOOiClZXzsdy=> M2jQVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC MWnGeY5kfGmxbjDhd5NigQ>? NV7SZ|dTeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM> M2nhbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB-EBc1 NVm4cWdiTnWwY4Tpc44h[XO|YYm= MX7xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJvRVLjNUBk\Wyucx?= NFnVPZk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
LAN-5 MVXGeY5kfGmxbjDhd5NigQ>? MmG0dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEyDTj21JINmdGy| MoDiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh18 NGe1TJNHfW6ldHnvckBie3OjeR?= MmrldWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqMUigZ4VtdHN? NWrPeW9IRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>

... Click to View More Cell Line Experimental Data

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

PubMed: 22932669     


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

22932669
Growth inhibition assay
Cell viability; 

PubMed: 24665203     


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

24665203
Immunofluorescence
LC3; 

PubMed: 24490764     


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

CFTR/LC3; 

PubMed: 28794469     


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

HMGA2; 

PubMed: 24476133     


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

24490764 28794469 24476133
ELISA
VEGFA; 

PubMed: 29449553     


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

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

Protocol

Kinase Assay:

[4]

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Akt kinases assay:

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

[2]

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

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


    (Only for Reference)
Animal Research:

[2]

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

Solubility (25°C)

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

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

Chemical Information

Molecular Weight 480.39
Formula

C25H21N5O.2HCl

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

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

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

Molarity Calculator

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Clinical Trial Information

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

Tech Support

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

Handling Instructions

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Frequently Asked Questions

  • Question 1:

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

  • Answer:

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

  • Question 2:

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

  • Answer:

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

Akt Signaling Pathway Map

Akt Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID