MK-2206 2HCl

Catalog No.S1078

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. Phase 2.

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MK-2206 2HCl Chemical Structure

MK-2206 2HCl Chemical Structure
Molecular Weight: 480.39

Validation & Quality Control

Cited by 179 publications:

18 customer reviews :

Quality Control & MSDS

Related Compound Libraries

MK-2206 2HCl is available in the following compound libraries:

Akt Inhibitors with Unique Features

  • Selective Akt Inhibitor

    CCT128930 AKT2-selective, IC50=6 nM.

  • Most Potent Akt Inhibitor

    AZD5363 Akt1, IC50=3 nM; Akt2, IC50=8 nM; Akt3, IC50=8 nM.

  • Akt Inhibitor in Clinical Trial

    Perifosine (KRX-0401) Phase III fro relapsed and refractory multiple myeloma.

  • Newest Akt Inhibitor

    AZD5363 Potent inhibitor of all isoforms of Akt (Akt1/Akt2/Akt3) with IC50 of 3 nM/8 nM/8 nM, similar to P70S6K/PKA and lower activity towards ROCK1/2.

Product Information

  • Compare Akt Inhibitors
    Compare Akt Products
  • Research Area
  • Inhibition Profile
  • Combination Therapy
    Combination Therapy

Product Description

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. Phase 2.
Targets Akt1 [1]
(Cell-free assay)
Akt2 [1]
(Cell-free assay)
Akt3 [1]
(Cell-free assay)
IC50 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
NCI-H292NGLIVnpEgXSxdH;4bYMhSXO|YYm=NIfPbXc{KM7:TR?=NITz[VQ4OiCqNVf1UnQ1TE2VTx?=NUP2UI17UW6qaXLpeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36=MWWyNFU4OTB4OR?=
A431M4rTUGtqdmG|ZTDBd5NigQ>?NInyT|U2KM7:TR?=NGDjc5g2KGh?MnH4SG1UVw>?NWrlfWk5W3WycILld5NmeyC2aHWgd4lodmGuaX7nJI9nKEGtdDDhcoQhTXKtM3HiW|IxPTdzME[5
HepG2MnrHR5l1d3SxeHnjJGF{e2G7MWCxNEDPxE1?NHj0S5AzPCCqMoDoSG1UVw>?Mom1V4Vve2m2aYrld{Bz\XOrc4ThcpQh[2WubIOgeI8hfGinIHP5eI91d3irYzDl[oZm[3Rib3[gd49z[W[nbnniMUSyNVIxPTl{NR?=
Sk-Hep1MVnDfZRwfG:6aXOgRZN{[Xl?NH;He5gyOCEQvF2=NWT6XVZYOjRiaB?=NUHPWpE4TE2VTx?=MV3T[Y5{cXSrenXzJJJme2m|dHHueEBk\WyuczD0c{B1cGViY4n0c5RwgGmlIHXm[oVkfCCxZjDzc5Ji\mWwaXK=MW[yNVIxPTl{NR?=
OCUT1 cells harbored PIK3CA (H1047R+/+)NFXicpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NFPKfGU{KM7:TR?=NHy3UW82KGR?NFH1cnlFVVORM{Hh[mlEPTB;MD6xOEDPxE1?NFT5bZIzOTJ6OUK2Oy=>
K1 cells harbored PIK3CA (E542K+/+)NHL3[mNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M4DYS|Mh|ryPM2jYS|Uh\A>?M3LkdmROW09?NUT1VlAyUUN3ME2wMlUzKM7:TR?=MX[yNVI5QTJ4Nx?=
FTC133 cells harbored PTEN (allele deletion and R130+)M4LiVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MWmzJO69VQ>?M3;r[|Uh\A>?NGHIOZdFVVORMWDJR|UxRTBwMUig{txONGTMd2IzOTJ6OUK2Oy=>
C643 cells harbored HRAS (G13R+/−)MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NVvESVNjOyEQvF2=MlvlOUBlM3rpUWROW09?NVuwVGM6UUN3ME2wMlI4KM7:TR?=NHrH[4QzOTJ6OUK2Oy=>
Hth7 cells harbored NRAS (Q61R+/−)M4Tj[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M3\GU|Mh|ryPNYOyWmdEPSCmMoTwSG1UVw>?MXjJR|UxRTRwNTFOwG0>NVSwT2M4OjF{OEmyOlc>
TPC1 cells harbored RET/PTC1 rearrangementNGi1[pJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M3\YfFMh|ryPM3;TblUh\A>?NWH1[5lUTE2VTx?=NH30fY1KSzVyPUCuOVkh|ryPNYPHclg4OjF{OEmyOlc>
Hth74NHe4cZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MlSzN{DPxE1?NETROZU2KGR?NFvxPVRFVVORM1HQSGlEPTB;Mj6xPUDPxE1?NV;vZYFVOjF{OEmyOlc>
KAT18NGXSPHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MoPxN{DPxE1?MVy1JIQ>NFLXSZdFVVORM4X3dWlEPTB;ND62NkDPxE1?NXPTOG5ZOjF{OEmyOlc>
SW1736MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M4T2b|ExOCEQvF2=MlvXOUBlMle3SG1UVw>?NXXYV|NZUUN3ME20O{42PiEQvF2=M17De|IyOjh7Mk[3
WRONXXvSJNuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NYXucYNZOTByMDFOwG0>NHjTbog2KGR?M2HoPGROW09?MWTJR|UxRjFyMECg{txOMlPPNlEzQDl{Nke=
TAD2NVHVV2N1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M3TQRlExODBizszNNF;3e4I2KGR?NWK5WplJTE2VTx?=NYLSe4w1UUN3ME6xNFAxKM7:TR?=MUGyNVI5QTJ4Nx?=
LN229M4rTWmFxd3C2b4Ppd{BCe3OjeR?=NUPudVJVOC53IN88US=>NWPU[HozPjBiaB?=M{jXc2ROW09?NHLjRZNCfWevZX70d{BieG:ydH;n[Y5q[yCnZn\lZ5R{KG:oIHfl[ol1cW6rYh?=NWTOOItvOjJyNUe5NVQ>
T98GNYLrd|czSXCxcITvd4l{KEG|c3H5NIfkbpAxNjVizszNM4C2UVYxKGh?M2\jT2ROW09?NGrucFJCfWevZX70d{BieG:ydH;n[Y5q[yCnZn\lZ5R{KG:oIHfl[ol1cW6rYh?=Moj2NlIxPTd7MUS=
HC11M1nlUmZ2dmO2aX;uJGF{e2G7NEnLXIIyOCEQvF2=MXWyOEBpNEjyW2VFVVORNFrkbZFKdmirYnn0d{DPui2lYYPlbY4h[W6mIFHEVnAhe3mwdHjld4l{MXiyNlQzPjZ{MR?=
MOLT-4MoTFR5l1d3SxeHnjJGF{e2G7NXfwWGpoOTBizszNMUO0PEBpMoLESG1UVw>?NGjoUpdKSzVyPUGuO-KBkc7:TR?=NI\lVFYzOjZzNEK0Ny=>
CEM-RMXrDfZRwfG:6aXOgRZN{[Xl?MkL1NVAh|ryPMV20PEBpNHv6OpFFVVORMVXJR|UxRTNwM,MAje69VQ>?MXyyNlYyPDJ2Mx?=
CEM-SNGjhR41EgXSxdH;4bYMhSXO|YYm=NGm0d2syOCEQvF2=MnzPOFghcA>?NYH3Z25OTE2VTx?=NVjSSpQ4UUN3ME21MlHjiIoQvF2=M1TETlIzPjF2MkSz
MOLT-4NUXMeHZXTnWwY4Tpc44hSXO|YYm=MonBNVAh|ryPNWSwXlhNOjRiaB?=MXPEUXNQMVHCcI9kc3NiY3XscJMhcW5idHjlJGcxN0dzIIDoZZNmKG:oIITo[UBk\WyuIHP5Z4xmNV3HfG43OjJ4MUSyOFM>
MOLT-4M{P0TWZ2dmO2aX;uJGF{e2G7NET0OoQ16oDLzszNM3;jeVQhcA>?Mn;aSG1UVw>?NFK0VWxKdmO{ZXHz[ZMhfGinIHHtc5VvfCCxZjDjcIVifmWmIFzDN2EwSixiYTD3[YxtNWW|dHHicIl{cGWmIHH1eI9xcGGpeTDtZZJs\XJ?NHXEXWYzOjZzNEK0Ny=>
CEM-RMmrUSpVv[3Srb36gRZN{[Xl?NYjoWWZHPOLCid88US=>NVLDW4JwPCCqM4rXemROW09?NFTweXVKdmO{ZXHz[ZMhfGinIHHtc5VvfCCxZjDjcIVifmWmIFzDOGEwSixiYTD3[YxtNWW|dHHicIl{cGWmIHH1eI9xcGGpeTDtZZJs\XJ?NYG0Tlk5OjJ4MUSyOFM>
CEM-SM3P4NmZ2dmO2aX;uJGF{e2G7NFjT[Hg16oDLzszNMUK0JIg>NHTSUHFFVVORMYXJcoNz\WG|ZYOgeIhmKGGvb4XueEBw\iClbHXheoVlKEyFNVGvRkwh[SC5ZXzsMYV{fGGkbHnzbIVlKGG3dH;wbIFogSCvYYLr[ZI>M4joPFIzPjF2MkSz
HepG2 cellMoTZT4lv[XOnIFHzd4F6MVmyNEDPxE1?M1zaVFI1KGh?NXzhU2dHTE2VTx?=MUHEc5dvemWpdXzheIV{KHSqZTDwbI9{eGixconsZZRqd25ib3[gRWtVM{nHO|I{Pzl5M{G5
HepG2 cellNFPvfVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MX6zNEDPxE1?M2D0eFI1KGh?MmnZSG1UVw>?M1HROGlvcGmkaYTzJINmdGxiZ4Lve5RpNFm4b2QzOzd7N{OxPS=>
HepG2 cellNHjL[3dCeG:ydH;zbZMhSXO|YYm=NYfi[llzOjBizszNNUWxOXc2OjRiaB?=NFj0d2FFVVORM3v6cGlv\HWlZYOgZ4VtdCCjcH;weI9{cXN?MX6yN|c6PzNzOR?=
GEOM1fPbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NU\WO21LPTByIH7NNYn2S|Y5PzJiaB?=NHzvPYVFVVORNX74fFBXUW6qaXLpeJMh[2WubDDndo94fGh?MYiyOFU5OTJ|MR?=
CNE-1MlnlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NHzI[I4yOCEQvF2=M2HNV|k3KGh?MYLEUXNQNFXERotKSzVyPUKuPVYh|ryPMkO4NlU{OzZ7MkW=
CNE-2M3\ufWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M2DxbVExKM7:TR?=NYrZNYt2QTZiaB?=NWTWNmxWTE2VTx?=MV\JR|UxRTRwNUOg{txONGLkTZgzPTN|NkmyOS=>
HONE-1NH:1SXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NFjZS20yOCEQvF2=NGW4coc6PiCqMlfwSG1UVw>?M{nOVGlEPTB;Mz6zO{DPxE1?MViyOVM{Pjl{NR?=
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CNE-2NFrwUpZHfW6ldHnvckBCe3OjeR?=MYSxNEDPxE1?NH[wd3Q1QCCqNFfRcnNFVVORNXHhRoNsUW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeEBifCCJMR?=NUDYTWNMOjV|M{[5NlU>
HONE-1M3rkVmZ2dmO2aX;uJGF{e2G7NYW2bVRsOTBizszNMnjtOFghcA>?MXTEUXNQM1rMUGlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4SgZZQhTzF?NV7QTmlSOjV|M{[5NlU>
NEC8NYPGXFRIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NV\FcIViUUN3ME2wMlA6PjVzIN88US=>NGTNNoNUSU6JRWK=
P12-ICHIKAWANUjpcod7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MYrJR|UxRTBwMUG2NkDPxE1?MYDTRW5ITVJ?
MDA-MB-175-VIIMWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NELiWVdKSzVyPUCuNVM4OzhizszNMV7TRW5ITVJ?
AsPC-1M1HpdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MlfKTWM2OD1yLkKyNVIzKM7:TR?=NX3HO|l6W0GQR1XS
T47DMnv4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MmW5TWM2OD1yLkK4NlUh|ryPNFG4WFlUSU6JRWK=
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MOLT-16NEDydZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NYfjPZNXUUN3ME2wMlMxOzJizszNMlSwV2FPT0WU
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KARPAS-45M3e4fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NUTI[IxXUUN3ME2wMlM4OzJzIN88US=>NUnMXmoyW0GQR1XS
NCI-H720NGPkWmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MlHKTWM2OD1yLkO3Olc6KM7:TR?=NH3zOJVUSU6JRWK=
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EFM-19NGPrZXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MX\JR|UxRTBwNESwNUDPxE1?NXW1PXA5W0GQR1XS
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HGC-27NW\MfXBoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NF;ubnJKSzVyPUCuOVY4QDNizszNMkLHV2FPT0WU
MDA-MB-361NV[0fVRUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M3;1UmlEPTB;MD61O|c3OSEQvF2=M1jpOHNCVkeHUh?=
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HCC70NETI[XNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MmrGTWM2OD1yLkW5PFI4KM7:TR?=M4nCdnNCVkeHUh?=
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EPLC-272HMXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NGSzZ25KSzVyPUGuNVczPTZizszNMnPTV2FPT0WU
COLO-684Ml7rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NFPaXZBKSzVyPUGuNlM4OjVizszNM1rafHNCVkeHUh?=
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DOHH-2M1XDS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7NITaNJFKSzVyPUGuNlgzODNizszNMWHTRW5ITVJ?
CTB-1NIm0WFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NGLKdWxKSzVyPUGuNlg6QSEQvF2=MWXTRW5ITVJ?
G-401M3XrSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NHjxT3pKSzVyPUGuNlk4QTVizszNNXm4RnNFW0GQR1XS
LoVoNVqzUlJrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NFjkS4FKSzVyPUGuN|I2OzRizszNM2rhNHNCVkeHUh?=
Ramos-2G6-4C10NXK1TYFXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NFXZZ4VKSzVyPUGuN|M4ODFizszNM331S3NCVkeHUh?=
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... Click to View More Cell Line Experimental Data

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]
Features The first allosteric small molecule inhibitor of Akt to enter clinical development.

Protocol(Only for 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 Assay: [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 Study: [2]

Animal Models SK-OV-3, NCI-H292, HCC70, PC-3, and NCI-H460 models in male CD1-nude mice
Formulation Formulated in 30% Captisol
Dosages 120 mg/kg
Administration Orally administered

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Yan L, AACR Annual Meeting 2009: Abstract Number: DDT01-1.

[2] Hirai H, et al. Mol Cancer Therapy, 2010, 9(7), 1956-1967.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT01802320 Active, not recruiting Colon Mucinous Adenocarcinoma|Colon Signet Ring Cell Adenocarcinoma|Rectal Mucinous Adenocarcinoma|Rectal Signet Ring Cell Adenocarcinoma|Recurrent  ...more Colon Mucinous Adenocarcinoma|Colon Signet Ring Cell Adenocarcinoma|Rectal Mucinous Adenocarcinoma|Rectal Signet Ring Cell Adenocarcinoma|Recurrent Colon Carcinoma|Recurrent Rectal Carcinoma|Stage IIIA Colon Cancer|Stage IIIA Rectal Cancer|Stage IIIB Colon Cancer|Stage IIIB Rectal Cancer|Stage IIIC Colon Cancer|Stage IIIC Rectal Cancer|Stage IVA Colon Cancer|Stage IVA Rectal Cancer|Stage IVB Colon Cancer|Stage IVB Rectal Cancer National Cancer Institute (NCI) March 2013 Phase 2
NCT01783171 Recruiting Pancreatic Adenocarcinoma|Recurrent Pancreatic Carcinoma|Stage III Pancreatic Cancer|Stage IV Pancreatic Cancer|Unresectable Pancreatic Carcinoma National Cancer Institute (NCI) January 2013 Phase 1
NCT01776008 Active, not recruiting Estrogen Receptor Positive|HER2/Neu Negative|Recurrent Breast Carcinoma|Stage IIA Breast Cancer|Stage IIB Breast Cancer|Stage IIIA Breast Cancer|St  ...more Estrogen Receptor Positive|HER2/Neu Negative|Recurrent Breast Carcinoma|Stage IIA Breast Cancer|Stage IIB Breast Cancer|Stage IIIA Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer National Cancer Institute (NCI) January 2013 Phase 2
NCT01859182 Withdrawn Adenocarcinoma of the Gallbladder|Adenocarcinoma With Squamous Metaplasia of the Gallbladder|Adult Primary Cholangiocellular Carcinoma|Advanced Adu  ...more Adenocarcinoma of the Gallbladder|Adenocarcinoma With Squamous Metaplasia of the Gallbladder|Adult Primary Cholangiocellular Carcinoma|Advanced Adult Primary Liver Cancer|Cholangiocarcinoma of the Extrahepatic Bile Duct|Localized Unresectable Adult Primary Liver Cancer|Metastatic Extrahepatic Bile Duct Cancer|Recurrent Adult Primary Liver Cancer|Recurrent Extrahepatic Bile Duct Cancer|Stage II Gallbladder Cancer|Stage IIIA Gallbladder Cancer|Stage IIIB Gallbladder Cancer|Stage IVA Gallbladder Cancer|Stage IVB Gallbladder Cancer|Unresectable Extrahepatic Bile Duct Cancer National Cancer Institute (NCI) January 2013 Phase 2
NCT01705340 Terminated Adenocarcinoma of the Gastroesophageal Junction|HER2-positive Breast Cancer|Male Breast Cancer|Recurrent Breast Cancer|Recurrent Esophageal Cancer|  ...more Adenocarcinoma of the Gastroesophageal Junction|HER2-positive Breast Cancer|Male Breast Cancer|Recurrent Breast Cancer|Recurrent Esophageal Cancer|Recurrent Gastric Cancer|Stage IIIC Breast Cancer|Stage IIIC Esophageal Cancer|Stage IIIC Gastric Cancer|Stage IV Breast Cancer|Stage IV Esophageal Cancer|Stage IV Gastric Cancer National Cancer Institute (NCI) September 2012 Phase 1

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Chemical Information

Download MK-2206 2HCl SDF
Molecular Weight (MW) 480.39
Formula

C25H21N5O.2HCl

CAS No. 1032350-13-2
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 14 mg/mL (29.14 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 15% Captisol 17 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name 8-(4-(1-aminocyclobutyl)phenyl)-9-phenyl-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3(2H)-one

Frequently Asked Questions

  • Question 1
    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.

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.

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

If you have any other enquiries, please leave a message.

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