GSK690693

Catalog No.S1113

For research use only.

GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively. GSK690693 affects Unc-51-like autophagy activating kinase 1 (ULK1) activity, robustly inhibits STING-dependent IRF3 activation. Phase 1.

GSK690693 Chemical Structure

CAS No. 937174-76-0

Selleck's GSK690693 has been cited by 101 publications

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Biological Activity

Description GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively. GSK690693 affects Unc-51-like autophagy activating kinase 1 (ULK1) activity, robustly inhibits STING-dependent IRF3 activation. Phase 1.
Targets
ULK1 [4] STING [4] AMPK [4] Akt1 [1]
(Cell-free assay)
PKCη [1]
(Cell-free assay)
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2 nM 2 nM
In vitro

GSK690693 is very selective for the Akt isoforms versus the majority of kinases in other families. However, GSK690693 is less selective for members of the AGC kinase family including PKA, PrkX, and PKC isozymes with IC50 of 24 nM, 5 nM, and 2-21 nM, respectively. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively, and PAK4, 5, and 6 from the STE family with IC50 of 10 nM, 52 nM, and 6 nM, respectively. GSK690693 inhibits the phosphorylation of GSK3β in tumor cells with IC50 ranging from 43 nM to 150 nM. GSK690693 treatment leads to a dose-dependent increase in the nuclear accumulation of the transcription factor FOXO3A. GSK690693 potently inhibits the proliferation of T47D, ZR-75-1, BT474, HCC1954, MDA-MB-453, and LNCaP cells with IC50 of 72 nM, 79 nM, 86 nM, 119 nM, 975 nM, and 147 nM, respectively. GSK690693 treatment induces apoptosis at concentrations >100 nM in both LNCaP and BT474 cells. [1] Consistent with the role of AKT in cell survival, GSK690693 induces apoptosis in sensitive ALL cell lines. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
LNCaP M{P2bXBzd2yrZnXyZZRqd25iYYPzZZk> M{XaOWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTF7DZXAh[2WubIOsJGlEPTB;MkCgcm0> NWe1cZliRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi4NFA4PjNpPkG4PFAxPzZ|PD;hQi=>
BT474 Ml;wVJJwdGmoZYLheIlwdiCjc4PhfS=> M4fZZWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQmS0O|Qh[2WubIOsJGlEPTB;NUCgcm0> M37EWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6OECwO|Y{Lz5zOEiwNFc3OzxxYU6=
Sf9 MmjkSpVv[3Srb36gZZN{[Xl? NF\LO2pKdmirYnn0bY9vKG:oIHj1cYFvKHKnY3;tZolv[W62IGLPR2syKGW6cILld5Nm\CCrbjDT[lkh[2WubIOsJGlEPTB;MD64PUDPxE1? NUm4W2hmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi4NFA4PjNpPkG4PFAxPzZ|PD;hQi=>
NCI-H460 M2\ZV2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkexO|IhcA>? MYfHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDOR2kuUDR4MDDj[YxteyCjZoTldkA4OiCqcoOgZpkh[2:3bITldkBkd3WwdHXyJI1mfGixZDygTWM2OD13LkSg{txO NXTSXWR4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA5PjJpPkK0PVAxQDZ{PD;hQi=>
PC3 NXvZU|NtWHKxbHnm[ZJifGmxbjDhd5NigQ>? Mk\JO|IhcA>? NGTOTG5CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGDDN{Bk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTF3LkWg{txO MnfKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|MEi5PVcoRjJ2M{C4PVk4RC:jPh?=
HFF M2XtTGN6fG:2b4jpZ:Kh[XO|YYm= M2rK[GN6fG:2b4jpZ4l1gSCjZ3HpcpN1KEiIRjDj[YxteyxiSVO1NF0yPi5|IN88US=> M4PiSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6OECwO|Y{Lz5zOEiwNFc3OzxxYU6=
LNCAP MXjBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MUDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEyQQ1HQJINmdGy|LDDJR|UxKD1iMD6wNlEh|ryPLh?= M3PRW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7MUe5NFcxLz5zOUG3PVA4ODxxYU6=
BT474 M2e0ZWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NX7TVHJkSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDCWFQ4PCClZXzsd{whUUN3MDC9JFAvODZ7IN88UU4> MnTEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTlzN{mwO|AoRjF7MUe5NFcxRC:jPh?=
BT474 NEH2e|RHfW6ldHnvckBie3OjeR?= MXXJcohq[mm2aX;uJI9nKEeVS{OtZoV1[SCyaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hSlR2N{SgZ4VtdHNuIFnDOVAhRSByLkGzPEDPxE1w NGXZUZQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUG3PVA4OCd-MUmxO|kxPzB:L3G+
JVM2 MmjZRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NYHYeJM1PzJiaILz NF72WHZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFrWUVIh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncjDHcI8h[XO|YYmsJGlEPTBiPTCxMlYh|ryPLh?= MnHLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh5MES3OVcoRjJ6N{C0O|U4RC:jPh?=
JeKo1 MVfBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NVvLRpl1PzJiaILz NWXsZpRmSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDK[WtwOSClZXzsd{Bi\nSncjC3NkBpenNiYomgR4VtdFSrdHXyJGdtdyCjc4PhfUwhUUN3MDC9JFMh|ryPLh?= Ml\3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh5MES3OVcoRjJ6N{C0O|U4RC:jPh?=
Z138 MVfBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MVS3NkBpenN? M4T2eGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iWkGzPEBk\WyuczDh[pRmeiB5MjDodpMh[nliQ3XscHRqfGW{IFfsc{Bie3OjeTygTWM2OCB;IEOuNUDPxE1w MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDdyNEe1O{c,Ojh5MES3OVc9N2F-
SP49 NG\FVmRCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MVy3NkBpenN? Ml;TRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVUES5JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJiR3zvJIF{e2G7LDDJR|UxKD1iND64JO69VS5? NEDxXHU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEewOFc2Pyd-Mki3NFQ4PTd:L3G+
Maver1 M2LTd2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 M1LDZVczKGi{cx?= NUP0d5oxSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNZZZmejFiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JGNmdGyWaYTldkBIdG9iYYPzZZktKEmFNUCgQUA2NjFizszNMi=> MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDdyNEe1O{c,Ojh5MES3OVc9N2F-
C6 MU\GeY5kfGmxbjDhd5NigQ>? M{jtb|I1KGi{cx?= M1v1Z2lvcGmkaYTpc44hd2ZiQXv0JIlvKHKjdDDDOkBk\WyuczDh[pRmeiB{NDDodpMh[nliRVzJV2EtKEmFNUCgQUA3Njl5IN88UU4> MkfrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl7Nk[5NVYoRjJ7OU[2PVE3RC:jPh?=
C6 NXfvTlltS3m2b4TvfIlkcXS7IHHzd4F6 MlyzNlQhcHK| MYTDfZRwfG:6aXPpeJkh[WejaX7zeEBz[XRiQ{[gZ4VtdHNiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4h[2WubDD2bYFjcWyrdImgZYZ1\XJiMkSgbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IEG0MlUh|ryPLh?= MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTl4NkmxOkc,Ojl7Nk[5NVY9N2F-
A549 NX;tXFdGTnWwY4Tpc44h[XO|YYm= MnmxNlQhcHK| NXLDU5F2UW6qaXLpeIlwdiCxZjDBb5QhcW5iaIXtZY4hSTV2OTDj[YxteyCjZoTldkAzPCCqcoOgZpkhTUyLU1GsJGlEPTBiPTCxO{4{OyEQvF2u Mln2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl7Nk[5NVYoRjJ7OU[2PVE3RC:jPh?=
Mino NYOyPGczSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MYS3NkBpenN? MnrpRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPaX7vJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJiR3zvJIF{e2G7LDDJR|UxKD1iMkCuPEDPxE1w MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDdyNEe1O{c,Ojh5MES3OVc9N2F-
A673 MVfxTHRUKGG|c3H5 MXzxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>? MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
RD M1fRVZFJXFNiYYPzZZk> MknJdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKGIHPlcIx{ NGPPPGE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB1643 MlzQdWhVWyCjc4PhfS=> NImyPJByUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKxOlQ{KGOnbHzz MoL5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SJ-GBM2 MY\xTHRUKGG|c3H5 NXHZfohIeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPKMWdDVTJiY3XscJM> M3mxcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC NUOwS3pHeUiWUzDhd5NigQ>? NUX5NJFOeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM> MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
NB-EBc1 M{TNUJFJXFNiYYPzZZk> MULxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJvRVLjNUBk\Wyucx?= NUex[|JwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
LAN-5 MUXxTHRUKGG|c3H5 NUPEOndueUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFzBUk02KGOnbHzz M3HqflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
MCL Mo\PRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NEn6NnkzPCCqcoO= MlS2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDwdolu[XK7IHj1cYFvKE2FTDDj[YxteyC3cDD0c{A3OCC3TTDh[pRmeiB{NDDodpMh[nliQ3XscHRqfGW{IFfsc{Bie3OjeR?= NXrINIRVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki3NFQ4PTdpPkK4O|A1PzV5PD;hQi=>
Assay
Methods Test Index PMID
Western blot p-Akt / Akt / p-GSK3 / p-mTOR / mTOR / p-p70S6K / p-FoxO3a / p-FoxO1 ; pPRAS40 / PRAS40 / pBAD / BAD 20075391 25551293
Growth inhibition assay Cell viability 20075391
In vivo

A single administration of GSK690693 inhibits GSK3β phosphorylation in human breast carcinoma (BT474) xenografts in a dose- and time-dependent manner. Similarly, GSK690693 induces a reduction in phosphorylation of the Akt substrates, PRAS40, and FKHR/FKHRL1. GSK690693 also results in an acute increase in blood glucose, returning to baseline 8 to 10 hours after drug administration. Administration of GSK690693 induces reductions in phosphorylated Akt substrates in vivo, and potently inhibits the growth of human SKOV-3 ovarian, LNCaP prostate, and BT474 and HCC-1954 breast carcinoma xenografts, with maximal inhibition of 58% to 75% at the dose of 30 mg/kg/day. [1] GSK690693 exhibits efficacy irrespective of the mechanism of Akt activation involved. GSK690693 is most effective in delaying tumor progression in Lck-MyrAkt2 mice expressing a membrane-bound, constitutively active form of Akt. [3]

Protocol (from reference)

Kinase Assay:

[1]

  • In vitro kinase assays:

    His-tagged full-length Akt1, 2, or 3 are expressed and purified from baculovirus. Activation is carried out with purified PDK1 to phosphorylate Thr308 and purified MK2 to phosphorylate Ser473. To more accurately measure time-dependent inhibition of Akt, activated Akt enzymes are incubated with GSK690693 at various concentrations at room temperature for 30 minutes before the reaction is initiated with the addition of substrate. Final reaction contains 5 nM to 15 nM Akt1, 2, and 3 enzymes; 2 μM ATP; 0.15 μCi/μL[γ-33P]ATP; 1 μM Peptide (Biotin-aminohexanoicacid-ARKR-ERAYSFGHHA-amide); 10 mM MgCl2; 25 mM MOPS (pH 7.5); 1 mM DTT; 1 mM CHAPS; and 50 mM KCl. The reactions are incubated at room temperature for 45 minutes, followed by termination with Leadseeker beads in PBS containing EDTA (final concentration, 2 mg/mL beads and 75 mM EDTA). The plates are then sealed, the beads are allowed to settle for at least 5 hours, and product formation is quantitated using a Viewlux Imager.

Cell Research:

[1]

  • Cell lines: T47D, ZR-75-1, BT474, HCC1954, MDA-MB-453, LNCaP, etc.
  • Concentrations: Dissolved in DMSO, final concentrations ~30 μM
  • Incubation Time: 72 hours
  • Method:

    Cells are plated at densities that allow untreated cells to grow logarithmically during the course of a 3-day assay. Briefly, cells are plated in 96- or 384-well plates and incubated overnight. Cells are then treated with GSK690693 (ranging from 30 μM-1.5 nM) and incubated for 72 hours. Cell proliferation is measured using the CellTiter Glo reagent. Data are analyzed using the XLFit curve-fitting tool for Microsoft Excel. IC50 values are obtained by fitting data to Eq, 2.

Animal Research:

[1]

  • Animal Models: Female CD1 Swiss Nude mice injected with LNCaP, SKOV-3, or PANC1 cells, and C.B-17 SCID mice with HCC1954, MDA-MB-453, or BT474 cells
  • Dosages: ~30 mg/kg/day
  • Administration: Administered via i.p.

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%PEG300+5% tween80+50% H2O
For best results, use promptly after mixing.

3mg/mL

Chemical Information

Molecular Weight 425.48
Formula

C21H27N7O3

CAS No. 937174-76-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCN1C2=C(C(=NC=C2OCC3CCCNC3)C#CC(C)(C)O)N=C1C4=NON=C4N

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
NCT00666081 Withdrawn Drug: GSK690693 Cancer GlaxoSmithKline April 2008 Phase 1
NCT00493818 Terminated Drug: GSK690693 Cancer GlaxoSmithKline April 2007 Phase 1

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

Tech Support

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

Handling Instructions

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Frequently Asked Questions

Question 1:
Why pAKT increased after treatment of the inhibitor ?

Answer:
GSK690693 actually inhibits AKT, but not necessarily decrease p-Akt level. Treatment with GSK690693 caused AKT hyper phosphorylation which has already been reported in some papers. (For example, http://www.bloodjournal.org/content/113/8/1723.short?sso-checked=true). To test the inhibition of AKT activity, you might have to look at the level of AKT substrates.

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