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 96 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)
Click to View More Targets
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 M1SzTnBzd2yrZnXyZZRqd25iYYPzZZk> MWTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEyQQ3HQJINmdGy|LDDJR|UxRTJyIH7N NV;WNm5KRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi4NFA4PjNpPkG4PFAxPzZ|PD;hQi=>
BT474 NXHoT3VDWHKxbHnm[ZJifGmxbjDhd5NigQ>? MWPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEKWNEe0JINmdGy|LDDJR|UxRTVyIH7N M1jWfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6OECwO|Y{Lz5zOEiwNFc3OzxxYU6=
Sf9 Moj2SpVv[3Srb36gZZN{[Xl? NUTwPYo4UW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDSU2NMOSCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzMEBKSzVyPUCuPFkh|ryP MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDhyMEe2N{c,OTh6MEC3OlM9N2F-
NCI-H460 NV\jXZFTT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NX\wV5BGPzJiaB?= MYHHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDOR2kuUDR4MDDj[YxteyCjZoTldkA4OiCqcoOgZpkh[2:3bITldkBkd3WwdHXyJI1mfGixZDygTWM2OD13LkSg{txO MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyMEi2Nkc,OjR7MEC4OlI9N2F-
PC3 MVHQdo9tcW[ncnH0bY9vKGG|c3H5 MkXRO|IhcA>? NHTYV3ZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGDDN{Bk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTF3LkWg{txO M{XmS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{C4PVk4Lz5{NEOwPFk6PzxxYU6=
HFF NYLRUpJ6S3m2b4TvfIlkyqCjc4PhfS=> NF3WTppEgXSxdH;4bYNqfHliYXfhbY5{fCCKRl[gZ4VtdHNuIFnDOVA:OTZwMzFOwG0> NEjBdlU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEiwNFc3Oyd-MUi4NFA4PjN:L3G+
LNCAP MX7BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M{nWeGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTF7DRXAh[2WubIOsJGlEPTBiPTCwMlAzOSEQvF2u NH72ZoE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUG3PVA4OCd-MUmxO|kxPzB:L3G+
BT474 NFTrSHpCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MXXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEKWNEe0JINmdGy|LDDJR|UxKD1iMD6wOlkh|ryPLh?= NHHTVJY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUG3PVA4OCd-MUmxO|kxPzB:L3G+
BT474 M1fpVGZ2dmO2aX;uJIF{e2G7 NXfDfnR{UW6qaXLpeIlwdiCxZjDHV2s{NWKndHGgdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIFLUOFc1KGOnbHzzMEBKSzVyIE2gNE4yOzhizszNMi=> NFO5fnk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUG3PVA4OCd-MUmxO|kxPzB:L3G+
JVM2 Mn7XRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MnzMO|IhcHK| MXPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEqYTUKgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KEOnbHzUbZRmeiCJbH:gZZN{[XluIFnDOVAhRSBzLk[g{txONg>? NYrJRlJLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki3NFQ4PTdpPkK4O|A1PzV5PD;hQi=>
JeKo1 NEjmdGxCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NWftdpo6PzJiaILz M4fOOWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSnXLc|Eh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncjDHcI8h[XO|YYmsJGlEPTBiPTCzJO69VS5? MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDdyNEe1O{c,Ojh5MES3OVc9N2F-
Z138 NUntSXg{SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NIDHS3Y4OiCqcoO= MlPpRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCcMUO4JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJiR3zvJIF{e2G7LDDJR|UxKD1iMz6xJO69VS5? NX7QdnVMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki3NFQ4PTdpPkK4O|A1PzV5PD;hQi=>
SP49 NHTOb4hCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NGjHU3U4OiCqcoO= MmHXRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVUES5JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJiR3zvJIF{e2G7LDDJR|UxKD1iND64JO69VS5? MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDdyNEe1O{c,Ojh5MES3OVc9N2F-
Maver1 M{i3cWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MYO3NkBpenN? MoixRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPYY\ldlEh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncjDHcI8h[XO|YYmsJGlEPTBiPTC1MlEh|ryPLh?= NEXrTZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEewOFc2Pyd-Mki3NFQ4PTd:L3G+
C6 NXzDVpdOTnWwY4Tpc44h[XO|YYm= M{DxSFI1KGi{cx?= MV\Jcohq[mm2aX;uJI9nKEGtdDDpckBz[XRiQ{[gZ4VtdHNiYX\0[ZIhOjRiaILzJIJ6KEWOSWPBMEBKSzVyIE2gOk46PyEQvF2u M3vFOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7OU[2PVE3Lz5{OUm2OlkyPjxxYU6=
C6 NWHm[npbS3m2b4TvfIlkcXS7IHHzd4F6 NYPiOZVpOjRiaILz NFL4c2pEgXSxdH;4bYNqfHliYXfhbY5{fCC{YYSgR|Yh[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgNlQhcHK|IHL5JG1VXCCjc4PhfUwhUUN3MDC9JFE1NjVizszNMi=> NHP5cZA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUm2OlkyPid-Mkm5OlY6OTZ:L3G+
A549 NV\SWHI{TnWwY4Tpc44h[XO|YYm= NFKwfFIzPCCqcoO= NVn2R4szUW6qaXLpeIlwdiCxZjDBb5QhcW5iaIXtZY4hSTV2OTDj[YxteyCjZoTldkAzPCCqcoOgZpkhTUyLU1GsJGlEPTBiPTCxO{4{OyEQvF2u MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTl4NkmxOkc,Ojl7Nk[5NVY9N2F-
Mino MmjQRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NXvpN4ZuPzJiaILz NWXzZ2JKSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNbY5wKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDD[YxtXGm2ZYKgS4xwKGG|c3H5MEBKSzVyIE2gNlAvQCEQvF2u M1nHelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6N{C0O|U4Lz5{OEewOFc2PzxxYU6=
A673 NVv0eZAxeUiWUzDhd5NigQ>? M1ryOJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCDNkezJINmdGy| NI\H[os9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
RD MWXxTHRUKGG|c3H5 MlfIdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKGIHPlcIx{ NYD5[3JIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB1643 MYHxTHRUKGG|c3H5 Ml;2dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6EMU[0N{Bk\Wyucx?= NF3XTpo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SJ-GBM2 M2LxfJFJXFNiYYPzZZk> M3q1bpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSj3HRm0zKGOnbHzz MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-MC MmTGdWhVWyCjc4PhfS=> NHnxdVRyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1OSyClZXzsdy=> MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
NB-EBc1 MYDxTHRUKGG|c3H5 NVrOZVU3eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CMWVD[zFiY3XscJM> MnGyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
LAN-5 MUjxTHRUKGG|c3H5 NGK5Z4hyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTFHOMVUh[2WubIO= M120flxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
MCL NFHmN|FCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MoqzNlQhcHK| NWn5cIo3SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBxemmvYYL5JIh2dWGwIF3DUEBk\WyuczD1dEB1dyB4MDD1UUBi\nSncjCyOEBpenNiYomgR4VtdFSrdHXyJGdtdyCjc4PhfS=> NHy3[W89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEewOFc2Pyd-Mki3NFQ4PTd:L3G+
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.

  • (Only for Reference)
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.
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 39 mg/mL
(91.66 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%PEG300+5% tween80+50% H2O
For best results, use promptly after mixing.

3mg/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 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 2021-09-06)

Tech Support

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

Handling Instructions

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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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