PI-103

For research use only.

Catalog No.S1038

62 publications

PI-103 Chemical Structure

Molecular Weight(MW): 348.36

PI-103 is a multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM in cell-free assays, less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM.

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Selleck's PI-103 has been cited by 62 publications

Purity & Quality Control

Choose Selective PI3K Inhibitors

Biological Activity

Description PI-103 is a multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM in cell-free assays, less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM.
Features The first potent, synthetic mTOR inhibitor.
Targets
p110α [3]
(Cell-free assay)
p110β [3]
(Cell-free assay)
p110δ [3]
(Cell-free assay)
p110γ [3]
(Cell-free assay)
DNA-PK [3]
(Cell-free assay)
2 nM 3 nM 3 nM 15 nM 23 nM
In vitro

PI-103 potently inhibits both the rapamycin-sensitive (mTORC1) and rapamycin-insensitive (mTORC2) complexes of the protein kinase mTOR. [1] PI-103 inhibits constitutive and growth factor-induced PI3K/Akt, as well as mTORC1 activation. [2] In blast cells, PI-103 inhibits leukemic proliferation, the clonogenicity of leukemic progenitors and induces mitochondrial apoptosis, especially in the compartment containing leukemic stem cells. PI-103 inhibits p110α >200-fold more potently than p110β. PI-103 also potently blocks production of PI(3,4)P2 and PIP3 in adipocytes and PIP3 in myotubes. [2] PI-103 inhibits phosphorylation of Akt with an IC95 100-fold lower than that for LY294002. Strikingly, PI-103 completely protects animals from insulin-stimulated decline in blood glucose. PI-103 has additive proapoptotic effects with etoposide in blast cells and in immature leukemic cells. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SK-N-BE NGT5ZpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHJeW4xNThizszN NGHJeWUzPC92OD:3NkBp NVq4UII6cW6mdXPld{B1cW2nLTDhcoQh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgbY5pcWKrdHnvckBwdiCQQjDj[YxtKGe{b4f0bC=> NHO3OnMzPjJ{NE[4NS=>
SH-SY5Y NYTxN|d[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHmNE05KM7:TR?= MVyyOE81QC95MjDo MVnpcoR2[2W|IITpcYUuKGGwZDDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCrbnjpZol1cW:wIH;uJG5DKGOnbHyg[5Jwf3Sq NIPu[nUzPjJ{NE[4NS=>
SH-SY5Y  NUjSbolZSXCxcITvd4l{KEG|c3H5 NETDd|IyKM7:TR?= NELhVmMxNjVvMkSgbC=> MnjJd4Vve2m2aYrld{Bv\XW{b3LsZZN1d22jIHPlcIx{KHSxIHTvfI9zfWKrY3nuMYlv\HWlZXSgZZBweHSxc3nz NFrzT2QzPjJ{NE[4NS=>
G 35 SC NIfY[lRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HLelAvODVvMkCg{txO NHTBXIkzPC95MjDo M4XLZ2ROW09? M1H0PYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? MVeyOlEzOTJ3MR?=
G 38 SC NVXaWYF3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PReVAvODVvMkCg{txO NY[2bXFvOjRxN{KgbC=> NUXYdnZGTE2VTx?= MmPHbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBidmRidHnt[UBl\XCnbnTlcpRtgQ>? MVeyOlEzOTJ3MR?=
G 40 SC NVK1PHpET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHL0O5AxNjB3LUKwJO69VQ>? NEG3VY8zPC95MjDo NGHMfmxFVVOR NH21ZndqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 MnLINlYyOjF{NUG=
G 35 DC NX6w[Hh6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfPNE4xPS1{MDFOwG0> M3nTV|I1Nzd{IHi= NV\VS|J5TE2VTx?= M2HUR4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? NU[wT4lGOjZzMkGyOVE>
G 38 DC NX6wbYlVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDJNE4xPS1{MDFOwG0> NV3NU3pZOjRxN{KgbC=> MnTaSG1UVw>? M4TZZ4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? NHPxdIQzPjF{MUK1NS=>
G 40 DC MnvmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYGwMlA2NTJyIN88US=> M{Pse|I1Nzd{IHi= MkXpSG1UVw>? NFTIXXNqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 M1jTPFI3OTJzMkWx
RD MlyxRZBweHSxc3nzJGF{e2G7 MV:xM|EvPS9{IN88US=> M4rGZ|czKGh? NVTmO3V1cW6mdXPld{BieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDHRW5VPjF? MoXYNlU4PDl|N{i=
TE381.T MmPGRZBweHSxc3nzJGF{e2G7 MUKxM|EvPS9{IN88US=> M1i5S|czKGh? MYnpcoR2[2W|IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKEeDTmS2NS=> NVviWVgzOjV5NEmzO|g>
RMS13 MUjBdI9xfG:|aYOgRZN{[Xl? MofVNU8yNjVxMjFOwG0> NFu1RYE4OiCq NVi3eFFVcW6mdXPld{BieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDHRW5VPjF? MYKyOVc1QTN5OB?=
RH30  MUHBdI9xfG:|aYOgRZN{[Xl? NU\mRpAyOS9zLkWvNkDPxE1? M4PKNFczKGh? NXjyUYZrcW6mdXPld{BieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDHRW5VPjF? MmXzNlU4PDl|N{i=
VJ M{nMW2Fxd3C2b4Ppd{BCe3OjeR?= NGHBNWsyNzFwNT:yJO69VQ>? M4LBeFczKGh? M3XQS4lv\HWlZYOgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiR1HOWFYy MVqyOVc1QTN5OB?=
HS578T NED3fW1E\WyuIG\pZYJqdGm2eTDBd5NigQ>? NFfxWGExNTNizszN NUjYOmR1PzJiaB?= MmW2bY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? M33rPVI2PzJzNEG5
BT549 MoX5R4VtdCCYaXHibYxqfHliQYPzZZk> MniyNE0{KM7:TR?= NXfROYF7PzJiaB?= NI[zTmpqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NWm0[2pWOjV5MkG0NVk>
MDA-MB-231 NIHPU2ZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NGDCeXoxNTNizszN NH\FVpY4OiCq M2iwN4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MkXQNlU4OjF2MUm=
MDA-MB-468 NEn4O|BE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NIXrSWExNTNizszN MkSxO|IhcA>? NHPIbXdqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NEnlfVQzPTd{MUSxPS=>
MDA-MB-436 M1TzZmNmdGxiVnnhZoltcXS7IFHzd4F6 MUSwMVMh|ryP MkHsO|IhcA>? NHnMZXRqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MUCyOVczOTRzOR?=
SUM149PT MX\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> M1fFUFAuOyEQvF2= Ml\qO|IhcA>? Ml;wbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NWL3c4xHOjV5MkG0NVk>
MDA-MB-468 M1PaSGZ2dmO2aX;uJGF{e2G7 NWLyW|M3OC5yMT2xNEDPxE1? MVOyOEBp NX[wPFk3\G:5boLl[5Vt[XSnczD0bIUhdGW4ZXzzJI9nKM7{LWTyR3AyNCClLV35Z{BidmRiY4njcIlvKEVicILveIVqdnQEoB?= NGDDPZczPTd{MUSxPS=>
MDA-MB-231 M4HoVmZ2dmO2aX;uJGF{e2G7 MXOwMlAyNTFyIN88US=> NWq4OYdmOjRiaB?= MWXkc5dvemWpdXzheIV{KHSqZTDs[ZZmdHNib3[g{tIuXHKFUEGsJIMuVXmlIHHu[EBkgWOuaX6gSUBxem:2ZXnud:Kh MnPNNlU4OjF2MUm=
HS578T M33YOGZ2dmO2aX;uJGF{e2G7 NH;aZW8xNjBzLUGwJO69VQ>? MYSyOEBp NYnONnlK\G:5boLl[5Vt[XSnczD0bIUhdGW4ZXzzJI9nKM7{LWTyR3AyNCClLV35Z{BidmRiY4njcIlvKEVicILveIVqdnQEoB?= M3nSWFI2PzJzNEG5
SW872 MXXGeY5kfGmxbjDBd5NigQ>? M3HKZlAvODFvMD61JO69VQ>? M3G3dFI1KGh? M1q3[JJm\HWlZYOgRWtVKHCqb4PwbI9zgWyjdHnvckApeEGNVDmgZY5lKDSHQmCxJJBpd3OyaH;yfYxifGmxbjCodFRGSlBzKTDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nctMg M2e3WFI1Pjl3NkOy
SW982 NWL4b2ZsTnWwY4Tpc44hSXO|YYm= NUn0U2RqOC5yMT2wMlUh|ryP M1ryeVI1KGh? Mn\1doVlfWOnczDBT3QheGixc4Doc5J6dGG2aX;uJEhxSUuWKTDhcoQhPEWEUEGgdIhwe3Cqb4L5cIF1cW:wIDjwOGVDWDFrIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{wrC= M2HQUVI1Pjl3NkOy
SW872 NIS4N49CeG:ydH;zbZMhSXO|YYm= NIDqe2MxNjBzLUCuOUDPxE1? MVS0PEBp MXzpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MUCyOFY6PTZ|Mh?=
SW982 MVfBdI9xfG:|aYOgRZN{[Xl? NYj4[41uOC5yMT2wMlUh|ryP NFewd401QCCq M{nQcolv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= MV6yOFY6PTZ|Mh?=
AGS HG MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTBwNkigxtEhOC5yM{Gg{txO NHG3clIzPDV7N{S3PC=>
AGS LG NF3pdG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTBwMEWgxtEhOC5yMEGg{txO Mnu1NlQ2QTd2N{i=
HGC27 HG M{T6bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzKTWM2OD1yLkO4JOKyKDBwMEKyJO69VQ>? MlzmNlQ2QTd2N{i=
HGC27 LG NHPJbINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLiVHdVUUN3ME2wMlAzKMLzIECuNFA1KM7:TR?= MkjtNlQ2QTd2N{i=
MKN45 HG M2TuUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFn6eWpKSzVyPUGuNFEhyrFiMD6wOVEh|ryP MUCyOFU6PzR5OB?=
MKN45 LG M1e1bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PNUmlEPTB;MD64O{DDuSByLkCzNEDPxE1? MoLRNlQ2QTd2N{i=
NUGC4 HG NYfib5gxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7ISnhKSzVyPUG0MlAhyrFiMz65NVMh|ryP NXjWTGhtOjR3OUe0O|g>
NUGC4 LG MlK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\TTWM2OD1zND6wJOKyKDVwM{KxJO69VQ>? NEXBZlQzPDV7N{S3PC=>
A549 MkfKSpVv[3Srb36gRZN{[Xl? NWLrdVlbOC5{NT:wMlUwOSEQvF2= MVmyOEBp MXHpcohq[mm2czDBb5QheGixc4Doc5J6dGG2aX;uJJNtcWeqdHz5 NVX3eHJxOjR|NUG0NlU>
H460 NGe2UIRHfW6ldHnvckBCe3OjeR?= MlzzNE4zPS9yLkWvNUDPxE1? NFnCTYIzPCCq M3OwS4lvcGmkaYTzJGFsfCCyaH;zdIhwenmuYYTpc44he2yrZ3j0cJk> MlL6NlQ{PTF2MkW=
H661 Ml;JSpVv[3Srb36gRZN{[Xl? NUm0eHk1OC5{NT:wMlUwOSEQvF2= NX2yO2E2OjRiaB?= M4nXeYlvcGmkaYTzJGFsfCCyaH;zdIhwenmuYYTpc44he2mpbnnmbYNidnSueR?= MlHmNlQ{PTF2MkW=
SAS M{O3[GZ2dmO2aX;uJGF{e2G7 NUThRW9OOC5{NT:wMlUwOSEQvF2= MUCyOEBp MWHpcohq[mm2czDBb5QheGixc4Doc5J6dGG2aX;uJJNq\26rZnnjZY51dHl? MofzNlQ{PTF2MkW=
UT5 NEfWb3pHfW6ldHnvckBCe3OjeR?= M4rY[VAvOjVxMD61M|Eh|ryP MljwNlQhcA>? MkPSbY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7 MV:yOFM2OTR{NR?=
FaDu M{fYNWZ2dmO2aX;uJGF{e2G7 MlW3NE4zPS9yLkWvNUDPxE1? NVjkfGYyOjRiaB?= NGq1V49qdmirYnn0d{BCc3RicHjvd5Bpd3K7bHH0bY9vKHOrZ37p[olk[W62bIm= M1voZlI1OzVzNEK1
RD MljmRZBweHSxc3nzJGF{e2G7 NIrUcYUyNzFwNT:yJO69VQ>? NEnyPVE4OiCq MlTRSG1UVw>? M4jS[Ylv\HWlZYOgZ4F{eGG|ZT3k[ZBmdmSnboSgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiVV:xNlY> NH73XI4zOzZ6NEmyOS=>
TE671 M2jINmFxd3C2b4Ppd{BCe3OjeR?= M4LsTFEwOS53L{Kg{txO NFTyUok4OiCq MUnEUXNQ M3rMTIlv\HWlZYOgZ4F{eGG|ZT3k[ZBmdmSnboSgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiVV:xNlY> MlfMNlM3QDR7MkW=
RH30  MlXHRZBweHSxc3nzJGF{e2G7 MoixNU8yNjVxMjFOwG0> MVK3NkBp M4HTWGROW09? MnnnbY5lfWOnczDjZZNx[XOnLXTldIVv\GWwdDDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCXT{GyOi=> NWjVSYtWOjN4OES5NlU>
RMS13 MmG5RZBweHSxc3nzJGF{e2G7 M1TSRlEwOS53L{Kg{txO MVK3NkBp M4TaTGROW09? MVnpcoR2[2W|IHPhd5Bie2VvZHXw[Y5l\W62IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKFWRMUK2 NWPlSWZCOjN4OES5NlU>
SUM149PT MoTJR4VtdCCYaXHibYxqfHliQYPzZZk> M3jGNlAvOyEQvF2= NVXGZXNxPzJiaB?= M4rafoVvcGGwY3XzJIN6fG:2b4jpZ{Bm\m[nY4TzJI9nKFCLM1uvRWtVKHCjdHj3ZZkhcW6qaXLpeI9zew>? NGq3eHUzOzZyMUC3OC=>
MDA-MB-468 MXXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MnzINE4{KM7:TR?= NYjsUIx2PzJiaB?= NHLCSJhmdmijbnPld{BkgXSxdH;4bYMh\W[oZXP0d{Bw\iCSSUPLM2FMXCCyYYToe4F6KGmwaHnibZRwenN? NV\1cFF1OjN4MEGwO|Q>
MDA-MB-231 MV\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MnjjNE4{KM7:TR?= NY\IXpJCPzJiaB?= NXnCOFJm\W6qYX7j[ZMh[3m2b4TvfIlkKGWoZnXjeJMhd2ZiUFmzT{9CU1RicHH0bJdigSCrbnjpZol1d3K| NHnSc|czOzZyMUC3OC=>
SY5Y M1PiOmZ2dmO2aX;uJGF{e2G7 MVKxMlUwOi53L{Wg{txO NYHCXI1KOjRiaB?= MWXpcoR2[2W|IFexxsBk\WyuLXP5Z4xmKGG{cnXzeEBidmRiYYDvdJRwe2m| MmC2NlM{Pzh|NEG=
SKNBE(2c) NEPCRmdHfW6ldHnvckBCe3OjeR?= MoTZNU42NzJwNT:1JO69VQ>? MVmyOEBp MY\pcoR2[2W|IFexxsBk\WyuLXP5Z4xmKGG{cnXzeEBidmRiYYDvdJRwe2m| MX:yN|M4QDN2MR?=
RD MlH5RZBweHSxc3nzJGF{e2G7 M1PxSVMhyrWP MVqxNkBp MXPEUXNQ MXHz[Y5{cXSrenXzJHJFKGOnbHzzJJRwKESRWD3pcoR2[2WmIHHwc5B1d3Orcx?= NYfFSIJJOjN|MEC4NFk>
TP5014 MVvBdI9xfG:|aYOgRZN{[Xl? NXHQXGhWOyEEtV2= MXyxNkBp M2L4PGROW09? NX3T[pJTe2Wwc3n0bZpmeyCURDDj[YxteyC2bzDEU3gucW6mdXPl[EBieG:ydH;zbZM> NELyZXYzOzNyMEiwPS=>
HT1080 NG\OOWxCeG:ydH;zbZMhSXO|YYm= NInJXow{KML3TR?= MmnqNVIhcA>? MUPEUXNQ MVnz[Y5{cXSrenXzJHJFKGOnbHzzJJRwKESRWD3pcoR2[2WmIHHwc5B1d3Orcx?= MnO4NlM{ODB6MEm=
A549 NFrqTlNHfW6ldHnvckBCe3OjeR?= MVOwMVMvOyEQvF2= NVPlcZlzPzJiaB?= MWnpcoR2[2W|IHPvcZBt\XSnIHTve45z\We3bHH0bY9vKG:oIIDBT3Q> MYeyN|I2QTV7MR?=
HCC827 NUHVT3d6TnWwY4Tpc44hSXO|YYm= NX7wZnIxOC1|LkOg{txO NFfCboo4OiCq M2XPb4lv\HWlZYOgZ49ueGyndHWg[I94dnKnZ4XsZZRqd25ib3[gdGFMXA>? M{HhWlI{OjV7NUmx
H3122 M2HINmZ2dmO2aX;uJGF{e2G7 MXGwMVMvOyEQvF2= NXPPenVpPzJiaB?= MmDIbY5lfWOnczDjc41xdGW2ZTDkc5dvemWpdXzheIlwdiCxZjDwRWtV M2r6cVI{OjV7NUmx
TALL-1 M1GxWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVqx5qCK|ryP MkjLO{Bl NVi5dZZV\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 NGXycVMzOzB|OEK3Ny=>
HPB-ALL Mne5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV2x5qCK|ryP NF\YR|A4KGR? M2HyV4Rm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? NHT3bYEzOzB|OEK3Ny=>
DND41 NYPRVZFYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWSyR3VjOeLCid88US=> NVjCOnhEPyCm Ml\T[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 MUSyN|A{QDJ5Mx?=
SUP-T1 NXX6VGxwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jndlHjiIoQvF2= MVe3JIQ> NHfC[Ghl\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? MnPGNlMxOzh{N{O=
PEER NFf3T41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPTNgKBkc7:TR?= M3TIW|ch\A>? NWLzcGZL\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 M2fjW|I{ODN6Mkez
ALL-SIL M3SyR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fXU|HjiIoQvF2= MXS3JIQ> M3rkfYRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? NIqxU2YzOzB|OEK3Ny=>
KE37 MoXsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETWOpUy6oDLzszN NFXM[Wg4KGR? MYfk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> NYq5U217OjNyM{iyO|M>
Karpas-45 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnf3NgKBkc7:TR?= MUW3JIQ> M3;SRYRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? NYjUV4R[OjNyM{iyO|M>
RPMI-8402 MonnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPVcGoy6oDLzszN NWnzeZdPPyCm Mm\W[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 NF3Hb5YzOzB|OEK3Ny=>
Jurkat MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXyx5qCK|ryP NX\KcIgyPyCm MV3k[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> MVWyN|A{QDJ5Mx?=
MOLT-4 NY[1S2ZNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPpTpIy6oDLzszN NV7iZWR7PyCm MlvL[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 M2PqZ|I{ODN6Mkez
PF-382 M{H4dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXKx5qCK|ryP MmHJO{Bl MWjk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> MUKyN|A{QDJ5Mx?=
CCRF-CEM M3L6Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH65XXYy6oDLzszN NH3yZo04KGR? NWHsVm5F\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 NV7nbVhiOjNyM{iyO|M>
LOUCY Ml;2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfPNgKBkc7:TR?= NEXUXVc4KGR? Mnvy[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 MUOyN|A{QDJ5Mx?=
MOLT-16 NEHGc3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV[2b5hPOeLCid88US=> NILqO484KGR? M33UNYRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? NFLu[mczOzB|OEK3Ny=>
MM1S NEn4eVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXKwMVIh|ryP MlnCNlQhcA>? MkLsTWM2OD1yLkWg{txO NH3xUYgzOjh{OUKzOC=>
NCI-H929 NFnqR3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjzNE0zKM7:TR?= NInaVZAzPCCq Mn3iTWM2OD1yLkK1JO69VQ>? MUWyNlgzQTJ|NB?=
KMS12-BM  NV3zUnBWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYX0[|NIOC1{IN88US=> MoLINlQhcA>? NYTHe4lPUUN3MP-8olIh|ryP MXeyNlgzQTJ|NB?=
MDA-MB-436 NF\hOGJHfW6ldHnvckBCe3OjeR?= NH3vbIgyKM7:TR?= MoPUNlQhcA>? NFixeIhz\WS3Y3XzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvU NVXmVVBGOjJ2OEi1PVA>
SUM149PT M1q5RWZ2dmO2aX;uJGF{e2G7 MkHINUDPxE1? NFrPcpEzPCCq NXLsbWhGemWmdXPld{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWC=> M2G5VFIzPDh6NUmw
SUM1315MO2 MkTMSpVv[3Srb36gRZN{[Xl? M1nhflEh|ryP MlzkNlQhcA>? MlfWdoVlfWOnczD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVB?= NWPRe5ZDOjJ2OEi1PVA>
HCC1937 NF;mbYZHfW6ldHnvckBCe3OjeR?= NITCbXkyKM7:TR?= M13UflI1KGh? MUjy[YR2[2W|IITo[UBxcG:|cHjvdplt[XSrb36gc4YhSUuW M4rpdVIzPDh6NUmw
HCC827 NFXRVXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXENE0{KM7:TR?= NIL2Npc4OiCq NGPlPGdKSzVyPUCuN{DPxE1? M3rFb|IyOjJyNEe0
PC-9  MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7jNE0{KM7:TR?= NGPiN484OiCq MlPxTWM2OD1yLkig{txO NWW1PZZjOjF{MkC0O|Q>
LN229 M3rFSWZ2dmO2aX;uJGF{e2G7 NV7OXXVoOSEQvF2= MoHVOFghcA>? NXLVTZk1cW6mdXPld{BifXSxcHjh[49{d22nIH\vdo1ifGmxbh?= NXflepdTOjFyNkK5PVM>
U87 M{LGfGZ2dmO2aX;uJGF{e2G7 M4LiUFEh|ryP M1XZb|Q5KGh? Mm\jbY5lfWOnczDheZRweGijZ3;zc41mKG[xcn3heIlwdg>? M2\yU|IyODZ{OUmz
U373 MVrGeY5kfGmxbjDBd5NigQ>? NWq4TIU2OSEQvF2= MXy0PEBp MYDpcoR2[2W|IHH1eI9xcGGpb4PvcYUh\m:{bXH0bY9v M{nndFIyODZ{OUmz
SF767 NXrW[YV5TnWwY4Tpc44hSXO|YYm= NF\1cZoyKM7:TR?= NGTRTI41QCCq MkHEbY5lfWOnczDheZRweGijZ3;zc41mKG[xcn3heIlwdg>? MVmyNVA3Ojl7Mx?=
Mel-Juso M4LuVGNmdGxiVnnhZoltcXS7IFHzd4F6 M{HNOFAvODIkgKOxNQKBkc7:TR?= M4TFdVczKGh? Mnj6bY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NVPLRnVkOjFyNEi3PFU>
518A2  Mmr1R4VtdCCYaXHibYxqfHliQYPzZZk> M3:5NlAvODIkgKOxNQKBkc7:TR?= MlXYO|IhcA>? MnrLbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MYeyNVA1QDd6NR?=
Mel-Juso  M1nORWZ2dmO2aX;uJGF{e2G7 NUXzdWlsOC5yMEJihLMy6oDLzszN NHPFeHYzPCCq NV3q[pRCe3WycILld5NmeyCyaH;zdIhwenmuYYTpc44hd2ZicHjvd5Bp[XSrZInsJIlvd3OrdH;sJFMuc2mwYYPlJIRwf26|dILlZY0hfGG{Z3X0dy=> Ml73NlExPDh5OEW=
518A2 M4C1RWZ2dmO2aX;uJGF{e2G7 NXOybHlwOC5yMEJihLMy6oDLzszN NEnKRoUzPCCq NH36VXJ{fXCycnXzd4V{KHCqb4PwbI9zgWyjdHnvckBw\iCyaH;zdIhifGmmeXygbY5we2m2b3ygN{1scW6jc3Wg[I94dnO2cnXhcUB1[XKpZYTz NWHkd5VOOjFyNEi3PFU>
PC3  MoLaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVf5O|JOOjSq NYHXdplrT0l3MNMgQUAyODBibl2= M2f1b|IxPTVzME[x
U87MG M1\2UWZ2dmO2aX;uJGF{e2G7 MkjGNE4yNTFizszN MVeyOQKBkWkEoB?= MmHSSG1UVw>? MkfzbY5pcWKrdIOgVGk{Uy2vZXTpZZRm\CC|aXfuZYxqdmd? NGHkXZYyQTZ|M{[4Ny=>
U138MG M3vrdmZ2dmO2aX;uJGF{e2G7 NWXLWGl1OC5zLUGg{txO NWm3bHh2OjUkgJnoxsA> M1LZd2ROW09? MoTTbY5pcWKrdIOgVGk{Uy2vZXTpZZRm\CC|aXfuZYxqdmd? NUf0e2hOOTl4M{O2PFM>
U118MG MUPGeY5kfGmxbjDBd5NigQ>? NETsSowxNjFvMTFOwG0> Mn;6NlTjiImqwrC= MVPEUXNQ MmHjbY5pcWKrdIOgVGk{Uy2vZXTpZZRm\CC|aXfuZYxqdmd? MnPhNVk3OzN4OEO=
U87MG M132UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTBwMUSg{txO MlLZNVk2QDR{Mke=
IGROV-1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7DN2dMUUN3ME2wMlA3KM7:TR?= MnfoNVk2QDR{Mke=
DETROIT562 NFTiV2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHOTWM2OD1yLkGzJO69VQ>? NIDwdVQyQTV6NEKyOy=>
PC3  NIPpSINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\GTWM2OD1yLkGwJO69VQ>? M{DL[VE6PTh2MkK3
SKOV-3 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTBwMUKg{txO NWn5dJdFOTl3OESyNlc>
HUVEC NGq1d5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTBwMEig{txO MXOxPVU5PDJ{Nx?=
UCH-1  NUTh[nNYTnWwY4Tpc44hSXO|YYm= Mn;YNE02KM7:TR?= M{\hSolvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiYn;0bEBCU1RiYX7kJI1VV1JiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M3nUWlE6PTJ6NESx
UCH-1  M1zOZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmruNE4xOS1zMDFOwG0> NWDOfXpjPiCm NVLzWWRXcW6qaXLpeJMheHKxbHnm[ZJifGmxbjDkc5NmKGSncHXu[IVvfGy7 MVyxPVUzQDR2MR?=
UCH-1  M1KzNGFxd3C2b4Ppd{BCe3OjeR?= NGL5V|UxNjFvMUCg{txO NUi5TGY1OjRiaB?= MWLEUXNQ NH;PcohqdmS3Y3XzJIFxd3C2b4Ppdy=> M2f0e|E6PTJ6NESx

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-AKT / AKT / p-S6K / S6K / p-S6 / S6 / p-p38 / p38; 

PubMed: 18922908     


Immunodetection of the levels of P-Akt, Akt, P-S6K, S6K, P-S6, S6, P-p38 or p38 of EC-vGPCR cells treated with increasing doses of PI-103 or DMSO (control) for 6 hours.

p-GSK3 / GSK3 / p-BAD / BAD / p-MDM2 / MDM2 / p-p27 / p27 ; 

PubMed: 18922908     


Immunodetection of the levels of P-Akt, Akt, P-GSK3, GSK3, P-BAD BAD, P-Mdm2, Mdm2, P-p27 or p27 of EC-vGPCR cells treated with increasing doses of PI-103 or DMSO (control) for 6 hours.

β-TrCP1 / p-mTOR; 

PubMed: 25721419     


PI-103 reduced the level of β-TrCP1 protein in TNBC cells. Cells were treated with 3 μm of PI-103 for 24 h and subjected to western blot analysis with indicated antibodies. HSP90 or β-actin was used as a loading control.

18922908 25721419
Immunofluorescence
autophagosomes / autolysosomes; 

PubMed: 26814436     


mRFP-GFP-LC3 stably expressing HeLa cells were treated with vehicle, PI (1uM), Baf (100nM) or PI (1uM)+Baf (100nM) for 20 hours. Cells were then fixed and confocal images were acquired. The numbers of autophagosomes (green vesicles) and autolysosomes (red vesicles minus green vesicles) were assessed with automated Cellomics microscopy (n = 12). Data are shown as mean ±sd. ***: P < 0.001. Scale bar: 20um.

26814436
Growth inhibition assay
Cell viability; 

PubMed: 25721419     


PI-103 reduced the viable TNBC cells in a dose-dependent manner. Cells were treated with increasing amounts of PI-103 up to 72 h and the viable cells were measured by MTT assay. Data from two independent experiments performed in triplicate are shown as mean±s.e.m.

25721419
In vivo When tumors reach 50-100 mm3, animals are randomized and treated with vehicle or PI-103. PI-103 exhibits significant activity, decreasing average tumor size by 4-fold after 18 days. [2] Mice treated with PI-103 have no obvious signs of toxicity premorbidly (based on body weight, food and water intake, activity, and general exam) or at necropsy. Treated tumors display decreased levels of phosphorylated Akt and S6, consistent with blockade of p110α and mTOR. PI-103 treatment is cytostatic to glioma xenografts. [2]

Protocol

Kinase Assay:[3]
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Enzyme Assays:

Phosphatidylinositide 3-kinase inhibitory activity was determined using a scintillation proximity assay in the presence of 1 μmol/L ATP. Inhibition of mTOR protein kinase was determined using a TR-FRET-based LanthaScreen method from Invitrogen. Compounds were assayed at a maximum concentration of 10 μmol/L in the presence of 1 μmol/L ATP, and IC50 values were determined using GraphPad Prism software.
Cell Research:[2]
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  • Cell lines: U87MG cells
  • Concentrations: 0.5 μM
  • Incubation Time: 24 hours
  • Method: U87MG cells are treated with PI-103 for 24 hours. Cell death is quantified by colorimetric determination of LDH activity using a cytotoxicity detection kit. Percentage of cell death (mean of three 12-well plates per experimental point) is calculated [(experimental value- low control)/(high control -low control) × 100], where the low-control cells are DMSO treated and high-control cells are Triton treated (1% Triton X-100, 30 min, 37 °
    (Only for Reference)
Animal Research:[2]
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  • Animal Models: 6- to 12-week-old Balbc nu/nu mice bearing U87MG:ΔEGFR cells
  • Dosages: 5 mg/kg
  • Administration: Administered via i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 24 mg/mL (68.89 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%ddH2O
For best results, use promptly after mixing.
1 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 348.36
Formula

C19H16N4O3

CAS No. 371935-74-9
Storage powder
in solvent
Synonyms N/A
Smiles OC1=CC(=CC=C1)C2=NC3=C(OC4=C3C=CC=N4)C(=N2)N5CCOCC5

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

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

Mass Concentration Volume Molecular Weight

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

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

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID