PI-103

For research use only.

Catalog No.S1038

64 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. PI-103 induces apoptosis in murine T-cell Lymphoma.

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10mM (1mL in DMSO) EUR 131 In stock
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Selleck's PI-103 has been cited by 64 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. PI-103 induces apoptosis in murine T-cell Lymphoma.
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 M{X4U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjCUVl1OC16IN88US=> NVXi[YJuOjRxNEivO|IhcA>? MoLNbY5lfWOnczD0bY1mNSCjbnSgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRiaX7obYJqfGmxbjDvckBPSiClZXzsJIdzd3e2aB?= M1[xTVI3OjJ2Nkix
SH-SY5Y NInnU4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPWcJpEOC16IN88US=> MnHQNlQwPDhxN{KgbC=> MYDpcoR2[2W|IITpcYUuKGGwZDDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCrbnjpZol1cW:wIH;uJG5DKGOnbHyg[5Jwf3Sq Mof6NlYzOjR4OEG=
SH-SY5Y  Mn7ORZBweHSxc3nzJGF{e2G7 M3j2elEh|ryP M3vSfFAvPS1{NDDo NFTRfWd{\W6|aYTpfoV{KG6ndYLvZoxie3SxbXGgZ4VtdHNidH:g[I95d3K3YnnjbY4ucW6mdXPl[EBieG:ydH;zbZM> MXSyOlIzPDZ6MR?=
G 35 SC NXnLTYpnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX6wMlA2NTJyIN88US=> MnH2NlQwPzJiaB?= MmDZSG1UVw>? MmOwbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBidmRidHnt[UBl\XCnbnTlcpRtgQ>? MnPMNlYyOjF{NUG=
G 38 SC NW\CeHRTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFe0VWcxNjB3LUKwJO69VQ>? M1HaRVI1Nzd{IHi= NGLBVm9FVVOR NYHqRpUxcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= NWS5enI6OjZzMkGyOVE>
G 40 SC MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jhflAvODVvMkCg{txO NHzjXmIzPC95MjDo NHPGe|lFVVOR NFu2[G1qdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 Ml\3NlYyOjF{NUG=
G 35 DC NWjJXpFkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\ubVAvODVvMkCg{txO NFm2PWgzPC95MjDo M{PE[WROW09? MXPpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueIx6 M{npblI3OTJzMkWx
G 38 DC M1mxVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTGNE4xPS1{MDFOwG0> NHTsT24zPC95MjDo NFnJeJhFVVOR M1Pn[IlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? NHLaelEzPjF{MUK1NS=>
G 40 DC NIKwRWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fPbFAvODVvMkCg{txO NIH6bpEzPC95MjDo M1K1b2ROW09? NIHWVFJqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 NEnHfoozPjF{MUK1NS=>
RD MkHHRZBweHSxc3nzJGF{e2G7 M3zS[|EwOS53L{Kg{txO MWi3NkBp MlzvbY5lfWOnczDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCJQV7UOlE> M3rJWFI2PzR7M{e4
TE381.T NH;FO5FCeG:ydH;zbZMhSXO|YYm= M1Pl[lEwOS53L{Kg{txO MYe3NkBp M1zReYlv\HWlZYOgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiR1HOWFYy NU\nZ|hKOjV5NEmzO|g>
RMS13 NF\aT5JCeG:ydH;zbZMhSXO|YYm= NV7vVZlvOS9zLkWvNkDPxE1? M3LQSlczKGh? M4r0dolv\HWlZYOgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiR1HOWFYy M{PoW|I2PzR7M{e4
RH30  M2PXcWFxd3C2b4Ppd{BCe3OjeR?= MYOxM|EvPS9{IN88US=> M2jicVczKGh? NE[5[oNqdmS3Y3XzJIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIFfBUnQ3OQ>? NV\Ec|lROjV5NEmzO|g>
VJ M3znSGFxd3C2b4Ppd{BCe3OjeR?= NX7EOVFSOS9zLkWvNkDPxE1? MnT5O|IhcA>? NHjqXZRqdmS3Y3XzJIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIFfBUnQ3OQ>? MYGyOVc1QTN5OB?=
HS578T M3HmNmNmdGxiVnnhZoltcXS7IFHzd4F6 MkfaNE0{KM7:TR?= NYPa[FZRPzJiaB?= NWfWVFAxcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MY[yOVczOTRzOR?=
BT549 MWXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MWKwMVMh|ryP NU\pO|BxPzJiaB?= Mm\WbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NFOxNo8zPTd{MUSxPS=>
MDA-MB-231 M3jHO2NmdGxiVnnhZoltcXS7IFHzd4F6 M4fReVAuOyEQvF2= NUjV[pV5PzJiaB?= MlPobY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NIPtWogzPTd{MUSxPS=>
MDA-MB-468 NGHFSHhE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MXOwMVMh|ryP M4H6TlczKGh? NEjVSo1qdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NVHob2wyOjV5MkG0NVk>
MDA-MB-436 NHPINIFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MmfPNE0{KM7:TR?= NIXhNG04OiCq NXXTfWZWcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MonTNlU4OjF2MUm=
SUM149PT NHHEO2VE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MYmwMVMh|ryP MUi3NkBp NX\DXlVrcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MXeyOVczOTRzOR?=
MDA-MB-468 NIrUOHBHfW6ldHnvckBCe3OjeR?= NX24[|N7OC5yMT2xNEDPxE1? NULQb5VOOjRiaB?= MmXa[I94dnKnZ4XsZZRmeyC2aHWgcIV3\Wy|IH;mJO6zNVS{Q2CxMEBkNU27YzDhcoQh[3mlbHnuJGUheHKxdHXpcpPDqA>? NIjwSpMzPTd{MUSxPS=>
MDA-MB-231 MXjGeY5kfGmxbjDBd5NigQ>? NFvkVFYxNjBzLUGwJO69VQ>? NVjXW4NEOjRiaB?= MWfkc5dvemWpdXzheIV{KHSqZTDs[ZZmdHNib3[g{tIuXHKFUEGsJIMuVXmlIHHu[EBkgWOuaX6gSUBxem:2ZXnud:Kh MmjBNlU4OjF2MUm=
HS578T M1fRU2Z2dmO2aX;uJGF{e2G7 MoLxNE4xOS1zMDFOwG0> NIrYS5gzPCCq MknC[I94dnKnZ4XsZZRmeyC2aHWgcIV3\Wy|IH;mJO6zNVS{Q2CxMEBkNU27YzDhcoQh[3mlbHnuJGUheHKxdHXpcpPDqA>? NG\vUXYzPTd{MUSxPS=>
SW872 M4rBNGZ2dmO2aX;uJGF{e2G7 NUnyclMzOC5yMT2wMlUh|ryP M1j5RlI1KGh? M2fjWpJm\HWlZYOgRWtVKHCqb4PwbI9zgWyjdHnvckApeEGNVDmgZY5lKDSHQmCxJJBpd3OyaH;yfYxifGmxbjCodFRGSlBzKTDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nctMg NWjudHJ[OjR4OUW2N|I>
SW982 MVLGeY5kfGmxbjDBd5NigQ>? M{fR[lAvODFvMD61JO69VQ>? NFW2ZmMzPCCq MWXy[YR2[2W|IFHLWEBxcG:|cHjvdplt[XSrb36gLJBCU1RrIHHu[EA1TUKSMTDwbI9{eGixconsZZRqd25iKIC0SWJROSliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= NWHON4g1OjR4OUW2N|I>
SW872 M{fHUmFxd3C2b4Ppd{BCe3OjeR?= MX[wMlAyNTBwNTFOwG0> MUe0PEBp NUfNWlBzcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NH\aXnYzPDZ7NU[zNi=>
SW982 MYXBdI9xfG:|aYOgRZN{[Xl? M4PCVFAvODFvMD61JO69VQ>? NF;U[m41QCCq M2SxV4lv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NH;aT3kzPDZ7NU[zNi=>
AGS HG MlXkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvUTWM2OD1yLk[4JOKyKDBwMEOxJO69VQ>? MkjlNlQ2QTd2N{i=
AGS LG NVzvRohIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfUNFlKSzVyPUCuNFUhyrFiMD6wNFEh|ryP NHX6Wm0zPDV7N{S3PC=>
HGC27 HG NH\xbZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfibopKSzVyPUCuN|ghyrFiMD6wNlIh|ryP M1fJS|I1PTl5NEe4
HGC27 LG MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LGTGlEPTB;MD6wNkDDuSByLkCwOEDPxE1? MVeyOFU6PzR5OB?=
MKN45 HG MkfaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17vNmlEPTB;MT6wNUDDuSByLkC1NUDPxE1? MVWyOFU6PzR5OB?=
MKN45 LG MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Moq4TWM2OD1yLki3JOKyKDBwMEOwJO69VQ>? MmLXNlQ2QTd2N{i=
NUGC4 HG NIjYOo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVmyeYptUUN3ME2xOE4xKMLzIEOuPVE{KM7:TR?= MV[yOFU6PzR5OB?=
NUGC4 LG NYLoZ2o6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLO[IZFUUN3ME2xOE4xKMLzIEWuN|IyKM7:TR?= NEfLd5MzPDV7N{S3PC=>
A549 MnzjSpVv[3Srb36gRZN{[Xl? NU\sfmpHOC5{NT:wMlUwOSEQvF2= NVTmbYJWOjRiaB?= MX7pcohq[mm2czDBb5QheGixc4Doc5J6dGG2aX;uJJNtcWeqdHz5 MYSyOFM2OTR{NR?=
H460 NFL2R5lHfW6ldHnvckBCe3OjeR?= NVnkeY5TOC5{NT:wMlUwOSEQvF2= MXeyOEBp NGO4fndqdmirYnn0d{BCc3RicHjvd5Bpd3K7bHH0bY9vKHOuaXfoeIx6 NI[3[IkzPDN3MUSyOS=>
H661 NXLsNlZvTnWwY4Tpc44hSXO|YYm= Mme3NE4zPS9yLkWvNUDPxE1? NHO2bmkzPCCq MYDpcohq[mm2czDBb5QheGixc4Doc5J6dGG2aX;uJJNq\26rZnnjZY51dHl? MnXwNlQ{PTF2MkW=
SAS NUS0[W5STnWwY4Tpc44hSXO|YYm= MYWwMlI2NzBwNT:xJO69VQ>? MoCxNlQhcA>? MknTbY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7 NVXsbGczOjR|NUG0NlU>
UT5 M3jMT2Z2dmO2aX;uJGF{e2G7 NHv2cYwxNjJ3L{CuOU8yKM7:TR?= MnG3NlQhcA>? NF\ueZhqdmirYnn0d{BCc3RicHjvd5Bpd3K7bHH0bY9vKHOrZ37p[olk[W62bIm= MVOyOFM2OTR{NR?=
FaDu MoC1SpVv[3Srb36gRZN{[Xl? M3juWlAvOjVxMD61M|Eh|ryP NHXMSJIzPCCq NHzmT5pqdmirYnn0d{BCc3RicHjvd5Bpd3K7bHH0bY9vKHOrZ37p[olk[W62bIm= MWSyOFM2OTR{NR?=
RD NWLqW|R1SXCxcITvd4l{KEG|c3H5 NX3OZXhsOS9zLkWvNkDPxE1? M3\lR|czKGh? M1zPUGROW09? MlrJbY5lfWOnczDjZZNx[XOnLXTldIVv\GWwdDDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCXT{GyOi=> M2fUO|I{Pjh2OUK1
TE671 MnL6RZBweHSxc3nzJGF{e2G7 NH7FcGgyNzFwNT:yJO69VQ>? MWG3NkBp NF\heI5FVVOR NYTiOY9xcW6mdXPld{Bk[XOyYYPlMYRmeGWwZHXueEBieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDVU|EzPg>? Mn\GNlM3QDR7MkW=
RH30  NH3lWpdCeG:ydH;zbZMhSXO|YYm= M3m2VlEwOS53L{Kg{txO NUO5NXVVPzJiaB?= NUTGTo95TE2VTx?= MXfpcoR2[2W|IHPhd5Bie2VvZHXw[Y5l\W62IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKFWRMUK2 NUC5UWs1OjN4OES5NlU>
RMS13 MkjQRZBweHSxc3nzJGF{e2G7 MUGxM|EvPS9{IN88US=> MV[3NkBp NHX4XndFVVOR M3izSolv\HWlZYOgZ4F{eGG|ZT3k[ZBmdmSnboSgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiVV:xNlY> M3\IbFI{Pjh2OUK1
SUM149PT MUDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NHX3NVIxNjNizszN M{TINFczKGh? M{C3Z4VvcGGwY3XzJIN6fG:2b4jpZ{Bm\m[nY4TzJI9nKFCLM1uvRWtVKHCjdHj3ZZkhcW6qaXLpeI9zew>? NI\2b2MzOzZyMUC3OC=>
MDA-MB-468 NXi0cJdtS2WubDDWbYFjcWyrdImgRZN{[Xl? NXnY[HVrOC5|IN88US=> M1zP[FczKGh? M3\jVoVvcGGwY3XzJIN6fG:2b4jpZ{Bm\m[nY4TzJI9nKFCLM1uvRWtVKHCjdHj3ZZkhcW6qaXLpeI9zew>? MXyyN|YxOTB5NB?=
MDA-MB-231 M1z0PWNmdGxiVnnhZoltcXS7IFHzd4F6 Ml:1NE4{KM7:TR?= NVy5fI9TPzJiaB?= NXTscnlr\W6qYX7j[ZMh[3m2b4TvfIlkKGWoZnXjeJMhd2ZiUFmzT{9CU1RicHH0bJdigSCrbnjpZol1d3K| Ml\TNlM3ODFyN{S=
SY5Y MWrGeY5kfGmxbjDBd5NigQ>? M4\SclEvPS9{LkWvOUDPxE1? NVG3Z4RGOjRiaB?= NWHMSJl3cW6mdXPld{BIOcLiY3XscE1kgWOuZTDhdpJme3RiYX7kJIFxd3C2b4Ppdy=> NFjFeGwzOzN5OEO0NS=>
SKNBE(2c) NFf6eJZHfW6ldHnvckBCe3OjeR?= MYCxMlUwOi53L{Wg{txO M{DYTlI1KGh? Mof6bY5lfWOnczDHNeKh[2WubD3jfYNt\SCjcoLld5Qh[W6mIHHwc5B1d3Orcx?= M3m2flI{Ozd6M{Sx
RD M37wdmFxd3C2b4Ppd{BCe3OjeR?= NWCxfVlqOyEEtV2= NX3FUlE6OTJiaB?= NI\Rd|ZFVVOR MlLGd4Vve2m2aYrld{BTTCClZXzsd{B1dyCGT2itbY5lfWOnZDDhdI9xfG:|aYO= M3j6NFI{OzByOEC5
TP5014 NGnzeoVCeG:ydH;zbZMhSXO|YYm= NHOye5Y{KML3TR?= M33CXlEzKGh? NXvIWlBiTE2VTx?= NEnuXXF{\W6|aYTpfoV{KFKGIHPlcIx{KHSxIFTPXE1qdmS3Y3XkJIFxd3C2b4Ppdy=> NGTBZ5IzOzNyMEiwPS=>
HT1080 NX\GeHFDSXCxcITvd4l{KEG|c3H5 M{nkRVMhyrWP MkL0NVIhcA>? MnHLSG1UVw>? NHnq[IF{\W6|aYTpfoV{KFKGIHPlcIx{KHSxIFTPXE1qdmS3Y3XkJIFxd3C2b4Ppdy=> NGC4XVEzOzNyMEiwPS=>
A549 M4TQVmZ2dmO2aX;uJGF{e2G7 NITQVGwxNTNwMzFOwG0> MXO3NkBp MVHpcoR2[2W|IHPvcZBt\XSnIHTve45z\We3bHH0bY9vKG:oIIDBT3Q> MViyN|I2QTV7MR?=
HCC827 NIDtT5BHfW6ldHnvckBCe3OjeR?= NFXxVpExNTNwMzFOwG0> NV\td5BXPzJiaB?= M1Xrb4lv\HWlZYOgZ49ueGyndHWg[I94dnKnZ4XsZZRqd25ib3[gdGFMXA>? MkP3NlMzPTl3OUG=
H3122 NFjGdFdHfW6ldHnvckBCe3OjeR?= M12wb|AuOy5|IN88US=> NHvk[YE4OiCq MYLpcoR2[2W|IHPvcZBt\XSnIHTve45z\We3bHH0bY9vKG:oIIDBT3Q> NVSzOJRmOjN{NUm1PVE>
TALL-1 NX;sZ4NnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;tNgKBkc7:TR?= NIHzR2E4KGR? Mof5[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 MXSyN|A{QDJ5Mx?=
HPB-ALL MnnYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHZcnMy6oDLzszN NF3BPGQ4KGR? M1rEVoRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? NE\5R3AzOzB|OEK3Ny=>
DND41 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\lTYREOeLCid88US=> NX7W[2xoPyCm MYXk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> M{fmPVI{ODN6Mkez
SUP-T1 NF:3fI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYCx5qCK|ryP NXjv[pNnPyCm MVnk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> Mnq4NlMxOzh{N{O=
PEER MljDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHUNm0y6oDLzszN NYHJemJzPyCm MX7k[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> NV7FOZAzOjNyM{iyO|M>
ALL-SIL MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYW1PYNSOeLCid88US=> NEjRTmc4KGR? NFS0TWtl\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? NU\IbolHOjNyM{iyO|M>
KE37 NWXvPY54T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPBZmIy6oDLzszN MWK3JIQ> NFjRTWpl\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? MkXaNlMxOzh{N{O=
Karpas-45 MnnNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPCeJEy6oDLzszN MXy3JIQ> NHSwbmhl\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? NV;iN5NmOjNyM{iyO|M>
RPMI-8402 M4\TSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGriN5Iy6oDLzszN NFTKOIE4KGR? MlnB[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 NHL1bJgzOzB|OEK3Ny=>
Jurkat MmO5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUOx5qCK|ryP NH7XdoQ4KGR? NUfJXlFN\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 M4\1UlI{ODN6Mkez
MOLT-4 M4L6ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYex5qCK|ryP M4HwWFch\A>? Ml[3[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 NX7iUnVrOjNyM{iyO|M>
PF-382 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnFV4l4OeLCid88US=> MUO3JIQ> MXjk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> MWeyN|A{QDJ5Mx?=
CCRF-CEM MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWix5qCK|ryP M3;SPFch\A>? Mn6z[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 NX3ZfFV7OjNyM{iyO|M>
LOUCY NYXLWGZiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHP[IpnOeLCid88US=> MUW3JIQ> NGXSRZJl\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? NX3zXHBxOjNyM{iyO|M>
MOLT-16 NVzWOJJWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPTS|Ey6oDLzszN NUPaVJh2PyCm MX;k[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> NEL3S|QzOzB|OEK3Ny=>
MM1S MnezS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3H4eVAuOiEQvF2= M1fkWFI1KGh? NXy1epp7UUN3ME2wMlUh|ryP MnKwNlI5Ojl{M{S=
NCI-H929 NYXneGNQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjEVooxNTJizszN MXSyOEBp MoO4TWM2OD1yLkK1JO69VQ>? Mme5NlI5Ojl{M{S=
KMS12-BM  Ml;GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXDNE0zKM7:TR?= NIXKT5ozPCCq M4X1TmlEPTExvK6yJO69VQ>? NGjzWFYzOjh{OUKzOC=>
MDA-MB-436 MlT5SpVv[3Srb36gRZN{[Xl? NV3tV|JYOSEQvF2= NHfFT48zPCCq MWjy[YR2[2W|IITo[UBxcG:|cHjvdplt[XSrb36gc4YhSUuW MVGyNlQ5QDV7MB?=
SUM149PT Mlf5SpVv[3Srb36gRZN{[Xl? NEHq[4cyKM7:TR?= MV[yOEBp MlTjdoVlfWOnczD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVB?= MUKyNlQ5QDV7MB?=
SUM1315MO2 NGf6R5RHfW6ldHnvckBCe3OjeR?= MV6xJO69VQ>? MXGyOEBp M4G4PJJm\HWlZYOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2S= MX6yNlQ5QDV7MB?=
HCC1937 NX7vPVczTnWwY4Tpc44hSXO|YYm= M{\hUlEh|ryP NXHoe256OjRiaB?= MWjy[YR2[2W|IITo[UBxcG:|cHjvdplt[XSrb36gc4YhSUuW NWXm[VZ6OjJ2OEi1PVA>
HCC827 M2jQd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnTUXAxNTNizszN NGTDXVU4OiCq M1\yfmlEPTB;MD6zJO69VQ>? NYfKdmNpOjF{MkC0O|Q>
PC-9  MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PHTFAuOyEQvF2= NUnPW5dMPzJiaB?= NVrNVmZ6UUN3ME2wMlgh|ryP NFzk[Y4zOTJ{MES3OC=>
LN229 MXfGeY5kfGmxbjDBd5NigQ>? NUWwUWxnOSEQvF2= NFT0RpM1QCCq M3Tsfolv\HWlZYOgZZV1d3CqYXfvd49u\SCob4LtZZRqd25? M{XyRVIyODZ{OUmz
U87 NHzUfVVHfW6ldHnvckBCe3OjeR?= NWjVWnViOSEQvF2= MYq0PEBp MmLwbY5lfWOnczDheZRweGijZ3;zc41mKG[xcn3heIlwdg>? NHftUHIzOTB4Mkm5Ny=>
U373 MYHGeY5kfGmxbjDBd5NigQ>? MUOxJO69VQ>? M{P6fFQ5KGh? M2Xsdolv\HWlZYOgZZV1d3CqYXfvd49u\SCob4LtZZRqd25? NV3QU4d[OjFyNkK5PVM>
SF767 NGS2VJhHfW6ldHnvckBCe3OjeR?= NE[4U2IyKM7:TR?= MUm0PEBp MljDbY5lfWOnczDheZRweGijZ3;zc41mKG[xcn3heIlwdg>? NYDCPXRpOjFyNkK5PVM>
Mel-Juso MYPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NVHsNYkyOC5yMfMAl|Ex6oDLzszN MnfLO|IhcA>? NX3LUZZycW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NXPZNFdxOjFyNEi3PFU>
518A2  NGiyZWFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MU[wMlAy6oDVMUFihKnPxE1? M3HvRlczKGh? NHr3WIRqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MWSyNVA1QDd6NR?=
Mel-Juso  MUPGeY5kfGmxbjDBd5NigQ>? NVPKWYl5OC5yMEJihLMy6oDLzszN Mmm4NlQhcA>? M3e3cJN2eHC{ZYPz[ZMheGixc4Doc5J6dGG2aX;uJI9nKHCqb4PwbIF1cWS7bDDpco9{cXSxbDCzMYtqdmG|ZTDkc5dve3S{ZXHtJJRiemendIO= NUjNO5ByOjFyNEi3PFU>
518A2 MmfVSpVv[3Srb36gRZN{[Xl? M{TkUVAvODBz4pETNgKBkc7:TR?= NVT4eGtqOjRiaB?= MYTzeZBxemW|c3XzJJBpd3OyaH;yfYxifGmxbjDv[kBxcG:|cHjheIllgWxiaX7vd4l1d2xiMz3rbY5ie2ViZH;3cpN1emWjbTD0ZZJo\XS| MmP0NlExPDh5OEW=
PC3  MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkW5NlRp NHv5UGJIUTVywrC9JFExOCCwTR?= MUiyNFU2OTB4MR?=
U87MG NYLZW3cyTnWwY4Tpc44hSXO|YYm= NUXVeGVmOC5zLUGg{txO NIf5UpYzPOLCiXlCpC=> M3TuPWROW09? NGLN[GlqdmirYnn0d{BRUTONLX3l[IlifGWmIIPp[45idGmwZx?= NITDeHgyQTZ|M{[4Ny=>
U138MG NHjjbXlHfW6ldHnvckBCe3OjeR?= Mn3UNE4yNTFizszN MX2yOQKBkWkEoB?= M3fMUWROW09? M{\sdolvcGmkaYTzJHBKO0tvbXXkbYF1\WRic3nncoFtcW6p MkXBNVk3OzN4OEO=
U118MG MUfGeY5kfGmxbjDBd5NigQ>? MVewMlEuOSEQvF2= MYKyOQKBkWkEoB?= NUfid5FNTE2VTx?= MYfpcohq[mm2czDQTVNMNW2nZHnheIVlKHOrZ37hcIlv\w>? NUi3Om94OTl4M{O2PFM>
U87MG MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfZb5dKSzVyPUCuNVQh|ryP MUCxPVU5PDJ{Nx?=
IGROV-1 NFrocm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTBwME[g{txO M3fUT|E6PTh2MkK3
DETROIT562 M13JNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPvcnBKSzVyPUCuNVMh|ryP M1Kw[VE6PTh2MkK3
PC3  NFvrfoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTBwMUCg{txO NHv6TFEyQTV6NEKyOy=>
SKOV-3 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPETWM2OD1yLkGyJO69VQ>? NUKweY81OTl3OESyNlc>
HUVEC MmnzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXYZnpKSzVyPUCuNFgh|ryP M3uyZ|E6PTh2MkK3
UCH-1  NWjoVnNNTnWwY4Tpc44hSXO|YYm= NUHheHVGOC13IN88US=> NWHaOm8{cW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDic5RpKEGNVDDhcoQhdVSRUjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MVSxPVUzQDR2MR?=
UCH-1  NGjxenZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjVNE4xOS1zMDFOwG0> NFjRNFY3KGR? NFvTblVqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHTvd4Uh\GWyZX7k[Y51dHl? NWf6e483OTl3Mki0OFE>
UCH-1  MV\BdI9xfG:|aYOgRZN{[Xl? NWXZdmk6OC5zLUGwJO69VQ>? Ml7MNlQhcA>? NXLGdmhqTE2VTx?= NITxeo1qdmS3Y3XzJIFxd3C2b4Ppdy=> M2LsXVE6PTJ6NESx

... 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 C1COCCN1C2=NC(=NC3=C2OC4=C3C=CC=N4)C5=CC(=CC=C5)O

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 ()
% 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