PI-103

Catalog No.S1038

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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In DMSO USD 134 In stock
USD 147 In stock
USD 270 In stock
USD 370 In stock
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Cited by 38 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
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SH-SY5Y MlfrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDNWo9{OC16IN88US=> MnL5NlQwPDhxN{KgbC=> NIPuUopqdmS3Y3XzJJRqdWVvIHHu[EBkd26lZX70doF1cW:wLXTldIVv\GWwdDDpcohq[mm2aX;uJI9vKE6EIHPlcIwh\3Kxd4To MlqyNlYzOjR4OEG=
SH-SY5Y  MUHBdI9xfG:|aYOgRZN{[Xl? M3XHdVEh|ryP M4PxS|AvPS1{NDDo NYDvcmd7e2Wwc3n0bZpmeyCwZYXyc4Jt[XO2b33hJINmdGy|IITvJIRwgG:{dXLpZ4lvNWmwZIXj[YQh[XCxcITvd4l{ NFe2ZW0zPjJ{NE[4NS=>
G 35 SC NX\ZZmpbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjSNE4xPS1{MDFOwG0> MmfkNlQwPzJiaB?= MV;EUXNQ NET4bXdqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 MUSyOlEzOTJ3MR?=
G 38 SC MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLZNE4xPS1{MDFOwG0> MmLDNlQwPzJiaB?= MYrEUXNQ NFrTNGtqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 MnzINlYyOjF{NUG=
G 40 SC MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLtNE4xPS1{MDFOwG0> M3XZS|I1Nzd{IHi= M{DTPGROW09? M4faNYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? Mkj3NlYyOjF{NUG=
G 35 DC M2L3WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHEfY4xNjB3LUKwJO69VQ>? MnHpNlQwPzJiaB?= NWTsXYxbTE2VTx?= M2XXcYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? M2DvW|I3OTJzMkWx
G 38 DC MlzES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPTNE4xPS1{MDFOwG0> NF\2N2czPC95MjDo NE\wSpJFVVOR MY\pcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueIx6 NGLtWI8zPjF{MUK1NS=>
G 40 DC M2LSTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\FNI8xNjB3LUKwJO69VQ>? MVmyOE84OiCq M4WybGROW09? Mo[3bY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBidmRidHnt[UBl\XCnbnTlcpRtgQ>? M{XCTFI3OTJzMkWx
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SUM149PT NUPjT4NZS2WubDDWbYFjcWyrdImgRZN{[Xl? MX2wMVMh|ryP NXqxbWxNPzJiaB?= MXzpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NHW4PGozPTd{MUSxPS=>
MDA-MB-468 NGqxXpBHfW6ldHnvckBCe3OjeR?= NWjhcnhEOC5yMT2xNEDPxE1? MYWyOEBp NIXDbIZld3ewcnXneYxifGW|IITo[UBt\X[nbIOgc4Yh|rJvVILDVFEtKGNvTYnjJIFv\CCleXPsbY4hTSCycn;0[Ylve8Li NEnXeVIzPTd{MUSxPS=>
MDA-MB-231 M3ntPGZ2dmO2aX;uJGF{e2G7 M3vWSlAvODFvMUCg{txO NFrkd3MzPCCq MVHkc5dvemWpdXzheIV{KHSqZTDs[ZZmdHNib3[g{tIuXHKFUEGsJIMuVXmlIHHu[EBkgWOuaX6gSUBxem:2ZXnud:Kh NELhVVkzPTd{MUSxPS=>
HS578T M1LaTWZ2dmO2aX;uJGF{e2G7 NUHMWoJMOC5yMT2xNEDPxE1? MWKyOEBp NV;CeGJ2\G:5boLl[5Vt[XSnczD0bIUhdGW4ZXzzJI9nKM7{LWTyR3AyNCClLV35Z{BidmRiY4njcIlvKEVicILveIVqdnQEoB?= NIXqbpMzPTd{MUSxPS=>
SW872 NXmxU2k6TnWwY4Tpc44hSXO|YYm= M4ryfVAvODFvMD61JO69VQ>? MWeyOEBp NETaSYxz\WS3Y3XzJGFMXCCyaH;zdIhwenmuYYTpc44hMHCDS2SpJIFv\CB2RVLQNUBxcG:|cHjvdplt[XSrb36gLJA1TUKSMTmgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYNCpC=> MXqyOFY6PTZ|Mh?=
SW982 M3PONGZ2dmO2aX;uJGF{e2G7 MWmwMlAyNTBwNTFOwG0> NUDRVYtrOjRiaB?= NITaNFdz\WS3Y3XzJGFMXCCyaH;zdIhwenmuYYTpc44hMHCDS2SpJIFv\CB2RVLQNUBxcG:|cHjvdplt[XSrb36gLJA1TUKSMTmgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYNCpC=> MmDONlQ3QTV4M{K=
SW872 NF7MTVBCeG:ydH;zbZMhSXO|YYm= NX7DSGtlOC5yMT2wMlUh|ryP M{P5XFQ5KGh? NE[zeXhqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NF3mNXIzPDZ7NU[zNi=>
SW982 NVjrUZJqSXCxcITvd4l{KEG|c3H5 MVKwMlAyNTBwNTFOwG0> NULnS5VHPDhiaB?= MkLybY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NELjV|czPDZ7NU[zNi=>
AGS HG MnLUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTBwNkigxtEhOC5yM{Gg{txO M1TJXlI1PTl5NEe4
AGS LG NHfGS4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTBwMEWgxtEhOC5yMEGg{txO NFnOeFkzPDV7N{S3PC=>
HGC27 HG NHLPRWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTBwM{igxtEhOC5yMkKg{txO M3LtOFI1PTl5NEe4
HGC27 LG MojrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHoTo5CUUN3ME2wMlAzKMLzIECuNFA1KM7:TR?= MYqyOFU6PzR5OB?=
MKN45 HG NHj1elBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTFwMEGgxtEhOC5yNUGg{txO NUOwWJNmOjR3OUe0O|g>
MKN45 LG MmfFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYL4[nBnUUN3ME2wMlg4KMLzIECuNFMxKM7:TR?= NYrkfWkzOjR3OUe0O|g>
NUGC4 HG MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnBNWd[UUN3ME2xOE4xKMLzIEOuPVE{KM7:TR?= NIDzWWkzPDV7N{S3PC=>
NUGC4 LG MmfqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jkT2lEPTB;MUSuNEDDuSB3LkOyNUDPxE1? NITxZnIzPDV7N{S3PC=>
A549 NWS3c5dZTnWwY4Tpc44hSXO|YYm= NELybHExNjJ3L{CuOU8yKM7:TR?= NHLX[4czPCCq NXO2d|MxcW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|bHnnbJRtgQ>? MVeyOFM2OTR{NR?=
H460 NGqwS5ZHfW6ldHnvckBCe3OjeR?= MUmwMlI2NzBwNT:xJO69VQ>? NYnDR5FKOjRiaB?= M1TDUYlvcGmkaYTzJGFsfCCyaH;zdIhwenmuYYTpc44he2yrZ3j0cJk> MYWyOFM2OTR{NR?=
H661 MVjGeY5kfGmxbjDBd5NigQ>? NVzZSGFnOC5{NT:wMlUwOSEQvF2= M3:zTlI1KGh? NEDTU4FqdmirYnn0d{BCc3RicHjvd5Bpd3K7bHH0bY9vKHOrZ37p[olk[W62bIm= MnjTNlQ{PTF2MkW=
SAS M2fCdmZ2dmO2aX;uJGF{e2G7 MofUNE4zPS9yLkWvNUDPxE1? NXnL[WVKOjRiaB?= M2XESYlvcGmkaYTzJGFsfCCyaH;zdIhwenmuYYTpc44he2mpbnnmbYNidnSueR?= NHvWZo0zPDN3MUSyOS=>
UT5 MoPqSpVv[3Srb36gRZN{[Xl? NEe2coExNjJ3L{CuOU8yKM7:TR?= M2fGT|I1KGh? NXnTPJpFcW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|aXfubYZq[2GwdHz5 M4r3blI1OzVzNEK1
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RD MYTBdI9xfG:|aYOgRZN{[Xl? MXSxM|EvPS9{IN88US=> MVe3NkBp NU\n[|R[TE2VTx?= NELCZYRqdmS3Y3XzJINie3Cjc3Wt[IVx\W6mZX70JIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIGXPNVI3 NVzqelhQOjN4OES5NlU>
TE671 M2nnTWFxd3C2b4Ppd{BCe3OjeR?= NFm1d3gyNzFwNT:yJO69VQ>? NVPJSnR{PzJiaB?= MorLSG1UVw>? MljFbY5lfWOnczDjZZNx[XOnLXTldIVv\GWwdDDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCXT{GyOi=> NH\qTG8zOzZ6NEmyOS=>
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RMS13 NHy0TZVCeG:ydH;zbZMhSXO|YYm= MmTNNU8yNjVxMjFOwG0> NW\hRWRxPzJiaB?= NELTbXhFVVOR NIHjbG5qdmS3Y3XzJINie3Cjc3Wt[IVx\W6mZX70JIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIGXPNVI3 NGn0c|gzOzZ6NEmyOS=>
SUM149PT MYPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M1zZOVAvOyEQvF2= NULtblVFPzJiaB?= MnO4[Y5p[W6lZYOgZ5l1d3SxeHnjJIVn\mWldIOgc4YhWEl|Sz;BT3QheGG2aIfhfUBqdmirYnn0c5J{ MWWyN|YxOTB5NB?=
MDA-MB-468 NYX6e4F1S2WubDDWbYFjcWyrdImgRZN{[Xl? MXWwMlMh|ryP NEfWTYQ4OiCq NFjmXGRmdmijbnPld{BkgXSxdH;4bYMh\W[oZXP0d{Bw\iCSSUPLM2FMXCCyYYToe4F6KGmwaHnibZRwenN? NUK4VFdKOjN4MEGwO|Q>
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HT1080 MmXyRZBweHSxc3nzJGF{e2G7 MlnGN{DDvU1? M3\Me|EzKGh? NHO3OIdFVVOR M3TXPZNmdnOrdHn6[ZMhWkRiY3XscJMhfG9iRF;YMYlv\HWlZXSgZZBweHSxc3nz M{TUPFI{OzByOEC5
A549 NU\qVmM4TnWwY4Tpc44hSXO|YYm= MmHyNE0{NjNizszN NFPZRm44OiCq MVnpcoR2[2W|IHPvcZBt\XSnIHTve45z\We3bHH0bY9vKG:oIIDBT3Q> MW[yN|I2QTV7MR?=
HCC827 MoLrSpVv[3Srb36gRZN{[Xl? M2SyUFAuOy5|IN88US=> M122flczKGh? NHrPNYdqdmS3Y3XzJINwdXCuZYTlJIRwf26{ZXf1cIF1cW:wIH;mJJBCU1R? MVSyN|I2QTV7MR?=
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Karpas-45 NIOw[FJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLkNgKBkc7:TR?= NVrEW|NJPyCm Mni5[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 NY\zTHBROjNyM{iyO|M>
RPMI-8402 NXTmd3hrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLLU5hqOeLCid88US=> NX;Nd2hjPyCm NXHJcnVC\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 NEHVbYYzOzB|OEK3Ny=>
Jurkat Ml7RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV[x5qCK|ryP MmD3O{Bl M{T6T4Rm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? Mn;jNlMxOzh{N{O=
MOLT-4 M2LZ[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUex5qCK|ryP M{\hNlch\A>? NIfMfW1l\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? MkPWNlMxOzh{N{O=
PF-382 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HucFHjiIoQvF2= MlL5O{Bl Mljq[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 MknqNlMxOzh{N{O=
CCRF-CEM MnvJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LoNVHjiIoQvF2= NWTTXW5KPyCm MYPk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> MWeyN|A{QDJ5Mx?=
LOUCY NXjzXnU2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTvPVIy6oDLzszN NFW1Zpg4KGR? MYnk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> MVKyN|A{QDJ5Mx?=
MOLT-16 NIf3epJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVWx5qCK|ryP M2DuNFch\A>? NWnZbHZC\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 MVyyN|A{QDJ5Mx?=
MM1S NUnRR4V5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWL2b5Z{OC1{IN88US=> M2CzfFI1KGh? MV;JR|UxRTBwNTFOwG0> NFK2c5AzOjh{OUKzOC=>
NCI-H929 NV[4UFJCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjUd2kxNTJizszN NFLNc4MzPCCq NF7BTWZKSzVyPUCuNlUh|ryP Mmj6NlI5Ojl{M{S=
KMS12-BM  MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPBNE0zKM7:TR?= MUmyOEBp M2PJUmlEPTExvK6yJO69VQ>? MoDYNlI5Ojl{M{S=
MDA-MB-436 NHzpSHNHfW6ldHnvckBCe3OjeR?= NEHMcWcyKM7:TR?= NUi2TnBmOjRiaB?= NGjm[HFz\WS3Y3XzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvU NFzxNYYzOjR6OEW5NC=>
SUM149PT M3[0RWZ2dmO2aX;uJGF{e2G7 NGTZdZEyKM7:TR?= MnTwNlQhcA>? NIrSdGdz\WS3Y3XzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvU MnvQNlI1QDh3OUC=
SUM1315MO2 Mo\FSpVv[3Srb36gRZN{[Xl? NWDWSYxJOSEQvF2= MnPzNlQhcA>? M3\ofJJm\HWlZYOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2S= NUi2c49xOjJ2OEi1PVA>
HCC1937 M3:1WmZ2dmO2aX;uJGF{e2G7 MoH5NUDPxE1? MlnhNlQhcA>? MkftdoVlfWOnczD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVB?= MViyNlQ5QDV7MB?=
HCC827 NUjadY5ZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlL2NE0{KM7:TR?= MWO3NkBp NEXOdWFKSzVyPUCuN{DPxE1? MmHhNlEzOjB2N{S=
PC-9  MorhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjmV|AxNTNizszN NE\Rbpc4OiCq MUTJR|UxRTBwODFOwG0> NEjXR3EzOTJ{MES3OC=>
LN229 M3voS2Z2dmO2aX;uJGF{e2G7 NW\SS4V6OSEQvF2= MYO0PEBp M3zWcolv\HWlZYOgZZV1d3CqYXfvd49u\SCob4LtZZRqd25? Mn\4NlExPjJ7OUO=
U87 NIDucJdHfW6ldHnvckBCe3OjeR?= M3LqblEh|ryP NFmwN5k1QCCq NH34N2lqdmS3Y3XzJIF2fG:yaHHnc5NwdWViZn;ycYF1cW:w NFe5dmkzOTB4Mkm5Ny=>
U373 NXq4elRyTnWwY4Tpc44hSXO|YYm= M1LVT|Eh|ryP MoHtOFghcA>? NIi3dZpqdmS3Y3XzJIF2fG:yaHHnc5NwdWViZn;ycYF1cW:w MVmyNVA3Ojl7Mx?=
SF767 MYDGeY5kfGmxbjDBd5NigQ>? MoD2NUDPxE1? NXXwemljPDhiaB?= NXSwdpdYcW6mdXPld{BifXSxcHjh[49{d22nIH\vdo1ifGmxbh?= MoTlNlExPjJ7OUO=
Mel-Juso NUDlU3NiS2WubDDWbYFjcWyrdImgRZN{[Xl? NWfTVYhLOC5yMfMAl|Ex6oDLzszN MUG3NkBp NHvQZlVqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MVyyNVA1QDd6NR?=
518A2  MoXtR4VtdCCYaXHibYxqfHliQYPzZZk> MoLYNE4xOeLCk{Gw5qCK|ryP MWi3NkBp M1rmXolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MnLmNlExPDh5OEW=
Mel-Juso  MlfGSpVv[3Srb36gRZN{[Xl? M4HDVVAvODBz4pETNgKBkc7:TR?= M4roVFI1KGh? MYrzeZBxemW|c3XzJJBpd3OyaH;yfYxifGmxbjDv[kBxcG:|cHjheIllgWxiaX7vd4l1d2xiMz3rbY5ie2ViZH;3cpN1emWjbTD0ZZJo\XS| M2\V[|IyODR6N{i1
518A2 MU\GeY5kfGmxbjDBd5NigQ>? M4KwOFAvODBz4pETNgKBkc7:TR?= MX[yOEBp M{\RTZN2eHC{ZYPz[ZMheGixc4Doc5J6dGG2aX;uJI9nKHCqb4PwbIF1cWS7bDDpco9{cXSxbDCzMYtqdmG|ZTDkc5dve3S{ZXHtJJRiemendIO= NWHYVYMyOjFyNEi3PFU>
PC3  NULFPZNZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPpPZRPOjSq M3nDNWdKPTEEoE2gNVAxKG6P NH35ZXkzODV3MUC2NS=>
U87MG NIO2eXlHfW6ldHnvckBCe3OjeR?= M3HDWFAvOS1zIN88US=> NUjJZWJiOjUkgJnoxsA> MlXISG1UVw>? NYfZXotHcW6qaXLpeJMhWEl|Sz3t[YRq[XSnZDDzbYdv[Wyrbne= NHv6NHkyQTZ|M{[4Ny=>
U138MG NILCfGNHfW6ldHnvckBCe3OjeR?= MoLwNE4yNTFizszN MlPJNlTjiImqwrC= NV\4R5ZUTE2VTx?= NI\5dZpqdmirYnn0d{BRUTONLX3l[IlifGWmIIPp[45idGmwZx?= NVXpSohpOTl4M{O2PFM>
U118MG MXnGeY5kfGmxbjDBd5NigQ>? M1yxclAvOS1zIN88US=> NEXVV24zPOLCiXlCpC=> MoDPSG1UVw>? M2flNolvcGmkaYTzJHBKO0tvbXXkbYF1\WRic3nncoFtcW6p NEnRUXkyQTZ|M{[4Ny=>
U87MG MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVO0U2o5UUN3ME2wMlE1KM7:TR?= MWKxPVU5PDJ{Nx?=
IGROV-1 M1Lp[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfsTWM2OD1yLkC2JO69VQ>? NHe4T|cyQTV6NEKyOy=>
DETROIT562 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFiwVnBKSzVyPUCuNVMh|ryP MVKxPVU5PDJ{Nx?=
PC3  NHrYV3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\GTWM2OD1yLkGwJO69VQ>? NXHyNmNOOTl3OESyNlc>
SKOV-3 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTBwMUKg{txO MYCxPVU5PDJ{Nx?=
HUVEC NYDPZ41mT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\6dHdwUUN3ME2wMlA5KM7:TR?= MknSNVk2QDR{Mke=
UCH-1  Mnm1SpVv[3Srb36gRZN{[Xl? M1zy[|AuPSEQvF2= NIDTW2JqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIHLveIghSUuWIHHu[EBuXE:UIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NUmwVnVlOTl3Mki0OFE>
UCH-1  NHP4[lVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILJclIxNjBzLUGwJO69VQ>? MVW2JIQ> MmHjbY5pcWKrdIOgdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 NUS1UIx1OTl3Mki0OFE>
UCH-1  NG\C[5BCeG:ydH;zbZMhSXO|YYm= MYWwMlEuOTBizszN NF7x[YYzPCCq MoTmSG1UVw>? NHzBe4VqdmS3Y3XzJIFxd3C2b4Ppdy=> MmjTNVk2Ojh2NEG=

... 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]
+ Expand

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]
+ Expand
  • 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]
+ Expand
  • Animal Models: 6- to 12-week-old Balbc nu/nu mice bearing U87MG:ΔEGFR cells
  • Formulation: 50% DMSO
  • 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):
1% DMSO+30% polyethylene glycol+1% Tween 80
For best results, use promptly after mixing.
30 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

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