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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5 Customer Reviews

  • (D) IGROV parental, shControl (two independent clones) and ShPKCiota (two independent clones) were treated with 5 μM GDC-0941 and 1.5 μM PI-103 for 24 hours and subjected to western blot analysis with the indicated antibodies. Each experiment was performed in triplicate.

    Oncogene, 2016, 35(19):2428-40. PI-103 purchased from Selleck.

    (A) MCF7 cells pre-treated with 100 nM siRNA for 72 h were re-seeded with normal growth media and grown overnight, then further transfected by 100nM of fresh siRNA. Twenty-(A) four hours after transfection, the cells were further treated with PI-103 for 24 h and the cell lysates were immunoblotted with the indicated antibodies. (B) Breast cancer cells carrying BRCA1 mutations were treated with 1 mM of PI-103 for 24h (left) or increasing amounts of PI-103 for 24 h (right). Cell lysates were analyzed by Western blotting with the indicated antibodies.

    Mol Carcinog 2012 52, 667-75 . PI-103 purchased from Selleck.

  • Knockdown of BRCA1 sensitizes cells to PI3K/AKT pathway inhibitors. MCF7 cells transfected with either BRCA1-siRNA or control-siRNA were treated with increasing amounts of inhibitors targeting the PI3K/AKT pathway for 48 h in triplicate. Viable cells were measured by MTT assay.

    Mol Carcinog 2012 ahead of print. PI-103 purchased from Selleck.

    We treated all of drugs in T47D which has a PI3KCA H1044R mutation with the concentration shown below for 1 hour and performed western blot analysis using antibodies to phospho-AKT(SERINE 472), and total AKT.

     

     

    Saraswati Sukumar of Johns Hopkins University School of Medicine PI-103 purchased from Selleck.

  • Breast cancer cells were pretreated with 100ng/ml EGF for 15 min and then treated with the indicated concentrations of PI-103 for 24 hours.

     

     

    Dr. Zhang of Tianjin Medical University. PI-103 purchased from Selleck.

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 M1;tO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLPNE05KM7:TR?= MnjDNlQwPDhxN{KgbC=> NUe3UIlFcW6mdXPld{B1cW2nLTDhcoQh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgbY5pcWKrdHnvckBwdiCQQjDj[YxtKGe{b4f0bC=> MmHuNlYzOjR4OEG=
SH-SY5Y MmfhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml30NE05KM7:TR?= NEPqe3ozPC92OD:3NkBp NWOzbpFMcW6mdXPld{B1cW2nLTDhcoQh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgbY5pcWKrdHnvckBwdiCQQjDj[YxtKGe{b4f0bC=> MlHSNlYzOjR4OEG=
SH-SY5Y  MUDBdI9xfG:|aYOgRZN{[Xl? M{S4R|Eh|ryP MnvyNE42NTJ2IHi= NGT4SFF{\W6|aYTpfoV{KG6ndYLvZoxie3SxbXGgZ4VtdHNidH:g[I95d3K3YnnjbY4ucW6mdXPl[EBieG:ydH;zbZM> NH71TY4zPjJ{NE[4NS=>
G 35 SC MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlT6NE4xPS1{MDFOwG0> NWD5S5l5OjRxN{KgbC=> NVvnbW9ETE2VTx?= MVnpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueIx6 NXv4W25KOjZzMkGyOVE>
G 38 SC MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nHbVAvODVvMkCg{txO MVmyOE84OiCq NFfleGRFVVOR NH7XXpdqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 MXeyOlEzOTJ3MR?=
G 40 SC MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnnSJgxNjB3LUKwJO69VQ>? MmLxNlQwPzJiaB?= M1zPPGROW09? Mly4bY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBidmRidHnt[UBl\XCnbnTlcpRtgQ>? MkH4NlYyOjF{NUG=
G 35 DC NG\QdpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXywMlA2NTJyIN88US=> MknENlQwPzJiaB?= MkTtSG1UVw>? MkDEbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBidmRidHnt[UBl\XCnbnTlcpRtgQ>? Ml24NlYyOjF{NUG=
G 38 DC MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPkb3ZEOC5yNT2yNEDPxE1? MnnqNlQwPzJiaB?= NGjLV|FFVVOR NX;NempEcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= NGL6PGszPjF{MUK1NS=>
G 40 DC Mn\uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LtdlAvODVvMkCg{txO NV[3TlZSOjRxN{KgbC=> MkWxSG1UVw>? M3jWUIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? MYSyOlEzOTJ3MR?=
RD M3LON2Fxd3C2b4Ppd{BCe3OjeR?= MV2xM|EvPS9{IN88US=> NXvDelZuPzJiaB?= NVnVVYNNcW6mdXPld{BieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDHRW5VPjF? MXWyOVc1QTN5OB?=
TE381.T NHfHVpdCeG:ydH;zbZMhSXO|YYm= NYrvS5ZDOS9zLkWvNkDPxE1? MmrYO|IhcA>? NHvJeY1qdmS3Y3XzJIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIFfBUnQ3OQ>? NUi3Z3NPOjV5NEmzO|g>
RMS13 NFLQS5lCeG:ydH;zbZMhSXO|YYm= MVOxM|EvPS9{IN88US=> MmGzO|IhcA>? MoTybY5lfWOnczDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCJQV7UOlE> M4jwRVI2PzR7M{e4
RH30  MUnBdI9xfG:|aYOgRZN{[Xl? NXLybJNsOS9zLkWvNkDPxE1? MXG3NkBp NV\zSVdMcW6mdXPld{BieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDHRW5VPjF? NGLieXczPTd2OUO3PC=>
VJ M4Sy[2Fxd3C2b4Ppd{BCe3OjeR?= M1naTVEwOS53L{Kg{txO NXXlRWlwPzJiaB?= NXexUZZVcW6mdXPld{BieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDHRW5VPjF? M1npRlI2PzR7M{e4
HS578T NIm3RWxE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MnjENE0{KM7:TR?= NFPiRok4OiCq MmrUbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MkfZNlU4OjF2MUm=
BT549 NY[3VlZqS2WubDDWbYFjcWyrdImgRZN{[Xl? NGO2Z2cxNTNizszN NF\5[Vc4OiCq MWDpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MYeyOVczOTRzOR?=
MDA-MB-231 MUPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NUPVO4xMOC1|IN88US=> MX[3NkBp NELQNJRqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 M3LscFI2PzJzNEG5
MDA-MB-468 NYO3UmZ7S2WubDDWbYFjcWyrdImgRZN{[Xl? NWP2b5RlOC1|IN88US=> M4\xU|czKGh? MVrpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 M3\OV|I2PzJzNEG5
MDA-MB-436 MYHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M4D3TlAuOyEQvF2= M1HKOlczKGh? NWfXc2E6cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NV3QNoxDOjV5MkG0NVk>
SUM149PT NVXuTZE2S2WubDDWbYFjcWyrdImgRZN{[Xl? NXjHWWJQOC1|IN88US=> MXm3NkBp MoDxbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MXiyOVczOTRzOR?=
MDA-MB-468 MWLGeY5kfGmxbjDBd5NigQ>? M4H5VFAvODFvMUCg{txO NH7MSHQzPCCq NWDxV4hx\G:5boLl[5Vt[XSnczD0bIUhdGW4ZXzzJI9nKM7{LWTyR3AyNCClLV35Z{BidmRiY4njcIlvKEVicILveIVqdnQEoB?= MWmyOVczOTRzOR?=
MDA-MB-231 MYrGeY5kfGmxbjDBd5NigQ>? NF;oSFAxNjBzLUGwJO69VQ>? MoCwNlQhcA>? NHvIWGlld3ewcnXneYxifGW|IITo[UBt\X[nbIOgc4Yh|rJvVILDVFEtKGNvTYnjJIFv\CCleXPsbY4hTSCycn;0[Ylve8Li MUSyOVczOTRzOR?=
HS578T M3G2U2Z2dmO2aX;uJGF{e2G7 NWrFU5JmOC5yMT2xNEDPxE1? NU\WfGRQOjRiaB?= NHi2PFJld3ewcnXneYxifGW|IITo[UBt\X[nbIOgc4Yh|rJvVILDVFEtKGNvTYnjJIFv\CCleXPsbY4hTSCycn;0[Ylve8Li MWKyOVczOTRzOR?=
SW872 MV\GeY5kfGmxbjDBd5NigQ>? M3fiOlAvODFvMD61JO69VQ>? NFjGVXQzPCCq MlnXdoVlfWOnczDBT3QheGixc4Doc5J6dGG2aX;uJEhxSUuWKTDhcoQhPEWEUEGgdIhwe3Cqb4L5cIF1cW:wIDjwOGVDWDFrIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{wrC= M3zQ[|I1Pjl3NkOy
SW982 NUfBUGlDTnWwY4Tpc44hSXO|YYm= M1rPT|AvODFvMD61JO69VQ>? MWWyOEBp M2m3W5Jm\HWlZYOgRWtVKHCqb4PwbI9zgWyjdHnvckApeEGNVDmgZY5lKDSHQmCxJJBpd3OyaH;yfYxifGmxbjCodFRGSlBzKTDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nctMg MWWyOFY6PTZ|Mh?=
SW872 NHvPZWJCeG:ydH;zbZMhSXO|YYm= MkLPNE4xOS1yLkWg{txO M2LsPVQ5KGh? M33rdIlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NVfVXFAxOjR4OUW2N|I>
SW982 MY\BdI9xfG:|aYOgRZN{[Xl? MX:wMlAyNTBwNTFOwG0> MUm0PEBp MmfLbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= M{njVFI1Pjl3NkOy
AGS HG M2LaZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTBwNkigxtEhOC5yM{Gg{txO NHv3UWszPDV7N{S3PC=>
AGS LG NHHwRlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTBwMEWgxtEhOC5yMEGg{txO NXv4eIFiOjR3OUe0O|g>
HGC27 HG M3\lT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHtWmNoUUN3ME2wMlM5KMLzIECuNFIzKM7:TR?= MnPuNlQ2QTd2N{i=
HGC27 LG NGL2VmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTBwMEKgxtEhOC5yMESg{txO NYrXNlVyOjR3OUe0O|g>
MKN45 HG MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIW2V2NKSzVyPUGuNFEhyrFiMD6wOVEh|ryP M3fzNlI1PTl5NEe4
MKN45 LG Moq3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fPZWlEPTB;MD64O{DDuSByLkCzNEDPxE1? MlXHNlQ2QTd2N{i=
NUGC4 HG Mn3ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TwTWlEPTB;MUSuNEDDuSB|LkmxN{DPxE1? NX\lbmFIOjR3OUe0O|g>
NUGC4 LG Mm\KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTF2LkCgxtEhPS5|MkGg{txO M{XoeFI1PTl5NEe4
A549 NGPKd5hHfW6ldHnvckBCe3OjeR?= MnrKNE4zPS9yLkWvNUDPxE1? NFLFOYszPCCq Mle4bY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{dGmpaITsfS=> MVeyOFM2OTR{NR?=
H460 MnmxSpVv[3Srb36gRZN{[Xl? NITKNGYxNjJ3L{CuOU8yKM7:TR?= M{HkRlI1KGh? MlvPbY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{dGmpaITsfS=> M4rIc|I1OzVzNEK1
H661 NWHmcpNlTnWwY4Tpc44hSXO|YYm= MXmwMlI2NzBwNT:xJO69VQ>? NVjQfoFmOjRiaB?= NXXZNVh{cW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|aXfubYZq[2GwdHz5 NWnCfYRGOjR|NUG0NlU>
SAS MXTGeY5kfGmxbjDBd5NigQ>? NVTqcWhTOC5{NT:wMlUwOSEQvF2= NUnlOJFFOjRiaB?= M1TBOolvcGmkaYTzJGFsfCCyaH;zdIhwenmuYYTpc44he2mpbnnmbYNidnSueR?= MWqyOFM2OTR{NR?=
UT5 NIfKU49HfW6ldHnvckBCe3OjeR?= NHXHSXIxNjJ3L{CuOU8yKM7:TR?= MWmyOEBp MX\pcohq[mm2czDBb5QheGixc4Doc5J6dGG2aX;uJJNq\26rZnnjZY51dHl? NWXtZ2FxOjR|NUG0NlU>
FaDu NV32W5BXTnWwY4Tpc44hSXO|YYm= Mn7NNE4zPS9yLkWvNUDPxE1? MkX0NlQhcA>? Mkn0bY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7 NIH2WG4zPDN3MUSyOS=>
RD NFPS[XdCeG:ydH;zbZMhSXO|YYm= MWexM|EvPS9{IN88US=> MYe3NkBp MWjEUXNQ MV\pcoR2[2W|IHPhd5Bie2VvZHXw[Y5l\W62IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKFWRMUK2 MXuyN|Y5PDl{NR?=
TE671 M1LaVGFxd3C2b4Ppd{BCe3OjeR?= MWSxM|EvPS9{IN88US=> MnrhO|IhcA>? MVHEUXNQ NVS2Z4cxcW6mdXPld{Bk[XOyYYPlMYRmeGWwZHXueEBieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDVU|EzPg>? MlSzNlM3QDR7MkW=
RH30  NUG5ToM6SXCxcITvd4l{KEG|c3H5 NEHXbVIyNzFwNT:yJO69VQ>? M1LSfVczKGh? MofxSG1UVw>? MU\pcoR2[2W|IHPhd5Bie2VvZHXw[Y5l\W62IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKFWRMUK2 MlPSNlM3QDR7MkW=
RMS13 NH;HdlVCeG:ydH;zbZMhSXO|YYm= NWq4bJJwOS9zLkWvNkDPxE1? M3TMNlczKGh? NXzOOVhiTE2VTx?= MUXpcoR2[2W|IHPhd5Bie2VvZHXw[Y5l\W62IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKFWRMUK2 NHi1NJAzOzZ6NEmyOS=>
SUM149PT M1XT[2NmdGxiVnnhZoltcXS7IFHzd4F6 NHOwWIYxNjNizszN M4C1clczKGh? M{TZSIVvcGGwY3XzJIN6fG:2b4jpZ{Bm\m[nY4TzJI9nKFCLM1uvRWtVKHCjdHj3ZZkhcW6qaXLpeI9zew>? NUDGV446OjN4MEGwO|Q>
MDA-MB-468 MYnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M1jCXlAvOyEQvF2= MXK3NkBp NUO4Nm5C\W6qYX7j[ZMh[3m2b4TvfIlkKGWoZnXjeJMhd2ZiUFmzT{9CU1RicHH0bJdigSCrbnjpZol1d3K| MXuyN|YxOTB5NB?=
MDA-MB-231 MmKwR4VtdCCYaXHibYxqfHliQYPzZZk> NVn6NIhIOC5|IN88US=> MXi3NkBp MUPlcohidmOnczDjfZRwfG:6aXOg[YZn\WO2czDv[kBRUTONL1HLWEBx[XSqd3H5JIlvcGmkaYTvdpM> Mmj4NlM3ODFyN{S=
SY5Y NFLBcm9HfW6ldHnvckBCe3OjeR?= M1fvflEvPS9{LkWvOUDPxE1? NU\wR2M1OjRiaB?= NYfHO24ycW6mdXPld{BIOcLiY3XscE1kgWOuZTDhdpJme3RiYX7kJIFxd3C2b4Ppdy=> NHPmXHUzOzN5OEO0NS=>
SKNBE(2c) MlHhSpVv[3Srb36gRZN{[Xl? M{TMZVEvPS9{LkWvOUDPxE1? MUeyOEBp NVrVRXd[cW6mdXPld{BIOcLiY3XscE1kgWOuZTDhdpJme3RiYX7kJIFxd3C2b4Ppdy=> M3rQPFI{Ozd6M{Sx
RD NWDEcmRVSXCxcITvd4l{KEG|c3H5 NF32OVE{KML3TR?= M3TLTlEzKGh? M{HRcGROW09? MVfz[Y5{cXSrenXzJHJFKGOnbHzzJJRwKESRWD3pcoR2[2WmIHHwc5B1d3Orcx?= MV6yN|MxODhyOR?=
TP5014 NVfRSXRTSXCxcITvd4l{KEG|c3H5 M4jxelMhyrWP NVTJeYZiOTJiaB?= NU\HWlJ1TE2VTx?= NGP3eoZ{\W6|aYTpfoV{KFKGIHPlcIx{KHSxIFTPXE1qdmS3Y3XkJIFxd3C2b4Ppdy=> NE\zN2czOzNyMEiwPS=>
HT1080 M4HSSmFxd3C2b4Ppd{BCe3OjeR?= MmDXN{DDvU1? NYfzNYsxOTJiaB?= M3HH[WROW09? NYrMUnhUe2Wwc3n0bZpmeyCURDDj[YxteyC2bzDEU3gucW6mdXPl[EBieG:ydH;zbZM> MXiyN|MxODhyOR?=
A549 MV;GeY5kfGmxbjDBd5NigQ>? M1XhfVAuOy5|IN88US=> M2LGTVczKGh? M2fiVYlv\HWlZYOgZ49ueGyndHWg[I94dnKnZ4XsZZRqd25ib3[gdGFMXA>? MkDGNlMzPTl3OUG=
HCC827 MV3GeY5kfGmxbjDBd5NigQ>? MnnoNE0{NjNizszN NFjYN3U4OiCq M{TaTolv\HWlZYOgZ49ueGyndHWg[I94dnKnZ4XsZZRqd25ib3[gdGFMXA>? M3zvXlI{OjV7NUmx
H3122 NXm0eVZ[TnWwY4Tpc44hSXO|YYm= NXT4O4IxOC1|LkOg{txO NITuR3U4OiCq MYjpcoR2[2W|IHPvcZBt\XSnIHTve45z\We3bHH0bY9vKG:oIIDBT3Q> MVKyN|I2QTV7MR?=
TALL-1 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\ONgKBkc7:TR?= NVn2epFvPyCm M{PvVoRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? MXqyN|A{QDJ5Mx?=
HPB-ALL MnzxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWWx5qCK|ryP NV\tWoN1PyCm MnHX[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 NUm5XHJtOjNyM{iyO|M>
DND41 M3vjcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2H4XlHjiIoQvF2= NEHZXlk4KGR? NGPjOotl\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? NVTrTY01OjNyM{iyO|M>
SUP-T1 NUWybI5TT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3ENgKBkc7:TR?= MkX0O{Bl MlrY[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 NIXTN3AzOzB|OEK3Ny=>
PEER M2\GZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3f2b|HjiIoQvF2= MnvIO{Bl NVezcI5J\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 NEHPZWQzOzB|OEK3Ny=>
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KMS12-BM  NYnye|hJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHMRlYxNTJizszN M4f4R|I1KGh? MWjJR|Ux97zgMjFOwG0> MWqyNlgzQTJ|NB?=
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PC-9  NXP1RY1wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3T1TlAuOyEQvF2= MlHMO|IhcA>? NFLL[29KSzVyPUCuPEDPxE1? NXfQfmJmOjF{MkC0O|Q>
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SF767 NWXHcFA6TnWwY4Tpc44hSXO|YYm= MVGxJO69VQ>? M2K3dVQ5KGh? M{jZeYlv\HWlZYOgZZV1d3CqYXfvd49u\SCob4LtZZRqd25? NES2PJozOTB4Mkm5Ny=>
Mel-Juso NWDjWZRHS2WubDDWbYFjcWyrdImgRZN{[Xl? MoW0NE4xOeLCk{Gw5qCK|ryP MVu3NkBp M2TMcolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? M{\yWVIyODR6N{i1
518A2  MmX6R4VtdCCYaXHibYxqfHliQYPzZZk> MmS1NE4xOeLCk{Gw5qCK|ryP NX3md4U6PzJiaB?= M2\aVolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NELjdlEzOTB2OEe4OS=>
Mel-Juso  MVHGeY5kfGmxbjDBd5NigQ>? M{PhcVAvODBz4pETNgKBkc7:TR?= M3HMVlI1KGh? M4DESZN2eHC{ZYPz[ZMheGixc4Doc5J6dGG2aX;uJI9nKHCqb4PwbIF1cWS7bDDpco9{cXSxbDCzMYtqdmG|ZTDkc5dve3S{ZXHtJJRiemendIO= NITBSIIzOTB2OEe4OS=>
518A2 NIW4PIJHfW6ldHnvckBCe3OjeR?= M37SeFAvODBz4pETNgKBkc7:TR?= NUW3e4d1OjRiaB?= NVnUfJZKe3WycILld5NmeyCyaH;zdIhwenmuYYTpc44hd2ZicHjvd5Bp[XSrZInsJIlvd3OrdH;sJFMuc2mwYYPlJIRwf26|dILlZY0hfGG{Z3X0dy=> NHfGfVczOTB2OEe4OS=>
PC3  NVziVlc3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlO5NlRp MnvMS2k2OMLiPTCxNFAhdk1? M2PvN|IxPTVzME[x
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U118MG NHfDT2hHfW6ldHnvckBCe3OjeR?= NFrIZ|kxNjFvMTFOwG0> NXrkb3JoOjUkgJnoxsA> MYnEUXNQ MmDkbY5pcWKrdIOgVGk{Uy2vZXTpZZRm\CC|aXfuZYxqdmd? NF3HS2gyQTZ|M{[4Ny=>
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DETROIT562 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEiyU|RKSzVyPUCuNVMh|ryP M2L4cFE6PTh2MkK3
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HUVEC NGrXfHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTBwMEig{txO NFzmNYEyQTV6NEKyOy=>
UCH-1  MmjxSpVv[3Srb36gRZN{[Xl? NGfiNFgxNTVizszN M2m5TolvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiYn;0bEBCU1RiYX7kJI1VV1JiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NELISGIyQTV{OES0NS=>
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UCH-1  MYLBdI9xfG:|aYOgRZN{[Xl? NWXpc5ZjOC5zLUGwJO69VQ>? NGW3fJMzPCCq NUH4fmhbTE2VTx?= M2jsOIlv\HWlZYOgZZBweHSxc3nz Mlz2NVk2Ojh2NEG=

... Click to View More Cell Line Experimental Data

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 individually and in order:
1% DMSO+30% polyethylene glycol+1% Tween 80
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
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 (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
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*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):
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    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

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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID