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 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEK2NJExNThizszN MUKyOE81QC95MjDo NVjqfJNFcW6mdXPld{B1cW2nLTDhcoQh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgbY5pcWKrdHnvckBwdiCQQjDj[YxtKGe{b4f0bC=> Mn7WNlYzOjR4OEG=
SH-SY5Y MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHVNE05KM7:TR?= MXWyOE81QC95MjDo Mnz2bY5lfWOnczD0bY1mNSCjbnSgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRiaX7obYJqfGmxbjDvckBPSiClZXzsJIdzd3e2aB?= M2HrbVI3OjJ2Nkix
SH-SY5Y  NXS0OFRJSXCxcITvd4l{KEG|c3H5 NWLH[Wk6OSEQvF2= M1TITFAvPS1{NDDo NYn1dlF6e2Wwc3n0bZpmeyCwZYXyc4Jt[XO2b33hJINmdGy|IITvJIRwgG:{dXLpZ4lvNWmwZIXj[YQh[XCxcITvd4l{ Mon6NlYzOjR4OEG=
G 35 SC MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWe4S|FvOC5yNT2yNEDPxE1? NWr0[YVwOjRxN{KgbC=> NFvKW5NFVVOR M4DPZYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? MWeyOlEzOTJ3MR?=
G 38 SC M4rkW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vXXFAvODVvMkCg{txO NXnaRoZ6OjRxN{KgbC=> MmfSSG1UVw>? M1PLSIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? MojHNlYyOjF{NUG=
G 40 SC NEPJUYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{K1SlAvODVvMkCg{txO NITYWmwzPC95MjDo NGXsXJRFVVOR NFfKXWVqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 MUCyOlEzOTJ3MR?=
G 35 DC MkHCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWWwMlA2NTJyIN88US=> MomyNlQwPzJiaB?= M2fLR2ROW09? NIjlVY5qdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 MkniNlYyOjF{NUG=
G 38 DC M3HEOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHj5emMxNjB3LUKwJO69VQ>? M2i3elI1Nzd{IHi= MVnEUXNQ M4\Pe4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? MV6yOlEzOTJ3MR?=
G 40 DC NITUfmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDTVWtWOC5yNT2yNEDPxE1? NV;mbW04OjRxN{KgbC=> M16yU2ROW09? M3nq[YlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? Mm\ENlYyOjF{NUG=
RD MXrBdI9xfG:|aYOgRZN{[Xl? MWCxM|EvPS9{IN88US=> M4S0VlczKGh? MnLZbY5lfWOnczDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCJQV7UOlE> NFTV[mgzPTd2OUO3PC=>
TE381.T MX;BdI9xfG:|aYOgRZN{[Xl? MYKxM|EvPS9{IN88US=> NETm[oM4OiCq M4nMeYlv\HWlZYOgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiR1HOWFYy MYmyOVc1QTN5OB?=
RMS13 MVLBdI9xfG:|aYOgRZN{[Xl? MoL6NU8yNjVxMjFOwG0> MmLTO|IhcA>? MW\pcoR2[2W|IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKEeDTmS2NS=> MWqyOVc1QTN5OB?=
RH30  NGXuVnBCeG:ydH;zbZMhSXO|YYm= MlHwNU8yNjVxMjFOwG0> M2X1O|czKGh? MmP2bY5lfWOnczDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCJQV7UOlE> M2XFS|I2PzR7M{e4
VJ NG\jS5JCeG:ydH;zbZMhSXO|YYm= M2rhcVEwOS53L{Kg{txO NUnFdoxRPzJiaB?= MnT3bY5lfWOnczDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCJQV7UOlE> M3fW[lI2PzR7M{e4
HS578T Mm\hR4VtdCCYaXHibYxqfHliQYPzZZk> MnjKNE0{KM7:TR?= NGPiVVM4OiCq NVLucXp{cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NEDZc2UzPTd{MUSxPS=>
BT549 MYLD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NYXBVpk1OC1|IN88US=> MnfLO|IhcA>? MVXpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 M4fwdVI2PzJzNEG5
MDA-MB-231 NHHVV|NE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NEfBSXcxNTNizszN MYC3NkBp M3rqU4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MmrPNlU4OjF2MUm=
MDA-MB-468 Mm\3R4VtdCCYaXHibYxqfHliQYPzZZk> MVKwMVMh|ryP NGH4VJc4OiCq MmLvbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MmjWNlU4OjF2MUm=
MDA-MB-436 M2LXTmNmdGxiVnnhZoltcXS7IFHzd4F6 NXT5N|R7OC1|IN88US=> NYLiXYVvPzJiaB?= NXrwdW9xcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MWiyOVczOTRzOR?=
SUM149PT NF7RNnVE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M4G2T|AuOyEQvF2= M2DwPVczKGh? MXTpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 M3nETlI2PzJzNEG5
MDA-MB-468 NXO0b3JYTnWwY4Tpc44hSXO|YYm= M1jZSVAvODFvMUCg{txO NW\NVppDOjRiaB?= NVzuU5VS\G:5boLl[5Vt[XSnczD0bIUhdGW4ZXzzJI9nKM7{LWTyR3AyNCClLV35Z{BidmRiY4njcIlvKEVicILveIVqdnQEoB?= MYGyOVczOTRzOR?=
MDA-MB-231 MWPGeY5kfGmxbjDBd5NigQ>? MlP0NE4xOS1zMDFOwG0> NX\3[VNmOjRiaB?= NGH4OVhld3ewcnXneYxifGW|IITo[UBt\X[nbIOgc4Yh|rJvVILDVFEtKGNvTYnjJIFv\CCleXPsbY4hTSCycn;0[Ylve8Li NYLHOJVLOjV5MkG0NVk>
HS578T NFLxVHhHfW6ldHnvckBCe3OjeR?= NHnXNGYxNjBzLUGwJO69VQ>? Ml3VNlQhcA>? M{XJeYRwf26{ZXf1cIF1\XNidHjlJIxmfmWuczDv[kDPui2WclPQNUwh[y2PeXOgZY5lKGO7Y3zpckBGKHC{b4TlbY5{yqB? M2PqPVI2PzJzNEG5
SW872 MmrMSpVv[3Srb36gRZN{[Xl? MmjNNE4xOS1yLkWg{txO NYDVR2xKOjRiaB?= MkfOdoVlfWOnczDBT3QheGixc4Doc5J6dGG2aX;uJEhxSUuWKTDhcoQhPEWEUEGgdIhwe3Cqb4L5cIF1cW:wIDjwOGVDWDFrIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{wrC= NVXTUWNxOjR4OUW2N|I>
SW982 MorvSpVv[3Srb36gRZN{[Xl? MWGwMlAyNTBwNTFOwG0> NEnxNpMzPCCq M3X1e5Jm\HWlZYOgRWtVKHCqb4PwbI9zgWyjdHnvckApeEGNVDmgZY5lKDSHQmCxJJBpd3OyaH;yfYxifGmxbjCodFRGSlBzKTDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nctMg MWGyOFY6PTZ|Mh?=
SW872 M3PzU2Fxd3C2b4Ppd{BCe3OjeR?= MXmwMlAyNTBwNTFOwG0> MYG0PEBp NXT6clducW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> M3TyN|I1Pjl3NkOy
SW982 MVvBdI9xfG:|aYOgRZN{[Xl? MV[wMlAyNTBwNTFOwG0> NGHyWlQ1QCCq M17UOYlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NHzh[3gzPDZ7NU[zNi=>
AGS HG NV:5fm1DT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTBwNkigxtEhOC5yM{Gg{txO MnLMNlQ2QTd2N{i=
AGS LG NHflS5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG[0ZY9KSzVyPUCuNFUhyrFiMD6wNFEh|ryP MoLWNlQ2QTd2N{i=
HGC27 HG M2[4[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLlTWM2OD1yLkO4JOKyKDBwMEKyJO69VQ>? MlLlNlQ2QTd2N{i=
HGC27 LG M2Hqdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknHTWM2OD1yLkCyJOKyKDBwMEC0JO69VQ>? M1\WUVI1PTl5NEe4
MKN45 HG NG\qUYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDxTWM2OD1zLkCxJOKyKDBwMEWxJO69VQ>? MV6yOFU6PzR5OB?=
MKN45 LG MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LNU2lEPTB;MD64O{DDuSByLkCzNEDPxE1? NYP4d4pLOjR3OUe0O|g>
NUGC4 HG NEf0cm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTF2LkCgxtEhOy57MUOg{txO M3LO[FI1PTl5NEe4
NUGC4 LG Mm\HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTF2LkCgxtEhPS5|MkGg{txO MWCyOFU6PzR5OB?=
A549 MofKSpVv[3Srb36gRZN{[Xl? NWnmXIVyOC5{NT:wMlUwOSEQvF2= NEnOcW0zPCCq NYXuXGVIcW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|bHnnbJRtgQ>? NUjTPWZIOjR|NUG0NlU>
H460 M1jUcWZ2dmO2aX;uJGF{e2G7 MmDiNE4zPS9yLkWvNUDPxE1? NFqxNYczPCCq M3L3[olvcGmkaYTzJGFsfCCyaH;zdIhwenmuYYTpc44he2yrZ3j0cJk> M3rx[|I1OzVzNEK1
H661 NFLvUFJHfW6ldHnvckBCe3OjeR?= MYOwMlI2NzBwNT:xJO69VQ>? M3zrV|I1KGh? MnLzbY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7 MoLSNlQ{PTF2MkW=
SAS NGTMc|hHfW6ldHnvckBCe3OjeR?= NVS0c45POC5{NT:wMlUwOSEQvF2= MVSyOEBp MnrUbY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7 MVuyOFM2OTR{NR?=
UT5 NFT1WlFHfW6ldHnvckBCe3OjeR?= M4X1dlAvOjVxMD61M|Eh|ryP MUCyOEBp MVHpcohq[mm2czDBb5QheGixc4Doc5J6dGG2aX;uJJNq\26rZnnjZY51dHl? MoPhNlQ{PTF2MkW=
FaDu NWOwb3VLTnWwY4Tpc44hSXO|YYm= MU[wMlI2NzBwNT:xJO69VQ>? NXizc3U3OjRiaB?= NHvUfJNqdmirYnn0d{BCc3RicHjvd5Bpd3K7bHH0bY9vKHOrZ37p[olk[W62bIm= NHvJ[GkzPDN3MUSyOS=>
RD MnXQRZBweHSxc3nzJGF{e2G7 MYWxM|EvPS9{IN88US=> MUO3NkBp NUe2dYJLTE2VTx?= MnT5bY5lfWOnczDjZZNx[XOnLXTldIVv\GWwdDDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCXT{GyOi=> NYjWWFRFOjN4OES5NlU>
TE671 MoD5RZBweHSxc3nzJGF{e2G7 MnvYNU8yNjVxMjFOwG0> Mni2O|IhcA>? M17vUWROW09? NV;IdodMcW6mdXPld{Bk[XOyYYPlMYRmeGWwZHXueEBieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDVU|EzPg>? MWeyN|Y5PDl{NR?=
RH30  Mo\0RZBweHSxc3nzJGF{e2G7 M{HRUVEwOS53L{Kg{txO NH7kVlc4OiCq M{\oV2ROW09? NXHycY1VcW6mdXPld{Bk[XOyYYPlMYRmeGWwZHXueEBieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDVU|EzPg>? MkT1NlM3QDR7MkW=
RMS13 NHS2O3hCeG:ydH;zbZMhSXO|YYm= NG\2V44yNzFwNT:yJO69VQ>? MXm3NkBp M2rDbGROW09? M4T2OYlv\HWlZYOgZ4F{eGG|ZT3k[ZBmdmSnboSgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiVV:xNlY> MnPwNlM3QDR7MkW=
SUM149PT M1zkSGNmdGxiVnnhZoltcXS7IFHzd4F6 NXfMR|B7OC5|IN88US=> M3LzOVczKGh? NFf6TXlmdmijbnPld{BkgXSxdH;4bYMh\W[oZXP0d{Bw\iCSSUPLM2FMXCCyYYToe4F6KGmwaHnibZRwenN? Ml;xNlM3ODFyN{S=
MDA-MB-468 MWXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NHLIZVUxNjNizszN NHH3SGk4OiCq Ml3k[Y5p[W6lZYOgZ5l1d3SxeHnjJIVn\mWldIOgc4YhWEl|Sz;BT3QheGG2aIfhfUBqdmirYnn0c5J{ MkTmNlM3ODFyN{S=
MDA-MB-231 MoH1R4VtdCCYaXHibYxqfHliQYPzZZk> M1HzXVAvOyEQvF2= MUK3NkBp NVLrT4pr\W6qYX7j[ZMh[3m2b4TvfIlkKGWoZnXjeJMhd2ZiUFmzT{9CU1RicHH0bJdigSCrbnjpZol1d3K| M1LGbFI{PjBzMEe0
SY5Y NXHLVGdxTnWwY4Tpc44hSXO|YYm= Mnn3NU42NzJwNT:1JO69VQ>? M4PLZ|I1KGh? MkP2bY5lfWOnczDHNeKh[2WubD3jfYNt\SCjcoLld5Qh[W6mIHHwc5B1d3Orcx?= NX7hTJg2OjN|N{izOFE>
SKNBE(2c) NXiyUmJuTnWwY4Tpc44hSXO|YYm= NVfTeW9ROS53L{KuOU82KM7:TR?= NUPmOoZOOjRiaB?= NGTpVnlqdmS3Y3XzJGcyyqClZXzsMYN6[2ynIHHydoV{fCCjbnSgZZBweHSxc3nz MXmyN|M4QDN2MR?=
RD M1j2dGFxd3C2b4Ppd{BCe3OjeR?= MnPRN{DDvU1? NUXZUXk2OTJiaB?= MonPSG1UVw>? NFjLO2l{\W6|aYTpfoV{KFKGIHPlcIx{KHSxIFTPXE1qdmS3Y3XkJIFxd3C2b4Ppdy=> MYmyN|MxODhyOR?=
TP5014 MmHSRZBweHSxc3nzJGF{e2G7 MoDCN{DDvU1? MVGxNkBp MoHSSG1UVw>? M3naZZNmdnOrdHn6[ZMhWkRiY3XscJMhfG9iRF;YMYlv\HWlZXSgZZBweHSxc3nz NH;lVZAzOzNyMEiwPS=>
HT1080 Mk\iRZBweHSxc3nzJGF{e2G7 Mlr0N{DDvU1? NFvsdlMyOiCq MoHlSG1UVw>? M4nhWpNmdnOrdHn6[ZMhWkRiY3XscJMhfG9iRF;YMYlv\HWlZXSgZZBweHSxc3nz MWGyN|MxODhyOR?=
A549 M1XHcmZ2dmO2aX;uJGF{e2G7 MWmwMVMvOyEQvF2= M2nZdVczKGh? M4Dib4lv\HWlZYOgZ49ueGyndHWg[I94dnKnZ4XsZZRqd25ib3[gdGFMXA>? NF3JUYozOzJ3OUW5NS=>
HCC827 NUjy[mpITnWwY4Tpc44hSXO|YYm= MnyxNE0{NjNizszN NXXsO3NMPzJiaB?= MYHpcoR2[2W|IHPvcZBt\XSnIHTve45z\We3bHH0bY9vKG:oIIDBT3Q> MYSyN|I2QTV7MR?=
H3122 NITtXHNHfW6ldHnvckBCe3OjeR?= M3z5PVAuOy5|IN88US=> Mmj4O|IhcA>? NUe2T3ZzcW6mdXPld{Bkd22ybHX0[UBld3ewcnXneYxifGmxbjDv[kBxSUuW NWD5cVN4OjN{NUm1PVE>
TALL-1 M4CwUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvIUHhKOeLCid88US=> NV76TnQ1PyCm NHjsblll\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? NXnyOXZbOjNyM{iyO|M>
HPB-ALL M1rxd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHv4Z4Ey6oDLzszN NV6wPXhoPyCm MUPk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> MWiyN|A{QDJ5Mx?=
DND41 M1e3UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLhW3Z3OeLCid88US=> MmL0O{Bl NXjJXmNm\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 M1XvUFI{ODN6Mkez
SUP-T1 M{TkXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVix5qCK|ryP NX6ySplXPyCm M1fGNYRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? MVeyN|A{QDJ5Mx?=
PEER NXzvVpJvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXKNgKBkc7:TR?= MVW3JIQ> MYjk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> MnTZNlMxOzh{N{O=
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HCC827 MlPKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELkXpQxNTNizszN M1zvfVczKGh? NVnNNnJRUUN3ME2wMlMh|ryP NFvhcnYzOTJ{MES3OC=>
PC-9  NUfmdWJ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUSwMVMh|ryP NEjuSmU4OiCq NWrQfFc2UUN3ME2wMlgh|ryP MUGyNVIzODR5NB?=
LN229 MnPFSpVv[3Srb36gRZN{[Xl? M3O5RlEh|ryP MlfQOFghcA>? MnzabY5lfWOnczDheZRweGijZ3;zc41mKG[xcn3heIlwdg>? MViyNVA3Ojl7Mx?=
U87 MnvZSpVv[3Srb36gRZN{[Xl? M4myWlEh|ryP Mn[2OFghcA>? M2rHe4lv\HWlZYOgZZV1d3CqYXfvd49u\SCob4LtZZRqd25? NX7p[YtSOjFyNkK5PVM>
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518A2  M3v4PWNmdGxiVnnhZoltcXS7IFHzd4F6 M1nDfVAvODIkgKOxNQKBkc7:TR?= NUPZdZBTPzJiaB?= Ml6wbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NICwNWUzOTB2OEe4OS=>
Mel-Juso  MnP1SpVv[3Srb36gRZN{[Xl? MnK4NE4xODIkgKOx5qCK|ryP MmDDNlQhcA>? M1HNPJN2eHC{ZYPz[ZMheGixc4Doc5J6dGG2aX;uJI9nKHCqb4PwbIF1cWS7bDDpco9{cXSxbDCzMYtqdmG|ZTDkc5dve3S{ZXHtJJRiemendIO= NX7EcJY2OjFyNEi3PFU>
518A2 NXrCR5E1TnWwY4Tpc44hSXO|YYm= M3S4N|AvODBz4pETNgKBkc7:TR?= MnjpNlQhcA>? NXHlXIxYe3WycILld5NmeyCyaH;zdIhwenmuYYTpc44hd2ZicHjvd5Bp[XSrZInsJIlvd3OrdH;sJFMuc2mwYYPlJIRwf26|dILlZY0hfGG{Z3X0dy=> NVvYRZA5OjFyNEi3PFU>
PC3  MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DYd|I1cA>? NUCxW21mT0l3MNMgQUAyODBibl2= NIXPZmUzODV3MUC2NS=>
U87MG Ml\4SpVv[3Srb36gRZN{[Xl? MnLkNE4yNTFizszN NHj6doczPOLCiXlCpC=> MWjEUXNQ MlnSbY5pcWKrdIOgVGk{Uy2vZXTpZZRm\CC|aXfuZYxqdmd? Ml\5NVk3OzN4OEO=
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U87MG NILTZmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TPTGlEPTB;MD6xOEDPxE1? NGLuTWEyQTV6NEKyOy=>
IGROV-1 MoLtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTBwME[g{txO M{i1flE6PTh2MkK3
DETROIT562 NFPiT2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HqOmlEPTB;MD6xN{DPxE1? MXOxPVU5PDJ{Nx?=
PC3  MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvi[FhZUUN3ME2wMlExKM7:TR?= M13GXlE6PTh2MkK3
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HUVEC MoK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfHTWM2OD1yLkC4JO69VQ>? M2GyclE6PTh2MkK3
UCH-1  MkHiSpVv[3Srb36gRZN{[Xl? Mn;0NE02KM7:TR?= M4HHNolvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiYn;0bEBCU1RiYX7kJI1VV1JiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MX6xPVUzQDR2MR?=
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UCH-1  MYHBdI9xfG:|aYOgRZN{[Xl? MVqwMlEuOTBizszN M2HHTFI1KGh? NGrwToRFVVOR M4HLN4lv\HWlZYOgZZBweHSxc3nz NFrpSIwyQTV{OES0NS=>

... 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 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 (g) = Concentration (mol/L) × Volume (L) × 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.

  • * Indicates a Required Field

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID