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.

Size Price Stock Quantity  
In DMSO USD 134 In stock
USD 147 In stock
USD 270 In stock
USD 370 In stock

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4 Customer Reviews

  • (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

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 M33ZOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\EOFAuQCEQvF2= NVr3b2o5OjRxNEivO|IhcA>? M{nhRolv\HWlZYOgeIlu\S1iYX7kJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IHnubIljcXSrb36gc44hVkJiY3XscEBoem:5dHi= M{foR|I3OjJ2Nkix
SH-SY5Y MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV[wMVgh|ryP NHjTcXkzPC92OD:3NkBp NUXVUop7cW6mdXPld{B1cW2nLTDhcoQh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgbY5pcWKrdHnvckBwdiCQQjDj[YxtKGe{b4f0bC=> NIXmVmIzPjJ{NE[4NS=>
SH-SY5Y  MWDBdI9xfG:|aYOgRZN{[Xl? MmXINUDPxE1? NHi0bmQxNjVvMkSgbC=> Mli1d4Vve2m2aYrld{Bv\XW{b3LsZZN1d22jIHPlcIx{KHSxIHTvfI9zfWKrY3nuMYlv\HWlZXSgZZBweHSxc3nz MXiyOlIzPDZ6MR?=
G 35 SC MkfCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDsV|YxNjB3LUKwJO69VQ>? NEfJSnEzPC95MjDo MmeySG1UVw>? M134N4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? MnLxNlYyOjF{NUG=
G 38 SC MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mny4NE4xPS1{MDFOwG0> NUT0[GlSOjRxN{KgbC=> MU\EUXNQ M2DBVIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? MWOyOlEzOTJ3MR?=
G 40 SC NVqwblhxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoqwNE4xPS1{MDFOwG0> MXWyOE84OiCq NIPENWFFVVOR MkG1bY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBidmRidHnt[UBl\XCnbnTlcpRtgQ>? NHLhS|gzPjF{MUK1NS=>
G 35 DC NHS3S2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnuxNE4xPS1{MDFOwG0> MYCyOE84OiCq M1naXWROW09? NFnQe25qdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 NX\KOWdJOjZzMkGyOVE>
G 38 DC NIjadGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjlTVgxNjB3LUKwJO69VQ>? MV2yOE84OiCq NYD5N3pMTE2VTx?= MVXpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueIx6 NXe4[ZBwOjZzMkGyOVE>
G 40 DC M3XpOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1n4VlAvODVvMkCg{txO NWPlXm5LOjRxN{KgbC=> NIjyNpZFVVOR M{nHfolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? NHrob48zPjF{MUK1NS=>
RD MlPFRZBweHSxc3nzJGF{e2G7 NFPqNmgyNzFwNT:yJO69VQ>? M3;KOlczKGh? MnnLbY5lfWOnczDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCJQV7UOlE> NX3nZo9mOjV5NEmzO|g>
TE381.T MVjBdI9xfG:|aYOgRZN{[Xl? NXm0coR{OS9zLkWvNkDPxE1? MlXXO|IhcA>? MV\pcoR2[2W|IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKEeDTmS2NS=> MVmyOVc1QTN5OB?=
RMS13 NH2y[XFCeG:ydH;zbZMhSXO|YYm= MkDJNU8yNjVxMjFOwG0> M37DW|czKGh? NF\FXmFqdmS3Y3XzJIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIFfBUnQ3OQ>? MVGyOVc1QTN5OB?=
RH30  MkfWRZBweHSxc3nzJGF{e2G7 MofXNU8yNjVxMjFOwG0> NILvPZA4OiCq M3TDc4lv\HWlZYOgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiR1HOWFYy M1XvWlI2PzR7M{e4
VJ MUfBdI9xfG:|aYOgRZN{[Xl? NVvUbXpPOS9zLkWvNkDPxE1? NHu1dpM4OiCq M2jwbolv\HWlZYOgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiR1HOWFYy NIXlS|kzPTd2OUO3PC=>
HS578T M2DscGNmdGxiVnnhZoltcXS7IFHzd4F6 MUmwMVMh|ryP NHXi[ZI4OiCq M3TYbYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? Mor4NlU4OjF2MUm=
BT549 M2PGd2NmdGxiVnnhZoltcXS7IFHzd4F6 NX3PU3dNOC1|IN88US=> MlPkO|IhcA>? NHi4eFVqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NYPROZRzOjV5MkG0NVk>
MDA-MB-231 MV;D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MnHvNE0{KM7:TR?= NEmwZWQ4OiCq MlKzbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? M{XzXFI2PzJzNEG5
MDA-MB-468 MoHYR4VtdCCYaXHibYxqfHliQYPzZZk> NE\1XGoxNTNizszN NHvzdHU4OiCq NH7BTYNqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 M3fUOlI2PzJzNEG5
MDA-MB-436 M1vCSWNmdGxiVnnhZoltcXS7IFHzd4F6 NWTHfnJLOC1|IN88US=> NVHuPGczPzJiaB?= MYLpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NYG3d4xCOjV5MkG0NVk>
SUM149PT NUXaW41zS2WubDDWbYFjcWyrdImgRZN{[Xl? MoLDNE0{KM7:TR?= M1HpclczKGh? NULURWZscW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MXuyOVczOTRzOR?=
MDA-MB-468 MX3GeY5kfGmxbjDBd5NigQ>? NInm[lgxNjBzLUGwJO69VQ>? MVKyOEBp M{Pj[IRwf26{ZXf1cIF1\XNidHjlJIxmfmWuczDv[kDPui2WclPQNUwh[y2PeXOgZY5lKGO7Y3zpckBGKHC{b4TlbY5{yqB? NXvEeoJxOjV5MkG0NVk>
MDA-MB-231 NInYeYZHfW6ldHnvckBCe3OjeR?= NUe5dXpYOC5yMT2xNEDPxE1? MUKyOEBp NXT5NpF6\G:5boLl[5Vt[XSnczD0bIUhdGW4ZXzzJI9nKM7{LWTyR3AyNCClLV35Z{BidmRiY4njcIlvKEVicILveIVqdnQEoB?= MlP6NlU4OjF2MUm=
HS578T NWDM[ppzTnWwY4Tpc44hSXO|YYm= MVqwMlAyNTFyIN88US=> MoTmNlQhcA>? NF:0OXVld3ewcnXneYxifGW|IITo[UBt\X[nbIOgc4Yh|rJvVILDVFEtKGNvTYnjJIFv\CCleXPsbY4hTSCycn;0[Ylve8Li MoTXNlU4OjF2MUm=
SW872 NETwN2xHfW6ldHnvckBCe3OjeR?= M2niUFAvODFvMD61JO69VQ>? MojBNlQhcA>? NFHMNWpz\WS3Y3XzJGFMXCCyaH;zdIhwenmuYYTpc44hMHCDS2SpJIFv\CB2RVLQNUBxcG:|cHjvdplt[XSrb36gLJA1TUKSMTmgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYNCpC=> MUGyOFY6PTZ|Mh?=
SW982 MlPBSpVv[3Srb36gRZN{[Xl? NIfUS28xNjBzLUCuOUDPxE1? NH[wbHkzPCCq NX60d4p{emWmdXPld{BCU1RicHjvd5Bpd3K7bHH0bY9vKCiyQVvULUBidmRiNFXCVFEheGixc4Doc5J6dGG2aX;uJEhxPEWEUEGpJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXyxsA> MYmyOFY6PTZ|Mh?=
SW872 M2LoVWFxd3C2b4Ppd{BCe3OjeR?= MYOwMlAyNTBwNTFOwG0> NEPyZlA1QCCq M3Tzd4lv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NFXve5ozPDZ7NU[zNi=>
SW982 MoWyRZBweHSxc3nzJGF{e2G7 NVLDbmlxOC5yMT2wMlUh|ryP MU[0PEBp NFzRcm9qdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 M4XUXlI1Pjl3NkOy
AGS HG NHvFbVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHvTWM2OD1yLk[4JOKyKDBwMEOxJO69VQ>? MX2yOFU6PzR5OB?=
AGS LG MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF64WlRKSzVyPUCuNFUhyrFiMD6wNFEh|ryP MXOyOFU6PzR5OB?=
HGC27 HG NXXFdXFbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlj5TWM2OD1yLkO4JOKyKDBwMEKyJO69VQ>? NVzlc4tQOjR3OUe0O|g>
HGC27 LG MoHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzUTWM2OD1yLkCyJOKyKDBwMEC0JO69VQ>? NXPZdo5COjR3OUe0O|g>
MKN45 HG M1nadWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTFwMEGgxtEhOC5yNUGg{txO NIjMbJczPDV7N{S3PC=>
MKN45 LG NX3LS2lZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2H6cmlEPTB;MD64O{DDuSByLkCzNEDPxE1? MnT6NlQ2QTd2N{i=
NUGC4 HG M1n3d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrIRnBKSzVyPUG0MlAhyrFiMz65NVMh|ryP M1XjXFI1PTl5NEe4
NUGC4 LG NIWzOXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\DNYVKSzVyPUG0MlAhyrFiNT6zNlEh|ryP NEntXIszPDV7N{S3PC=>
A549 M1TFOmZ2dmO2aX;uJGF{e2G7 Mof0NE4zPS9yLkWvNUDPxE1? NUOw[m1QOjRiaB?= M4\afIlvcGmkaYTzJGFsfCCyaH;zdIhwenmuYYTpc44he2yrZ3j0cJk> MoG0NlQ{PTF2MkW=
H460 MWLGeY5kfGmxbjDBd5NigQ>? MmX0NE4zPS9yLkWvNUDPxE1? M13KTVI1KGh? MWXpcohq[mm2czDBb5QheGixc4Doc5J6dGG2aX;uJJNtcWeqdHz5 NHTxNZAzPDN3MUSyOS=>
H661 NUH3fYpITnWwY4Tpc44hSXO|YYm= NUT5emx3OC5{NT:wMlUwOSEQvF2= M4qwfVI1KGh? NXL2VYR[cW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|aXfubYZq[2GwdHz5 NUPySHN{OjR|NUG0NlU>
SAS NITHV2lHfW6ldHnvckBCe3OjeR?= NXjFfYlDOC5{NT:wMlUwOSEQvF2= MVeyOEBp NEi3WJRqdmirYnn0d{BCc3RicHjvd5Bpd3K7bHH0bY9vKHOrZ37p[olk[W62bIm= MVmyOFM2OTR{NR?=
UT5 MYHGeY5kfGmxbjDBd5NigQ>? M3rheFAvOjVxMD61M|Eh|ryP NV;tWng5OjRiaB?= MlvhbY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7 NI\kZnczPDN3MUSyOS=>
FaDu MkXSSpVv[3Srb36gRZN{[Xl? M1zrRlAvOjVxMD61M|Eh|ryP MmrNNlQhcA>? NWC1VFRXcW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|aXfubYZq[2GwdHz5 NWqzbXR[OjR|NUG0NlU>
RD MW\BdI9xfG:|aYOgRZN{[Xl? MlXQNU8yNjVxMjFOwG0> NVSzOWllPzJiaB?= NX73bXFyTE2VTx?= MW\pcoR2[2W|IHPhd5Bie2VvZHXw[Y5l\W62IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKFWRMUK2 M4jjZVI{Pjh2OUK1
TE671 MkDyRZBweHSxc3nzJGF{e2G7 M4\BWFEwOS53L{Kg{txO NX\MbFZZPzJiaB?= NFLCOm9FVVOR M{X6WYlv\HWlZYOgZ4F{eGG|ZT3k[ZBmdmSnboSgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiVV:xNlY> NVTiU5ZiOjN4OES5NlU>
RH30  MmnCRZBweHSxc3nzJGF{e2G7 NWHFWmhmOS9zLkWvNkDPxE1? MkDpO|IhcA>? MoDmSG1UVw>? MVXpcoR2[2W|IHPhd5Bie2VvZHXw[Y5l\W62IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKFWRMUK2 NVG4cWh5OjN4OES5NlU>
RMS13 MXzBdI9xfG:|aYOgRZN{[Xl? MlH0NU8yNjVxMjFOwG0> Ml\OO|IhcA>? M4L5RmROW09? MVTpcoR2[2W|IHPhd5Bie2VvZHXw[Y5l\W62IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKFWRMUK2 NGjjOFAzOzZ6NEmyOS=>
SUM149PT Mmr3R4VtdCCYaXHibYxqfHliQYPzZZk> M4q5fFAvOyEQvF2= MmLMO|IhcA>? NHHRbGVmdmijbnPld{BkgXSxdH;4bYMh\W[oZXP0d{Bw\iCSSUPLM2FMXCCyYYToe4F6KGmwaHnibZRwenN? NYLuelBNOjN4MEGwO|Q>
MDA-MB-468 Mn[5R4VtdCCYaXHibYxqfHliQYPzZZk> MkC5NE4{KM7:TR?= NEfofZU4OiCq NUHtb2hL\W6qYX7j[ZMh[3m2b4TvfIlkKGWoZnXjeJMhd2ZiUFmzT{9CU1RicHH0bJdigSCrbnjpZol1d3K| NX7j[Y01OjN4MEGwO|Q>
MDA-MB-231 NGrtWpdE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M{D3TlAvOyEQvF2= NWDybpRlPzJiaB?= M2nueIVvcGGwY3XzJIN6fG:2b4jpZ{Bm\m[nY4TzJI9nKFCLM1uvRWtVKHCjdHj3ZZkhcW6qaXLpeI9zew>? M3PqNlI{PjBzMEe0
SY5Y M2XXbWZ2dmO2aX;uJGF{e2G7 NVLKVYpSOS53L{KuOU82KM7:TR?= Mn\HNlQhcA>? M2\Id4lv\HWlZYOgS|HDqGOnbHytZ5lkdGViYYLy[ZN1KGGwZDDhdI9xfG:|aYO= NVjVS4VVOjN|N{izOFE>
SKNBE(2c) MlrZSpVv[3Srb36gRZN{[Xl? MVKxMlUwOi53L{Wg{txO NULoRXdZOjRiaB?= NWTZWmlXcW6mdXPld{BIOcLiY3XscE1kgWOuZTDhdpJme3RiYX7kJIFxd3C2b4Ppdy=> MX6yN|M4QDN2MR?=
RD Ml3rRZBweHSxc3nzJGF{e2G7 NXy1R4RTOyEEtV2= MnzPNVIhcA>? NEX4cHdFVVOR M4HmUJNmdnOrdHn6[ZMhWkRiY3XscJMhfG9iRF;YMYlv\HWlZXSgZZBweHSxc3nz NWXmc29NOjN|MEC4NFk>
TP5014 Ml;TRZBweHSxc3nzJGF{e2G7 MUizJOK2VQ>? NHu5bWgyOiCq MVTEUXNQ NF;EZ45{\W6|aYTpfoV{KFKGIHPlcIx{KHSxIFTPXE1qdmS3Y3XkJIFxd3C2b4Ppdy=> MkjsNlM{ODB6MEm=
HT1080 M33ONWFxd3C2b4Ppd{BCe3OjeR?= NH7zSIc{KML3TR?= MoiyNVIhcA>? MlvlSG1UVw>? MlXNd4Vve2m2aYrld{BTTCClZXzsd{B1dyCGT2itbY5lfWOnZDDhdI9xfG:|aYO= NGexT4wzOzNyMEiwPS=>
A549 NFPCOZNHfW6ldHnvckBCe3OjeR?= NWLVRWVQOC1|LkOg{txO Mn7sO|IhcA>? NVSzT3RscW6mdXPld{Bkd22ybHX0[UBld3ewcnXneYxifGmxbjDv[kBxSUuW NF74[3MzOzJ3OUW5NS=>
HCC827 M2DiXmZ2dmO2aX;uJGF{e2G7 M{XNNFAuOy5|IN88US=> MXK3NkBp NY\NO4F{cW6mdXPld{Bkd22ybHX0[UBld3ewcnXneYxifGmxbjDv[kBxSUuW MWmyN|I2QTV7MR?=
H3122 MXfGeY5kfGmxbjDBd5NigQ>? NF\GN|kxNTNwMzFOwG0> M1TlO|czKGh? NWXOc5hDcW6mdXPld{Bkd22ybHX0[UBld3ewcnXneYxifGmxbjDv[kBxSUuW NEe1fpQzOzJ3OUW5NS=>
TALL-1 NWKxUHdNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXqx5qCK|ryP MmH4O{Bl MX7k[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> NFz2UIQzOzB|OEK3Ny=>
HPB-ALL NGPPcnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzRW5dTOeLCid88US=> M370V|ch\A>? NVHaWJFr\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 NXfmWHViOjNyM{iyO|M>
DND41 NV7TcFdzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDOSZQxOeLCid88US=> M1HSdFch\A>? M{XmV4Rm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? MVeyN|A{QDJ5Mx?=
SUP-T1 NHi3UWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV:x5qCK|ryP MWK3JIQ> MV;k[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> M{X1[|I{ODN6Mkez
PEER MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnrepBxOeLCid88US=> NHjVW2c4KGR? Mnv6[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 MoL4NlMxOzh{N{O=
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MOLT-16 NG\TXGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLIdVRbOeLCid88US=> MojhO{Bl NILNOYJl\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? NW\RPYJ5OjNyM{iyO|M>
MM1S MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7GbIwxNTJizszN NIq4fmczPCCq MoHJTWM2OD1yLkWg{txO NHrGSmYzOjh{OUKzOC=>
NCI-H929 NYjDV2l7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYWwMVIh|ryP MkL0NlQhcA>? NFnRXXhKSzVyPUCuNlUh|ryP MmTmNlI5Ojl{M{S=
KMS12-BM  MmLwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXBNE0zKM7:TR?= MknaNlQhcA>? MWLJR|Ux97zgMjFOwG0> M2DtOVIzQDJ7MkO0
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HCC827 Mn;rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HwO|AuOyEQvF2= MnfSO|IhcA>? NYLYPHFIUUN3ME2wMlMh|ryP MmDTNlEzOjB2N{S=
PC-9  NVfR[VVRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWewMVMh|ryP Ml75O|IhcA>? M1j0TGlEPTB;MD64JO69VQ>? NYDtfZJOOjF{MkC0O|Q>
LN229 NWTlNFJ4TnWwY4Tpc44hSXO|YYm= M1HRN|Eh|ryP MojNOFghcA>? MlrCbY5lfWOnczDheZRweGijZ3;zc41mKG[xcn3heIlwdg>? NInLVIEzOTB4Mkm5Ny=>
U87 MWDGeY5kfGmxbjDBd5NigQ>? MWmxJO69VQ>? M4jad|Q5KGh? MV\pcoR2[2W|IHH1eI9xcGGpb4PvcYUh\m:{bXH0bY9v Mo\ONlExPjJ7OUO=
U373 NVrX[o9CTnWwY4Tpc44hSXO|YYm= NFKyO|cyKM7:TR?= MWi0PEBp NEXB[HJqdmS3Y3XzJIF2fG:yaHHnc5NwdWViZn;ycYF1cW:w NUezWVVmOjFyNkK5PVM>
SF767 M{PNfmZ2dmO2aX;uJGF{e2G7 MWmxJO69VQ>? NYm5[pBPPDhiaB?= M1HGPIlv\HWlZYOgZZV1d3CqYXfvd49u\SCob4LtZZRqd25? NGTWd4UzOTB4Mkm5Ny=>
Mel-Juso NFq0[YZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NFXtXYQxNjBz4pETNVDjiIoQvF2= MkSyO|IhcA>? NEDBTHhqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NH[yWlkzOTB2OEe4OS=>
518A2  M4TTfWNmdGxiVnnhZoltcXS7IFHzd4F6 MkS3NE4xOeLCk{Gw5qCK|ryP NHTWZ|M4OiCq MmPubY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? Mo\ZNlExPDh5OEW=
Mel-Juso  NFzRUGhHfW6ldHnvckBCe3OjeR?= Mn\aNE4xODIkgKOx5qCK|ryP MlrSNlQhcA>? NIDZPGJ{fXCycnXzd4V{KHCqb4PwbI9zgWyjdHnvckBw\iCyaH;zdIhifGmmeXygbY5we2m2b3ygN{1scW6jc3Wg[I94dnO2cnXhcUB1[XKpZYTz NFjE[|YzOTB2OEe4OS=>
518A2 NGLDcHNHfW6ldHnvckBCe3OjeR?= M4PUPVAvODBz4pETNgKBkc7:TR?= M2fQV|I1KGh? Mneyd5VxeHKnc4Pld{BxcG:|cHjvdplt[XSrb36gc4YheGixc4DoZZRq\HmuIHnuc5NqfG:uIEOtb4lv[XOnIHTve45{fHKnYX2geIFz\2W2cx?= NFPnZpIzOTB2OEe4OS=>
PC3  MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPSRXc6OjSq M4DoZ2dKPTEEoE2gNVAxKG6P NUTKRXZzOjB3NUGwOlE>
U87MG M1q2W2Z2dmO2aX;uJGF{e2G7 NF7aXY0xNjFvMTFOwG0> MkC1NlTjiImqwrC= M2O3NmROW09? MkXGbY5pcWKrdIOgVGk{Uy2vZXTpZZRm\CC|aXfuZYxqdmd? MYOxPVY{OzZ6Mx?=
U138MG Ml3GSpVv[3Srb36gRZN{[Xl? NXHTXo5lOC5zLUGg{txO NHTpTogzPOLCiXlCpC=> M4XHSmROW09? NWjjS49ncW6qaXLpeJMhWEl|Sz3t[YRq[XSnZDDzbYdv[Wyrbne= NGC3dmoyQTZ|M{[4Ny=>
U118MG MoLKSpVv[3Srb36gRZN{[Xl? Mk\PNE4yNTFizszN MnPQNlTjiImqwrC= M2exPWROW09? M{[zUolvcGmkaYTzJHBKO0tvbXXkbYF1\WRic3nncoFtcW6p NFr6[XYyQTZ|M{[4Ny=>
U87MG NUDJ[XV2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;PVmlEPTB;MD6xOEDPxE1? NFq4VmgyQTV6NEKyOy=>
IGROV-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTBwME[g{txO M4\qelE6PTh2MkK3
DETROIT562 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTwZXpKSzVyPUCuNVMh|ryP MV6xPVU5PDJ{Nx?=
PC3  MoPBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXsc4puUUN3ME2wMlExKM7:TR?= MmrnNVk2QDR{Mke=
SKOV-3 M1z0bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTBwMUKg{txO M3zQfFE6PTh2MkK3
HUVEC MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkftTWM2OD1yLkC4JO69VQ>? MmD5NVk2QDR{Mke=
UCH-1  MVLGeY5kfGmxbjDBd5NigQ>? NFzNbJMxNTVizszN M1[wUYlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiYn;0bEBCU1RiYX7kJI1VV1JiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NIXQWJgyQTV{OES0NS=>
UCH-1  MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWSwMlAyNTFyIN88US=> MUK2JIQ> M3jBOolvcGmkaYTzJJBzd2yrZnXyZZRqd25iZH;z[UBl\XCnbnTlcpRtgQ>? NUP4SYNbOTl3Mki0OFE>
UCH-1  MVXBdI9xfG:|aYOgRZN{[Xl? MmHSNE4yNTFyIN88US=> MoS3NlQhcA>? M3\ofGROW09? NGDMXGxqdmS3Y3XzJIFxd3C2b4Ppdy=> M3LVVFE6PTJ6NESx

... 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 <1 mg/mL
Ethanol <1 mg/mL
In vivo 1% DMSO+30% polyethylene glycol+1% Tween 80 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID