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 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\mTVAuQCEQvF2= MlHaNlQwPDhxN{KgbC=> MVHpcoR2[2W|IITpcYUuKGGwZDDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCrbnjpZol1cW:wIH;uJG5DKGOnbHyg[5Jwf3Sq NX;mN5lpOjZ{MkS2PFE>
SH-SY5Y M1TsZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7TXoQxNThizszN MmfWNlQwPDhxN{KgbC=> MXHpcoR2[2W|IITpcYUuKGGwZDDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCrbnjpZol1cW:wIH;uJG5DKGOnbHyg[5Jwf3Sq NETQRZUzPjJ{NE[4NS=>
SH-SY5Y  M17NWWFxd3C2b4Ppd{BCe3OjeR?= M4\PNVEh|ryP MmPUNE42NTJ2IHi= M1LaO5NmdnOrdHn6[ZMhdmW3cn;icIF{fG:vYTDj[YxteyC2bzDkc5hwenWkaXPpck1qdmS3Y3XkJIFxd3C2b4Ppdy=> MUWyOlIzPDZ6MR?=
G 35 SC MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7SSJpSOC5yNT2yNEDPxE1? NXexV3NkOjRxN{KgbC=> NEHmb2FFVVOR NV7WV5BScW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= NFzuZW0zPjF{MUK1NS=>
G 38 SC MnGwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFqwSo0xNjB3LUKwJO69VQ>? MXWyOE84OiCq MX7EUXNQ MWfpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueIx6 M{PkcVI3OTJzMkWx
G 40 SC MlPkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfabIsxNjB3LUKwJO69VQ>? NXG0R|MyOjRxN{KgbC=> MWfEUXNQ M3X6XYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? MV6yOlEzOTJ3MR?=
G 35 DC MoW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDaNE4xPS1{MDFOwG0> NEX6THEzPC95MjDo MlXGSG1UVw>? NICyXWpqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 MV2yOlEzOTJ3MR?=
G 38 DC MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWGwMlA2NTJyIN88US=> M1vBVlI1Nzd{IHi= MnKxSG1UVw>? NX\CNWR5cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= M{S0dVI3OTJzMkWx
G 40 DC NVvJZXcyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmL4NE4xPS1{MDFOwG0> NGHzfWgzPC95MjDo MmjsSG1UVw>? M3PkbYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? MVeyOlEzOTJ3MR?=
RD MnHORZBweHSxc3nzJGF{e2G7 NHTuTYoyNzFwNT:yJO69VQ>? NGn0NVg4OiCq NF;KbmVqdmS3Y3XzJIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIFfBUnQ3OQ>? NUDnTZFoOjV5NEmzO|g>
TE381.T NY\3OVAySXCxcITvd4l{KEG|c3H5 MVuxM|EvPS9{IN88US=> NEn0T5A4OiCq NUnIUnNOcW6mdXPld{BieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDHRW5VPjF? NUSyOZhmOjV5NEmzO|g>
RMS13 NWG5TW85SXCxcITvd4l{KEG|c3H5 Ml\INU8yNjVxMjFOwG0> M1;Cd|czKGh? NUTBVY97cW6mdXPld{BieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDHRW5VPjF? NUnYO2tTOjV5NEmzO|g>
RH30  NVz1VnI4SXCxcITvd4l{KEG|c3H5 MXOxM|EvPS9{IN88US=> NHzqd4U4OiCq MlPnbY5lfWOnczDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCJQV7UOlE> MWGyOVc1QTN5OB?=
VJ NH\pXIlCeG:ydH;zbZMhSXO|YYm= NIK3WoQyNzFwNT:yJO69VQ>? NUnIbXNrPzJiaB?= NH7JcXRqdmS3Y3XzJIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIFfBUnQ3OQ>? M1zkdlI2PzR7M{e4
HS578T MXrD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NXHxXVlvOC1|IN88US=> MUG3NkBp M17DeIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NFTOUpUzPTd{MUSxPS=>
BT549 NXrMd|d[S2WubDDWbYFjcWyrdImgRZN{[Xl? NFXFNnYxNTNizszN M3j3fFczKGh? MUnpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MXGyOVczOTRzOR?=
MDA-MB-231 NUnue2ZzS2WubDDWbYFjcWyrdImgRZN{[Xl? NUfleW9qOC1|IN88US=> MlK0O|IhcA>? MXLpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 M{Xyc|I2PzJzNEG5
MDA-MB-468 NV6xdIpYS2WubDDWbYFjcWyrdImgRZN{[Xl? NFHscFcxNTNizszN NWrmSG9xPzJiaB?= M{O4SolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NInNdGQzPTd{MUSxPS=>
MDA-MB-436 NYD5[Xd2S2WubDDWbYFjcWyrdImgRZN{[Xl? Ml;pNE0{KM7:TR?= MkWzO|IhcA>? NYj6W|VicW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= M{fRS|I2PzJzNEG5
SUM149PT NHPhUYVE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MkDINE0{KM7:TR?= NUjUd2RFPzJiaB?= Mon4bY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MkLrNlU4OjF2MUm=
MDA-MB-468 NYDiVZlYTnWwY4Tpc44hSXO|YYm= NX2xbmk{OC5yMT2xNEDPxE1? NVfvb3lOOjRiaB?= Mnj4[I94dnKnZ4XsZZRmeyC2aHWgcIV3\Wy|IH;mJO6zNVS{Q2CxMEBkNU27YzDhcoQh[3mlbHnuJGUheHKxdHXpcpPDqA>? MX:yOVczOTRzOR?=
MDA-MB-231 NY\qOoNVTnWwY4Tpc44hSXO|YYm= MYmwMlAyNTFyIN88US=> M1vseVI1KGh? NX\p[XFV\G:5boLl[5Vt[XSnczD0bIUhdGW4ZXzzJI9nKM7{LWTyR3AyNCClLV35Z{BidmRiY4njcIlvKEVicILveIVqdnQEoB?= NVLYOIc4OjV5MkG0NVk>
HS578T NIXhVGhHfW6ldHnvckBCe3OjeR?= NInyeJQxNjBzLUGwJO69VQ>? NIHiZVUzPCCq NX7yWY1w\G:5boLl[5Vt[XSnczD0bIUhdGW4ZXzzJI9nKM7{LWTyR3AyNCClLV35Z{BidmRiY4njcIlvKEVicILveIVqdnQEoB?= NFzOSVIzPTd{MUSxPS=>
SW872 NHfyO|ZHfW6ldHnvckBCe3OjeR?= M3PTe|AvODFvMD61JO69VQ>? NIq3[|MzPCCq NYrD[XNVemWmdXPld{BCU1RicHjvd5Bpd3K7bHH0bY9vKCiyQVvULUBidmRiNFXCVFEheGixc4Doc5J6dGG2aX;uJEhxPEWEUEGpJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXyxsA> MX:yOFY6PTZ|Mh?=
SW982 MkPsSpVv[3Srb36gRZN{[Xl? M4HJZ|AvODFvMD61JO69VQ>? MWKyOEBp NXTHPGdtemWmdXPld{BCU1RicHjvd5Bpd3K7bHH0bY9vKCiyQVvULUBidmRiNFXCVFEheGixc4Doc5J6dGG2aX;uJEhxPEWEUEGpJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXyxsA> MVmyOFY6PTZ|Mh?=
SW872 NFm0WHdCeG:ydH;zbZMhSXO|YYm= MlXvNE4xOS1yLkWg{txO MXK0PEBp MVrpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NFflR5kzPDZ7NU[zNi=>
SW982 MX\BdI9xfG:|aYOgRZN{[Xl? MXmwMlAyNTBwNTFOwG0> NV;6XVFzPDhiaB?= NGTSNZNqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 MV[yOFY6PTZ|Mh?=
AGS HG NHL2d2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnTWIJrUUN3ME2wMlY5KMLzIECuNFMyKM7:TR?= M1exPVI1PTl5NEe4
AGS LG MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LiUWlEPTB;MD6wOUDDuSByLkCwNUDPxE1? NIjF[3ozPDV7N{S3PC=>
HGC27 HG NEnLSW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TOTmlEPTB;MD6zPEDDuSByLkCyNkDPxE1? MmC4NlQ2QTd2N{i=
HGC27 LG MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7zRYIzUUN3ME2wMlAzKMLzIECuNFA1KM7:TR?= NXTFeGJFOjR3OUe0O|g>
MKN45 HG MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTFwMEGgxtEhOC5yNUGg{txO NWSyRmlvOjR3OUe0O|g>
MKN45 LG NYfwWGVmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;2dnRKSzVyPUCuPFchyrFiMD6wN|Ah|ryP NWPqOJNGOjR3OUe0O|g>
NUGC4 HG NV\vdHVmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTF2LkCgxtEhOy57MUOg{txO Mln2NlQ2QTd2N{i=
NUGC4 LG NYn3T3JwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzJbnFKSzVyPUG0MlAhyrFiNT6zNlEh|ryP NHnMNWIzPDV7N{S3PC=>
A549 NVrkTppjTnWwY4Tpc44hSXO|YYm= MWewMlI2NzBwNT:xJO69VQ>? M{fkbFI1KGh? M2jKRYlvcGmkaYTzJGFsfCCyaH;zdIhwenmuYYTpc44he2yrZ3j0cJk> MmTHNlQ{PTF2MkW=
H460 M13vSGZ2dmO2aX;uJGF{e2G7 MUSwMlI2NzBwNT:xJO69VQ>? MXeyOEBp MXXpcohq[mm2czDBb5QheGixc4Doc5J6dGG2aX;uJJNtcWeqdHz5 MY[yOFM2OTR{NR?=
H661 M{GzRWZ2dmO2aX;uJGF{e2G7 NH\FXmMxNjJ3L{CuOU8yKM7:TR?= MkGyNlQhcA>? Ml3GbY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7 NIH0NnczPDN3MUSyOS=>
SAS NXfLenJGTnWwY4Tpc44hSXO|YYm= MmXvNE4zPS9yLkWvNUDPxE1? M3;JeFI1KGh? MnzSbY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7 M1XEOlI1OzVzNEK1
UT5 MXPGeY5kfGmxbjDBd5NigQ>? MXOwMlI2NzBwNT:xJO69VQ>? NGHrOWczPCCq NYDJZWRrcW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|aXfubYZq[2GwdHz5 NXjjeJRLOjR|NUG0NlU>
FaDu NVHTbZZLTnWwY4Tpc44hSXO|YYm= MoXHNE4zPS9yLkWvNUDPxE1? MXyyOEBp NXf0PXRXcW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|aXfubYZq[2GwdHz5 NEjJfXUzPDN3MUSyOS=>
RD MVPBdI9xfG:|aYOgRZN{[Xl? MoPtNU8yNjVxMjFOwG0> NHXmN5U4OiCq MYXEUXNQ M1TNU4lv\HWlZYOgZ4F{eGG|ZT3k[ZBmdmSnboSgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiVV:xNlY> NWnTeG1COjN4OES5NlU>
TE671 MXzBdI9xfG:|aYOgRZN{[Xl? MXSxM|EvPS9{IN88US=> MYi3NkBp M3ywVWROW09? NYj1[Yd4cW6mdXPld{Bk[XOyYYPlMYRmeGWwZHXueEBieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDVU|EzPg>? NGKzTZczOzZ6NEmyOS=>
RH30  NVfMboJRSXCxcITvd4l{KEG|c3H5 MmnvNU8yNjVxMjFOwG0> NGm0V3A4OiCq NHjMRohFVVOR NVTOcWhQcW6mdXPld{Bk[XOyYYPlMYRmeGWwZHXueEBieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDVU|EzPg>? M4TUe|I{Pjh2OUK1
RMS13 NV7nN2JXSXCxcITvd4l{KEG|c3H5 NYPKXVZiOS9zLkWvNkDPxE1? NW\SZ29WPzJiaB?= NU[yTWI6TE2VTx?= NX[5dYlCcW6mdXPld{Bk[XOyYYPlMYRmeGWwZHXueEBieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDVU|EzPg>? MoLsNlM3QDR7MkW=
SUM149PT NGfISVJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NFXJWJUxNjNizszN NF\qVIs4OiCq MXHlcohidmOnczDjfZRwfG:6aXOg[YZn\WO2czDv[kBRUTONL1HLWEBx[XSqd3H5JIlvcGmkaYTvdpM> NUnyeIV2OjN4MEGwO|Q>
MDA-MB-468 MXHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M2LlT|AvOyEQvF2= NXr5SYZQPzJiaB?= NULOTpNO\W6qYX7j[ZMh[3m2b4TvfIlkKGWoZnXjeJMhd2ZiUFmzT{9CU1RicHH0bJdigSCrbnjpZol1d3K| M1P1[lI{PjBzMEe0
MDA-MB-231 NEH4XWdE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MkjsNE4{KM7:TR?= M{DiO|czKGh? NY\CN29z\W6qYX7j[ZMh[3m2b4TvfIlkKGWoZnXjeJMhd2ZiUFmzT{9CU1RicHH0bJdigSCrbnjpZol1d3K| Mk\KNlM3ODFyN{S=
SY5Y MWnGeY5kfGmxbjDBd5NigQ>? NGDqfo4yNjVxMj61M|Uh|ryP MYGyOEBp NVfGfG56cW6mdXPld{BIOcLiY3XscE1kgWOuZTDhdpJme3RiYX7kJIFxd3C2b4Ppdy=> Mn7GNlM{Pzh|NEG=
SKNBE(2c) NFf4SotHfW6ldHnvckBCe3OjeR?= NESwOI0yNjVxMj61M|Uh|ryP M3LOXFI1KGh? M1vT[olv\HWlZYOgS|HDqGOnbHytZ5lkdGViYYLy[ZN1KGGwZDDhdI9xfG:|aYO= NXSw[nN{OjN|N{izOFE>
RD MXfBdI9xfG:|aYOgRZN{[Xl? MVOzJOK2VQ>? M3;IT|EzKGh? M1XDPWROW09? MmP3d4Vve2m2aYrld{BTTCClZXzsd{B1dyCGT2itbY5lfWOnZDDhdI9xfG:|aYO= M1\oTVI{OzByOEC5
TP5014 M{XkZ2Fxd3C2b4Ppd{BCe3OjeR?= NXKzTlVpOyEEtV2= MX2xNkBp NIL3OmdFVVOR NX\0fFk4e2Wwc3n0bZpmeyCURDDj[YxteyC2bzDEU3gucW6mdXPl[EBieG:ydH;zbZM> MWWyN|MxODhyOR?=
HT1080 MVjBdI9xfG:|aYOgRZN{[Xl? NVP5SWg{OyEEtV2= NEXiXmwyOiCq MV\EUXNQ NFnRfoh{\W6|aYTpfoV{KFKGIHPlcIx{KHSxIFTPXE1qdmS3Y3XkJIFxd3C2b4Ppdy=> NGPuRoozOzNyMEiwPS=>
A549 MXvGeY5kfGmxbjDBd5NigQ>? NFG5VYsxNTNwMzFOwG0> MYq3NkBp M{XEVIlv\HWlZYOgZ49ueGyndHWg[I94dnKnZ4XsZZRqd25ib3[gdGFMXA>? NF65T|AzOzJ3OUW5NS=>
HCC827 NHPIfIJHfW6ldHnvckBCe3OjeR?= M4X4ZlAuOy5|IN88US=> M{naflczKGh? NXLxeXZTcW6mdXPld{Bkd22ybHX0[UBld3ewcnXneYxifGmxbjDv[kBxSUuW NF;jT5MzOzJ3OUW5NS=>
H3122 MWfGeY5kfGmxbjDBd5NigQ>? MUKwMVMvOyEQvF2= NYfmb5E2PzJiaB?= NIfQbJVqdmS3Y3XzJINwdXCuZYTlJIRwf26{ZXf1cIF1cW:wIH;mJJBCU1R? NHzzUmczOzJ3OUW5NS=>
TALL-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX2x5qCK|ryP NGHWdYE4KGR? NGDKWoZl\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? M1X1WlI{ODN6Mkez
HPB-ALL NInFcIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYSx5qCK|ryP Ml3aO{Bl NHP3c2Fl\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? NF;BeJMzOzB|OEK3Ny=>
DND41 NIi2S|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\LXlHjiIoQvF2= MniyO{Bl NFnX[pJl\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? NFqwXoczOzB|OEK3Ny=>
SUP-T1 NYrTTm81T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPHOVNOOeLCid88US=> NHW1SIM4KGR? MVzk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> NVvaZnc{OjNyM{iyO|M>
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KMS12-BM  MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PoS|AuOiEQvF2= M2fhVlI1KGh? MofBTWM2OO,:nkKg{txO MorNNlI5Ojl{M{S=
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HCC827 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HqUlAuOyEQvF2= NGPzbmI4OiCq NVnKXWtYUUN3ME2wMlMh|ryP NHHTXpczOTJ{MES3OC=>
PC-9  NGLuV3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnLSFVVOC1|IN88US=> NGSwbIc4OiCq MYrJR|UxRTBwODFOwG0> M2W2XlIyOjJyNEe0
LN229 MmLzSpVv[3Srb36gRZN{[Xl? M{XaW|Eh|ryP NUPDfJRiPDhiaB?= NFjGNHdqdmS3Y3XzJIF2fG:yaHHnc5NwdWViZn;ycYF1cW:w M1ficlIyODZ{OUmz
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SF767 MVjGeY5kfGmxbjDBd5NigQ>? M4\p[|Eh|ryP Ml\yOFghcA>? MnjrbY5lfWOnczDheZRweGijZ3;zc41mKG[xcn3heIlwdg>? M3Pn[VIyODZ{OUmz
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518A2  NV3RNpBnS2WubDDWbYFjcWyrdImgRZN{[Xl? MUWwMlAy6oDVMUFihKnPxE1? NXTJOo9RPzJiaB?= NXPMVphPcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= M1jNNVIyODR6N{i1
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518A2 NVu2b|BzTnWwY4Tpc44hSXO|YYm= MmL3NE4xODIkgKOx5qCK|ryP M1fqcFI1KGh? NUHyXWRne3WycILld5NmeyCyaH;zdIhwenmuYYTpc44hd2ZicHjvd5Bp[XSrZInsJIlvd3OrdH;sJFMuc2mwYYPlJIRwf26|dILlZY0hfGG{Z3X0dy=> MV2yNVA1QDd6NR?=
PC3  NHm1UVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInBdW0zPGh? MljHS2k2OMLiPTCxNFAhdk1? M3;sUFIxPTVzME[x
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U87MG MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HWTWlEPTB;MD6xOEDPxE1? MYSxPVU5PDJ{Nx?=
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DETROIT562 MnvaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfzfYJRUUN3ME2wMlE{KM7:TR?= MXmxPVU5PDJ{Nx?=
PC3  MnSxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnBTWM2OD1yLkGwJO69VQ>? MoHjNVk2QDR{Mke=
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UCH-1  NHfzWlNHfW6ldHnvckBCe3OjeR?= M{mwbFAuPSEQvF2= MX7pcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKGKxdHigRWtVKGGwZDDtWG9TKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NU\4cW9kOTl3Mki0OFE>
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UCH-1  NHTl[mhCeG:ydH;zbZMhSXO|YYm= NV[1cI5MOC5zLUGwJO69VQ>? MnfpNlQhcA>? NHv4eGJFVVOR Mlr4bY5lfWOnczDhdI9xfG:|aYO= MUexPVUzQDR2MR?=

... 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:
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
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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID