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 NH35[HRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1[4fFAuQCEQvF2= NH\GXFIzPC92OD:3NkBp MYLpcoR2[2W|IITpcYUuKGGwZDDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCrbnjpZol1cW:wIH;uJG5DKGOnbHyg[5Jwf3Sq MojSNlYzOjR4OEG=
SH-SY5Y NFLVR2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnwZpcxNThizszN MU[yOE81QC95MjDo NYTRbo1KcW6mdXPld{B1cW2nLTDhcoQh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgbY5pcWKrdHnvckBwdiCQQjDj[YxtKGe{b4f0bC=> MYGyOlIzPDZ6MR?=
SH-SY5Y  NYXv[|ZsSXCxcITvd4l{KEG|c3H5 NI\EVHoyKM7:TR?= MVqwMlUuOjRiaB?= M3;yNZNmdnOrdHn6[ZMhdmW3cn;icIF{fG:vYTDj[YxteyC2bzDkc5hwenWkaXPpck1qdmS3Y3XkJIFxd3C2b4Ppdy=> MYiyOlIzPDZ6MR?=
G 35 SC MnK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlWzNE4xPS1{MDFOwG0> MVqyOE84OiCq Mn7HSG1UVw>? MmDybY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBidmRidHnt[UBl\XCnbnTlcpRtgQ>? MlzTNlYyOjF{NUG=
G 38 SC NHO4cJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVK0dYlQOC5yNT2yNEDPxE1? NH7GSIgzPC95MjDo NHGzRWVFVVOR NF7KbWhqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 MXiyOlEzOTJ3MR?=
G 40 SC NEL4S2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4H0R|AvODVvMkCg{txO NFTxSHgzPC95MjDo M4XKUGROW09? NVnSfI5FcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= M1PTXVI3OTJzMkWx
G 35 DC NF;6bJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrjSHkxNjB3LUKwJO69VQ>? MlTtNlQwPzJiaB?= NGHSVWxFVVOR NWjLfZd6cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= MnvvNlYyOjF{NUG=
G 38 DC NHz6WndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PDVFAvODVvMkCg{txO NX7afW9HOjRxN{KgbC=> NV3y[ldYTE2VTx?= NFfpeHlqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 M2HseVI3OTJzMkWx
G 40 DC MojwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DNU|AvODVvMkCg{txO NF;DOVIzPC95MjDo MnvXSG1UVw>? NVflT4x{cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= NEDZWVkzPjF{MUK1NS=>
RD NXK1SVNpSXCxcITvd4l{KEG|c3H5 NHGwO2UyNzFwNT:yJO69VQ>? MWi3NkBp Mn3ZbY5lfWOnczDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCJQV7UOlE> MUGyOVc1QTN5OB?=
TE381.T MlTaRZBweHSxc3nzJGF{e2G7 NFPm[ocyNzFwNT:yJO69VQ>? NHrpV3U4OiCq NYLwdldUcW6mdXPld{BieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDHRW5VPjF? NVT1SIFbOjV5NEmzO|g>
RMS13 M4jT[WFxd3C2b4Ppd{BCe3OjeR?= M{TyT|EwOS53L{Kg{txO MlGyO|IhcA>? M1PBPIlv\HWlZYOgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiR1HOWFYy MkLXNlU4PDl|N{i=
RH30  NWnSbFFvSXCxcITvd4l{KEG|c3H5 MoO2NU8yNjVxMjFOwG0> M3rEe|czKGh? NELXZmxqdmS3Y3XzJIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIFfBUnQ3OQ>? MYCyOVc1QTN5OB?=
VJ NXvmNYNsSXCxcITvd4l{KEG|c3H5 MlzHNU8yNjVxMjFOwG0> M336XFczKGh? NWLQXVV7cW6mdXPld{BieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDHRW5VPjF? M2POdlI2PzR7M{e4
HS578T M3\ZVmNmdGxiVnnhZoltcXS7IFHzd4F6 MVmwMVMh|ryP MX:3NkBp MlTtbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NGn5PYozPTd{MUSxPS=>
BT549 MlG2R4VtdCCYaXHibYxqfHliQYPzZZk> M1XiUVAuOyEQvF2= MmnOO|IhcA>? MoXVbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NIXoOm0zPTd{MUSxPS=>
MDA-MB-231 M{LIRmNmdGxiVnnhZoltcXS7IFHzd4F6 NHyzWnoxNTNizszN NHTie5Y4OiCq MmHubY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? M4rMTFI2PzJzNEG5
MDA-MB-468 MWrD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NIKwUWsxNTNizszN NEP6fI04OiCq M13xN4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MoTaNlU4OjF2MUm=
MDA-MB-436 M1e0dGNmdGxiVnnhZoltcXS7IFHzd4F6 MmnlNE0{KM7:TR?= NVvtVpFWPzJiaB?= M3HKcYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MkHlNlU4OjF2MUm=
SUM149PT NX;jbIVUS2WubDDWbYFjcWyrdImgRZN{[Xl? MmLJNE0{KM7:TR?= NGj1fWM4OiCq MX;pcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 M2jqdlI2PzJzNEG5
MDA-MB-468 M1rJfGZ2dmO2aX;uJGF{e2G7 NFjCOmYxNjBzLUGwJO69VQ>? MXGyOEBp M2TRTIRwf26{ZXf1cIF1\XNidHjlJIxmfmWuczDv[kDPui2WclPQNUwh[y2PeXOgZY5lKGO7Y3zpckBGKHC{b4TlbY5{yqB? NHPG[lIzPTd{MUSxPS=>
MDA-MB-231 NVPZVG9pTnWwY4Tpc44hSXO|YYm= NXHWRXU{OC5yMT2xNEDPxE1? MWGyOEBp NEnSe5Bld3ewcnXneYxifGW|IITo[UBt\X[nbIOgc4Yh|rJvVILDVFEtKGNvTYnjJIFv\CCleXPsbY4hTSCycn;0[Ylve8Li MYCyOVczOTRzOR?=
HS578T MXHGeY5kfGmxbjDBd5NigQ>? MkHVNE4xOS1zMDFOwG0> NYPxTnhSOjRiaB?= NFm5dW5ld3ewcnXneYxifGW|IITo[UBt\X[nbIOgc4Yh|rJvVILDVFEtKGNvTYnjJIFv\CCleXPsbY4hTSCycn;0[Ylve8Li M13PNFI2PzJzNEG5
SW872 MljPSpVv[3Srb36gRZN{[Xl? Mlr2NE4xOS1yLkWg{txO M2rOTlI1KGh? MYLy[YR2[2W|IFHLWEBxcG:|cHjvdplt[XSrb36gLJBCU1RrIHHu[EA1TUKSMTDwbI9{eGixconsZZRqd25iKIC0SWJROSliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= NVHSWVJ5OjR4OUW2N|I>
SW982 MmPnSpVv[3Srb36gRZN{[Xl? MWOwMlAyNTBwNTFOwG0> MkLINlQhcA>? MnXVdoVlfWOnczDBT3QheGixc4Doc5J6dGG2aX;uJEhxSUuWKTDhcoQhPEWEUEGgdIhwe3Cqb4L5cIF1cW:wIDjwOGVDWDFrIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{wrC= MnS5NlQ3QTV4M{K=
SW872 MofQRZBweHSxc3nzJGF{e2G7 MV:wMlAyNTBwNTFOwG0> MnfqOFghcA>? M1\FS4lv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NUHGT3FbOjR4OUW2N|I>
SW982 MVLBdI9xfG:|aYOgRZN{[Xl? NWnsbmhYOC5yMT2wMlUh|ryP MnTEOFghcA>? NIDk[VBqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NETlfIYzPDZ7NU[zNi=>
AGS HG MmnrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTBwNkigxtEhOC5yM{Gg{txO NGDv[I4zPDV7N{S3PC=>
AGS LG NH\aeIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2S4RmlEPTB;MD6wOUDDuSByLkCwNUDPxE1? NHLQbWczPDV7N{S3PC=>
HGC27 HG NWnBbZBGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHnO5RKSzVyPUCuN|ghyrFiMD6wNlIh|ryP NYP3Sm1KOjR3OUe0O|g>
HGC27 LG NWLQdZFQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDOOY1bUUN3ME2wMlAzKMLzIECuNFA1KM7:TR?= MX[yOFU6PzR5OB?=
MKN45 HG NGXIeVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LXWWlEPTB;MT6wNUDDuSByLkC1NUDPxE1? NF\KbHMzPDV7N{S3PC=>
MKN45 LG NWPmUZp4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nXO2lEPTB;MD64O{DDuSByLkCzNEDPxE1? M1vvR|I1PTl5NEe4
NUGC4 HG NFHyT3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3obZI4UUN3ME2xOE4xKMLzIEOuPVE{KM7:TR?= MYKyOFU6PzR5OB?=
NUGC4 LG NEHkeWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlT1TWM2OD1zND6wJOKyKDVwM{KxJO69VQ>? NYfQfVdIOjR3OUe0O|g>
A549 M{nkbWZ2dmO2aX;uJGF{e2G7 NFvGU3kxNjJ3L{CuOU8yKM7:TR?= MkS1NlQhcA>? MWrpcohq[mm2czDBb5QheGixc4Doc5J6dGG2aX;uJJNtcWeqdHz5 NUn0[mJpOjR|NUG0NlU>
H460 NHiyTlBHfW6ldHnvckBCe3OjeR?= MVWwMlI2NzBwNT:xJO69VQ>? NWfwSJRyOjRiaB?= MnqxbY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{dGmpaITsfS=> M2D4OlI1OzVzNEK1
H661 MkjHSpVv[3Srb36gRZN{[Xl? NInFZ24xNjJ3L{CuOU8yKM7:TR?= MYKyOEBp Mo\tbY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7 Mn\RNlQ{PTF2MkW=
SAS MUfGeY5kfGmxbjDBd5NigQ>? MUGwMlI2NzBwNT:xJO69VQ>? MlfRNlQhcA>? MUHpcohq[mm2czDBb5QheGixc4Doc5J6dGG2aX;uJJNq\26rZnnjZY51dHl? NVXhZWFKOjR|NUG0NlU>
UT5 MmDhSpVv[3Srb36gRZN{[Xl? MYqwMlI2NzBwNT:xJO69VQ>? MYCyOEBp MnmzbY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7 M1vT[FI1OzVzNEK1
FaDu Mlm2SpVv[3Srb36gRZN{[Xl? NYLUVVQ5OC5{NT:wMlUwOSEQvF2= NYXUelFQOjRiaB?= MYrpcohq[mm2czDBb5QheGixc4Doc5J6dGG2aX;uJJNq\26rZnnjZY51dHl? M2i4[VI1OzVzNEK1
RD NYDHbIl2SXCxcITvd4l{KEG|c3H5 MW[xM|EvPS9{IN88US=> NEKwW3Q4OiCq NH7lTYlFVVOR NIS5RVRqdmS3Y3XzJINie3Cjc3Wt[IVx\W6mZX70JIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIGXPNVI3 M4XkXVI{Pjh2OUK1
TE671 NYroWpVqSXCxcITvd4l{KEG|c3H5 MWmxM|EvPS9{IN88US=> NGjPS3g4OiCq NIiwWmZFVVOR M1WwUYlv\HWlZYOgZ4F{eGG|ZT3k[ZBmdmSnboSgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiVV:xNlY> MWSyN|Y5PDl{NR?=
RH30  MonoRZBweHSxc3nzJGF{e2G7 NH;FZ4IyNzFwNT:yJO69VQ>? NHe4OZc4OiCq Mlq1SG1UVw>? Mn3BbY5lfWOnczDjZZNx[XOnLXTldIVv\GWwdDDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCXT{GyOi=> MmDxNlM3QDR7MkW=
RMS13 M1W2R2Fxd3C2b4Ppd{BCe3OjeR?= MVexM|EvPS9{IN88US=> MnXrO|IhcA>? MXvEUXNQ M4\4WYlv\HWlZYOgZ4F{eGG|ZT3k[ZBmdmSnboSgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiVV:xNlY> MXyyN|Y5PDl{NR?=
SUM149PT NYrXNVdzS2WubDDWbYFjcWyrdImgRZN{[Xl? MX6wMlMh|ryP M125cVczKGh? MnH4[Y5p[W6lZYOgZ5l1d3SxeHnjJIVn\mWldIOgc4YhWEl|Sz;BT3QheGG2aIfhfUBqdmirYnn0c5J{ MV6yN|YxOTB5NB?=
MDA-MB-468 NU\GUGRnS2WubDDWbYFjcWyrdImgRZN{[Xl? NF3hc|YxNjNizszN MUS3NkBp NHPvN2RmdmijbnPld{BkgXSxdH;4bYMh\W[oZXP0d{Bw\iCSSUPLM2FMXCCyYYToe4F6KGmwaHnibZRwenN? MnPHNlM3ODFyN{S=
MDA-MB-231 MkK5R4VtdCCYaXHibYxqfHliQYPzZZk> NFWxSXkxNjNizszN M1XjWVczKGh? NUHOOXdx\W6qYX7j[ZMh[3m2b4TvfIlkKGWoZnXjeJMhd2ZiUFmzT{9CU1RicHH0bJdigSCrbnjpZol1d3K| NH;nVoMzOzZyMUC3OC=>
SY5Y NH\FUJZHfW6ldHnvckBCe3OjeR?= NFG1WoIyNjVxMj61M|Uh|ryP MoP6NlQhcA>? NUSzZ5FjcW6mdXPld{BIOcLiY3XscE1kgWOuZTDhdpJme3RiYX7kJIFxd3C2b4Ppdy=> M2T1dFI{Ozd6M{Sx
SKNBE(2c) Mo\4SpVv[3Srb36gRZN{[Xl? NVm5[5FnOS53L{KuOU82KM7:TR?= NGPOZYczPCCq NV3JSW97cW6mdXPld{BIOcLiY3XscE1kgWOuZTDhdpJme3RiYX7kJIFxd3C2b4Ppdy=> MXeyN|M4QDN2MR?=
RD MnPFRZBweHSxc3nzJGF{e2G7 NVO5d5dvOyEEtV2= MV:xNkBp MVrEUXNQ NF:wPFl{\W6|aYTpfoV{KFKGIHPlcIx{KHSxIFTPXE1qdmS3Y3XkJIFxd3C2b4Ppdy=> MknENlM{ODB6MEm=
TP5014 NFr6O3FCeG:ydH;zbZMhSXO|YYm= NX;K[G8{OyEEtV2= NUO4[Vc3OTJiaB?= NVuzOVB1TE2VTx?= Mn\Yd4Vve2m2aYrld{BTTCClZXzsd{B1dyCGT2itbY5lfWOnZDDhdI9xfG:|aYO= NWHxN2RnOjN|MEC4NFk>
HT1080 MmrTRZBweHSxc3nzJGF{e2G7 MYWzJOK2VQ>? NV:we4lLOTJiaB?= Ml;ZSG1UVw>? MYfz[Y5{cXSrenXzJHJFKGOnbHzzJJRwKESRWD3pcoR2[2WmIHHwc5B1d3Orcx?= NWi4XohFOjN|MEC4NFk>
A549 NEPjUZpHfW6ldHnvckBCe3OjeR?= NVf2VnM5OC1|LkOg{txO M1vh[lczKGh? MWTpcoR2[2W|IHPvcZBt\XSnIHTve45z\We3bHH0bY9vKG:oIIDBT3Q> NVTNemRJOjN{NUm1PVE>
HCC827 NGiwNnhHfW6ldHnvckBCe3OjeR?= MmPGNE0{NjNizszN M3vNTVczKGh? NUPJVplQcW6mdXPld{Bkd22ybHX0[UBld3ewcnXneYxifGmxbjDv[kBxSUuW NV7iRlZ5OjN{NUm1PVE>
H3122 M3PoNGZ2dmO2aX;uJGF{e2G7 MVuwMVMvOyEQvF2= NVLaWIdIPzJiaB?= MX;pcoR2[2W|IHPvcZBt\XSnIHTve45z\We3bHH0bY9vKG:oIIDBT3Q> M2HVbFI{OjV7NUmx
TALL-1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYCx5qCK|ryP MUW3JIQ> MnLY[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 Mm\ONlMxOzh{N{O=
HPB-ALL Ml3RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYmx5qCK|ryP NYfMNXFsPyCm MWfk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> Ml7DNlMxOzh{N{O=
DND41 M{PaWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\5e5J7OeLCid88US=> NX;VTXozPyCm M4DpPIRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? MX6yN|A{QDJ5Mx?=
SUP-T1 NE[4fndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVix5qCK|ryP NHj6Z5I4KGR? NGjzfXNl\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? MoH4NlMxOzh{N{O=
PEER NWKyd25IT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDvS4R6OeLCid88US=> NV7UcFg2PyCm M{nzcoRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? NULBcmd[OjNyM{iyO|M>
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PC-9  NXXId5N6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjBR3IxNTNizszN M3[zRlczKGh? MkTZTWM2OD1yLkig{txO M4eycFIyOjJyNEe0
LN229 MlPkSpVv[3Srb36gRZN{[Xl? NVjX[GN[OSEQvF2= NV7tbm1LPDhiaB?= MmLkbY5lfWOnczDheZRweGijZ3;zc41mKG[xcn3heIlwdg>? NG\pe2UzOTB4Mkm5Ny=>
U87 MkHDSpVv[3Srb36gRZN{[Xl? NYjNepBrOSEQvF2= MV20PEBp NF;VZZhqdmS3Y3XzJIF2fG:yaHHnc5NwdWViZn;ycYF1cW:w MX6yNVA3Ojl7Mx?=
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Mel-Juso MUDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MnGxNE4xOeLCk{Gw5qCK|ryP NYPocoJPPzJiaB?= M{nLNolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? M4DvNlIyODR6N{i1
518A2  NUe2VIxvS2WubDDWbYFjcWyrdImgRZN{[Xl? NHfCNXkxNjBz4pETNVDjiIoQvF2= NETSZ4o4OiCq MWLpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NFzPeGUzOTB2OEe4OS=>
Mel-Juso  NUT2d3pFTnWwY4Tpc44hSXO|YYm= M1Tmb|AvODBz4pETNgKBkc7:TR?= NXHLcFR1OjRiaB?= NEKxUZJ{fXCycnXzd4V{KHCqb4PwbI9zgWyjdHnvckBw\iCyaH;zdIhifGmmeXygbY5we2m2b3ygN{1scW6jc3Wg[I94dnO2cnXhcUB1[XKpZYTz M1rkZ|IyODR6N{i1
518A2 NHrqT5BHfW6ldHnvckBCe3OjeR?= NGjRS5YxNjByMfMAl|HjiIoQvF2= MUCyOEBp M{jCTZN2eHC{ZYPz[ZMheGixc4Doc5J6dGG2aX;uJI9nKHCqb4PwbIF1cWS7bDDpco9{cXSxbDCzMYtqdmG|ZTDkc5dve3S{ZXHtJJRiemendIO= NXnpVo5nOjFyNEi3PFU>
PC3  M2LtNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\lT|I1cA>? MVPHTVUxyqB;IEGwNEBvVQ>? M3rW[VIxPTVzME[x
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U118MG MWPGeY5kfGmxbjDBd5NigQ>? MV2wMlEuOSEQvF2= NY\WXo92OjUkgJnoxsA> NXPqZpNQTE2VTx?= NHzEVY5qdmirYnn0d{BRUTONLX3l[IlifGWmIIPp[45idGmwZx?= MYWxPVY{OzZ6Mx?=
U87MG M2TDNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTBwMUSg{txO Mk\BNVk2QDR{Mke=
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DETROIT562 NUHi[oxNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXzTFRKSzVyPUCuNVMh|ryP M2nDUVE6PTh2MkK3
PC3  NULPbolpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrJTWM2OD1yLkGwJO69VQ>? NXnp[5Y1OTl3OESyNlc>
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HUVEC M{TqfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTG[ZpKSzVyPUCuNFgh|ryP NILqV|gyQTV6NEKyOy=>
UCH-1  NVfO[Wg6TnWwY4Tpc44hSXO|YYm= Mo\iNE02KM7:TR?= MoezbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCkb4ToJGFMXCCjbnSgcXRQWiCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M4TNPVE6PTJ6NESx
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UCH-1  M3XWSWFxd3C2b4Ppd{BCe3OjeR?= MUGwMlEuOTBizszN NW\0b4pJOjRiaB?= MUTEUXNQ NV;LeWVwcW6mdXPld{BieG:ydH;zbZM> NID2T40yQTV{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