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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Cited by 25 Publications

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 NIXVN2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXTW5cxNThizszN MWWyOE81QC95MjDo NHq2cHpqdmS3Y3XzJJRqdWVvIHHu[EBkd26lZX70doF1cW:wLXTldIVv\GWwdDDpcohq[mm2aX;uJI9vKE6EIHPlcIwh\3Kxd4To MmnTNlYzOjR4OEG=
SH-SY5Y NGTyS4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1naV|AuQCEQvF2= MV2yOE81QC95MjDo M3fteolv\HWlZYOgeIlu\S1iYX7kJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IHnubIljcXSrb36gc44hVkJiY3XscEBoem:5dHi= MoXGNlYzOjR4OEG=
SH-SY5Y  NWOze3RuSXCxcITvd4l{KEG|c3H5 MX[xJO69VQ>? MkTiNE42NTJ2IHi= NI[zXGt{\W6|aYTpfoV{KG6ndYLvZoxie3SxbXGgZ4VtdHNidH:g[I95d3K3YnnjbY4ucW6mdXPl[EBieG:ydH;zbZM> MYiyOlIzPDZ6MR?=
G 35 SC NVHjRo1MT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\C[|AvODVvMkCg{txO NX;KVlRoOjRxN{KgbC=> Ml;RSG1UVw>? NFTtWXVqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 NEHvcHUzPjF{MUK1NS=>
G 38 SC NHrMcG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vQSFAvODVvMkCg{txO MYOyOE84OiCq NHO1S5JFVVOR MYnpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueIx6 M1OyTlI3OTJzMkWx
G 40 SC NFfLbmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUC1UllXOC5yNT2yNEDPxE1? NGHNWpEzPC95MjDo MX7EUXNQ NGHaXVNqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 NXm3O29bOjZzMkGyOVE>
G 35 DC MnHoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrENE4xPS1{MDFOwG0> NYrRfGx{OjRxN{KgbC=> M2rZWmROW09? MXzpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueIx6 MXWyOlEzOTJ3MR?=
G 38 DC MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoG4NE4xPS1{MDFOwG0> MlP6NlQwPzJiaB?= MnzSSG1UVw>? MlTLbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBidmRidHnt[UBl\XCnbnTlcpRtgQ>? NWTMOGZtOjZzMkGyOVE>
G 40 DC MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGe5NHgxNjB3LUKwJO69VQ>? MmL2NlQwPzJiaB?= MUTEUXNQ MUfpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueIx6 MojnNlYyOjF{NUG=
RD NY\5RWdMSXCxcITvd4l{KEG|c3H5 MoTBNU8yNjVxMjFOwG0> NXfVWG5lPzJiaB?= Ml;jbY5lfWOnczDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCJQV7UOlE> NVWwcnFtOjV5NEmzO|g>
TE381.T NWDMToVISXCxcITvd4l{KEG|c3H5 MYmxM|EvPS9{IN88US=> MX:3NkBp Mm\jbY5lfWOnczDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCJQV7UOlE> MlTJNlU4PDl|N{i=
RMS13 MWDBdI9xfG:|aYOgRZN{[Xl? MlKyNU8yNjVxMjFOwG0> M1HOO|czKGh? MUTpcoR2[2W|IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKEeDTmS2NS=> NEm5So4zPTd2OUO3PC=>
RH30  NIDsOY5CeG:ydH;zbZMhSXO|YYm= NGrs[FYyNzFwNT:yJO69VQ>? MVe3NkBp MVvpcoR2[2W|IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKEeDTmS2NS=> M3\VXlI2PzR7M{e4
VJ MX\BdI9xfG:|aYOgRZN{[Xl? MXOxM|EvPS9{IN88US=> MlfvO|IhcA>? M4\FN4lv\HWlZYOgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiR1HOWFYy NFjx[YwzPTd2OUO3PC=>
HS578T M13KUGNmdGxiVnnhZoltcXS7IFHzd4F6 NHPROY0xNTNizszN M3zhWlczKGh? MXLpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MX2yOVczOTRzOR?=
BT549 NF\CbXdE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NV;0fHQxOC1|IN88US=> MmjrO|IhcA>? NULMRW54cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NIXVZ|AzPTd{MUSxPS=>
MDA-MB-231 NH7ldphE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M1rkfVAuOyEQvF2= M2f6SFczKGh? MULpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 Mlq5NlU4OjF2MUm=
MDA-MB-468 NELwWWtE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NV3LOIpZOC1|IN88US=> NFGxdJQ4OiCq NIXSRWZqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NH\XfVQzPTd{MUSxPS=>
MDA-MB-436 NFLRR3ZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MWmwMVMh|ryP MYe3NkBp MXfpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NXW3ZXZuOjV5MkG0NVk>
SUM149PT MlSzR4VtdCCYaXHibYxqfHliQYPzZZk> NGj4V2ExNTNizszN NV7QcHVZPzJiaB?= MX\pcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MV:yOVczOTRzOR?=
MDA-MB-468 MlrYSpVv[3Srb36gRZN{[Xl? M1LhUFAvODFvMUCg{txO M3j0flI1KGh? NUnLclFL\G:5boLl[5Vt[XSnczD0bIUhdGW4ZXzzJI9nKM7{LWTyR3AyNCClLV35Z{BidmRiY4njcIlvKEVicILveIVqdnQEoB?= MnLmNlU4OjF2MUm=
MDA-MB-231 NXLue3dTTnWwY4Tpc44hSXO|YYm= MWqwMlAyNTFyIN88US=> NVnCc5A5OjRiaB?= NUP0ZZFN\G:5boLl[5Vt[XSnczD0bIUhdGW4ZXzzJI9nKM7{LWTyR3AyNCClLV35Z{BidmRiY4njcIlvKEVicILveIVqdnQEoB?= NHe1cFMzPTd{MUSxPS=>
HS578T MYDGeY5kfGmxbjDBd5NigQ>? NFr0VWkxNjBzLUGwJO69VQ>? M1XNXVI1KGh? NFXsOnpld3ewcnXneYxifGW|IITo[UBt\X[nbIOgc4Yh|rJvVILDVFEtKGNvTYnjJIFv\CCleXPsbY4hTSCycn;0[Ylve8Li MlfONlU4OjF2MUm=
SW872 MlXrSpVv[3Srb36gRZN{[Xl? MnjzNE4xOS1yLkWg{txO MnjCNlQhcA>? NGLDNJZz\WS3Y3XzJGFMXCCyaH;zdIhwenmuYYTpc44hMHCDS2SpJIFv\CB2RVLQNUBxcG:|cHjvdplt[XSrb36gLJA1TUKSMTmgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYNCpC=> NU[1WoNpOjR4OUW2N|I>
SW982 NHraem9HfW6ldHnvckBCe3OjeR?= M2DvXlAvODFvMD61JO69VQ>? MX[yOEBp M{nVSpJm\HWlZYOgRWtVKHCqb4PwbI9zgWyjdHnvckApeEGNVDmgZY5lKDSHQmCxJJBpd3OyaH;yfYxifGmxbjCodFRGSlBzKTDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nctMg M4C0VlI1Pjl3NkOy
SW872 MkLGRZBweHSxc3nzJGF{e2G7 MUWwMlAyNTBwNTFOwG0> NVrRdJZqPDhiaB?= MmXNbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MnrsNlQ3QTV4M{K=
SW982 M3HY[2Fxd3C2b4Ppd{BCe3OjeR?= NYTDWJI{OC5yMT2wMlUh|ryP MXO0PEBp M{PKWIlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= MnzuNlQ3QTV4M{K=
AGS HG M2P4fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTBwNkigxtEhOC5yM{Gg{txO NV;adHVZOjR3OUe0O|g>
AGS LG MoexS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PZT2lEPTB;MD6wOUDDuSByLkCwNUDPxE1? NIK2SWczPDV7N{S3PC=>
HGC27 HG NGDTdnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjXZ4ZvUUN3ME2wMlM5KMLzIECuNFIzKM7:TR?= Ml7FNlQ2QTd2N{i=
HGC27 LG NHi4OVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXLO|hIUUN3ME2wMlAzKMLzIECuNFA1KM7:TR?= MlnmNlQ2QTd2N{i=
MKN45 HG MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TV[mlEPTB;MT6wNUDDuSByLkC1NUDPxE1? Mkm2NlQ2QTd2N{i=
MKN45 LG Mn73S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LNNGlEPTB;MD64O{DDuSByLkCzNEDPxE1? M1ziXVI1PTl5NEe4
NUGC4 HG M1XQUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfpTWM2OD1zND6wJOKyKDNwOUGzJO69VQ>? MmjXNlQ2QTd2N{i=
NUGC4 LG M{fNW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{Xj[WlEPTB;MUSuNEDDuSB3LkOyNUDPxE1? M1rieVI1PTl5NEe4
A549 MWPGeY5kfGmxbjDBd5NigQ>? MXqwMlI2NzBwNT:xJO69VQ>? NVTsU49nOjRiaB?= MoDLbY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{dGmpaITsfS=> M4HnPFI1OzVzNEK1
H460 NHKyS4xHfW6ldHnvckBCe3OjeR?= M3\WUVAvOjVxMD61M|Eh|ryP MXmyOEBp NYrTdFBucW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|bHnnbJRtgQ>? NGjGXpEzPDN3MUSyOS=>
H661 MmnuSpVv[3Srb36gRZN{[Xl? M1HHO|AvOjVxMD61M|Eh|ryP NFi5R2MzPCCq MorxbY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7 MmHVNlQ{PTF2MkW=
SAS M1Xwc2Z2dmO2aX;uJGF{e2G7 M2G5V|AvOjVxMD61M|Eh|ryP NVLIcpZJOjRiaB?= MUfpcohq[mm2czDBb5QheGixc4Doc5J6dGG2aX;uJJNq\26rZnnjZY51dHl? M17ITVI1OzVzNEK1
UT5 MmHLSpVv[3Srb36gRZN{[Xl? M2[1elAvOjVxMD61M|Eh|ryP NETncI4zPCCq NVzORnJxcW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|aXfubYZq[2GwdHz5 NFXPZ3EzPDN3MUSyOS=>
FaDu M3HPfmZ2dmO2aX;uJGF{e2G7 NXrJZpc2OC5{NT:wMlUwOSEQvF2= MlnRNlQhcA>? NW\sXlg6cW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|aXfubYZq[2GwdHz5 MWWyOFM2OTR{NR?=
RD M4DEZWFxd3C2b4Ppd{BCe3OjeR?= Mo\1NU8yNjVxMjFOwG0> M2nGOFczKGh? MYHEUXNQ MmXYbY5lfWOnczDjZZNx[XOnLXTldIVv\GWwdDDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCXT{GyOi=> MnnYNlM3QDR7MkW=
TE671 M3L4UmFxd3C2b4Ppd{BCe3OjeR?= M{nZTlEwOS53L{Kg{txO MUC3NkBp NEKwfmhFVVOR NXXUcmxmcW6mdXPld{Bk[XOyYYPlMYRmeGWwZHXueEBieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDVU|EzPg>? NHTDVXUzOzZ6NEmyOS=>
RH30  MWLBdI9xfG:|aYOgRZN{[Xl? M1qwNVEwOS53L{Kg{txO NH;EXm04OiCq NH\rN2RFVVOR NHTHR5lqdmS3Y3XzJINie3Cjc3Wt[IVx\W6mZX70JIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIGXPNVI3 M1PJWVI{Pjh2OUK1
RMS13 MYPBdI9xfG:|aYOgRZN{[Xl? NHK0U2oyNzFwNT:yJO69VQ>? MVS3NkBp MWXEUXNQ MnPJbY5lfWOnczDjZZNx[XOnLXTldIVv\GWwdDDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCXT{GyOi=> NWH5W2cxOjN4OES5NlU>
SUM149PT NHXFVWpE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NUjMVY5VOC5|IN88US=> NX63NYV6PzJiaB?= MXflcohidmOnczDjfZRwfG:6aXOg[YZn\WO2czDv[kBRUTONL1HLWEBx[XSqd3H5JIlvcGmkaYTvdpM> MlTXNlM3ODFyN{S=
MDA-MB-468 NXHIdW9QS2WubDDWbYFjcWyrdImgRZN{[Xl? MX6wMlMh|ryP MWm3NkBp MXPlcohidmOnczDjfZRwfG:6aXOg[YZn\WO2czDv[kBRUTONL1HLWEBx[XSqd3H5JIlvcGmkaYTvdpM> NUXnfFI2OjN4MEGwO|Q>
MDA-MB-231 MlPKR4VtdCCYaXHibYxqfHliQYPzZZk> NUHJTnllOC5|IN88US=> MUm3NkBp Mnvr[Y5p[W6lZYOgZ5l1d3SxeHnjJIVn\mWldIOgc4YhWEl|Sz;BT3QheGG2aIfhfUBqdmirYnn0c5J{ MW[yN|YxOTB5NB?=
SY5Y NHPWUG5HfW6ldHnvckBCe3OjeR?= MnnQNU42NzJwNT:1JO69VQ>? MmLqNlQhcA>? NFjXUXNqdmS3Y3XzJGcyyqClZXzsMYN6[2ynIHHydoV{fCCjbnSgZZBweHSxc3nz NHzmTlIzOzN5OEO0NS=>
SKNBE(2c) NUi0SlI5TnWwY4Tpc44hSXO|YYm= MWexMlUwOi53L{Wg{txO NIrueoIzPCCq MnfPbY5lfWOnczDHNeKh[2WubD3jfYNt\SCjcoLld5Qh[W6mIHHwc5B1d3Orcx?= Mn20NlM{Pzh|NEG=
RD M{HRUmFxd3C2b4Ppd{BCe3OjeR?= M33lW|MhyrWP NI\CTHcyOiCq NELidlRFVVOR M3XSOZNmdnOrdHn6[ZMhWkRiY3XscJMhfG9iRF;YMYlv\HWlZXSgZZBweHSxc3nz M4LqVFI{OzByOEC5
TP5014 NYrDPVkxSXCxcITvd4l{KEG|c3H5 NXzsU|hiOyEEtV2= MVuxNkBp NHLy[XhFVVOR MYTz[Y5{cXSrenXzJHJFKGOnbHzzJJRwKESRWD3pcoR2[2WmIHHwc5B1d3Orcx?= NHLsNlMzOzNyMEiwPS=>
HT1080 MUXBdI9xfG:|aYOgRZN{[Xl? M2DROFMhyrWP M4nIUFEzKGh? MlfKSG1UVw>? MkjBd4Vve2m2aYrld{BTTCClZXzsd{B1dyCGT2itbY5lfWOnZDDhdI9xfG:|aYO= MXOyN|MxODhyOR?=
A549 MWrGeY5kfGmxbjDBd5NigQ>? M4DyZVAuOy5|IN88US=> NIXwOIM4OiCq Mn;ibY5lfWOnczDjc41xdGW2ZTDkc5dvemWpdXzheIlwdiCxZjDwRWtV M{HxOVI{OjV7NUmx
HCC827 NGryVW1HfW6ldHnvckBCe3OjeR?= NWqzXXp6OC1|LkOg{txO Mmf4O|IhcA>? MY\pcoR2[2W|IHPvcZBt\XSnIHTve45z\We3bHH0bY9vKG:oIIDBT3Q> M{O2ZlI{OjV7NUmx
H3122 M4n4fWZ2dmO2aX;uJGF{e2G7 M1TtcFAuOy5|IN88US=> MorsO|IhcA>? NVfyTZZJcW6mdXPld{Bkd22ybHX0[UBld3ewcnXneYxifGmxbjDv[kBxSUuW NIflR5UzOzJ3OUW5NS=>
TALL-1 M{i5emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTGNgKBkc7:TR?= NHvEWGc4KGR? NWK0elNE\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 NHT5RoszOzB|OEK3Ny=>
HPB-ALL MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3qNgKBkc7:TR?= MY[3JIQ> MknC[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 MXuyN|A{QDJ5Mx?=
DND41 NE\P[XdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWix5qCK|ryP NGf3XYk4KGR? M4f4fYRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? M3vDXFI{ODN6Mkez
SUP-T1 NVrWcXl7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LKOVHjiIoQvF2= NF\JfIk4KGR? NV\ucol[\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 MnfhNlMxOzh{N{O=
PEER MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3tNgKBkc7:TR?= MkLQO{Bl NW[5cIhr\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 NYrSOnBNOjNyM{iyO|M>
ALL-SIL Ml7BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITFOJYy6oDLzszN NXnkOWtJPyCm M4HxfoRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? NWfjVoViOjNyM{iyO|M>
KE37 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlX5NgKBkc7:TR?= MVW3JIQ> NHnkOXVl\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? MlXHNlMxOzh{N{O=
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RPMI-8402 MmnMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV2x5qCK|ryP MmTFO{Bl NGjUV|Fl\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? MmnMNlMxOzh{N{O=
Jurkat NVrqeodiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYP4N|ZYOeLCid88US=> MmDMO{Bl M4fKeIRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? Ml;yNlMxOzh{N{O=
MOLT-4 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDqdoZxOeLCid88US=> NIraPXQ4KGR? NULXXpdz\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 NYHUWHJOOjNyM{iyO|M>
PF-382 NGHzWIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVyx5qCK|ryP M1nqWFch\A>? M2jwZoRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? NF;YOZgzOzB|OEK3Ny=>
CCRF-CEM MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfQ[pNDOeLCid88US=> MlX2O{Bl NIDvdWll\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? NUPyU25vOjNyM{iyO|M>
LOUCY Mn7oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7tRWUy6oDLzszN M3XxTlch\A>? Mn3l[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 MYKyN|A{QDJ5Mx?=
MOLT-16 NF7w[2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWOx5qCK|ryP MWK3JIQ> MkO4[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 M1rGWVI{ODN6Mkez
MM1S Mli4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rue|AuOiEQvF2= M1Hw[FI1KGh? M{Pp[mlEPTB;MD61JO69VQ>? MYmyNlgzQTJ|NB?=
NCI-H929 NXLYT4FkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4r2TFAuOiEQvF2= MmDvNlQhcA>? MWjJR|UxRTBwMkWg{txO MUKyNlgzQTJ|NB?=
KMS12-BM  MkPxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnLNE0zKM7:TR?= NVPLUFkzOjRiaB?= MUfJR|Ux97zgMjFOwG0> MWOyNlgzQTJ|NB?=
MDA-MB-436 NHXiTVJHfW6ldHnvckBCe3OjeR?= NVHhZYtqOSEQvF2= MkDWNlQhcA>? MnzvdoVlfWOnczD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVB?= NHLCRpYzOjR6OEW5NC=>
SUM149PT Mnn5SpVv[3Srb36gRZN{[Xl? NXHlfnJYOSEQvF2= M1TqO|I1KGh? NUDrTm9UemWmdXPld{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWC=> NXP1VYdROjJ2OEi1PVA>
SUM1315MO2 M{DBRWZ2dmO2aX;uJGF{e2G7 MYmxJO69VQ>? NFHPXGgzPCCq MYHy[YR2[2W|IITo[UBxcG:|cHjvdplt[XSrb36gc4YhSUuW NIq3WZUzOjR6OEW5NC=>
HCC1937 MWDGeY5kfGmxbjDBd5NigQ>? Mmj3NUDPxE1? M{TtdFI1KGh? NXTSdHhpemWmdXPld{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWC=> M2i2W|IzPDh6NUmw
HCC827 NHTtRoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLMNE0{KM7:TR?= NHftS2E4OiCq NYq1TXFKUUN3ME2wMlMh|ryP MX[yNVIzODR5NB?=
PC-9  M2jKWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVSwMVMh|ryP NF3RWpk4OiCq NXP3XJVXUUN3ME2wMlgh|ryP MmjrNlEzOjB2N{S=
LN229 MWPGeY5kfGmxbjDBd5NigQ>? MVOxJO69VQ>? M2LRNFQ5KGh? NYfIblFicW6mdXPld{BifXSxcHjh[49{d22nIH\vdo1ifGmxbh?= MkPNNlExPjJ7OUO=
U87 M2Pvc2Z2dmO2aX;uJGF{e2G7 MkPMNUDPxE1? NV3Hcmd{PDhiaB?= NH7nbJhqdmS3Y3XzJIF2fG:yaHHnc5NwdWViZn;ycYF1cW:w MkjFNlExPjJ7OUO=
U373 NIW2epZHfW6ldHnvckBCe3OjeR?= MV6xJO69VQ>? NFvv[W01QCCq M4q4b4lv\HWlZYOgZZV1d3CqYXfvd49u\SCob4LtZZRqd25? MnHxNlExPjJ7OUO=
SF767 NVH1V4xrTnWwY4Tpc44hSXO|YYm= NFjMVmMyKM7:TR?= MlTlOFghcA>? M1i0colv\HWlZYOgZZV1d3CqYXfvd49u\SCob4LtZZRqd25? M37XZVIyODZ{OUmz
Mel-Juso MYfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M2rsdFAvODIkgKOxNQKBkc7:TR?= MonhO|IhcA>? NGDBOI5qdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NWL5OZFiOjFyNEi3PFU>
518A2  M4TkbWNmdGxiVnnhZoltcXS7IFHzd4F6 NFPZbZMxNjBz4pETNVDjiIoQvF2= MU[3NkBp NVXxcWtucW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NV;rXohMOjFyNEi3PFU>
Mel-Juso  NX;KO21yTnWwY4Tpc44hSXO|YYm= MVqwMlAxOeLCk{JihKnPxE1? M{fPUlI1KGh? MkL1d5VxeHKnc4Pld{BxcG:|cHjvdplt[XSrb36gc4YheGixc4DoZZRq\HmuIHnuc5NqfG:uIEOtb4lv[XOnIHTve45{fHKnYX2geIFz\2W2cx?= NE\rNJYzOTB2OEe4OS=>
518A2 NWG4b3h6TnWwY4Tpc44hSXO|YYm= M2rLcFAvODBz4pETNgKBkc7:TR?= MUeyOEBp Mlfod5VxeHKnc4Pld{BxcG:|cHjvdplt[XSrb36gc4YheGixc4DoZZRq\HmuIHnuc5NqfG:uIEOtb4lv[XOnIHTve45{fHKnYX2geIFz\2W2cx?= MVWyNVA1QDd6NR?=
PC3  NIfTUm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWWyOIg> M1O4bGdKPTEEoE2gNVAxKG6P MWSyNFU2OTB4MR?=
U87MG MUjGeY5kfGmxbjDBd5NigQ>? M37ZVlAvOS1zIN88US=> MkDTNlTjiImqwrC= NFjYVphFVVOR NVvRU|RzcW6qaXLpeJMhWEl|Sz3t[YRq[XSnZDDzbYdv[Wyrbne= NWnCeY5kOTl4M{O2PFM>
U138MG NXfWPVRGTnWwY4Tpc44hSXO|YYm= MU[wMlEuOSEQvF2= MWOyOQKBkWkEoB?= MWPEUXNQ MUPpcohq[mm2czDQTVNMNW2nZHnheIVlKHOrZ37hcIlv\w>? NXjXR|FrOTl4M{O2PFM>
U118MG Ml73SpVv[3Srb36gRZN{[Xl? MVqwMlEuOSEQvF2= MVOyOQKBkWkEoB?= MVPEUXNQ MWDpcohq[mm2czDQTVNMNW2nZHnheIVlKHOrZ37hcIlv\w>? NXG1O3ZlOTl4M{O2PFM>
U87MG M321d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LiZmlEPTB;MD6xOEDPxE1? NXv1OpV1OTl3OESyNlc>
IGROV-1 NV\ENJhlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTBwME[g{txO NFfmeIEyQTV6NEKyOy=>
DETROIT562 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHD[oJKSzVyPUCuNVMh|ryP M4XwclE6PTh2MkK3
PC3  M2jjeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHtTWM2OD1yLkGwJO69VQ>? MXGxPVU5PDJ{Nx?=
SKOV-3 NWPHV4RZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfnXHFKSzVyPUCuNVIh|ryP MYKxPVU5PDJ{Nx?=
HUVEC MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LKb2lEPTB;MD6wPEDPxE1? M1\hRVE6PTh2MkK3
UCH-1  MVnGeY5kfGmxbjDBd5NigQ>? NFrMXGwxNTVizszN NEnFOXlqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIHLveIghSUuWIHHu[EBuXE:UIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ Mm[2NVk2Ojh2NEG=
UCH-1  NHvmSGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnraNE4xOS1zMDFOwG0> MWG2JIQ> MUfpcohq[mm2czDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> M37QRlE6PTJ6NESx
UCH-1  MlTnRZBweHSxc3nzJGF{e2G7 MoHkNE4yNTFyIN88US=> M2j5SVI1KGh? M{fJUWROW09? NHf2VWtqdmS3Y3XzJIFxd3C2b4Ppdy=> NYPq[HF2OTl3Mki0OFE>

... 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

PI3K Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID