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

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 Mo[5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXSwMVgh|ryP M4XKXFI1NzR6L{eyJIg> NEHre5lqdmS3Y3XzJJRqdWVvIHHu[EBkd26lZX70doF1cW:wLXTldIVv\GWwdDDpcohq[mm2aX;uJI9vKE6EIHPlcIwh\3Kxd4To Ml7CNlYzOjR4OEG=
SH-SY5Y NIjYZ2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVOwMVgh|ryP NH3OT|EzPC92OD:3NkBp NGnxdYhqdmS3Y3XzJJRqdWVvIHHu[EBkd26lZX70doF1cW:wLXTldIVv\GWwdDDpcohq[mm2aX;uJI9vKE6EIHPlcIwh\3Kxd4To NGPsXm8zPjJ{NE[4NS=>
SH-SY5Y  NGHhR3lCeG:ydH;zbZMhSXO|YYm= M{XpdlEh|ryP MkHCNE42NTJ2IHi= NETy[oZ{\W6|aYTpfoV{KG6ndYLvZoxie3SxbXGgZ4VtdHNidH:g[I95d3K3YnnjbY4ucW6mdXPl[EBieG:ydH;zbZM> MYGyOlIzPDZ6MR?=
G 35 SC MmXOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLRTXN2OC5yNT2yNEDPxE1? MV6yOE84OiCq MYTEUXNQ MorTbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBidmRidHnt[UBl\XCnbnTlcpRtgQ>? NVH1WGtkOjZzMkGyOVE>
G 38 SC Mke2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;FOZExNjB3LUKwJO69VQ>? NEmyVY4zPC95MjDo M3jMT2ROW09? MmHpbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBidmRidHnt[UBl\XCnbnTlcpRtgQ>? NF25dVQzPjF{MUK1NS=>
G 40 SC NIGyUFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvvNE4xPS1{MDFOwG0> M1LLVlI1Nzd{IHi= NU\Qe4g3TE2VTx?= NUnLR4VTcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= NGrpXVAzPjF{MUK1NS=>
G 35 DC NVrSTZpST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYf0bFJxOC5yNT2yNEDPxE1? MoTsNlQwPzJiaB?= MlGzSG1UVw>? NF7oTo9qdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 M2jnbFI3OTJzMkWx
G 38 DC MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHFNE4xPS1{MDFOwG0> MYKyOE84OiCq MWDEUXNQ NXv4enlZcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= MojLNlYyOjF{NUG=
G 40 DC M{nkXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjzbYoxNjB3LUKwJO69VQ>? M1G3fFI1Nzd{IHi= M4W1OWROW09? MoDvbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBidmRidHnt[UBl\XCnbnTlcpRtgQ>? M{T5W|I3OTJzMkWx
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TE381.T M4jQWGFxd3C2b4Ppd{BCe3OjeR?= NEDyNFgyNzFwNT:yJO69VQ>? NUPiUnlDPzJiaB?= MWLpcoR2[2W|IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKEeDTmS2NS=> MUWyOVc1QTN5OB?=
RMS13 NUL4e|Z1SXCxcITvd4l{KEG|c3H5 NWHIW3B1OS9zLkWvNkDPxE1? MXy3NkBp M3qx[Ilv\HWlZYOgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiR1HOWFYy NUfIVIhXOjV5NEmzO|g>
RH30  Ml3DRZBweHSxc3nzJGF{e2G7 NFn0R|kyNzFwNT:yJO69VQ>? MWq3NkBp M3y4PIlv\HWlZYOgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiR1HOWFYy MknRNlU4PDl|N{i=
VJ NH\JPY1CeG:ydH;zbZMhSXO|YYm= MXexM|EvPS9{IN88US=> NXLrXJFzPzJiaB?= M1\5fIlv\HWlZYOgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiR1HOWFYy M2nSdlI2PzR7M{e4
HS578T NUfhSGZFS2WubDDWbYFjcWyrdImgRZN{[Xl? NIXrR40xNTNizszN MoDZO|IhcA>? M160bolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NYTTc2xROjV5MkG0NVk>
BT549 MmnwR4VtdCCYaXHibYxqfHliQYPzZZk> NEmzdI0xNTNizszN M{SxNlczKGh? M2n2UIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? Mkf6NlU4OjF2MUm=
MDA-MB-231 MUHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MUCwMVMh|ryP M37LTFczKGh? NXjUe5lvcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= Mnq3NlU4OjF2MUm=
MDA-MB-468 MYrD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NVHDRWdpOC1|IN88US=> MnrZO|IhcA>? M4TvRolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? M1nyblI2PzJzNEG5
MDA-MB-436 NIPUe3NE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NXHWXHQyOC1|IN88US=> NIDGRYo4OiCq NWLQbZpscW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NYfJcJFUOjV5MkG0NVk>
SUM149PT M3\JXmNmdGxiVnnhZoltcXS7IFHzd4F6 NV7oXllROC1|IN88US=> MkTNO|IhcA>? MVLpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NITabIwzPTd{MUSxPS=>
MDA-MB-468 MmK3SpVv[3Srb36gRZN{[Xl? NYTpfos{OC5yMT2xNEDPxE1? NYrERYl4OjRiaB?= M4Lt[4Rwf26{ZXf1cIF1\XNidHjlJIxmfmWuczDv[kDPui2WclPQNUwh[y2PeXOgZY5lKGO7Y3zpckBGKHC{b4TlbY5{yqB? MYKyOVczOTRzOR?=
MDA-MB-231 NETVSlBHfW6ldHnvckBCe3OjeR?= M{[0cFAvODFvMUCg{txO M3nrPVI1KGh? M1vCNIRwf26{ZXf1cIF1\XNidHjlJIxmfmWuczDv[kDPui2WclPQNUwh[y2PeXOgZY5lKGO7Y3zpckBGKHC{b4TlbY5{yqB? MoX3NlU4OjF2MUm=
HS578T NX:2NVJ6TnWwY4Tpc44hSXO|YYm= M2DDcFAvODFvMUCg{txO M2HNdVI1KGh? NWHUco9x\G:5boLl[5Vt[XSnczD0bIUhdGW4ZXzzJI9nKM7{LWTyR3AyNCClLV35Z{BidmRiY4njcIlvKEVicILveIVqdnQEoB?= NWrpenZkOjV5MkG0NVk>
SW872 MY\GeY5kfGmxbjDBd5NigQ>? NELkcZQxNjBzLUCuOUDPxE1? NWHiT|hrOjRiaB?= M2fzPZJm\HWlZYOgRWtVKHCqb4PwbI9zgWyjdHnvckApeEGNVDmgZY5lKDSHQmCxJJBpd3OyaH;yfYxifGmxbjCodFRGSlBzKTDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nctMg Mli3NlQ3QTV4M{K=
SW982 NV\wPY9MTnWwY4Tpc44hSXO|YYm= MV:wMlAyNTBwNTFOwG0> M4XHOFI1KGh? NXnV[ph4emWmdXPld{BCU1RicHjvd5Bpd3K7bHH0bY9vKCiyQVvULUBidmRiNFXCVFEheGixc4Doc5J6dGG2aX;uJEhxPEWEUEGpJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXyxsA> M2fZdlI1Pjl3NkOy
SW872 NV71R4Q5SXCxcITvd4l{KEG|c3H5 M37wNVAvODFvMD61JO69VQ>? NFHuZnQ1QCCq MWnpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NUXUbGpTOjR4OUW2N|I>
SW982 MVnBdI9xfG:|aYOgRZN{[Xl? M12zRlAvODFvMD61JO69VQ>? M3;2O|Q5KGh? NHjnWVJqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 MmfyNlQ3QTV4M{K=
AGS HG MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTBwNkigxtEhOC5yM{Gg{txO NWrHcmU3OjR3OUe0O|g>
AGS LG MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTBwMEWgxtEhOC5yMEGg{txO M2L2dFI1PTl5NEe4
HGC27 HG NFLVc3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTBwM{igxtEhOC5yMkKg{txO NF7tT4UzPDV7N{S3PC=>
HGC27 LG M{PmXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjITWM2OD1yLkCyJOKyKDBwMEC0JO69VQ>? NVnoUGNFOjR3OUe0O|g>
MKN45 HG MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXyTWM2OD1zLkCxJOKyKDBwMEWxJO69VQ>? M4HubVI1PTl5NEe4
MKN45 LG MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTBwOEegxtEhOC5yM{Cg{txO M2[ySFI1PTl5NEe4
NUGC4 HG NIizcnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4rrbWlEPTB;MUSuNEDDuSB|LkmxN{DPxE1? M1frNVI1PTl5NEe4
NUGC4 LG M2WzfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;TS2VKSzVyPUG0MlAhyrFiNT6zNlEh|ryP M2XoSlI1PTl5NEe4
A549 NYLITWM5TnWwY4Tpc44hSXO|YYm= M3\rOVAvOjVxMD61M|Eh|ryP MlHwNlQhcA>? M1[zU4lvcGmkaYTzJGFsfCCyaH;zdIhwenmuYYTpc44he2yrZ3j0cJk> MXOyOFM2OTR{NR?=
H460 MlHKSpVv[3Srb36gRZN{[Xl? M4mweVAvOjVxMD61M|Eh|ryP MYWyOEBp NV;XTXg2cW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|bHnnbJRtgQ>? NGGxUHMzPDN3MUSyOS=>
H661 NVnvNoIzTnWwY4Tpc44hSXO|YYm= MUOwMlI2NzBwNT:xJO69VQ>? MorxNlQhcA>? NX76TXpxcW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|aXfubYZq[2GwdHz5 NIDOT3MzPDN3MUSyOS=>
SAS M{T0SGZ2dmO2aX;uJGF{e2G7 M4T5PVAvOjVxMD61M|Eh|ryP M4C5R|I1KGh? MVPpcohq[mm2czDBb5QheGixc4Doc5J6dGG2aX;uJJNq\26rZnnjZY51dHl? MV:yOFM2OTR{NR?=
UT5 NF\LV2JHfW6ldHnvckBCe3OjeR?= MV[wMlI2NzBwNT:xJO69VQ>? NX;rZnRyOjRiaB?= NYnOfXcycW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|aXfubYZq[2GwdHz5 NITQdZczPDN3MUSyOS=>
FaDu NH3JXHNHfW6ldHnvckBCe3OjeR?= NHTBXG8xNjJ3L{CuOU8yKM7:TR?= NV[xb|NZOjRiaB?= NI\wPW1qdmirYnn0d{BCc3RicHjvd5Bpd3K7bHH0bY9vKHOrZ37p[olk[W62bIm= NYrmNXhyOjR|NUG0NlU>
RD MWPBdI9xfG:|aYOgRZN{[Xl? NWjEboxwOS9zLkWvNkDPxE1? M3XlTVczKGh? NWqyV5pMTE2VTx?= NITBOWJqdmS3Y3XzJINie3Cjc3Wt[IVx\W6mZX70JIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIGXPNVI3 NHTxOm8zOzZ6NEmyOS=>
TE671 M1\6WGFxd3C2b4Ppd{BCe3OjeR?= MUCxM|EvPS9{IN88US=> NYL0bWd[PzJiaB?= MUHEUXNQ MV\pcoR2[2W|IHPhd5Bie2VvZHXw[Y5l\W62IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKFWRMUK2 NXeycmRkOjN4OES5NlU>
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RMS13 MVrBdI9xfG:|aYOgRZN{[Xl? Mo\KNU8yNjVxMjFOwG0> MW[3NkBp NHL6W5BFVVOR MWjpcoR2[2W|IHPhd5Bie2VvZHXw[Y5l\W62IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKFWRMUK2 MXeyN|Y5PDl{NR?=
SUM149PT NUHpbVdwS2WubDDWbYFjcWyrdImgRZN{[Xl? MUKwMlMh|ryP M3PTU|czKGh? M2TKcIVvcGGwY3XzJIN6fG:2b4jpZ{Bm\m[nY4TzJI9nKFCLM1uvRWtVKHCjdHj3ZZkhcW6qaXLpeI9zew>? Mn31NlM3ODFyN{S=
MDA-MB-468 NI\LUVhE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M3;WW|AvOyEQvF2= MY[3NkBp NFnPWnhmdmijbnPld{BkgXSxdH;4bYMh\W[oZXP0d{Bw\iCSSUPLM2FMXCCyYYToe4F6KGmwaHnibZRwenN? NX33b4FQOjN4MEGwO|Q>
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SY5Y MXvGeY5kfGmxbjDBd5NigQ>? NYnNOVNJOS53L{KuOU82KM7:TR?= Mon3NlQhcA>? NWTld5A{cW6mdXPld{BIOcLiY3XscE1kgWOuZTDhdpJme3RiYX7kJIFxd3C2b4Ppdy=> M1m1ZVI{Ozd6M{Sx
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TP5014 MXnBdI9xfG:|aYOgRZN{[Xl? M3\4eVMhyrWP NGO2NGEyOiCq M1XYS2ROW09? MUnz[Y5{cXSrenXzJHJFKGOnbHzzJJRwKESRWD3pcoR2[2WmIHHwc5B1d3Orcx?= NILrcZEzOzNyMEiwPS=>
HT1080 M4TMR2Fxd3C2b4Ppd{BCe3OjeR?= MV6zJOK2VQ>? MXuxNkBp M1rHU2ROW09? MoK2d4Vve2m2aYrld{BTTCClZXzsd{B1dyCGT2itbY5lfWOnZDDhdI9xfG:|aYO= MW[yN|MxODhyOR?=
A549 M4Gzc2Z2dmO2aX;uJGF{e2G7 MUKwMVMvOyEQvF2= MWW3NkBp MWXpcoR2[2W|IHPvcZBt\XSnIHTve45z\We3bHH0bY9vKG:oIIDBT3Q> NHrOZ4wzOzJ3OUW5NS=>
HCC827 Mn70SpVv[3Srb36gRZN{[Xl? M1PKUlAuOy5|IN88US=> MUO3NkBp MUfpcoR2[2W|IHPvcZBt\XSnIHTve45z\We3bHH0bY9vKG:oIIDBT3Q> Mn7kNlMzPTl3OUG=
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TALL-1 NFy3bm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XmfVHjiIoQvF2= M{i1W|ch\A>? NEW0Wphl\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? MYWyN|A{QDJ5Mx?=
HPB-ALL MkKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkS1NgKBkc7:TR?= NWXJbopFPyCm NFnUN|Vl\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? NFPiclkzOzB|OEK3Ny=>
DND41 M2fZNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn62NgKBkc7:TR?= NIHBNIU4KGR? Mmno[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 MVSyN|A{QDJ5Mx?=
SUP-T1 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPrUWwy6oDLzszN MXq3JIQ> M4XXeoRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? NEDQWVczOzB|OEK3Ny=>
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MM1S MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTFNE0zKM7:TR?= MlX2NlQhcA>? NETEUnFKSzVyPUCuOUDPxE1? MXKyNlgzQTJ|NB?=
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PC-9  NXnCeYo2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYOwMVMh|ryP MVO3NkBp NV;O[oxYUUN3ME2wMlgh|ryP MlfLNlEzOjB2N{S=
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SF767 M1XmfWZ2dmO2aX;uJGF{e2G7 MVixJO69VQ>? MXm0PEBp M{fB[4lv\HWlZYOgZZV1d3CqYXfvd49u\SCob4LtZZRqd25? NF;QZnMzOTB4Mkm5Ny=>
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518A2  MkezR4VtdCCYaXHibYxqfHliQYPzZZk> NUC5WoJ7OC5yMfMAl|Ex6oDLzszN NXv3ZWx6PzJiaB?= MUjpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MVuyNVA1QDd6NR?=
Mel-Juso  MmrYSpVv[3Srb36gRZN{[Xl? MVWwMlAxOeLCk{JihKnPxE1? NGH3Z3AzPCCq MmK2d5VxeHKnc4Pld{BxcG:|cHjvdplt[XSrb36gc4YheGixc4DoZZRq\HmuIHnuc5NqfG:uIEOtb4lv[XOnIHTve45{fHKnYX2geIFz\2W2cx?= Mmn1NlExPDh5OEW=
518A2 MUDGeY5kfGmxbjDBd5NigQ>? NXLEcGdXOC5yMEJihLMy6oDLzszN M3XhPFI1KGh? Mnj1d5VxeHKnc4Pld{BxcG:|cHjvdplt[XSrb36gc4YheGixc4DoZZRq\HmuIHnuc5NqfG:uIEOtb4lv[XOnIHTve45{fHKnYX2geIFz\2W2cx?= M2X0cFIyODR6N{i1
PC3  MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHBNlRp NYLLUYVXT0l3MNMgQUAyODBibl2= Mn\PNlA2PTFyNkG=
U87MG Mmi4SpVv[3Srb36gRZN{[Xl? MWCwMlEuOSEQvF2= MkX1NlTjiImqwrC= MVfEUXNQ NIPQS5VqdmirYnn0d{BRUTONLX3l[IlifGWmIIPp[45idGmwZx?= MoXLNVk3OzN4OEO=
U138MG MUnGeY5kfGmxbjDBd5NigQ>? M2H4R|AvOS1zIN88US=> NGDKRnQzPOLCiXlCpC=> MlPDSG1UVw>? NEmwdXpqdmirYnn0d{BRUTONLX3l[IlifGWmIIPp[45idGmwZx?= NV\pdZJNOTl4M{O2PFM>
U118MG M1;KdGZ2dmO2aX;uJGF{e2G7 M4\BSFAvOS1zIN88US=> NIHuOoIzPOLCiXlCpC=> M4HJdWROW09? M2LQbolvcGmkaYTzJHBKO0tvbXXkbYF1\WRic3nncoFtcW6p NWHyZm1sOTl4M{O2PFM>
U87MG NGjP[5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTBwMUSg{txO NVfaeoE3OTl3OESyNlc>
IGROV-1 M4XjSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\LNmlEPTB;MD6wOkDPxE1? NWm2bVRJOTl3OESyNlc>
DETROIT562 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUjJR|UxRTBwMUOg{txO NVLyOVZpOTl3OESyNlc>
PC3  M1eyXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvWWIpwUUN3ME2wMlExKM7:TR?= M{XXclE6PTh2MkK3
SKOV-3 M{H3Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTBwMUKg{txO MlLWNVk2QDR{Mke=
HUVEC M3zJZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFj6PJFKSzVyPUCuNFgh|ryP M1yxR|E6PTh2MkK3
UCH-1  M1vSZmZ2dmO2aX;uJGF{e2G7 M4rlV|AuPSEQvF2= MkXNbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCkb4ToJGFMXCCjbnSgcXRQWiCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MYOxPVUzQDR2MR?=
UCH-1  MkL0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknrNE4xOS1zMDFOwG0> Mlz3OkBl M3;kUolvcGmkaYTzJJBzd2yrZnXyZZRqd25iZH;z[UBl\XCnbnTlcpRtgQ>? MnTBNVk2Ojh2NEG=
UCH-1  MXvBdI9xfG:|aYOgRZN{[Xl? MorqNE4yNTFyIN88US=> NFPW[20zPCCq NHzkV5FFVVOR NF\NV5VqdmS3Y3XzJIFxd3C2b4Ppdy=> MUSxPVUzQDR2MR?=

... 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

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