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 NEPtUpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVOwMVgh|ryP Mn\VNlQwPDhxN{KgbC=> MofDbY5lfWOnczD0bY1mNSCjbnSgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRiaX7obYJqfGmxbjDvckBPSiClZXzsJIdzd3e2aB?= NUPtWpBIOjZ{MkS2PFE>
SH-SY5Y MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjVNE05KM7:TR?= NX7M[|JQOjRxNEivO|IhcA>? MXTpcoR2[2W|IITpcYUuKGGwZDDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCrbnjpZol1cW:wIH;uJG5DKGOnbHyg[5Jwf3Sq MW[yOlIzPDZ6MR?=
SH-SY5Y  Ml\4RZBweHSxc3nzJGF{e2G7 M4DiZ|Eh|ryP MV[wMlUuOjRiaB?= M1\YXZNmdnOrdHn6[ZMhdmW3cn;icIF{fG:vYTDj[YxteyC2bzDkc5hwenWkaXPpck1qdmS3Y3XkJIFxd3C2b4Ppdy=> MlTzNlYzOjR4OEG=
G 35 SC NVnJdlFZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;BPVE1OC5yNT2yNEDPxE1? NITZbZUzPC95MjDo MU\EUXNQ M136XIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? NXnIUYpYOjZzMkGyOVE>
G 38 SC MkG1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUCwMlA2NTJyIN88US=> MoLSNlQwPzJiaB?= Mm\DSG1UVw>? NUDEUodrcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= M121W|I3OTJzMkWx
G 40 SC NYr2eVNPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUewMlA2NTJyIN88US=> MWqyOE84OiCq M2W0NGROW09? NEe3T|BqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 MYOyOlEzOTJ3MR?=
G 35 DC MmHpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjTeGlDOC5yNT2yNEDPxE1? M3\vSlI1Nzd{IHi= M4CxOWROW09? NXrS[3VWcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= M1LSU|I3OTJzMkWx
G 38 DC NV34d41RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XMT|AvODVvMkCg{txO NYD3clFMOjRxN{KgbC=> NUHmc5g3TE2VTx?= NEGzSohqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 NEG1XI0zPjF{MUK1NS=>
G 40 DC NWPHXnN1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEfVNmgxNjB3LUKwJO69VQ>? MXWyOE84OiCq MUjEUXNQ MlW5bY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBidmRidHnt[UBl\XCnbnTlcpRtgQ>? M4WyT|I3OTJzMkWx
RD MVzBdI9xfG:|aYOgRZN{[Xl? NHfFbpkyNzFwNT:yJO69VQ>? NUfZUlFFPzJiaB?= NH;0[mxqdmS3Y3XzJIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIFfBUnQ3OQ>? NET0dGUzPTd2OUO3PC=>
TE381.T NWntSmMxSXCxcITvd4l{KEG|c3H5 NH\TfmwyNzFwNT:yJO69VQ>? MXO3NkBp NWj6[ok5cW6mdXPld{BieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDHRW5VPjF? M{\o[VI2PzR7M{e4
RMS13 NF3L[VNCeG:ydH;zbZMhSXO|YYm= NGmyTlMyNzFwNT:yJO69VQ>? MUK3NkBp M2PHUolv\HWlZYOgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiR1HOWFYy M3XEe|I2PzR7M{e4
RH30  NXnYNoFnSXCxcITvd4l{KEG|c3H5 M2\6PFEwOS53L{Kg{txO M1XLbVczKGh? MX;pcoR2[2W|IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKEeDTmS2NS=> Mo\NNlU4PDl|N{i=
VJ NYfES2hYSXCxcITvd4l{KEG|c3H5 MmLJNU8yNjVxMjFOwG0> MY[3NkBp MVrpcoR2[2W|IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKEeDTmS2NS=> MVyyOVc1QTN5OB?=
HS578T MUXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NFPSOG8xNTNizszN NGnRUFM4OiCq MX;pcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NFL5Z4UzPTd{MUSxPS=>
BT549 NV;kdZpGS2WubDDWbYFjcWyrdImgRZN{[Xl? MoTtNE0{KM7:TR?= NWHvVWExPzJiaB?= NFq5WZNqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NWLJV|A{OjV5MkG0NVk>
MDA-MB-231 MWfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M3vwTVAuOyEQvF2= NH7EbZA4OiCq NFT0[lRqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NV:5T3U2OjV5MkG0NVk>
MDA-MB-468 NIXxU2lE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M1nvUlAuOyEQvF2= M12yPVczKGh? NULoT3llcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NX7UWXJuOjV5MkG0NVk>
MDA-MB-436 NEXpe3RE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NYGyO2JxOC1|IN88US=> NWXkd|RYPzJiaB?= NUXEPVlicW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= M3H4NlI2PzJzNEG5
SUM149PT M{jXVGNmdGxiVnnhZoltcXS7IFHzd4F6 NEPsXlMxNTNizszN MUC3NkBp M4XmUolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? Mlm1NlU4OjF2MUm=
MDA-MB-468 MXzGeY5kfGmxbjDBd5NigQ>? NVPVdW51OC5yMT2xNEDPxE1? NHzBPGgzPCCq M2CwT4Rwf26{ZXf1cIF1\XNidHjlJIxmfmWuczDv[kDPui2WclPQNUwh[y2PeXOgZY5lKGO7Y3zpckBGKHC{b4TlbY5{yqB? NFLUXZQzPTd{MUSxPS=>
MDA-MB-231 NVf4cHBZTnWwY4Tpc44hSXO|YYm= MYKwMlAyNTFyIN88US=> NHfNSZgzPCCq NVvFTnFX\G:5boLl[5Vt[XSnczD0bIUhdGW4ZXzzJI9nKM7{LWTyR3AyNCClLV35Z{BidmRiY4njcIlvKEVicILveIVqdnQEoB?= MVeyOVczOTRzOR?=
HS578T Mm\SSpVv[3Srb36gRZN{[Xl? NWL4NYt5OC5yMT2xNEDPxE1? MXeyOEBp MXTkc5dvemWpdXzheIV{KHSqZTDs[ZZmdHNib3[g{tIuXHKFUEGsJIMuVXmlIHHu[EBkgWOuaX6gSUBxem:2ZXnud:Kh MkTwNlU4OjF2MUm=
SW872 NY\tS2FrTnWwY4Tpc44hSXO|YYm= MlvjNE4xOS1yLkWg{txO NEjhPGEzPCCq MX\y[YR2[2W|IFHLWEBxcG:|cHjvdplt[XSrb36gLJBCU1RrIHHu[EA1TUKSMTDwbI9{eGixconsZZRqd25iKIC0SWJROSliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= MYOyOFY6PTZ|Mh?=
SW982 M13Fc2Z2dmO2aX;uJGF{e2G7 NH3MTnYxNjBzLUCuOUDPxE1? M4XONVI1KGh? M1jWZpJm\HWlZYOgRWtVKHCqb4PwbI9zgWyjdHnvckApeEGNVDmgZY5lKDSHQmCxJJBpd3OyaH;yfYxifGmxbjCodFRGSlBzKTDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nctMg NUfWT|MxOjR4OUW2N|I>
SW872 NXe3UWpPSXCxcITvd4l{KEG|c3H5 MlfMNE4xOS1yLkWg{txO NVzhOI06PDhiaB?= MnLmbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NVPHPXA6OjR4OUW2N|I>
SW982 Mo\yRZBweHSxc3nzJGF{e2G7 NYrmN4VCOC5yMT2wMlUh|ryP NGmzR4k1QCCq MlfKbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NYqx[I9UOjR4OUW2N|I>
AGS HG MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUjJR|UxRTBwNkigxtEhOC5yM{Gg{txO M3fndFI1PTl5NEe4
AGS LG MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\mZ|lKSzVyPUCuNFUhyrFiMD6wNFEh|ryP MUGyOFU6PzR5OB?=
HGC27 HG M2PRNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHMRYE{UUN3ME2wMlM5KMLzIECuNFIzKM7:TR?= NX[3XVk6OjR3OUe0O|g>
HGC27 LG MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzTTWM2OD1yLkCyJOKyKDBwMEC0JO69VQ>? M2XFcVI1PTl5NEe4
MKN45 HG MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXOyU4VMUUN3ME2xMlAyKMLzIECuNFUyKM7:TR?= M4HBXFI1PTl5NEe4
MKN45 LG M2DHfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7KN2JKSzVyPUCuPFchyrFiMD6wN|Ah|ryP NXHoN2x{OjR3OUe0O|g>
NUGC4 HG NXXTOmNIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfGTWM2OD1zND6wJOKyKDNwOUGzJO69VQ>? MXuyOFU6PzR5OB?=
NUGC4 LG MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXf4bZN7UUN3ME2xOE4xKMLzIEWuN|IyKM7:TR?= NIXzdZIzPDV7N{S3PC=>
A549 NHrEXmNHfW6ldHnvckBCe3OjeR?= Ml20NE4zPS9yLkWvNUDPxE1? M1HaPVI1KGh? NH[zVnZqdmirYnn0d{BCc3RicHjvd5Bpd3K7bHH0bY9vKHOuaXfoeIx6 NG\vdXQzPDN3MUSyOS=>
H460 MX7GeY5kfGmxbjDBd5NigQ>? M4LMclAvOjVxMD61M|Eh|ryP NV3NR21pOjRiaB?= NVrMWVBbcW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|bHnnbJRtgQ>? NFXURlgzPDN3MUSyOS=>
H661 MmXISpVv[3Srb36gRZN{[Xl? NH7PdYQxNjJ3L{CuOU8yKM7:TR?= NIruNlkzPCCq MXPpcohq[mm2czDBb5QheGixc4Doc5J6dGG2aX;uJJNq\26rZnnjZY51dHl? NYf4dVNMOjR|NUG0NlU>
SAS Mm\jSpVv[3Srb36gRZN{[Xl? NFjkXWUxNjJ3L{CuOU8yKM7:TR?= NUfETmdGOjRiaB?= NYn3SHVMcW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|aXfubYZq[2GwdHz5 MVqyOFM2OTR{NR?=
UT5 MXfGeY5kfGmxbjDBd5NigQ>? M1GxUVAvOjVxMD61M|Eh|ryP NV60OFEzOjRiaB?= NGfWNVRqdmirYnn0d{BCc3RicHjvd5Bpd3K7bHH0bY9vKHOrZ37p[olk[W62bIm= NVK2UZFQOjR|NUG0NlU>
FaDu NYrz[npoTnWwY4Tpc44hSXO|YYm= NHvqSogxNjJ3L{CuOU8yKM7:TR?= Ml\JNlQhcA>? Mn3qbY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7 MlHMNlQ{PTF2MkW=
RD NGO1[WRCeG:ydH;zbZMhSXO|YYm= MoXHNU8yNjVxMjFOwG0> NVLUSZF1PzJiaB?= NEKxV|dFVVOR MV;pcoR2[2W|IHPhd5Bie2VvZHXw[Y5l\W62IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKFWRMUK2 M4P6SVI{Pjh2OUK1
TE671 NFjwNYVCeG:ydH;zbZMhSXO|YYm= Mlq2NU8yNjVxMjFOwG0> NYL6bpJwPzJiaB?= MYLEUXNQ NFu0ZYxqdmS3Y3XzJINie3Cjc3Wt[IVx\W6mZX70JIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIGXPNVI3 NGixfmczOzZ6NEmyOS=>
RH30  NH3vTY5CeG:ydH;zbZMhSXO|YYm= NHj4RngyNzFwNT:yJO69VQ>? NELyR244OiCq MmDWSG1UVw>? NXXNNYlrcW6mdXPld{Bk[XOyYYPlMYRmeGWwZHXueEBieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDVU|EzPg>? MUKyN|Y5PDl{NR?=
RMS13 MVXBdI9xfG:|aYOgRZN{[Xl? NFvFb3oyNzFwNT:yJO69VQ>? MnfzO|IhcA>? NGW3cIRFVVOR NFvCPG9qdmS3Y3XzJINie3Cjc3Wt[IVx\W6mZX70JIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIGXPNVI3 MlHiNlM3QDR7MkW=
SUM149PT NELFRY1E\WyuIG\pZYJqdGm2eTDBd5NigQ>? MX[wMlMh|ryP NEDaXHM4OiCq MlTp[Y5p[W6lZYOgZ5l1d3SxeHnjJIVn\mWldIOgc4YhWEl|Sz;BT3QheGG2aIfhfUBqdmirYnn0c5J{ M1iyTFI{PjBzMEe0
MDA-MB-468 NWD0OI93S2WubDDWbYFjcWyrdImgRZN{[Xl? NUjGfVJxOC5|IN88US=> MVm3NkBp Ml2w[Y5p[W6lZYOgZ5l1d3SxeHnjJIVn\mWldIOgc4YhWEl|Sz;BT3QheGG2aIfhfUBqdmirYnn0c5J{ MWqyN|YxOTB5NB?=
MDA-MB-231 MnfzR4VtdCCYaXHibYxqfHliQYPzZZk> NYrtV4oyOC5|IN88US=> M1SzOFczKGh? MV3lcohidmOnczDjfZRwfG:6aXOg[YZn\WO2czDv[kBRUTONL1HLWEBx[XSqd3H5JIlvcGmkaYTvdpM> NWDFN3hrOjN4MEGwO|Q>
SY5Y MXPGeY5kfGmxbjDBd5NigQ>? MmfkNU42NzJwNT:1JO69VQ>? NEPjNXUzPCCq MVnpcoR2[2W|IFexxsBk\WyuLXP5Z4xmKGG{cnXzeEBidmRiYYDvdJRwe2m| MojxNlM{Pzh|NEG=
SKNBE(2c) NE[1[2RHfW6ldHnvckBCe3OjeR?= MUKxMlUwOi53L{Wg{txO M2X0UlI1KGh? MmHWbY5lfWOnczDHNeKh[2WubD3jfYNt\SCjcoLld5Qh[W6mIHHwc5B1d3Orcx?= MnvNNlM{Pzh|NEG=
RD M1OwOWFxd3C2b4Ppd{BCe3OjeR?= NILhdpA{KML3TR?= MljnNVIhcA>? NEi4dXlFVVOR NWjBPWRVe2Wwc3n0bZpmeyCURDDj[YxteyC2bzDEU3gucW6mdXPl[EBieG:ydH;zbZM> NIm5bJczOzNyMEiwPS=>
TP5014 MWjBdI9xfG:|aYOgRZN{[Xl? M4PhVFMhyrWP NU\0WI9YOTJiaB?= M3T1bmROW09? NFHKTIJ{\W6|aYTpfoV{KFKGIHPlcIx{KHSxIFTPXE1qdmS3Y3XkJIFxd3C2b4Ppdy=> MknXNlM{ODB6MEm=
HT1080 MYPBdI9xfG:|aYOgRZN{[Xl? NEX5UoM{KML3TR?= MY[xNkBp M{jpWGROW09? NWKyZmJje2Wwc3n0bZpmeyCURDDj[YxteyC2bzDEU3gucW6mdXPl[EBieG:ydH;zbZM> MYKyN|MxODhyOR?=
A549 NF\RO25HfW6ldHnvckBCe3OjeR?= NInF[YExNTNwMzFOwG0> NHfvUWM4OiCq NFvHTmFqdmS3Y3XzJINwdXCuZYTlJIRwf26{ZXf1cIF1cW:wIH;mJJBCU1R? M1;mNVI{OjV7NUmx
HCC827 Ml;QSpVv[3Srb36gRZN{[Xl? MlvyNE0{NjNizszN MkfxO|IhcA>? M1zxc4lv\HWlZYOgZ49ueGyndHWg[I94dnKnZ4XsZZRqd25ib3[gdGFMXA>? M4P1VFI{OjV7NUmx
H3122 NILxboVHfW6ldHnvckBCe3OjeR?= MU[wMVMvOyEQvF2= M4DFRVczKGh? NXG0[29NcW6mdXPld{Bkd22ybHX0[UBld3ewcnXneYxifGmxbjDv[kBxSUuW M{DrUlI{OjV7NUmx
TALL-1 NU\TTVhvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13XbFHjiIoQvF2= MljiO{Bl M3;ud4Rm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? M37FUFI{ODN6Mkez
HPB-ALL NVewNolDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDxNgKBkc7:TR?= MYe3JIQ> NVj5cWpk\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 MYOyN|A{QDJ5Mx?=
DND41 MnjhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojpNgKBkc7:TR?= NXvEd2xyPyCm NVj6Wnh[\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 M1TVT|I{ODN6Mkez
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PC-9  MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3THR|AuOyEQvF2= NV\vW3hEPzJiaB?= MojkTWM2OD1yLkig{txO MkHiNlEzOjB2N{S=
LN229 NVzoVZNMTnWwY4Tpc44hSXO|YYm= M2XnVlEh|ryP NF[3XIk1QCCq M{nVR4lv\HWlZYOgZZV1d3CqYXfvd49u\SCob4LtZZRqd25? NX23V2NQOjFyNkK5PVM>
U87 NFPZbJBHfW6ldHnvckBCe3OjeR?= M2f2blEh|ryP MnrlOFghcA>? NEjVe2RqdmS3Y3XzJIF2fG:yaHHnc5NwdWViZn;ycYF1cW:w MXiyNVA3Ojl7Mx?=
U373 MnTJSpVv[3Srb36gRZN{[Xl? MXqxJO69VQ>? NFf4NI01QCCq M1zKRolv\HWlZYOgZZV1d3CqYXfvd49u\SCob4LtZZRqd25? NELlbVEzOTB4Mkm5Ny=>
SF767 MlzTSpVv[3Srb36gRZN{[Xl? M3TYS|Eh|ryP M3vwU|Q5KGh? NF7Q[3ZqdmS3Y3XzJIF2fG:yaHHnc5NwdWViZn;ycYF1cW:w MXiyNVA3Ojl7Mx?=
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518A2  NFLmXVNE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MViwMlAy6oDVMUFihKnPxE1? MVi3NkBp MmjybY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MmfTNlExPDh5OEW=
Mel-Juso  NYq1dXU{TnWwY4Tpc44hSXO|YYm= NH3Ub|IxNjByMfMAl|HjiIoQvF2= M{Pzc|I1KGh? MVfzeZBxemW|c3XzJJBpd3OyaH;yfYxifGmxbjDv[kBxcG:|cHjheIllgWxiaX7vd4l1d2xiMz3rbY5ie2ViZH;3cpN1emWjbTD0ZZJo\XS| MnfpNlExPDh5OEW=
518A2 MlfzSpVv[3Srb36gRZN{[Xl? NULZbIk3OC5yMEJihLMy6oDLzszN MYCyOEBp NHjOUJl{fXCycnXzd4V{KHCqb4PwbI9zgWyjdHnvckBw\iCyaH;zdIhifGmmeXygbY5we2m2b3ygN{1scW6jc3Wg[I94dnO2cnXhcUB1[XKpZYTz M16yXFIyODR6N{i1
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IGROV-1 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3v1cWlEPTB;MD6wOkDPxE1? MX:xPVU5PDJ{Nx?=
DETROIT562 NFjLbo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjFTWM2OD1yLkGzJO69VQ>? MkjSNVk2QDR{Mke=
PC3  M{L3PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTBwMUCg{txO M3PYT|E6PTh2MkK3
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UCH-1  MULGeY5kfGmxbjDBd5NigQ>? NWXo[5JpOC13IN88US=> NYPUdY5bcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDic5RpKEGNVDDhcoQhdVSRUjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NI\McWoyQTV{OES0NS=>
UCH-1  MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnTnNE4xOS1zMDFOwG0> M{PHNlYh\A>? MXXpcohq[mm2czDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> NGG0OIMyQTV{OES0NS=>
UCH-1  NHzTd|lCeG:ydH;zbZMhSXO|YYm= NX3MSo5wOC5zLUGwJO69VQ>? MmDmNlQhcA>? Mne2SG1UVw>? NUPKWm1wcW6mdXPld{BieG:ydH;zbZM> MlLvNVk2Ojh2NEG=

... 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
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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
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  • 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
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  • 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
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*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):
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    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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID