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 Mlv6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGezPHcxNThizszN NVLBV4NjOjRxNEivO|IhcA>? NGrUc|VqdmS3Y3XzJJRqdWVvIHHu[EBkd26lZX70doF1cW:wLXTldIVv\GWwdDDpcohq[mm2aX;uJI9vKE6EIHPlcIwh\3Kxd4To NYHaV5FrOjZ{MkS2PFE>
SH-SY5Y M4LCTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIO1WmExNThizszN M1HiNVI1NzR6L{eyJIg> NXfLZWlCcW6mdXPld{B1cW2nLTDhcoQh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgbY5pcWKrdHnvckBwdiCQQjDj[YxtKGe{b4f0bC=> MUCyOlIzPDZ6MR?=
SH-SY5Y  MlvDRZBweHSxc3nzJGF{e2G7 MUexJO69VQ>? M{HIclAvPS1{NDDo NV7RSIc6e2Wwc3n0bZpmeyCwZYXyc4Jt[XO2b33hJINmdGy|IITvJIRwgG:{dXLpZ4lvNWmwZIXj[YQh[XCxcITvd4l{ M3fvOlI3OjJ2Nkix
G 35 SC NGnrT49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37WRlAvODVvMkCg{txO M{\0blI1Nzd{IHi= MkjRSG1UVw>? MYTpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueIx6 M1Xue|I3OTJzMkWx
G 38 SC MoXCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1ThS|AvODVvMkCg{txO NF7h[VgzPC95MjDo NX;wVW9STE2VTx?= M17t[YlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? MYKyOlEzOTJ3MR?=
G 40 SC NVTGSmtmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXOwMlA2NTJyIN88US=> NXHQW29QOjRxN{KgbC=> MU\EUXNQ MXnpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueIx6 NWP3dG06OjZzMkGyOVE>
G 35 DC NUjaU|RkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\COVAvODVvMkCg{txO NWnMdXVDOjRxN{KgbC=> NI\wTnRFVVOR NFyySmJqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 NH32SogzPjF{MUK1NS=>
G 38 DC MnWxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXKwMlA2NTJyIN88US=> Mn7UNlQwPzJiaB?= MmLnSG1UVw>? M2\OOolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? M3rsRlI3OTJzMkWx
G 40 DC NUDtTHloT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjveGpLOC5yNT2yNEDPxE1? NUnkTXJtOjRxN{KgbC=> M2TyVmROW09? MmDRbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBidmRidHnt[UBl\XCnbnTlcpRtgQ>? NYHPcVZ1OjZzMkGyOVE>
RD NEfkSZNCeG:ydH;zbZMhSXO|YYm= MVWxM|EvPS9{IN88US=> MUi3NkBp NHflOYhqdmS3Y3XzJIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIFfBUnQ3OQ>? MnvtNlU4PDl|N{i=
TE381.T MVLBdI9xfG:|aYOgRZN{[Xl? NEnWSGsyNzFwNT:yJO69VQ>? M1XKNFczKGh? NFjPW|ZqdmS3Y3XzJIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIFfBUnQ3OQ>? MWiyOVc1QTN5OB?=
RMS13 NVzUVlNOSXCxcITvd4l{KEG|c3H5 NEC0[GcyNzFwNT:yJO69VQ>? NGDhe3I4OiCq NV;GV416cW6mdXPld{BieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDHRW5VPjF? M3XG[FI2PzR7M{e4
RH30  M{XrV2Fxd3C2b4Ppd{BCe3OjeR?= MnvoNU8yNjVxMjFOwG0> MUm3NkBp M1OzeYlv\HWlZYOgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiR1HOWFYy NIPScVczPTd2OUO3PC=>
VJ MVfBdI9xfG:|aYOgRZN{[Xl? MmS0NU8yNjVxMjFOwG0> M1TiNVczKGh? NGXT[FNqdmS3Y3XzJIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIFfBUnQ3OQ>? NIXkZYYzPTd2OUO3PC=>
HS578T NE\HUVRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NXiyWYJrOC1|IN88US=> MVq3NkBp NIj1b45qdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NWTtZlRmOjV5MkG0NVk>
BT549 M2rhdmNmdGxiVnnhZoltcXS7IFHzd4F6 Mo[yNE0{KM7:TR?= Mn7jO|IhcA>? NVv5OHlocW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NEjsVYgzPTd{MUSxPS=>
MDA-MB-231 NVXhOll[S2WubDDWbYFjcWyrdImgRZN{[Xl? M3nQ[lAuOyEQvF2= NXe4PFhNPzJiaB?= NFzJNoNqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NIGzZmYzPTd{MUSxPS=>
MDA-MB-468 Mnm4R4VtdCCYaXHibYxqfHliQYPzZZk> NUX3OmpLOC1|IN88US=> MV:3NkBp NEDEUWJqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NEC4N2MzPTd{MUSxPS=>
MDA-MB-436 NUTKZYNUS2WubDDWbYFjcWyrdImgRZN{[Xl? M4Cx[|AuOyEQvF2= MWe3NkBp MUfpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 M3TSUFI2PzJzNEG5
SUM149PT MXnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> Mn7HNE0{KM7:TR?= M3rMfVczKGh? M{DtfIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? M{nySFI2PzJzNEG5
MDA-MB-468 MWjGeY5kfGmxbjDBd5NigQ>? NInGO4gxNjBzLUGwJO69VQ>? Ml\zNlQhcA>? NIjHUYJld3ewcnXneYxifGW|IITo[UBt\X[nbIOgc4Yh|rJvVILDVFEtKGNvTYnjJIFv\CCleXPsbY4hTSCycn;0[Ylve8Li MUCyOVczOTRzOR?=
MDA-MB-231 NIXVS2dHfW6ldHnvckBCe3OjeR?= M{LtN|AvODFvMUCg{txO NHPFVI0zPCCq NFT4XpZld3ewcnXneYxifGW|IITo[UBt\X[nbIOgc4Yh|rJvVILDVFEtKGNvTYnjJIFv\CCleXPsbY4hTSCycn;0[Ylve8Li M{[x[lI2PzJzNEG5
HS578T MYHGeY5kfGmxbjDBd5NigQ>? M4\uVFAvODFvMUCg{txO MWCyOEBp Morn[I94dnKnZ4XsZZRmeyC2aHWgcIV3\Wy|IH;mJO6zNVS{Q2CxMEBkNU27YzDhcoQh[3mlbHnuJGUheHKxdHXpcpPDqA>? NHe1VIUzPTd{MUSxPS=>
SW872 M1i3dmZ2dmO2aX;uJGF{e2G7 MYqwMlAyNTBwNTFOwG0> M2\UOVI1KGh? M3\OVpJm\HWlZYOgRWtVKHCqb4PwbI9zgWyjdHnvckApeEGNVDmgZY5lKDSHQmCxJJBpd3OyaH;yfYxifGmxbjCodFRGSlBzKTDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nctMg M3HEOlI1Pjl3NkOy
SW982 MUXGeY5kfGmxbjDBd5NigQ>? MXywMlAyNTBwNTFOwG0> NXvRNItyOjRiaB?= NFLKXHpz\WS3Y3XzJGFMXCCyaH;zdIhwenmuYYTpc44hMHCDS2SpJIFv\CB2RVLQNUBxcG:|cHjvdplt[XSrb36gLJA1TUKSMTmgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYNCpC=> MlnlNlQ3QTV4M{K=
SW872 NYjsXHR2SXCxcITvd4l{KEG|c3H5 NFK3XVAxNjBzLUCuOUDPxE1? NUXyZYdyPDhiaB?= MUjpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NEK1c5YzPDZ7NU[zNi=>
SW982 MlzjRZBweHSxc3nzJGF{e2G7 M2r0cVAvODFvMD61JO69VQ>? NH\qNIs1QCCq NG\hWHhqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 M17ublI1Pjl3NkOy
AGS HG M3LDWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7DTJNxUUN3ME2wMlY5KMLzIECuNFMyKM7:TR?= NEC0W2IzPDV7N{S3PC=>
AGS LG NGnWPJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDOPHVKSzVyPUCuNFUhyrFiMD6wNFEh|ryP NEn1TIQzPDV7N{S3PC=>
HGC27 HG M1ywV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HJemlEPTB;MD6zPEDDuSByLkCyNkDPxE1? MnO4NlQ2QTd2N{i=
HGC27 LG MoTyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTJb|JKSzVyPUCuNFIhyrFiMD6wNFQh|ryP Mn[1NlQ2QTd2N{i=
MKN45 HG NGOyXXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PZNWlEPTB;MT6wNUDDuSByLkC1NUDPxE1? M4PoXFI1PTl5NEe4
MKN45 LG M1HXb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX6yU2h{UUN3ME2wMlg4KMLzIECuNFMxKM7:TR?= NFLpN2ozPDV7N{S3PC=>
NUGC4 HG MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13FW2lEPTB;MUSuNEDDuSB|LkmxN{DPxE1? MoLhNlQ2QTd2N{i=
NUGC4 LG M3v3SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPLS4VKSzVyPUG0MlAhyrFiNT6zNlEh|ryP MnjMNlQ2QTd2N{i=
A549 M1XVfmZ2dmO2aX;uJGF{e2G7 NVywTVJGOC5{NT:wMlUwOSEQvF2= NFnoT2czPCCq NWHKW4xDcW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|bHnnbJRtgQ>? NUjtWIdHOjR|NUG0NlU>
H460 MVrGeY5kfGmxbjDBd5NigQ>? Mn6zNE4zPS9yLkWvNUDPxE1? NEjiOogzPCCq M3PC[4lvcGmkaYTzJGFsfCCyaH;zdIhwenmuYYTpc44he2yrZ3j0cJk> MXOyOFM2OTR{NR?=
H661 NF30PVlHfW6ldHnvckBCe3OjeR?= MViwMlI2NzBwNT:xJO69VQ>? MYSyOEBp NYD0SFRncW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|aXfubYZq[2GwdHz5 M1zRNFI1OzVzNEK1
SAS NYLDR|ZwTnWwY4Tpc44hSXO|YYm= M3HF[|AvOjVxMD61M|Eh|ryP NFTU[5IzPCCq MljUbY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7 MX:yOFM2OTR{NR?=
UT5 MX\GeY5kfGmxbjDBd5NigQ>? MYCwMlI2NzBwNT:xJO69VQ>? M1v6e|I1KGh? MXfpcohq[mm2czDBb5QheGixc4Doc5J6dGG2aX;uJJNq\26rZnnjZY51dHl? M2Ln[VI1OzVzNEK1
FaDu NH7kUIFHfW6ldHnvckBCe3OjeR?= NHzBOocxNjJ3L{CuOU8yKM7:TR?= NWLVS5pnOjRiaB?= MkfzbY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7 NFm5c3EzPDN3MUSyOS=>
RD M3e0SWFxd3C2b4Ppd{BCe3OjeR?= MnnBNU8yNjVxMjFOwG0> MWG3NkBp MYTEUXNQ Mo\kbY5lfWOnczDjZZNx[XOnLXTldIVv\GWwdDDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCXT{GyOi=> NVrK[lZSOjN4OES5NlU>
TE671 MV\BdI9xfG:|aYOgRZN{[Xl? NHj2WoMyNzFwNT:yJO69VQ>? MnTaO|IhcA>? NGK4fVRFVVOR MlTKbY5lfWOnczDjZZNx[XOnLXTldIVv\GWwdDDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCXT{GyOi=> M3PRcFI{Pjh2OUK1
RH30  NYnyR2lISXCxcITvd4l{KEG|c3H5 MV:xM|EvPS9{IN88US=> MVu3NkBp NFHIT2dFVVOR M1;hSYlv\HWlZYOgZ4F{eGG|ZT3k[ZBmdmSnboSgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiVV:xNlY> MV6yN|Y5PDl{NR?=
RMS13 M4LHVWFxd3C2b4Ppd{BCe3OjeR?= NV3ldmVGOS9zLkWvNkDPxE1? MYe3NkBp M{jQXmROW09? NU[xV|BUcW6mdXPld{Bk[XOyYYPlMYRmeGWwZHXueEBieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDVU|EzPg>? NGjuenEzOzZ6NEmyOS=>
SUM149PT NHfLdFFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M3jsO|AvOyEQvF2= M4\qXVczKGh? MoW1[Y5p[W6lZYOgZ5l1d3SxeHnjJIVn\mWldIOgc4YhWEl|Sz;BT3QheGG2aIfhfUBqdmirYnn0c5J{ NYjBO45iOjN4MEGwO|Q>
MDA-MB-468 MYDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NH3nRnkxNjNizszN M2\CU|czKGh? NVHHSFhZ\W6qYX7j[ZMh[3m2b4TvfIlkKGWoZnXjeJMhd2ZiUFmzT{9CU1RicHH0bJdigSCrbnjpZol1d3K| Ml3ONlM3ODFyN{S=
MDA-MB-231 MYrD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MoT0NE4{KM7:TR?= M{nTblczKGh? Mmnx[Y5p[W6lZYOgZ5l1d3SxeHnjJIVn\mWldIOgc4YhWEl|Sz;BT3QheGG2aIfhfUBqdmirYnn0c5J{ M2jVRlI{PjBzMEe0
SY5Y NGfCfXJHfW6ldHnvckBCe3OjeR?= NWTMUlRHOS53L{KuOU82KM7:TR?= MWKyOEBp NIWyXIpqdmS3Y3XzJGcyyqClZXzsMYN6[2ynIHHydoV{fCCjbnSgZZBweHSxc3nz MYiyN|M4QDN2MR?=
SKNBE(2c) NFH2RnBHfW6ldHnvckBCe3OjeR?= NHLlbVQyNjVxMj61M|Uh|ryP MnLYNlQhcA>? NWq0V4VGcW6mdXPld{BIOcLiY3XscE1kgWOuZTDhdpJme3RiYX7kJIFxd3C2b4Ppdy=> MlKxNlM{Pzh|NEG=
RD MmTyRZBweHSxc3nzJGF{e2G7 MYSzJOK2VQ>? MW[xNkBp NUi5TGNlTE2VTx?= NYTWdpA1e2Wwc3n0bZpmeyCURDDj[YxteyC2bzDEU3gucW6mdXPl[EBieG:ydH;zbZM> Ml\1NlM{ODB6MEm=
TP5014 Ml\LRZBweHSxc3nzJGF{e2G7 NGTkcmM{KML3TR?= Ml3kNVIhcA>? NXf6TVdDTE2VTx?= NGqzTZR{\W6|aYTpfoV{KFKGIHPlcIx{KHSxIFTPXE1qdmS3Y3XkJIFxd3C2b4Ppdy=> MlzpNlM{ODB6MEm=
HT1080 MXfBdI9xfG:|aYOgRZN{[Xl? M{HlTFMhyrWP M3S3VVEzKGh? MkHWSG1UVw>? MYPz[Y5{cXSrenXzJHJFKGOnbHzzJJRwKESRWD3pcoR2[2WmIHHwc5B1d3Orcx?= NWe2[XZzOjN|MEC4NFk>
A549 NX3mc|M4TnWwY4Tpc44hSXO|YYm= NU[3cmtlOC1|LkOg{txO MmPkO|IhcA>? NIToclFqdmS3Y3XzJINwdXCuZYTlJIRwf26{ZXf1cIF1cW:wIH;mJJBCU1R? MWOyN|I2QTV7MR?=
HCC827 M2\ibGZ2dmO2aX;uJGF{e2G7 Mn7YNE0{NjNizszN NYXie4xvPzJiaB?= NG\le3hqdmS3Y3XzJINwdXCuZYTlJIRwf26{ZXf1cIF1cW:wIH;mJJBCU1R? M3L5WlI{OjV7NUmx
H3122 NW[5cVlRTnWwY4Tpc44hSXO|YYm= MYCwMVMvOyEQvF2= MVS3NkBp MWPpcoR2[2W|IHPvcZBt\XSnIHTve45z\We3bHH0bY9vKG:oIIDBT3Q> M2HBRlI{OjV7NUmx
TALL-1 NVTMO5FnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYC1WYh[OeLCid88US=> NUHZeY13PyCm MYXk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> MV2yN|A{QDJ5Mx?=
HPB-ALL M1e0OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX[x5qCK|ryP MojuO{Bl M1jQXIRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? NXLK[WxjOjNyM{iyO|M>
DND41 NYDMOlQ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PJWFHjiIoQvF2= M4PGWVch\A>? Mn3F[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 MmKyNlMxOzh{N{O=
SUP-T1 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLhOYx1OeLCid88US=> MofiO{Bl MnLK[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 NX6xV4RxOjNyM{iyO|M>
PEER NUW5XJRJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2P1eFHjiIoQvF2= MnPoO{Bl NVG2PVNu\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 MoDONlMxOzh{N{O=
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PC-9  NUnPfWhXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVOwMVMh|ryP M{ewe|czKGh? M3PkUGlEPTB;MD64JO69VQ>? NV62SnpSOjF{MkC0O|Q>
LN229 NIX4[|NHfW6ldHnvckBCe3OjeR?= MoL1NUDPxE1? MkDHOFghcA>? NFXOV5dqdmS3Y3XzJIF2fG:yaHHnc5NwdWViZn;ycYF1cW:w MmXhNlExPjJ7OUO=
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SF767 MlrRSpVv[3Srb36gRZN{[Xl? NHriclUyKM7:TR?= M3TRZVQ5KGh? MWDpcoR2[2W|IHH1eI9xcGGpb4PvcYUh\m:{bXH0bY9v M{DOSFIyODZ{OUmz
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518A2  NYHZ[Wg5S2WubDDWbYFjcWyrdImgRZN{[Xl? MX[wMlAy6oDVMUFihKnPxE1? NV;2PI9CPzJiaB?= NWXENpk4cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NEDhUJYzOTB2OEe4OS=>
Mel-Juso  NIHndWlHfW6ldHnvckBCe3OjeR?= MnLWNE4xODIkgKOx5qCK|ryP MYmyOEBp MUnzeZBxemW|c3XzJJBpd3OyaH;yfYxifGmxbjDv[kBxcG:|cHjheIllgWxiaX7vd4l1d2xiMz3rbY5ie2ViZH;3cpN1emWjbTD0ZZJo\XS| MkW5NlExPDh5OEW=
518A2 M1TXfGZ2dmO2aX;uJGF{e2G7 NUTUSZlGOC5yMEJihLMy6oDLzszN MmD5NlQhcA>? MnHWd5VxeHKnc4Pld{BxcG:|cHjvdplt[XSrb36gc4YheGixc4DoZZRq\HmuIHnuc5NqfG:uIEOtb4lv[XOnIHTve45{fHKnYX2geIFz\2W2cx?= NH;BTIkzOTB2OEe4OS=>
PC3  MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7udJJCOjSq NH3nOI1IUTVywrC9JFExOCCwTR?= NEPQSpYzODV3MUC2NS=>
U87MG MYXGeY5kfGmxbjDBd5NigQ>? M3yyc|AvOS1zIN88US=> MmnWNlTjiImqwrC= MmfESG1UVw>? MnnzbY5pcWKrdIOgVGk{Uy2vZXTpZZRm\CC|aXfuZYxqdmd? MkHTNVk3OzN4OEO=
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U118MG MmDTSpVv[3Srb36gRZN{[Xl? MXiwMlEuOSEQvF2= MmX3NlTjiImqwrC= MmLOSG1UVw>? NY\1WpVOcW6qaXLpeJMhWEl|Sz3t[YRq[XSnZDDzbYdv[Wyrbne= MVGxPVY{OzZ6Mx?=
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IGROV-1 M4TDd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rDNWlEPTB;MD6wOkDPxE1? Mlj0NVk2QDR{Mke=
DETROIT562 NV:2OGlIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\RO2tRUUN3ME2wMlE{KM7:TR?= M3zVTFE6PTh2MkK3
PC3  M2XOVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojmTWM2OD1yLkGwJO69VQ>? NFX3RVEyQTV6NEKyOy=>
SKOV-3 NYjvRoxlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTBwMUKg{txO MYOxPVU5PDJ{Nx?=
HUVEC MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPiTWM2OD1yLkC4JO69VQ>? M{\sWVE6PTh2MkK3
UCH-1  MkDmSpVv[3Srb36gRZN{[Xl? NXq5[2tTOC13IN88US=> MY\pcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKGKxdHigRWtVKGGwZDDtWG9TKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz Ml;sNVk2Ojh2NEG=
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UCH-1  Mn7vRZBweHSxc3nzJGF{e2G7 NG\zb4UxNjFvMUCg{txO NIq5[nUzPCCq MY\EUXNQ MUjpcoR2[2W|IHHwc5B1d3Orcx?= MnXCNVk2Ojh2NEG=

... 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 individually and in order:
1% DMSO+30% polyethylene glycol+1% Tween 80
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
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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

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID