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

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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 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY[wMVgh|ryP NInSVlYzPC92OD:3NkBp NVjqSVE3cW6mdXPld{B1cW2nLTDhcoQh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgbY5pcWKrdHnvckBwdiCQQjDj[YxtKGe{b4f0bC=> NXjGO4F1OjZ{MkS2PFE>
SH-SY5Y M4nGSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFX1WGUxNThizszN NEH5WnAzPC92OD:3NkBp NFjVVGpqdmS3Y3XzJJRqdWVvIHHu[EBkd26lZX70doF1cW:wLXTldIVv\GWwdDDpcohq[mm2aX;uJI9vKE6EIHPlcIwh\3Kxd4To MVyyOlIzPDZ6MR?=
SH-SY5Y  M2DkVGFxd3C2b4Ppd{BCe3OjeR?= NWXIXGlCOSEQvF2= NInUPWExNjVvMkSgbC=> MWTz[Y5{cXSrenXzJI5mfXKxYnzhd5RwdWFiY3XscJMhfG9iZH;4c5J2[mmlaX6tbY5lfWOnZDDhdI9xfG:|aYO= Mn73NlYzOjR4OEG=
G 35 SC MkDNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvpRVkxNjB3LUKwJO69VQ>? NWDBVIpUOjRxN{KgbC=> M3m2XmROW09? M2P6b4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? M1f0OFI3OTJzMkWx
G 38 SC NWT1[phlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYSwMlA2NTJyIN88US=> M{flSVI1Nzd{IHi= M1\kbmROW09? MmSzbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBidmRidHnt[UBl\XCnbnTlcpRtgQ>? M1Hv[VI3OTJzMkWx
G 40 SC MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW[wMlA2NTJyIN88US=> NXL6Umw3OjRxN{KgbC=> NYjuU3dHTE2VTx?= M1u2OYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? MnnHNlYyOjF{NUG=
G 35 DC NWD1b3RkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXBNE4xPS1{MDFOwG0> MXSyOE84OiCq M2m0dGROW09? NVr6V4ttcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= M{ntd|I3OTJzMkWx
G 38 DC NV[2VGE6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXETYlkOC5yNT2yNEDPxE1? NX\pVIxrOjRxN{KgbC=> NH\0W3dFVVOR Mkn5bY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBidmRidHnt[UBl\XCnbnTlcpRtgQ>? M37sXlI3OTJzMkWx
G 40 DC MnrNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDnOHAxNjB3LUKwJO69VQ>? NUPCdGNrOjRxN{KgbC=> MVjEUXNQ NG\SRnhqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 NFXvOoEzPjF{MUK1NS=>
RD NF[3RmxCeG:ydH;zbZMhSXO|YYm= NGPU[ZYyNzFwNT:yJO69VQ>? MYW3NkBp NE[2SZVqdmS3Y3XzJIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIFfBUnQ3OQ>? MUiyOVc1QTN5OB?=
TE381.T M1;RTGFxd3C2b4Ppd{BCe3OjeR?= MnTRNU8yNjVxMjFOwG0> NYDibmF1PzJiaB?= NXzKfI9lcW6mdXPld{BieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDHRW5VPjF? NVrYPWpjOjV5NEmzO|g>
RMS13 MlvxRZBweHSxc3nzJGF{e2G7 MnHaNU8yNjVxMjFOwG0> NGrwSGM4OiCq MmLobY5lfWOnczDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCJQV7UOlE> MYWyOVc1QTN5OB?=
RH30  MlXuRZBweHSxc3nzJGF{e2G7 NEXjT5EyNzFwNT:yJO69VQ>? NY\lUmd1PzJiaB?= NGfHUZFqdmS3Y3XzJIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIFfBUnQ3OQ>? MoTLNlU4PDl|N{i=
VJ Ml7uRZBweHSxc3nzJGF{e2G7 NIT5S|QyNzFwNT:yJO69VQ>? NWD4N4F3PzJiaB?= MWHpcoR2[2W|IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKEeDTmS2NS=> M{njZlI2PzR7M{e4
HS578T MlXKR4VtdCCYaXHibYxqfHliQYPzZZk> NHjKdm0xNTNizszN MXm3NkBp NITWfZRqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NUPBcVBoOjV5MkG0NVk>
BT549 M3LGWWNmdGxiVnnhZoltcXS7IFHzd4F6 M1PXUlAuOyEQvF2= NUX2U4FnPzJiaB?= M2Xxe4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MX2yOVczOTRzOR?=
MDA-MB-231 NVHGdpRYS2WubDDWbYFjcWyrdImgRZN{[Xl? M{[2WVAuOyEQvF2= M2TuWFczKGh? NYXGfpV4cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MlS4NlU4OjF2MUm=
MDA-MB-468 MmPzR4VtdCCYaXHibYxqfHliQYPzZZk> MVmwMVMh|ryP MX[3NkBp M4PKTolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MVuyOVczOTRzOR?=
MDA-MB-436 NFPsOZJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M2DYblAuOyEQvF2= MYO3NkBp MnG5bY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NWrD[Jd[OjV5MkG0NVk>
SUM149PT MYXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MVywMVMh|ryP MlvPO|IhcA>? M3vTfolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NIr2dZEzPTd{MUSxPS=>
MDA-MB-468 NIG2OoRHfW6ldHnvckBCe3OjeR?= NHjhVJIxNjBzLUGwJO69VQ>? NUXqfFMxOjRiaB?= NHjaNJZld3ewcnXneYxifGW|IITo[UBt\X[nbIOgc4Yh|rJvVILDVFEtKGNvTYnjJIFv\CCleXPsbY4hTSCycn;0[Ylve8Li MYSyOVczOTRzOR?=
MDA-MB-231 Mlu2SpVv[3Srb36gRZN{[Xl? Mlm1NE4xOS1zMDFOwG0> NHjB[WczPCCq NGS0OW9ld3ewcnXneYxifGW|IITo[UBt\X[nbIOgc4Yh|rJvVILDVFEtKGNvTYnjJIFv\CCleXPsbY4hTSCycn;0[Ylve8Li NUCyb5cxOjV5MkG0NVk>
HS578T M4H5WGZ2dmO2aX;uJGF{e2G7 NHPoWI4xNjBzLUGwJO69VQ>? M2fvflI1KGh? MWHkc5dvemWpdXzheIV{KHSqZTDs[ZZmdHNib3[g{tIuXHKFUEGsJIMuVXmlIHHu[EBkgWOuaX6gSUBxem:2ZXnud:Kh NVfNemRvOjV5MkG0NVk>
SW872 MmDSSpVv[3Srb36gRZN{[Xl? M{LZO|AvODFvMD61JO69VQ>? NV7EcZllOjRiaB?= MlvGdoVlfWOnczDBT3QheGixc4Doc5J6dGG2aX;uJEhxSUuWKTDhcoQhPEWEUEGgdIhwe3Cqb4L5cIF1cW:wIDjwOGVDWDFrIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{wrC= MlnLNlQ3QTV4M{K=
SW982 MVHGeY5kfGmxbjDBd5NigQ>? NVrSS4FtOC5yMT2wMlUh|ryP M3fPeVI1KGh? NYC0W|dQemWmdXPld{BCU1RicHjvd5Bpd3K7bHH0bY9vKCiyQVvULUBidmRiNFXCVFEheGixc4Doc5J6dGG2aX;uJEhxPEWEUEGpJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXyxsA> MYSyOFY6PTZ|Mh?=
SW872 M{nkTWFxd3C2b4Ppd{BCe3OjeR?= Mm\6NE4xOS1yLkWg{txO MW[0PEBp NF3m[3dqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 MY[yOFY6PTZ|Mh?=
SW982 MUHBdI9xfG:|aYOgRZN{[Xl? MnPsNE4xOS1yLkWg{txO M1rQ[lQ5KGh? MlrwbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MonvNlQ3QTV4M{K=
AGS HG NHj4[XdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PBSGlEPTB;MD62PEDDuSByLkCzNUDPxE1? MUiyOFU6PzR5OB?=
AGS LG MoDNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjyXYlKSzVyPUCuNFUhyrFiMD6wNFEh|ryP M2H0[|I1PTl5NEe4
HGC27 HG MnzZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13kW2lEPTB;MD6zPEDDuSByLkCyNkDPxE1? MnH1NlQ2QTd2N{i=
HGC27 LG M4rP[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInYXoVKSzVyPUCuNFIhyrFiMD6wNFQh|ryP Mo\kNlQ2QTd2N{i=
MKN45 HG NV:5SZFNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jNO2lEPTB;MT6wNUDDuSByLkC1NUDPxE1? M2XuWlI1PTl5NEe4
MKN45 LG NUTZZoNWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTBwOEegxtEhOC5yM{Cg{txO NIq1eY8zPDV7N{S3PC=>
NUGC4 HG MlXoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTIcZV1UUN3ME2xOE4xKMLzIEOuPVE{KM7:TR?= NHO1Z48zPDV7N{S3PC=>
NUGC4 LG NX65fo5ET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTF2LkCgxtEhPS5|MkGg{txO NVLMRppQOjR3OUe0O|g>
A549 NFPURXFHfW6ldHnvckBCe3OjeR?= M3m4RlAvOjVxMD61M|Eh|ryP M{ixfFI1KGh? MUnpcohq[mm2czDBb5QheGixc4Doc5J6dGG2aX;uJJNtcWeqdHz5 MVKyOFM2OTR{NR?=
H460 MVHGeY5kfGmxbjDBd5NigQ>? M3SwVlAvOjVxMD61M|Eh|ryP Mn\lNlQhcA>? M1TibYlvcGmkaYTzJGFsfCCyaH;zdIhwenmuYYTpc44he2yrZ3j0cJk> M17CRlI1OzVzNEK1
H661 MkT2SpVv[3Srb36gRZN{[Xl? Mmj5NE4zPS9yLkWvNUDPxE1? M4LaSVI1KGh? Mm\xbY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7 NIP5XnczPDN3MUSyOS=>
SAS MX7GeY5kfGmxbjDBd5NigQ>? NHXiZYExNjJ3L{CuOU8yKM7:TR?= NHqycI8zPCCq NE\MV4JqdmirYnn0d{BCc3RicHjvd5Bpd3K7bHH0bY9vKHOrZ37p[olk[W62bIm= MWOyOFM2OTR{NR?=
UT5 M3uwT2Z2dmO2aX;uJGF{e2G7 M1W1RVAvOjVxMD61M|Eh|ryP M1W0V|I1KGh? NVLsXYJTcW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|aXfubYZq[2GwdHz5 M4j5Z|I1OzVzNEK1
FaDu MX\GeY5kfGmxbjDBd5NigQ>? NGjUSGQxNjJ3L{CuOU8yKM7:TR?= M320UFI1KGh? M2nBOolvcGmkaYTzJGFsfCCyaH;zdIhwenmuYYTpc44he2mpbnnmbYNidnSueR?= NEPZU|MzPDN3MUSyOS=>
RD Mof4RZBweHSxc3nzJGF{e2G7 NInlbm0yNzFwNT:yJO69VQ>? NGnZe4U4OiCq MnrDSG1UVw>? NF\jNIdqdmS3Y3XzJINie3Cjc3Wt[IVx\W6mZX70JIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIGXPNVI3 MXGyN|Y5PDl{NR?=
TE671 NWPSdFN7SXCxcITvd4l{KEG|c3H5 NYn0[GVrOS9zLkWvNkDPxE1? NH;lO204OiCq MofDSG1UVw>? MljvbY5lfWOnczDjZZNx[XOnLXTldIVv\GWwdDDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCXT{GyOi=> MnzJNlM3QDR7MkW=
RH30  MUTBdI9xfG:|aYOgRZN{[Xl? MX:xM|EvPS9{IN88US=> NVXYS5pCPzJiaB?= M3\Rd2ROW09? NFPQbIdqdmS3Y3XzJINie3Cjc3Wt[IVx\W6mZX70JIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIGXPNVI3 NFf2clczOzZ6NEmyOS=>
RMS13 M4\XfmFxd3C2b4Ppd{BCe3OjeR?= Ml:zNU8yNjVxMjFOwG0> NWPYNWlNPzJiaB?= MYXEUXNQ NYDzbnVTcW6mdXPld{Bk[XOyYYPlMYRmeGWwZHXueEBieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDVU|EzPg>? MkjpNlM3QDR7MkW=
SUM149PT NUCwZmgzS2WubDDWbYFjcWyrdImgRZN{[Xl? MnXCNE4{KM7:TR?= MVu3NkBp NGjRd5NmdmijbnPld{BkgXSxdH;4bYMh\W[oZXP0d{Bw\iCSSUPLM2FMXCCyYYToe4F6KGmwaHnibZRwenN? MnjrNlM3ODFyN{S=
MDA-MB-468 MkLCR4VtdCCYaXHibYxqfHliQYPzZZk> NWnkUoY{OC5|IN88US=> NI\DTZQ4OiCq MWXlcohidmOnczDjfZRwfG:6aXOg[YZn\WO2czDv[kBRUTONL1HLWEBx[XSqd3H5JIlvcGmkaYTvdpM> NVXpXVBUOjN4MEGwO|Q>
MDA-MB-231 M3TTVmNmdGxiVnnhZoltcXS7IFHzd4F6 M{C5UlAvOyEQvF2= NXfndJM5PzJiaB?= NYDSS|k{\W6qYX7j[ZMh[3m2b4TvfIlkKGWoZnXjeJMhd2ZiUFmzT{9CU1RicHH0bJdigSCrbnjpZol1d3K| MlLrNlM3ODFyN{S=
SY5Y NYnZU4hHTnWwY4Tpc44hSXO|YYm= NVzSfFVmOS53L{KuOU82KM7:TR?= MoT5NlQhcA>? MkHnbY5lfWOnczDHNeKh[2WubD3jfYNt\SCjcoLld5Qh[W6mIHHwc5B1d3Orcx?= MnPWNlM{Pzh|NEG=
SKNBE(2c) M1HvPGZ2dmO2aX;uJGF{e2G7 MY[xMlUwOi53L{Wg{txO MV:yOEBp MVXpcoR2[2W|IFexxsBk\WyuLXP5Z4xmKGG{cnXzeEBidmRiYYDvdJRwe2m| NWrKd3N4OjN|N{izOFE>
RD NE\TZpJCeG:ydH;zbZMhSXO|YYm= NYfxSWMzOyEEtV2= MYSxNkBp NYjCe5BMTE2VTx?= NWLFfmVle2Wwc3n0bZpmeyCURDDj[YxteyC2bzDEU3gucW6mdXPl[EBieG:ydH;zbZM> MWqyN|MxODhyOR?=
TP5014 MlTBRZBweHSxc3nzJGF{e2G7 NF\uRm0{KML3TR?= MnXwNVIhcA>? NYjBSWdGTE2VTx?= M1LrW5NmdnOrdHn6[ZMhWkRiY3XscJMhfG9iRF;YMYlv\HWlZXSgZZBweHSxc3nz NYjTSYxuOjN|MEC4NFk>
HT1080 M3PwbmFxd3C2b4Ppd{BCe3OjeR?= MnnGN{DDvU1? MYKxNkBp MUTEUXNQ Mlfyd4Vve2m2aYrld{BTTCClZXzsd{B1dyCGT2itbY5lfWOnZDDhdI9xfG:|aYO= MVyyN|MxODhyOR?=
A549 MVXGeY5kfGmxbjDBd5NigQ>? NYfqe2d6OC1|LkOg{txO NV21TI56PzJiaB?= NIH1b|ZqdmS3Y3XzJINwdXCuZYTlJIRwf26{ZXf1cIF1cW:wIH;mJJBCU1R? M4fLNFI{OjV7NUmx
HCC827 NIPlc2FHfW6ldHnvckBCe3OjeR?= MlLxNE0{NjNizszN M1;IcFczKGh? M2rqdYlv\HWlZYOgZ49ueGyndHWg[I94dnKnZ4XsZZRqd25ib3[gdGFMXA>? MmLLNlMzPTl3OUG=
H3122 NInkRVRHfW6ldHnvckBCe3OjeR?= NFnIS2oxNTNwMzFOwG0> NVTDeVg2PzJiaB?= Ml7VbY5lfWOnczDjc41xdGW2ZTDkc5dvemWpdXzheIlwdiCxZjDwRWtV M4\DcFI{OjV7NUmx
TALL-1 MojPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7YNgKBkc7:TR?= MoW2O{Bl MXXk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> M4H6flI{ODN6Mkez
HPB-ALL M{n0Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13pWlHjiIoQvF2= NHvofGQ4KGR? NH3oTJZl\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? NFLG[|AzOzB|OEK3Ny=>
DND41 NITWUWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPnSWNiOeLCid88US=> NI\EcVI4KGR? NFvSS5pl\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? NEPxe3MzOzB|OEK3Ny=>
SUP-T1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInKVmky6oDLzszN NYPkNZpGPyCm MUfk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> NHj6UVMzOzB|OEK3Ny=>
PEER MofTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnW3NgKBkc7:TR?= NVvqfIF4PyCm Mmqx[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 NF7aRVAzOzB|OEK3Ny=>
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MOLT-4 MojTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIrzc|Yy6oDLzszN NGTOcGQ4KGR? NXrSVJlU\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 NG\qW5IzOzB|OEK3Ny=>
PF-382 NEP6Z5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHLSZgy6oDLzszN MnjXO{Bl MUHk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> NIfvS2YzOzB|OEK3Ny=>
CCRF-CEM NE\OTnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfpV4Yy6oDLzszN NGjScJA4KGR? NFPxVYll\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? NIHvRZUzOzB|OEK3Ny=>
LOUCY MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XXR|HjiIoQvF2= MkHiO{Bl NEHDWo1l\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? NHntOoQzOzB|OEK3Ny=>
MOLT-16 NVf5cnhiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\ISWNZOeLCid88US=> NV\1S4N2PyCm NUXPN3RM\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 M2D2UVI{ODN6Mkez
MM1S NVTveWw{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\sNE0zKM7:TR?= NV2wUHdkOjRiaB?= Ml;sTWM2OD1yLkWg{txO MYmyNlgzQTJ|NB?=
NCI-H929 NVrvVJNoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVqwMVIh|ryP M3HId|I1KGh? NIHHVGRKSzVyPUCuNlUh|ryP NUe5SlRtOjJ6MkmyN|Q>
KMS12-BM  NUHYR2ZHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFz2XYMxNTJizszN NXzIco1yOjRiaB?= NYLlcHk3UUN3MP-8olIh|ryP MWeyNlgzQTJ|NB?=
MDA-MB-436 M4ftTGZ2dmO2aX;uJGF{e2G7 Mo\4NUDPxE1? NXP1O3hxOjRiaB?= NV3rb4E6emWmdXPld{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWC=> MUSyNlQ5QDV7MB?=
SUM149PT MYrGeY5kfGmxbjDBd5NigQ>? M4XMSFEh|ryP NUnHN41POjRiaB?= NVrXS48{emWmdXPld{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWC=> M2XaOVIzPDh6NUmw
SUM1315MO2 NFj6PYpHfW6ldHnvckBCe3OjeR?= NXWwS4NjOSEQvF2= NYnZSYdDOjRiaB?= Mn7WdoVlfWOnczD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVB?= NWHmNHBVOjJ2OEi1PVA>
HCC1937 MUfGeY5kfGmxbjDBd5NigQ>? MkPCNUDPxE1? NFmxPJUzPCCq MlfndoVlfWOnczD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVB?= MXSyNlQ5QDV7MB?=
HCC827 M{\MUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHXfJQyOC1|IN88US=> NFPTSVM4OiCq NFn3cJZKSzVyPUCuN{DPxE1? Mlv0NlEzOjB2N{S=
PC-9  NUL5THY4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LBb|AuOyEQvF2= MofEO|IhcA>? MoDETWM2OD1yLkig{txO MkfpNlEzOjB2N{S=
LN229 M1LBTmZ2dmO2aX;uJGF{e2G7 MXyxJO69VQ>? M{TwNVQ5KGh? NXK2UHg{cW6mdXPld{BifXSxcHjh[49{d22nIH\vdo1ifGmxbh?= MnT2NlExPjJ7OUO=
U87 MnHDSpVv[3Srb36gRZN{[Xl? M4Tt[FEh|ryP M3POTFQ5KGh? NXPlU5U3cW6mdXPld{BifXSxcHjh[49{d22nIH\vdo1ifGmxbh?= MlnDNlExPjJ7OUO=
U373 Mnv6SpVv[3Srb36gRZN{[Xl? MkHmNUDPxE1? MVO0PEBp MUPpcoR2[2W|IHH1eI9xcGGpb4PvcYUh\m:{bXH0bY9v MkiwNlExPjJ7OUO=
SF767 M1rWS2Z2dmO2aX;uJGF{e2G7 NUjWSHVvOSEQvF2= M2Tpd|Q5KGh? M4m2Volv\HWlZYOgZZV1d3CqYXfvd49u\SCob4LtZZRqd25? NWGzeZpUOjFyNkK5PVM>
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518A2  MXXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MVuwMlAy6oDVMUFihKnPxE1? NUXHVlZsPzJiaB?= NVe1dXRvcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MXOyNVA1QDd6NR?=
Mel-Juso  M1zJfmZ2dmO2aX;uJGF{e2G7 M2O1S|AvODBz4pETNgKBkc7:TR?= MYOyOEBp MXfzeZBxemW|c3XzJJBpd3OyaH;yfYxifGmxbjDv[kBxcG:|cHjheIllgWxiaX7vd4l1d2xiMz3rbY5ie2ViZH;3cpN1emWjbTD0ZZJo\XS| NVfuVFBWOjFyNEi3PFU>
518A2 NHfzd3hHfW6ldHnvckBCe3OjeR?= MWewMlAxOeLCk{JihKnPxE1? MoLwNlQhcA>? MmnNd5VxeHKnc4Pld{BxcG:|cHjvdplt[XSrb36gc4YheGixc4DoZZRq\HmuIHnuc5NqfG:uIEOtb4lv[XOnIHTve45{fHKnYX2geIFz\2W2cx?= NIG1ZmEzOTB2OEe4OS=>
PC3  Mk\TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\F[FI1cA>? MVnHTVUxyqB;IEGwNEBvVQ>? MUGyNFU2OTB4MR?=
U87MG MX3GeY5kfGmxbjDBd5NigQ>? MYmwMlEuOSEQvF2= MlPmNlTjiImqwrC= NG\wUFlFVVOR NIP0UW9qdmirYnn0d{BRUTONLX3l[IlifGWmIIPp[45idGmwZx?= MWSxPVY{OzZ6Mx?=
U138MG NX\ndHJ{TnWwY4Tpc44hSXO|YYm= NWrFfG5zOC5zLUGg{txO NFy1O3ozPOLCiXlCpC=> MojYSG1UVw>? MVrpcohq[mm2czDQTVNMNW2nZHnheIVlKHOrZ37hcIlv\w>? NYrveZNkOTl4M{O2PFM>
U118MG NFOydGFHfW6ldHnvckBCe3OjeR?= MnPVNE4yNTFizszN MVKyOQKBkWkEoB?= NWm1coRlTE2VTx?= Mn\nbY5pcWKrdIOgVGk{Uy2vZXTpZZRm\CC|aXfuZYxqdmd? NE\OeoMyQTZ|M{[4Ny=>
U87MG NIXIPIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTBwMUSg{txO MYexPVU5PDJ{Nx?=
IGROV-1 NF;oNIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLjTWM2OD1yLkC2JO69VQ>? NUS2bJdCOTl3OESyNlc>
DETROIT562 NH;KfZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTBwMUOg{txO NXTNd|g5OTl3OESyNlc>
PC3  NIHxb5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYD3cIttUUN3ME2wMlExKM7:TR?= MVGxPVU5PDJ{Nx?=
SKOV-3 NHHrPYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1m1WWlEPTB;MD6xNkDPxE1? NEe3UIsyQTV6NEKyOy=>
HUVEC Mmi1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEP4UHpKSzVyPUCuNFgh|ryP M4nXZlE6PTh2MkK3
UCH-1  MXTGeY5kfGmxbjDBd5NigQ>? NIq2fJcxNTVizszN M3jrSolvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiYn;0bEBCU1RiYX7kJI1VV1JiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NYD2cYVZOTl3Mki0OFE>
UCH-1  NISwfnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\mXZhHOC5yMT2xNEDPxE1? MXK2JIQ> M4HSb4lvcGmkaYTzJJBzd2yrZnXyZZRqd25iZH;z[UBl\XCnbnTlcpRtgQ>? MlfuNVk2Ojh2NEG=
UCH-1  NEm2cFFCeG:ydH;zbZMhSXO|YYm= NFTqOWExNjFvMUCg{txO NF\PfXYzPCCq MkjCSG1UVw>? NVTCNXZzcW6mdXPld{BieG:ydH;zbZM> MX2xPVUzQDR2MR?=

... 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