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 NWrGeI97T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVj1SVQxOC16IN88US=> MmXINlQwPDhxN{KgbC=> NUfSZZl3cW6mdXPld{B1cW2nLTDhcoQh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgbY5pcWKrdHnvckBwdiCQQjDj[YxtKGe{b4f0bC=> MXiyOlIzPDZ6MR?=
SH-SY5Y Mon5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLqNE05KM7:TR?= NYLHSpZ7OjRxNEivO|IhcA>? M4n5OYlv\HWlZYOgeIlu\S1iYX7kJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IHnubIljcXSrb36gc44hVkJiY3XscEBoem:5dHi= NWfjN3VLOjZ{MkS2PFE>
SH-SY5Y  NYrtNI9VSXCxcITvd4l{KEG|c3H5 NVy4doJvOSEQvF2= Mn\SNE42NTJ2IHi= NXHaeGxZe2Wwc3n0bZpmeyCwZYXyc4Jt[XO2b33hJINmdGy|IITvJIRwgG:{dXLpZ4lvNWmwZIXj[YQh[XCxcITvd4l{ NVfy[HExOjZ{MkS2PFE>
G 35 SC M4PiZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkKzNE4xPS1{MDFOwG0> NIjYS5MzPC95MjDo NUHKOo1JTE2VTx?= MYLpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueIx6 MV:yOlEzOTJ3MR?=
G 38 SC M2XH[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnXNE4xPS1{MDFOwG0> M4PYOlI1Nzd{IHi= NEXPNZRFVVOR MXTpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueIx6 MVeyOlEzOTJ3MR?=
G 40 SC NYTNdWdGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NET5SW0xNjB3LUKwJO69VQ>? MlzKNlQwPzJiaB?= MoqwSG1UVw>? M1nOTYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? M1radlI3OTJzMkWx
G 35 DC MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4K3TVAvODVvMkCg{txO NXLPe2xJOjRxN{KgbC=> NWDLeXd[TE2VTx?= NIjtTmRqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 M4DyZVI3OTJzMkWx
G 38 DC NH:ydJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfTd5FmOC5yNT2yNEDPxE1? NVXhTZlrOjRxN{KgbC=> NF3ZXINFVVOR NYLqTFZQcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= MnvRNlYyOjF{NUG=
G 40 DC MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3sNE4xPS1{MDFOwG0> NHX4SpIzPC95MjDo MnrsSG1UVw>? MmXtbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBidmRidHnt[UBl\XCnbnTlcpRtgQ>? MX[yOlEzOTJ3MR?=
RD NYD6O5luSXCxcITvd4l{KEG|c3H5 NH7KNHMyNzFwNT:yJO69VQ>? NEmy[Fg4OiCq MVHpcoR2[2W|IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKEeDTmS2NS=> NHK4WokzPTd2OUO3PC=>
TE381.T MYDBdI9xfG:|aYOgRZN{[Xl? MVexM|EvPS9{IN88US=> Mn64O|IhcA>? NGrZdoFqdmS3Y3XzJIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIFfBUnQ3OQ>? MnPmNlU4PDl|N{i=
RMS13 MYrBdI9xfG:|aYOgRZN{[Xl? MnjVNU8yNjVxMjFOwG0> M4W4WVczKGh? Mny5bY5lfWOnczDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCJQV7UOlE> NUmxVIZzOjV5NEmzO|g>
RH30  NHjDOI9CeG:ydH;zbZMhSXO|YYm= MXGxM|EvPS9{IN88US=> M3T5e|czKGh? NYfFN4F2cW6mdXPld{BieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDHRW5VPjF? NX7zOnhrOjV5NEmzO|g>
VJ NWHTTphGSXCxcITvd4l{KEG|c3H5 MUCxM|EvPS9{IN88US=> MljUO|IhcA>? MnrhbY5lfWOnczDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCJQV7UOlE> MoXyNlU4PDl|N{i=
HS578T Mm\1R4VtdCCYaXHibYxqfHliQYPzZZk> NFT3OpMxNTNizszN NVfuRYdSPzJiaB?= Mnq1bY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MWWyOVczOTRzOR?=
BT549 MlnwR4VtdCCYaXHibYxqfHliQYPzZZk> M1y0WlAuOyEQvF2= NFezR5E4OiCq M2L3eYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? M3n4dVI2PzJzNEG5
MDA-MB-231 MlnUR4VtdCCYaXHibYxqfHliQYPzZZk> NXjwdFRZOC1|IN88US=> Mm\oO|IhcA>? NX;LUo5mcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NUfpTGZiOjV5MkG0NVk>
MDA-MB-468 MkTnR4VtdCCYaXHibYxqfHliQYPzZZk> NGfJcmMxNTNizszN MWO3NkBp M3LyXYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? M2DiUFI2PzJzNEG5
MDA-MB-436 MX7D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MmP3NE0{KM7:TR?= MVy3NkBp NYnLWoVTcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NVrLVZJmOjV5MkG0NVk>
SUM149PT NGm4Z4xE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MlTmNE0{KM7:TR?= MkX2O|IhcA>? NIfGT4tqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NVL0PFdtOjV5MkG0NVk>
MDA-MB-468 M3rOS2Z2dmO2aX;uJGF{e2G7 NYjVXolOOC5yMT2xNEDPxE1? NVzkVpQ4OjRiaB?= NIrGPJhld3ewcnXneYxifGW|IITo[UBt\X[nbIOgc4Yh|rJvVILDVFEtKGNvTYnjJIFv\CCleXPsbY4hTSCycn;0[Ylve8Li M2\NN|I2PzJzNEG5
MDA-MB-231 M13KT2Z2dmO2aX;uJGF{e2G7 MlfPNE4xOS1zMDFOwG0> Mkf6NlQhcA>? M2DNTYRwf26{ZXf1cIF1\XNidHjlJIxmfmWuczDv[kDPui2WclPQNUwh[y2PeXOgZY5lKGO7Y3zpckBGKHC{b4TlbY5{yqB? MXuyOVczOTRzOR?=
HS578T Ml3nSpVv[3Srb36gRZN{[Xl? MWKwMlAyNTFyIN88US=> NETwUIgzPCCq NHWyc4Vld3ewcnXneYxifGW|IITo[UBt\X[nbIOgc4Yh|rJvVILDVFEtKGNvTYnjJIFv\CCleXPsbY4hTSCycn;0[Ylve8Li NX7NWVg5OjV5MkG0NVk>
SW872 NWHwVFFPTnWwY4Tpc44hSXO|YYm= NG\RelExNjBzLUCuOUDPxE1? NG[2NYszPCCq NEnVWVlz\WS3Y3XzJGFMXCCyaH;zdIhwenmuYYTpc44hMHCDS2SpJIFv\CB2RVLQNUBxcG:|cHjvdplt[XSrb36gLJA1TUKSMTmgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYNCpC=> MUmyOFY6PTZ|Mh?=
SW982 NIHte41HfW6ldHnvckBCe3OjeR?= MnPSNE4xOS1yLkWg{txO MoDaNlQhcA>? NHfvOJFz\WS3Y3XzJGFMXCCyaH;zdIhwenmuYYTpc44hMHCDS2SpJIFv\CB2RVLQNUBxcG:|cHjvdplt[XSrb36gLJA1TUKSMTmgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYNCpC=> MYmyOFY6PTZ|Mh?=
SW872 NWLF[5N7SXCxcITvd4l{KEG|c3H5 NIDFV2wxNjBzLUCuOUDPxE1? MnrIOFghcA>? MUnpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NGC1UY8zPDZ7NU[zNi=>
SW982 NUn6d3RmSXCxcITvd4l{KEG|c3H5 Mo\5NE4xOS1yLkWg{txO M3vBTlQ5KGh? MlvLbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MYOyOFY6PTZ|Mh?=
AGS HG NWjKVZNJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPWTWM2OD1yLk[4JOKyKDBwMEOxJO69VQ>? M3;sW|I1PTl5NEe4
AGS LG MnnUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nGNWlEPTB;MD6wOUDDuSByLkCwNUDPxE1? NWC3e4VqOjR3OUe0O|g>
HGC27 HG NGWyTGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnVXIdRUUN3ME2wMlM5KMLzIECuNFIzKM7:TR?= MV6yOFU6PzR5OB?=
HGC27 LG MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\5TWM2OD1yLkCyJOKyKDBwMEC0JO69VQ>? M4XLXlI1PTl5NEe4
MKN45 HG M2K5Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTFwMEGgxtEhOC5yNUGg{txO NXX3WphmOjR3OUe0O|g>
MKN45 LG MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vDXGlEPTB;MD64O{DDuSByLkCzNEDPxE1? MlXTNlQ2QTd2N{i=
NUGC4 HG M3n6eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTCTWM2OD1zND6wJOKyKDNwOUGzJO69VQ>? M2rsblI1PTl5NEe4
NUGC4 LG NUnRPVVDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmq3TWM2OD1zND6wJOKyKDVwM{KxJO69VQ>? NVfndGE{OjR3OUe0O|g>
A549 M2DPe2Z2dmO2aX;uJGF{e2G7 NYL1UZJ[OC5{NT:wMlUwOSEQvF2= MkO2NlQhcA>? MojEbY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{dGmpaITsfS=> NFLNfZAzPDN3MUSyOS=>
H460 MX3GeY5kfGmxbjDBd5NigQ>? NV3BZ4Z4OC5{NT:wMlUwOSEQvF2= Ml36NlQhcA>? NFvkXoJqdmirYnn0d{BCc3RicHjvd5Bpd3K7bHH0bY9vKHOuaXfoeIx6 NVzDfJFuOjR|NUG0NlU>
H661 MWDGeY5kfGmxbjDBd5NigQ>? MXOwMlI2NzBwNT:xJO69VQ>? NVHyTWhbOjRiaB?= NEfzR25qdmirYnn0d{BCc3RicHjvd5Bpd3K7bHH0bY9vKHOrZ37p[olk[W62bIm= M1zxdlI1OzVzNEK1
SAS M4jCe2Z2dmO2aX;uJGF{e2G7 MWWwMlI2NzBwNT:xJO69VQ>? MnPONlQhcA>? M1OyfYlvcGmkaYTzJGFsfCCyaH;zdIhwenmuYYTpc44he2mpbnnmbYNidnSueR?= Ml\JNlQ{PTF2MkW=
UT5 NX7zUG9ITnWwY4Tpc44hSXO|YYm= M{PsUlAvOjVxMD61M|Eh|ryP NULzXYN4OjRiaB?= MlLVbY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7 MmTPNlQ{PTF2MkW=
FaDu MW\GeY5kfGmxbjDBd5NigQ>? NU\RW5dlOC5{NT:wMlUwOSEQvF2= NUHzUVlZOjRiaB?= M2TOSolvcGmkaYTzJGFsfCCyaH;zdIhwenmuYYTpc44he2mpbnnmbYNidnSueR?= NEHu[HYzPDN3MUSyOS=>
RD MVPBdI9xfG:|aYOgRZN{[Xl? NUnUPXlVOS9zLkWvNkDPxE1? Ml63O|IhcA>? M4LWOGROW09? NXW1fGVDcW6mdXPld{Bk[XOyYYPlMYRmeGWwZHXueEBieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDVU|EzPg>? M{POOVI{Pjh2OUK1
TE671 MVzBdI9xfG:|aYOgRZN{[Xl? NGrET3IyNzFwNT:yJO69VQ>? MoTDO|IhcA>? M{LCdmROW09? MVLpcoR2[2W|IHPhd5Bie2VvZHXw[Y5l\W62IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKFWRMUK2 MX6yN|Y5PDl{NR?=
RH30  MYjBdI9xfG:|aYOgRZN{[Xl? MYSxM|EvPS9{IN88US=> MXO3NkBp M4PNNmROW09? MVPpcoR2[2W|IHPhd5Bie2VvZHXw[Y5l\W62IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKFWRMUK2 MkXMNlM3QDR7MkW=
RMS13 MkD1RZBweHSxc3nzJGF{e2G7 NHPHd5MyNzFwNT:yJO69VQ>? MoW1O|IhcA>? MWHEUXNQ NHO0OppqdmS3Y3XzJINie3Cjc3Wt[IVx\W6mZX70JIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIGXPNVI3 NWrwdYNPOjN4OES5NlU>
SUM149PT NV3RPIZGS2WubDDWbYFjcWyrdImgRZN{[Xl? M{jYN|AvOyEQvF2= MWG3NkBp M{n5d4VvcGGwY3XzJIN6fG:2b4jpZ{Bm\m[nY4TzJI9nKFCLM1uvRWtVKHCjdHj3ZZkhcW6qaXLpeI9zew>? NXnLcXNDOjN4MEGwO|Q>
MDA-MB-468 NXzxN2htS2WubDDWbYFjcWyrdImgRZN{[Xl? M1zuRlAvOyEQvF2= MmTUO|IhcA>? MXLlcohidmOnczDjfZRwfG:6aXOg[YZn\WO2czDv[kBRUTONL1HLWEBx[XSqd3H5JIlvcGmkaYTvdpM> NVTIeI5sOjN4MEGwO|Q>
MDA-MB-231 NX;Eeo9{S2WubDDWbYFjcWyrdImgRZN{[Xl? NFHLbGUxNjNizszN NF[1[3I4OiCq NUTve4Jp\W6qYX7j[ZMh[3m2b4TvfIlkKGWoZnXjeJMhd2ZiUFmzT{9CU1RicHH0bJdigSCrbnjpZol1d3K| MmW4NlM3ODFyN{S=
SY5Y NUHEOJNyTnWwY4Tpc44hSXO|YYm= NHHjNoEyNjVxMj61M|Uh|ryP MXKyOEBp NWPVU4RocW6mdXPld{BIOcLiY3XscE1kgWOuZTDhdpJme3RiYX7kJIFxd3C2b4Ppdy=> MlL5NlM{Pzh|NEG=
SKNBE(2c) M3XaOmZ2dmO2aX;uJGF{e2G7 MUGxMlUwOi53L{Wg{txO NUnreG9qOjRiaB?= NEW0Nm9qdmS3Y3XzJGcyyqClZXzsMYN6[2ynIHHydoV{fCCjbnSgZZBweHSxc3nz MWWyN|M4QDN2MR?=
RD MVXBdI9xfG:|aYOgRZN{[Xl? MmPiN{DDvU1? NXnRXFE3OTJiaB?= NFy3dpVFVVOR M3PVepNmdnOrdHn6[ZMhWkRiY3XscJMhfG9iRF;YMYlv\HWlZXSgZZBweHSxc3nz NIqwR2IzOzNyMEiwPS=>
TP5014 MoLSRZBweHSxc3nzJGF{e2G7 Ml21N{DDvU1? MVyxNkBp M3rX[mROW09? MnfUd4Vve2m2aYrld{BTTCClZXzsd{B1dyCGT2itbY5lfWOnZDDhdI9xfG:|aYO= M2XCbVI{OzByOEC5
HT1080 M3HtS2Fxd3C2b4Ppd{BCe3OjeR?= MnLtN{DDvU1? MWKxNkBp NUXUTphwTE2VTx?= MUnz[Y5{cXSrenXzJHJFKGOnbHzzJJRwKESRWD3pcoR2[2WmIHHwc5B1d3Orcx?= NEHqOoczOzNyMEiwPS=>
A549 MWfGeY5kfGmxbjDBd5NigQ>? MlLPNE0{NjNizszN M363NVczKGh? MYHpcoR2[2W|IHPvcZBt\XSnIHTve45z\We3bHH0bY9vKG:oIIDBT3Q> MUWyN|I2QTV7MR?=
HCC827 MXzGeY5kfGmxbjDBd5NigQ>? MUewMVMvOyEQvF2= M2rDTlczKGh? NFqwOo1qdmS3Y3XzJINwdXCuZYTlJIRwf26{ZXf1cIF1cW:wIH;mJJBCU1R? M4i5eVI{OjV7NUmx
H3122 MnTiSpVv[3Srb36gRZN{[Xl? MoHRNE0{NjNizszN Mke2O|IhcA>? MYrpcoR2[2W|IHPvcZBt\XSnIHTve45z\We3bHH0bY9vKG:oIIDBT3Q> NELuZY8zOzJ3OUW5NS=>
TALL-1 M3\mcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nBS|HjiIoQvF2= NXvuTldFPyCm MnPD[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 M1jne|I{ODN6Mkez
HPB-ALL MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX2x5qCK|ryP NITsXW04KGR? NFPxW|Vl\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? M3\FNVI{ODN6Mkez
DND41 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLv[mZYOeLCid88US=> NGfhTWM4KGR? M2OzfoRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? NH32dG0zOzB|OEK3Ny=>
SUP-T1 NUXkdoNXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;od5Iy6oDLzszN NFzxRo04KGR? MoPI[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 NWi0eW52OjNyM{iyO|M>
PEER NGHvPGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\oNgKBkc7:TR?= MVS3JIQ> NYnGeGZF\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 M2XLd|I{ODN6Mkez
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CCRF-CEM NV;yT5BXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;CPYZMOeLCid88US=> NIHFfIw4KGR? NF7NOFBl\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? NHrwNI8zOzB|OEK3Ny=>
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MM1S MkLnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmL1NE0zKM7:TR?= MUWyOEBp NFricFNKSzVyPUCuOUDPxE1? M3:2VVIzQDJ7MkO0
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HCC827 MkDES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{[4dlAuOyEQvF2= M3y4WVczKGh? NH;MO5VKSzVyPUCuN{DPxE1? NEjwVnczOTJ{MES3OC=>
PC-9  M2nXcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXWZ5oxNTNizszN M1jYSVczKGh? MorLTWM2OD1yLkig{txO MYWyNVIzODR5NB?=
LN229 MV;GeY5kfGmxbjDBd5NigQ>? MWixJO69VQ>? NYH2b3dQPDhiaB?= Ml;xbY5lfWOnczDheZRweGijZ3;zc41mKG[xcn3heIlwdg>? MWiyNVA3Ojl7Mx?=
U87 M2rGfmZ2dmO2aX;uJGF{e2G7 NVfGWXBPOSEQvF2= MXK0PEBp M1zJPIlv\HWlZYOgZZV1d3CqYXfvd49u\SCob4LtZZRqd25? NUSxcG5qOjFyNkK5PVM>
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518A2  NFX4cHpE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M1nCOVAvODIkgKOxNQKBkc7:TR?= MofCO|IhcA>? NIO4VIJqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 M3;IZVIyODR6N{i1
Mel-Juso  M2fjZmZ2dmO2aX;uJGF{e2G7 NHnMR2gxNjByMfMAl|HjiIoQvF2= MYmyOEBp NUHyT5F{e3WycILld5NmeyCyaH;zdIhwenmuYYTpc44hd2ZicHjvd5Bp[XSrZInsJIlvd3OrdH;sJFMuc2mwYYPlJIRwf26|dILlZY0hfGG{Z3X0dy=> NX7OdGFMOjFyNEi3PFU>
518A2 NEe3RoxHfW6ldHnvckBCe3OjeR?= NGjIc3QxNjByMfMAl|HjiIoQvF2= MX2yOEBp MnTSd5VxeHKnc4Pld{BxcG:|cHjvdplt[XSrb36gc4YheGixc4DoZZRq\HmuIHnuc5NqfG:uIEOtb4lv[XOnIHTve45{fHKnYX2geIFz\2W2cx?= MUeyNVA1QDd6NR?=
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U118MG MmHCSpVv[3Srb36gRZN{[Xl? M3mxSlAvOS1zIN88US=> MoXENlTjiImqwrC= Mo[4SG1UVw>? MUDpcohq[mm2czDQTVNMNW2nZHnheIVlKHOrZ37hcIlv\w>? MkDTNVk3OzN4OEO=
U87MG MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDaTWM2OD1yLkG0JO69VQ>? NXnkVFB6OTl3OESyNlc>
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PC3  NUHUV2hkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTBwMUCg{txO MWOxPVU5PDJ{Nx?=
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HUVEC MkXIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PFXGlEPTB;MD6wPEDPxE1? MUSxPVU5PDJ{Nx?=
UCH-1  NF[0T3JHfW6ldHnvckBCe3OjeR?= NFHJfmMxNTVizszN MXLpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKGKxdHigRWtVKGGwZDDtWG9TKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz Ml23NVk2Ojh2NEG=
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UCH-1  MXHBdI9xfG:|aYOgRZN{[Xl? MoC3NE4yNTFyIN88US=> NVz4d5VEOjRiaB?= MnvJSG1UVw>? NHz6cXpqdmS3Y3XzJIFxd3C2b4Ppdy=> NXLUb5FyOTl3Mki0OFE>

... 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:
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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID