PI-103

For research use only.

Catalog No.S1038

81 publications

PI-103 Chemical Structure

CAS No. 371935-74-9

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. PI-103 induces apoptosis in murine T-cell Lymphoma.

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Selleck's PI-103 has been cited by 81 publications

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. PI-103 induces apoptosis in murine T-cell Lymphoma.
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
UCH-1  NGjic|NCeG:ydH;zbZMhSXO|YYm= M{nKTlAvOS1zMDFOwG0> MXuyOEBp NYLVVGVFTE2VTx?= M3PhXIlv\HWlZYOgZZBweHSxc3nz Mm\KQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl3Mki0OFEoRjF7NUK4OFQyRC:jPh?=
UCH-1  M{\LXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGL5bGQxNjBzLUGwJO69VQ>? MlXZOkBl NFnXTVhqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHTvd4Uh\GWyZX7k[Y51dHl? NFHBTWo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUWyPFQ1OSd-MUm1Nlg1PDF:L3G+
UCH-1  MmXQSpVv[3Srb36gRZN{[Xl? NXPPT21EOC13IN88US=> NG[5OVJqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIHLveIghSUuWIHHu[EBuXE:UIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTV{OES0NUc,OTl3Mki0OFE9N2F-
HUVEC M3Lkfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPSWGIzUUN3ME2wMlA5KM7:TR?= NG\JN5o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUW4OFIzPyd-MUm1PFQzOjd:L3G+
SKOV-3 NF;Z[ItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTBwMUKg{txO MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTV6NEKyO{c,OTl3OESyNlc9N2F-
PC3  M2f3eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDlNnRKSzVyPUCuNVAh|ryP NIHnUXg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUW4OFIzPyd-MUm1PFQzOjd:L3G+
DETROIT562 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLvU2NbUUN3ME2wMlE{KM7:TR?= Mn\mQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl3OESyNlcoRjF7NUi0NlI4RC:jPh?=
IGROV-1 M3i2cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTBwME[g{txO MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTV6NEKyO{c,OTl3OESyNlc9N2F-
U87MG MlHvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjpPIJtUUN3ME2wMlE1KM7:TR?= MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTV6NEKyO{c,OTl3OESyNlc9N2F-
U118MG M320bGZ2dmO2aX;uJGF{e2G7 M{LwUFAvOS1zIN88US=> NIPHVokzPOLCiXlCpC=> MnjySG1UVw>? NVmySWM3cW6qaXLpeJMhWEl|Sz3t[YRq[XSnZDDzbYdv[Wyrbne= MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTZ|M{[4N{c,OTl4M{O2PFM9N2F-
U138MG MnrLSpVv[3Srb36gRZN{[Xl? Ml74NE4yNTFizszN M3jKXFI16oDLaNMg NVjy[Hl4TE2VTx?= M{D2NYlvcGmkaYTzJHBKO0tvbXXkbYF1\WRic3nncoFtcW6p NHXJOmg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOU[zN|Y5Oyd-MUm2N|M3QDN:L3G+
U87MG M4HVOGZ2dmO2aX;uJGF{e2G7 NVL0R4M1OC5zLUGg{txO M{W5clI16oDLaNMg NF3PSGlFVVOR NHSyb5JqdmirYnn0d{BRUTONLX3l[IlifGWmIIPp[45idGmwZx?= MmLDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl4M{O2PFMoRjF7NkOzOlg{RC:jPh?=
PC3  M4XMSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWeyOIg> NETlcXZIUTVywrC9JFExOCCwTR?= NHzIeVg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEW1NVA3OSd-MkC1OVExPjF:L3G+
518A2 NUPxcZVKTnWwY4Tpc44hSXO|YYm= MmDjNE4xODIkgKOx5qCK|ryP M4XGTlI1KGh? M1Hve5N2eHC{ZYPz[ZMheGixc4Doc5J6dGG2aX;uJI9nKHCqb4PwbIF1cWS7bDDpco9{cXSxbDCzMYtqdmG|ZTDkc5dve3S{ZXHtJJRiemendIO= NHnhb209[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUC0PFc5PSd-MkGwOFg4QDV:L3G+
Mel-Juso  NFfLVpBHfW6ldHnvckBCe3OjeR?= MUSwMlAxOeLCk{JihKnPxE1? M1zSVVI1KGh? NFnaXm1{fXCycnXzd4V{KHCqb4PwbI9zgWyjdHnvckBw\iCyaH;zdIhifGmmeXygbY5we2m2b3ygN{1scW6jc3Wg[I94dnO2cnXhcUB1[XKpZYTz MorFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjFyNEi3PFUoRjJzMES4O|g2RC:jPh?=
518A2  M2\hU2NmdGxiVnnhZoltcXS7IFHzd4F6 NY\zTm5pOC5yMfMAl|Ex6oDLzszN NWH2fIJLPzJiaB?= M1fSc4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MkC2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjFyNEi3PFUoRjJzMES4O|g2RC:jPh?=
Mel-Juso MVzD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MmHONE4xOeLCk{Gw5qCK|ryP NGXsNIE4OiCq NInP[VhqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NVKy[4RzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGwOFg4QDVpPkKxNFQ5Pzh3PD;hQi=>
SF767 NEDaOJVHfW6ldHnvckBCe3OjeR?= NY\JOG5KOSEQvF2= NWjPW3VWPDhiaB?= NFf5OVZqdmS3Y3XzJIF2fG:yaHHnc5NwdWViZn;ycYF1cW:w NUPUPIVDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGwOlI6QTNpPkKxNFYzQTl|PD;hQi=>
U373 M3PPbWZ2dmO2aX;uJGF{e2G7 MUCxJO69VQ>? M2rFZlQ5KGh? NGDFfFZqdmS3Y3XzJIF2fG:yaHHnc5NwdWViZn;ycYF1cW:w MmK0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjFyNkK5PVMoRjJzME[yPVk{RC:jPh?=
U87 MnHpSpVv[3Srb36gRZN{[Xl? NGXEXGMyKM7:TR?= MYm0PEBp NWjKS4ZUcW6mdXPld{BifXSxcHjh[49{d22nIH\vdo1ifGmxbh?= NFrUbYE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUC2Nlk6Oyd-MkGwOlI6QTN:L3G+
LN229 NEnCdVZHfW6ldHnvckBCe3OjeR?= M2\Ve|Eh|ryP NUnXeVQyPDhiaB?= M4HXdIlv\HWlZYOgZZV1d3CqYXfvd49u\SCob4LtZZRqd25? MmmwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjFyNkK5PVMoRjJzME[yPVk{RC:jPh?=
PC-9  M1HFbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4D6VFAuOyEQvF2= Mkf5O|IhcA>? M13QWGlEPTB;MD64JO69VQ>? NH:1NW09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUKyNFQ4PCd-MkGyNlA1PzR:L3G+
HCC827 M3;XUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjnUXE3OC1|IN88US=> Mn7SO|IhcA>? MXzJR|UxRTBwMzFOwG0> NYDCZllWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGyNlA1PzRpPkKxNlIxPDd2PD;hQi=>
HCC1937 NX\mbXd2TnWwY4Tpc44hSXO|YYm= NF;XOZoyKM7:TR?= M1vieFI1KGh? NXXqPWtEemWmdXPld{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWC=> M4PrTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NEi4OVkxLz5{MkS4PFU6ODxxYU6=
SUM1315MO2 MXXGeY5kfGmxbjDBd5NigQ>? MkL2NUDPxE1? M3TXSFI1KGh? NF7yeXVz\WS3Y3XzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvU NX\KfVFRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK0PFg2QTBpPkKyOFg5PTlyPD;hQi=>
SUM149PT Mmm1SpVv[3Srb36gRZN{[Xl? NHvOfWUyKM7:TR?= M1zhOlI1KGh? NF7vdllz\WS3Y3XzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvU NI\xfok9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkS4PFU6OCd-MkK0PFg2QTB:L3G+
MDA-MB-436 MnrXSpVv[3Srb36gRZN{[Xl? NWPCfnNZOSEQvF2= M4G5WFI1KGh? MYfy[YR2[2W|IITo[UBxcG:|cHjvdplt[XSrb36gc4YhSUuW M{jLbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NEi4OVkxLz5{MkS4PFU6ODxxYU6=
KMS12-BM  MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV[1W5JTOC1{IN88US=> NWTXRmFrOjRiaB?= M1zHRWlEPTExvK6yJO69VQ>? NGjFSJQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkiyPVI{PCd-MkK4NlkzOzR:L3G+
NCI-H929 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUGwMVIh|ryP NXPmd4ViOjRiaB?= NWjERVFKUUN3ME2wMlI2KM7:TR?= MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjh{OUKzOEc,OjJ6MkmyN|Q9N2F-
MM1S MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2SxOVAuOiEQvF2= M1jacFI1KGh? MXTJR|UxRTBwNTFOwG0> Mn3RQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ6MkmyN|QoRjJ{OEK5NlM1RC:jPh?=
MOLT-16 M1nI[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUGx5qCK|ryP MYq3JIQ> NVTIcYxI\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 NIPkNJA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{CzPFI4Oyd-MkOwN|gzPzN:L3G+
LOUCY MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYix5qCK|ryP NYPC[WtrPyCm MVfk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzB|OEK3N{c,OjNyM{iyO|M9N2F-
CCRF-CEM NETkWXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV6x5qCK|ryP MWO3JIQ> NXu2bVZ6\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 NUX2Um5sRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOwN|gzPzNpPkKzNFM5Ojd|PD;hQi=>
PF-382 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX:x5qCK|ryP M4DJUVch\A>? MU\k[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> NFToZYk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{CzPFI4Oyd-MkOwN|gzPzN:L3G+
MOLT-4 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFztcnEy6oDLzszN MYO3JIQ> M4CySIRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? NEmzbo09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{CzPFI4Oyd-MkOwN|gzPzN:L3G+
Jurkat MmPOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYOx5qCK|ryP NYG2UVdiPyCm NV\TT5B4\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzB|OEK3N{c,OjNyM{iyO|M9N2F-
RPMI-8402 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITFPXUy6oDLzszN NYfmOWNtPyCm MWLk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> M3LHZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MEO4Nlc{Lz5{M{CzPFI4OzxxYU6=
Karpas-45 M3fTXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfONgKBkc7:TR?= MV63JIQ> M1zoSYRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? M3v6[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MEO4Nlc{Lz5{M{CzPFI4OzxxYU6=
KE37 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXOx5qCK|ryP NH7YZVA4KGR? M3nIWYRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? NV7OcWpYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOwN|gzPzNpPkKzNFM5Ojd|PD;hQi=>
ALL-SIL NFLRNIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPrNgKBkc7:TR?= NHTUSYM4KGR? M4HaUYRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? NXfycGFQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOwN|gzPzNpPkKzNFM5Ojd|PD;hQi=>
PEER M{DuZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX[0[5VCOeLCid88US=> MWK3JIQ> NV3ENmFZ\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzB|OEK3N{c,OjNyM{iyO|M9N2F-
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SJ-GBM2 MVTxTHRUKGG|c3H5 NXjLeo1LeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhW0pvR1LNNkBk\Wyucx?= MmezQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
BT-37 NVrkT4lSeUiWUzDhd5NigQ>? MULxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDCWE0{PyClZXzsdy=> NHn5eGY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
TC32 MmK3dWhVWyCjc4PhfS=> NY\r[oNQeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhXEN|MjDj[Yxtew>? NUGxNGQ5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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Rh18 NXG5Wmh2eUiWUzDhd5NigQ>? NHzu[HZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBTcDF6IHPlcIx{ NX7GdHk{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Saos-2 M4j4VZFJXFNiYYPzZZk> M2\nW5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHNid3NvMjDj[Yxtew>? NYjTUYV[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
OHS-50 NH3QfZJyUFSVIHHzd4F6 NHOzS|NyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBQUFNvNUCgZ4VtdHN? MmTQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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Caco2 NX3sN2gxS2WubDDjfYNt\SCjc4PhfS=> NIPEbFdE\WyuIHP5Z4xmKGG{cnXzeEBqdiCqdX3hckBE[WOxMjDj[YxteyCjc4Pld5Nm\CCjczDhZ4N2dXWuYYTpc44h[XRiR{GvV{BxcGG|ZTDifUBJd2WlaIP0JJN1[WmwaX7nJIJie2WmIH\seY9z\XOlZX7j[UBie3OjeR?= MmrYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{MUSyN|EoRjJ6MkG0NlMyRC:jPh?=
HCT116 M4[z[WNmdGxiY4njcIUh[XO|YYm= MoHJR4VtdCCleXPs[UBienKnc4SgbY4hcHWvYX6gTGNVOTF4IHPlcIx{KGG|c3Xzd4VlKGG|IHHjZ5VufWyjdHnvckBifCCJMj;NJJBp[XOnIHL5JGhw\WOqc4Sgd5RicW6rbnegZoF{\WRiZnz1c5Jme2OnbnPlJIF{e2G7 Mmq4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{MUSyN|EoRjJ6MkG0NlMyRC:jPh?=
PC3 M1:1VWNmdGxiY4njcIUh[XO|YYm= NYrTXVZUS2WubDDjfYNt\SCjcoLld5QhcW5iaIXtZY4hWEN|IHPlcIx{KGG|c3Xzd4VlKGG|IHHjZ5VufWyjdHnvckBifCCJMT;TJJBp[XOnIHL5JGhw\WOqc4Sgd5RicW6rbnegZoF{\WRiZnz1c5Jme2OnbnPlJIF{e2G7 NVfMSoprRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyNVQzOzFpPkK4NlE1OjNzPD;hQi=>
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... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-AKT / AKT / p-S6K / S6K / p-S6 / S6 / p-p38 / p38; 

PubMed: 18922908     


Immunodetection of the levels of P-Akt, Akt, P-S6K, S6K, P-S6, S6, P-p38 or p38 of EC-vGPCR cells treated with increasing doses of PI-103 or DMSO (control) for 6 hours.

p-GSK3 / GSK3 / p-BAD / BAD / p-MDM2 / MDM2 / p-p27 / p27 ; 

PubMed: 18922908     


Immunodetection of the levels of P-Akt, Akt, P-GSK3, GSK3, P-BAD BAD, P-Mdm2, Mdm2, P-p27 or p27 of EC-vGPCR cells treated with increasing doses of PI-103 or DMSO (control) for 6 hours.

β-TrCP1 / p-mTOR; 

PubMed: 25721419     


PI-103 reduced the level of β-TrCP1 protein in TNBC cells. Cells were treated with 3 μm of PI-103 for 24 h and subjected to western blot analysis with indicated antibodies. HSP90 or β-actin was used as a loading control.

18922908 25721419
Immunofluorescence
autophagosomes / autolysosomes; 

PubMed: 26814436     


mRFP-GFP-LC3 stably expressing HeLa cells were treated with vehicle, PI (1uM), Baf (100nM) or PI (1uM)+Baf (100nM) for 20 hours. Cells were then fixed and confocal images were acquired. The numbers of autophagosomes (green vesicles) and autolysosomes (red vesicles minus green vesicles) were assessed with automated Cellomics microscopy (n = 12). Data are shown as mean ±sd. ***: P < 0.001. Scale bar: 20um.

26814436
Growth inhibition assay
Cell viability; 

PubMed: 25721419     


PI-103 reduced the viable TNBC cells in a dose-dependent manner. Cells were treated with increasing amounts of PI-103 up to 72 h and the viable cells were measured by MTT assay. Data from two independent experiments performed in triplicate are shown as mean±s.e.m.

25721419
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]
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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:[2]
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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:[2]
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  • Animal Models: 6- to 12-week-old Balbc nu/nu mice bearing U87MG:ΔEGFR cells
  • 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(Data is from Selleck tests instead of citations):
5%DMSO+40%PEG300+5%Tween80+50%ddH2O
For best results, use promptly after mixing.
1 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
Smiles C1COCCN1C2=NC(=NC3=C2OC4=C3C=CC=N4)C5=CC(=CC=C5)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

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 (mg) = Concentration (mM) × Volume (mL) × 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 SDS / 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 SDS / 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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