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.

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  MkPFRZBweHSxc3nzJGF{e2G7 NGT2dmoxNjFvMUCg{txO NYXhW2JwOjRiaB?= NYHkXXdwTE2VTx?= MVrpcoR2[2W|IHHwc5B1d3Orcx?= NUnRb4xjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm1Nlg1PDFpPkG5OVI5PDRzPD;hQi=>
UCH-1  NYHRUY1KT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXOwMlAyNTFyIN88US=> M2LkUlYh\A>? M1rGVIlvcGmkaYTzJJBzd2yrZnXyZZRqd25iZH;z[UBl\XCnbnTlcpRtgQ>? M1PiRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7NUK4OFQyLz5zOUWyPFQ1OTxxYU6=
UCH-1  NUK5PFN3TnWwY4Tpc44hSXO|YYm= NWTKSoxLOC13IN88US=> NX7NSYV{cW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDic5RpKEGNVDDhcoQhdVSRUjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NWnJRoRuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm1Nlg1PDFpPkG5OVI5PDRzPD;hQi=>
HUVEC NVe0blZNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF71XVdKSzVyPUCuNFgh|ryP M3PvV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7NUi0NlI4Lz5zOUW4OFIzPzxxYU6=
SKOV-3 NVPyfVI4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nqWGlEPTB;MD6xNkDPxE1? M{jGbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7NUi0NlI4Lz5zOUW4OFIzPzxxYU6=
PC3  M1PQPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTBwMUCg{txO M1XYXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7NUi0NlI4Lz5zOUW4OFIzPzxxYU6=
DETROIT562 M4nrPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvMOmFKSzVyPUCuNVMh|ryP NHfVTIU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUW4OFIzPyd-MUm1PFQzOjd:L3G+
IGROV-1 NEHnS|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTBwME[g{txO MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTV6NEKyO{c,OTl3OESyNlc9N2F-
U87MG NVr0eIQ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrOO|NKSzVyPUCuNVQh|ryP NIfKUVU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUW4OFIzPyd-MUm1PFQzOjd:L3G+
U118MG MoThSpVv[3Srb36gRZN{[Xl? NHnkVFcxNjFvMTFOwG0> NE\USJczPOLCiXlCpC=> NEfCN4tFVVOR MnTSbY5pcWKrdIOgVGk{Uy2vZXTpZZRm\CC|aXfuZYxqdmd? MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTZ|M{[4N{c,OTl4M{O2PFM9N2F-
U138MG M2WwV2Z2dmO2aX;uJGF{e2G7 NWPkW2xxOC5zLUGg{txO MmTSNlTjiImqwrC= MX3EUXNQ MUTpcohq[mm2czDQTVNMNW2nZHnheIVlKHOrZ37hcIlv\w>? MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTZ|M{[4N{c,OTl4M{O2PFM9N2F-
U87MG Mm\GSpVv[3Srb36gRZN{[Xl? MljBNE4yNTFizszN M3;5bFI16oDLaNMg NWLCTG9iTE2VTx?= NFrJWYtqdmirYnn0d{BRUTONLX3l[IlifGWmIIPp[45idGmwZx?= NWmyVYpORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm2N|M3QDNpPkG5OlM{Pjh|PD;hQi=>
PC3  MkDjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\ReoYzPGh? MlzvS2k2OMLiPTCxNFAhdk1? MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODV3MUC2NUc,OjB3NUGwOlE9N2F-
518A2 MnLDSpVv[3Srb36gRZN{[Xl? MWSwMlAxOeLCk{JihKnPxE1? MlPDNlQhcA>? MlHEd5VxeHKnc4Pld{BxcG:|cHjvdplt[XSrb36gc4YheGixc4DoZZRq\HmuIHnuc5NqfG:uIEOtb4lv[XOnIHTve45{fHKnYX2geIFz\2W2cx?= MlexQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjFyNEi3PFUoRjJzMES4O|g2RC:jPh?=
Mel-Juso  M4e1VWZ2dmO2aX;uJGF{e2G7 MWCwMlAxOeLCk{JihKnPxE1? M4fDfFI1KGh? MVfzeZBxemW|c3XzJJBpd3OyaH;yfYxifGmxbjDv[kBxcG:|cHjheIllgWxiaX7vd4l1d2xiMz3rbY5ie2ViZH;3cpN1emWjbTD0ZZJo\XS| MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTB2OEe4OUc,OjFyNEi3PFU9N2F-
518A2  MnfuR4VtdCCYaXHibYxqfHliQYPzZZk> M4jUUlAvODIkgKOxNQKBkc7:TR?= MUC3NkBp M{TxZolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NXWxSFQ2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGwOFg4QDVpPkKxNFQ5Pzh3PD;hQi=>
Mel-Juso M{DVOmNmdGxiVnnhZoltcXS7IFHzd4F6 NYr1WHE1OC5yMfMAl|Ex6oDLzszN MVS3NkBp M1;ZUYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NYTPcpF3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGwOFg4QDVpPkKxNFQ5Pzh3PD;hQi=>
SF767 NX3SPZFFTnWwY4Tpc44hSXO|YYm= M{i3bVEh|ryP MlH4OFghcA>? MlzsbY5lfWOnczDheZRweGijZ3;zc41mKG[xcn3heIlwdg>? M2e4S|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzME[yPVk{Lz5{MUC2Nlk6OzxxYU6=
U373 M3vzfGZ2dmO2aX;uJGF{e2G7 NU\ySmFOOSEQvF2= NInXNHM1QCCq M{\QdYlv\HWlZYOgZZV1d3CqYXfvd49u\SCob4LtZZRqd25? MmKxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjFyNkK5PVMoRjJzME[yPVk{RC:jPh?=
U87 M1fPSmZ2dmO2aX;uJGF{e2G7 NWH6UXBqOSEQvF2= MnjQOFghcA>? NXfHNndjcW6mdXPld{BifXSxcHjh[49{d22nIH\vdo1ifGmxbh?= M1i1UlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzME[yPVk{Lz5{MUC2Nlk6OzxxYU6=
LN229 NIj5dXpHfW6ldHnvckBCe3OjeR?= MVmxJO69VQ>? MUe0PEBp M{DxV4lv\HWlZYOgZZV1d3CqYXfvd49u\SCob4LtZZRqd25? NWT1U5E3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGwOlI6QTNpPkKxNFYzQTl|PD;hQi=>
PC-9  NXnNV21iT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEG5ZYYxNTNizszN NH22VZQ4OiCq NXjTR4ZzUUN3ME2wMlgh|ryP M{PjXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzMkKwOFc1Lz5{MUKyNFQ4PDxxYU6=
HCC827 NGXjSIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\iNFJTOC1|IN88US=> Ml7RO|IhcA>? M1v6c2lEPTB;MD6zJO69VQ>? NGfuOlY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUKyNFQ4PCd-MkGyNlA1PzR:L3G+
HCC1937 NG[2WmhHfW6ldHnvckBCe3OjeR?= NHv2Z4MyKM7:TR?= NWXTRZlOOjRiaB?= MmnndoVlfWOnczD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVB?= NHjReGQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkS4PFU6OCd-MkK0PFg2QTB:L3G+
SUM1315MO2 NVuzVZZ3TnWwY4Tpc44hSXO|YYm= MljhNUDPxE1? M1TmeVI1KGh? MXTy[YR2[2W|IITo[UBxcG:|cHjvdplt[XSrb36gc4YhSUuW M{K3WVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NEi4OVkxLz5{MkS4PFU6ODxxYU6=
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MDA-MB-436 NFnr[ZdHfW6ldHnvckBCe3OjeR?= MlLKNUDPxE1? MW[yOEBp NHzLVpdz\WS3Y3XzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvU MmDPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ2OEi1PVAoRjJ{NEi4OVkxRC:jPh?=
KMS12-BM  MorOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGH1S4sxNTJizszN NWXpXmxbOjRiaB?= NGHC[5RKSzVy78{eNkDPxE1? NW[5T3pGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK4NlkzOzRpPkKyPFI6OjN2PD;hQi=>
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Jurkat NIf6ZoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrCeIJ1OeLCid88US=> M330[lch\A>? M2XlbIRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? MoTzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyM{iyO|MoRjJ|MEO4Nlc{RC:jPh?=
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Saos-2 NWnIVJZKeUiWUzDhd5NigQ>? M130bpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVYX;zMVIh[2WubIO= MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-SH MXrxTHRUKGG|c3H5 MYXxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3TTEBk\Wyucx?= M3uwdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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OHS-50 NVrxSGN2eUiWUzDhd5NigQ>? Mlz1dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE:KUz21NEBk\Wyucx?= NXHQOGdkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
RD MW\xTHRUKGG|c3H5 MmnMdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKGIHPlcIx{ M4PZS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
MG 63 (6-TG R) M4XVNpFJXFNiYYPzZZk> M3TwbZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCPRzC2N{ApPi2WRzDSLUBk\Wyucx?= MmToQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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NB1643 NGLOVW9yUFSVIHHzd4F6 NYnTfo5zeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhVkJzNkSzJINmdGy| NUHne3hGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
A673 Ml[2dWhVWyCjc4PhfS=> NHuwfWpyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBCPjd|IHPlcIx{MQ>? MlnlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC NFrhOmRyUFSVIHHzd4F6 M{fRO5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHNMNU5vTVOgZ4VtdHN? NX61V3BoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
LAN-5 NHHGUWRyUFSVIHHzd4F6 MVPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDMRW4uPSClZXzsdy=> M1HFOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB-EBc1 NIj0PXVyUFSVIHHzd4F6 NH\xN|RyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBPSi2HQnOxJINmdGy| M4L0bFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SJ-GBM2 NFjQ[3RyUFSVIHHzd4F6 NEfQPWZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBUUi2JQl2yJINmdGy| M{jpW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
BT-37 MmrXdWhVWyCjc4PhfS=> MlSwdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgRnQuOzdiY3XscJM> NYPMd2M2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
TC32 Moq5dWhVWyCjc4PhfS=> MV\xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDUR|MzKGOnbHzz M1zlS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
MG 63 (6-TG R) MmXUdWhVWyCjc4PhfS=> MnPDdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgUWchPjNiKE[tWGchWiliY3XscJM> M1LqOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh41 MnnrdWhVWyCjc4PhfS=> MWfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDSbFQyKGOnbHzz NUfMdWlDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh18 MVTxTHRUKGG|c3H5 M3\RV5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHJpOThiY3XscJM> MoToQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Saos-2 MnK3dWhVWyCjc4PhfS=> NELDWJlyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBU[W:|LUKgZ4VtdHN? M{G5XlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
OHS-50 MknhdWhVWyCjc4PhfS=> Mn6wdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgU2hUNTVyIHPlcIx{ NGLJR2s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-SH MXTxTHRUKGG|c3H5 MVPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDTT{1PNVOKIHPlcIx{ M1PtOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Caco2 Mn3ZR4VtdCCleXPs[UBie3OjeR?= NYDCfGxFS2WubDDjfYNt\SCjcoLld5QhcW5iaIXtZY4hS2Glb{KgZ4VtdHNiYYPz[ZN{\WRiYYOgZYNkfW23bHH0bY9vKGG2IFexM3MheGijc3WgZpkhUG:nY3jzeEB{fGGrbnnu[{Bj[XOnZDDmcJVwemW|Y3XuZ4Uh[XO|YYm= NYfIWWtlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyNVQzOzFpPkK4NlE1OjNzPD;hQi=>
HCT116 MUHD[YxtKGO7Y3zlJIF{e2G7 MkfWR4VtdCCleXPs[UBienKnc4SgbY4hcHWvYX6gTGNVOTF4IHPlcIx{KGG|c3Xzd4VlKGG|IHHjZ5VufWyjdHnvckBifCCJMj;NJJBp[XOnIHL5JGhw\WOqc4Sgd5RicW6rbnegZoF{\WRiZnz1c5Jme2OnbnPlJIF{e2G7 MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJzNEKzNUc,Ojh{MUSyN|E9N2F-
PC3 NYLCbGVHS2WubDDjfYNt\SCjc4PhfS=> NWqwXWQ2S2WubDDjfYNt\SCjcoLld5QhcW5iaIXtZY4hWEN|IHPlcIx{KGG|c3Xzd4VlKGG|IHHjZ5VufWyjdHnvckBifCCJMT;TJJBp[XOnIHL5JGhw\WOqc4Sgd5RicW6rbnegZoF{\WRiZnz1c5Jme2OnbnPlJIF{e2G7 MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJzNEKzNUc,Ojh{MUSyN|E9N2F-
HaCaT NYnCe3JmS2WubDDjfYNt\SCjc4PhfS=> NIrIN3lE\WyuIHP5Z4xmKGG{cnXzeEBqdiCqdX3hckBJ[UOjVDDj[YxteyCjc4Pld5Nm\CCjczDhZ4N2dXWuYYTpc44h[XRiR{GvV{BxcGG|ZTDifUBJd2WlaIP0JJN1[WmwaX7nJIJie2WmIH\seY9z\XOlZX7j[UBie3OjeR?= NGXrN2w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEKxOFI{OSd-MkiyNVQzOzF:L3G+

... 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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