PI-103

製品コードS1038

PI-103化学構造

分子量(MW):348.36

PI-103は一種の多ターゲットPI3K阻害剤で、無細胞試験でp110α/β/δ/γに作用する時のIC50値は2 nM/3 nM/3 nM/15 nMです。PI-103はmTOR/DNA-PKに作用する効果が弱くて、このIC50値が30 nM/23 nMになります。

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カスタマーフィードバック(4)

  • (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.

  • 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.

    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.

製品安全説明書

PI3K阻害剤の選択性比較

生物活性

製品説明 PI-103は一種の多ターゲットPI3K阻害剤で、無細胞試験でp110α/β/δ/γに作用する時のIC50値は2 nM/3 nM/3 nM/15 nMです。PI-103はmTOR/DNA-PKに作用する効果が弱くて、このIC50値が30 nM/23 nMになります。
特性 The first potent, synthetic mTOR inhibitor.
靶点
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試験

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
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SH-SY5Y M4fM[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfnPG9YOC16IN88US=> NGLVeJQzPC92OD:3NkBp NGnZXI9qdmS3Y3XzJJRqdWVvIHHu[EBkd26lZX70doF1cW:wLXTldIVv\GWwdDDpcohq[mm2aX;uJI9vKE6EIHPlcIwh\3Kxd4To MVuyOlIzPDZ6MR?=
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G 38 SC MofyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX:wMlA2NTJyIN88US=> NUTpc4hKOjRxN{KgbC=> M17ieWROW09? NETq[WlqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 MljtNlYyOjF{NUG=
G 40 SC MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYqwMlA2NTJyIN88US=> M3LDNVI1Nzd{IHi= M3TpS2ROW09? MX\pcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueIx6 MknONlYyOjF{NUG=
G 35 DC NGjpSHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4X2bFAvODVvMkCg{txO M3vwOVI1Nzd{IHi= M3y3ZmROW09? NWnxd3JVcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= NX\h[XVCOjZzMkGyOVE>
G 38 DC MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HQdVAvODVvMkCg{txO MV2yOE84OiCq M{LaXWROW09? MUnpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueIx6 NXTHUo5pOjZzMkGyOVE>
G 40 DC M1\Cdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rSd|AvODVvMkCg{txO MXyyOE84OiCq NIPrZ5FFVVOR M1T2R4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? MWmyOlEzOTJ3MR?=
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TE381.T MVLBdI9xfG:|aYOgRZN{[Xl? NFi3V|gyNzFwNT:yJO69VQ>? M3\GeFczKGh? MnvmbY5lfWOnczDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCJQV7UOlE> NVfEWm16OjV5NEmzO|g>
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HS578T NW\xeXZnS2WubDDWbYFjcWyrdImgRZN{[Xl? M1npWlAuOyEQvF2= MWq3NkBp NFnOPVhqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MoDMNlU4OjF2MUm=
BT549 MX3D[YxtKF[rYXLpcIl1gSCDc4PhfS=> NHHvbmgxNTNizszN M3HRc|czKGh? M3TycYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? M1zsSlI2PzJzNEG5
MDA-MB-231 NGji[nZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M4L5b|AuOyEQvF2= NH6xXoY4OiCq MXPpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 Mn3HNlU4OjF2MUm=
MDA-MB-468 MWPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NXj4[JptOC1|IN88US=> Mn\kO|IhcA>? M2\TOYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NUnweYVJOjV5MkG0NVk>
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SUM149PT NX;WW|VGS2WubDDWbYFjcWyrdImgRZN{[Xl? NULHcmk{OC1|IN88US=> MkH5O|IhcA>? NV7OWXNHcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MX:yOVczOTRzOR?=
MDA-MB-468 MXjGeY5kfGmxbjDBd5NigQ>? MnrXNE4xOS1zMDFOwG0> MVOyOEBp MkDv[I94dnKnZ4XsZZRmeyC2aHWgcIV3\Wy|IH;mJO6zNVS{Q2CxMEBkNU27YzDhcoQh[3mlbHnuJGUheHKxdHXpcpPDqA>? NXrrPJhKOjV5MkG0NVk>
MDA-MB-231 M13EZWZ2dmO2aX;uJGF{e2G7 NW[zenhGOC5yMT2xNEDPxE1? MXiyOEBp MlTu[I94dnKnZ4XsZZRmeyC2aHWgcIV3\Wy|IH;mJO6zNVS{Q2CxMEBkNU27YzDhcoQh[3mlbHnuJGUheHKxdHXpcpPDqA>? MViyOVczOTRzOR?=
HS578T NEHvNoxHfW6ldHnvckBCe3OjeR?= Mn[1NE4xOS1zMDFOwG0> NIjrNFgzPCCq M1HDXYRwf26{ZXf1cIF1\XNidHjlJIxmfmWuczDv[kDPui2WclPQNUwh[y2PeXOgZY5lKGO7Y3zpckBGKHC{b4TlbY5{yqB? MkLtNlU4OjF2MUm=
SW872 M4XlVmZ2dmO2aX;uJGF{e2G7 NHP3[nIxNjBzLUCuOUDPxE1? MmjaNlQhcA>? NWf6boVGemWmdXPld{BCU1RicHjvd5Bpd3K7bHH0bY9vKCiyQVvULUBidmRiNFXCVFEheGixc4Doc5J6dGG2aX;uJEhxPEWEUEGpJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXyxsA> NVznN|RCOjR4OUW2N|I>
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SW872 M2[3NWFxd3C2b4Ppd{BCe3OjeR?= MVqwMlAyNTBwNTFOwG0> NXjHTnpYPDhiaB?= M3LkSIlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= M3XSUlI1Pjl3NkOy
SW982 NXrU[I5QSXCxcITvd4l{KEG|c3H5 MWWwMlAyNTBwNTFOwG0> MmDWOFghcA>? MU\pcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NFfXTFczPDZ7NU[zNi=>
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AGS LG NVm0dYFKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTBwMEWgxtEhOC5yMEGg{txO M1nLTFI1PTl5NEe4
HGC27 HG NF:xXW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{izWWlEPTB;MD6zPEDDuSByLkCyNkDPxE1? M13SNVI1PTl5NEe4
HGC27 LG MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFy5V4hKSzVyPUCuNFIhyrFiMD6wNFQh|ryP MnLWNlQ2QTd2N{i=
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NUGC4 HG MnjlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PYNmlEPTB;MUSuNEDDuSB|LkmxN{DPxE1? MoPBNlQ2QTd2N{i=
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A549 NIDXVmxHfW6ldHnvckBCe3OjeR?= NILuSnoxNjJ3L{CuOU8yKM7:TR?= NUm2V4JROjRiaB?= NU\UW|dCcW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|bHnnbJRtgQ>? NHTLd2kzPDN3MUSyOS=>
H460 MnTpSpVv[3Srb36gRZN{[Xl? NFPGb3MxNjJ3L{CuOU8yKM7:TR?= MYmyOEBp MX7pcohq[mm2czDBb5QheGixc4Doc5J6dGG2aX;uJJNtcWeqdHz5 M1jBTlI1OzVzNEK1
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SAS NFziRmRHfW6ldHnvckBCe3OjeR?= NEj1eIExNjJ3L{CuOU8yKM7:TR?= NEWxclAzPCCq M2LoeolvcGmkaYTzJGFsfCCyaH;zdIhwenmuYYTpc44he2mpbnnmbYNidnSueR?= NEi0T5MzPDN3MUSyOS=>
UT5 M3H1[2Z2dmO2aX;uJGF{e2G7 NEPmXFcxNjJ3L{CuOU8yKM7:TR?= NFvUO4IzPCCq MY\pcohq[mm2czDBb5QheGixc4Doc5J6dGG2aX;uJJNq\26rZnnjZY51dHl? MWmyOFM2OTR{NR?=
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SUM149PT Mm\5R4VtdCCYaXHibYxqfHliQYPzZZk> MUiwMlMh|ryP M2TxW|czKGh? MlLm[Y5p[W6lZYOgZ5l1d3SxeHnjJIVn\mWldIOgc4YhWEl|Sz;BT3QheGG2aIfhfUBqdmirYnn0c5J{ NWjDc|h6OjN4MEGwO|Q>
MDA-MB-468 NY\Sc|NPS2WubDDWbYFjcWyrdImgRZN{[Xl? NFuxU|YxNjNizszN NIjlSnU4OiCq MXflcohidmOnczDjfZRwfG:6aXOg[YZn\WO2czDv[kBRUTONL1HLWEBx[XSqd3H5JIlvcGmkaYTvdpM> MYCyN|YxOTB5NB?=
MDA-MB-231 NFL5bodE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MVewMlMh|ryP M17WSVczKGh? NHjqWHdmdmijbnPld{BkgXSxdH;4bYMh\W[oZXP0d{Bw\iCSSUPLM2FMXCCyYYToe4F6KGmwaHnibZRwenN? NEC4U3IzOzZyMUC3OC=>
SY5Y M33DUWZ2dmO2aX;uJGF{e2G7 MWKxMlUwOi53L{Wg{txO NHH1TFUzPCCq MUjpcoR2[2W|IFexxsBk\WyuLXP5Z4xmKGG{cnXzeEBidmRiYYDvdJRwe2m| NV\qPWZwOjN|N{izOFE>
SKNBE(2c) M1r5O2Z2dmO2aX;uJGF{e2G7 NFL6XoEyNjVxMj61M|Uh|ryP NEHrbJAzPCCq M3zvR4lv\HWlZYOgS|HDqGOnbHytZ5lkdGViYYLy[ZN1KGGwZDDhdI9xfG:|aYO= MmLkNlM{Pzh|NEG=
RD NH\LfGpCeG:ydH;zbZMhSXO|YYm= Mmn0N{DDvU1? MoXpNVIhcA>? NIDrU4FFVVOR NXjJcIdte2Wwc3n0bZpmeyCURDDj[YxteyC2bzDEU3gucW6mdXPl[EBieG:ydH;zbZM> NHf4bJEzOzNyMEiwPS=>
TP5014 MX3BdI9xfG:|aYOgRZN{[Xl? MljTN{DDvU1? MlzWNVIhcA>? MnHJSG1UVw>? MkHzd4Vve2m2aYrld{BTTCClZXzsd{B1dyCGT2itbY5lfWOnZDDhdI9xfG:|aYO= MYeyN|MxODhyOR?=
HT1080 MoPVRZBweHSxc3nzJGF{e2G7 NFj1b4I{KML3TR?= M1XCRVEzKGh? MnjpSG1UVw>? MV7z[Y5{cXSrenXzJHJFKGOnbHzzJJRwKESRWD3pcoR2[2WmIHHwc5B1d3Orcx?= NVLTclA4OjN|MEC4NFk>
A549 Mm\wSpVv[3Srb36gRZN{[Xl? NXfhZ|VpOC1|LkOg{txO Mn\tO|IhcA>? M2WzZ4lv\HWlZYOgZ49ueGyndHWg[I94dnKnZ4XsZZRqd25ib3[gdGFMXA>? M{\XZVI{OjV7NUmx
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HPB-ALL MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITrV3Qy6oDLzszN NGHjeYY4KGR? M2PxcYRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? M4n5b|I{ODN6Mkez
DND41 NILZb|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLaNgKBkc7:TR?= NHy4fJE4KGR? M13wSoRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? MonVNlMxOzh{N{O=
SUP-T1 NF;Tc|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3e5clHjiIoQvF2= MlO0O{Bl M2\mboRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? NUG5bGt6OjNyM{iyO|M>
PEER M1vtbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PVSFHjiIoQvF2= MX[3JIQ> MVfk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> MX2yN|A{QDJ5Mx?=
ALL-SIL MlzzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvrSJUy6oDLzszN MWe3JIQ> NEP0PHpl\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? NXnsNYpDOjNyM{iyO|M>
KE37 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7XNgKBkc7:TR?= NGexVWo4KGR? M1T2XoRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? NE\EUXUzOzB|OEK3Ny=>
Karpas-45 NUXsR5FET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnOyNgKBkc7:TR?= MXS3JIQ> MWDk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> M3XSelI{ODN6Mkez
RPMI-8402 NFq2PZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXux5qCK|ryP NGnzTnE4KGR? NXrpbphL\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 NXjSVFRUOjNyM{iyO|M>
Jurkat NXfhdHZoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnsU4w2OeLCid88US=> MVu3JIQ> NXjXdpFF\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 MmjvNlMxOzh{N{O=
MOLT-4 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUmx5qCK|ryP M2nw[lch\A>? MXnk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> M2j1bFI{ODN6Mkez
PF-382 MmLGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITZPW4y6oDLzszN MVK3JIQ> MVrk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> NIW3NJAzOzB|OEK3Ny=>
CCRF-CEM MmSwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jWc|HjiIoQvF2= NXXWeYN7PyCm M{H1V4Rm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? M{npPFI{ODN6Mkez
LOUCY M4\PU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoL3NgKBkc7:TR?= NFPOWFc4KGR? MmLV[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 MmDHNlMxOzh{N{O=
MOLT-16 M2[3fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLnNgKBkc7:TR?= MYC3JIQ> NFvMb|Vl\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? MnjUNlMxOzh{N{O=
MM1S NVX2OnZNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHEcXkxNTJizszN Mn;0NlQhcA>? MUjJR|UxRTBwNTFOwG0> Ml;4NlI5Ojl{M{S=
NCI-H929 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXWyb3VvOC1{IN88US=> MoXGNlQhcA>? M4XLPGlEPTB;MD6yOUDPxE1? M2PmSlIzQDJ7MkO0
KMS12-BM  NFrSUXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfQflZYOC1{IN88US=> Ml\DNlQhcA>? MXfJR|Ux97zgMjFOwG0> MVWyNlgzQTJ|NB?=
MDA-MB-436 NVvJOJQ2TnWwY4Tpc44hSXO|YYm= MljDNUDPxE1? M3PEbFI1KGh? MnjodoVlfWOnczD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVB?= NHLWWogzOjR6OEW5NC=>
SUM149PT NFvOcG1HfW6ldHnvckBCe3OjeR?= M{TRXFEh|ryP NXLHbI1wOjRiaB?= NHH5UVJz\WS3Y3XzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvU M4H2[lIzPDh6NUmw
SUM1315MO2 NHTXcYhHfW6ldHnvckBCe3OjeR?= NUHaXIQ1OSEQvF2= NFnmenQzPCCq MlnydoVlfWOnczD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVB?= M2fYZlIzPDh6NUmw
HCC1937 NXz0ZZBjTnWwY4Tpc44hSXO|YYm= NIDTRm4yKM7:TR?= MVKyOEBp MXjy[YR2[2W|IITo[UBxcG:|cHjvdplt[XSrb36gc4YhSUuW MlXmNlI1QDh3OUC=
HCC827 MnzyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYOwMVMh|ryP M3jkVlczKGh? NUHRXI9uUUN3ME2wMlMh|ryP NGfifoQzOTJ{MES3OC=>
PC-9  MkXnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWmwMVMh|ryP M{XlPVczKGh? Mn7JTWM2OD1yLkig{txO MoDPNlEzOjB2N{S=
LN229 MYDGeY5kfGmxbjDBd5NigQ>? NV7mW3hEOSEQvF2= MXK0PEBp NV3RUIZxcW6mdXPld{BifXSxcHjh[49{d22nIH\vdo1ifGmxbh?= NXnKWFlwOjFyNkK5PVM>
U87 M2SyUWZ2dmO2aX;uJGF{e2G7 NInnZnAyKM7:TR?= NXXTUmF4PDhiaB?= M3vXfolv\HWlZYOgZZV1d3CqYXfvd49u\SCob4LtZZRqd25? M3f0cFIyODZ{OUmz
U373 M36xWmZ2dmO2aX;uJGF{e2G7 MnPCNUDPxE1? Mo[4OFghcA>? Mn24bY5lfWOnczDheZRweGijZ3;zc41mKG[xcn3heIlwdg>? NULRSW84OjFyNkK5PVM>
SF767 MnX5SpVv[3Srb36gRZN{[Xl? NWPYXnBMOSEQvF2= NUjjS2xlPDhiaB?= MVzpcoR2[2W|IHH1eI9xcGGpb4PvcYUh\m:{bXH0bY9v NXTVXXpUOjFyNkK5PVM>
Mel-Juso MnjoR4VtdCCYaXHibYxqfHliQYPzZZk> M{L6T|AvODIkgKOxNQKBkc7:TR?= NFrQTIY4OiCq Mm\2bY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MmjYNlExPDh5OEW=
518A2  M17JUGNmdGxiVnnhZoltcXS7IFHzd4F6 NWP4OmZqOC5yMfMAl|Ex6oDLzszN NEPsPZc4OiCq MVHpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MUeyNVA1QDd6NR?=
Mel-Juso  M4G3OmZ2dmO2aX;uJGF{e2G7 NVHrc2JSOC5yMEJihLMy6oDLzszN M1r5S|I1KGh? MYrzeZBxemW|c3XzJJBpd3OyaH;yfYxifGmxbjDv[kBxcG:|cHjheIllgWxiaX7vd4l1d2xiMz3rbY5ie2ViZH;3cpN1emWjbTD0ZZJo\XS| NFrRcHAzOTB2OEe4OS=>
518A2 NXzoSohKTnWwY4Tpc44hSXO|YYm= M3nBc|AvODBz4pETNgKBkc7:TR?= MoPCNlQhcA>? NGfRNHV{fXCycnXzd4V{KHCqb4PwbI9zgWyjdHnvckBw\iCyaH;zdIhifGmmeXygbY5we2m2b3ygN{1scW6jc3Wg[I94dnO2cnXhcUB1[XKpZYTz M4W5flIyODR6N{i1
PC3  NIrPb3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULOOYYxOjSq MXvHTVUxyqB;IEGwNEBvVQ>? MkfFNlA2PTFyNkG=
U87MG M{LCUmZ2dmO2aX;uJGF{e2G7 MnLzNE4yNTFizszN Mlj3NlTjiImqwrC= MYPEUXNQ M1fYV4lvcGmkaYTzJHBKO0tvbXXkbYF1\WRic3nncoFtcW6p MVOxPVY{OzZ6Mx?=
U138MG NUXFbphwTnWwY4Tpc44hSXO|YYm= NHr1RW0xNjFvMTFOwG0> MUCyOQKBkWkEoB?= NY\ZNW5zTE2VTx?= NGXMTWVqdmirYnn0d{BRUTONLX3l[IlifGWmIIPp[45idGmwZx?= MmLONVk3OzN4OEO=
U118MG NF7S[3dHfW6ldHnvckBCe3OjeR?= MY[wMlEuOSEQvF2= M1nKNlI16oDLaNMg NHHqOVlFVVOR M1\UVIlvcGmkaYTzJHBKO0tvbXXkbYF1\WRic3nncoFtcW6p NWrQTHlMOTl4M{O2PFM>
U87MG NWfrTplrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjoSJhHUUN3ME2wMlE1KM7:TR?= Mmr3NVk2QDR{Mke=
IGROV-1 NYGyN5k4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoT3TWM2OD1yLkC2JO69VQ>? NV7oZpNtOTl3OESyNlc>
DETROIT562 NYfKbYcyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLOTWM2OD1yLkGzJO69VQ>? Mmq3NVk2QDR{Mke=
PC3  MmfKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkGwTWM2OD1yLkGwJO69VQ>? NHT4dlAyQTV6NEKyOy=>
SKOV-3 M4W5RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPqUndKSzVyPUCuNVIh|ryP NXTkd5k6OTl3OESyNlc>
HUVEC NIL0cGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTBwMEig{txO NILNS24yQTV6NEKyOy=>
UCH-1  MojsSpVv[3Srb36gRZN{[Xl? M4n2XVAuPSEQvF2= Ml\NbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCkb4ToJGFMXCCjbnSgcXRQWiCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NEDKV2MyQTV{OES0NS=>
UCH-1  NELPVYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLYOGMxNjBzLUGwJO69VQ>? NGjUdGY3KGR? M{m2[olvcGmkaYTzJJBzd2yrZnXyZZRqd25iZH;z[UBl\XCnbnTlcpRtgQ>? NEGy[lUyQTV{OES0NS=>
UCH-1  MnTxRZBweHSxc3nzJGF{e2G7 MU[wMlEuOTBizszN MXiyOEBp NXPZ[2dQTE2VTx?= M37LU4lv\HWlZYOgZZBweHSxc3nz M4\Sb|E6PTJ6NESx

... Click to View More Cell Line Experimental Data

In vivo試験 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]

プロトコル(参考用のみ)

キナーゼアッセイ:[3]
+ 展開

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.
細胞アッセイ: [2]
+ 展開
  • 細胞株: U87MG cells
  • 濃度: 0.5 μM
  • 反応時間: 24 hours
  • 実験の流れ: 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 °
    (参考用のみ)
動物実験:[2]
+ 展開
  • 動物モデル: 6- to 12-week-old Balbc nu/nu mice bearing U87MG:ΔEGFR cells
  • 製剤: 50% DMSO
  • 投薬量: 5 mg/kg
  • 投与方法: Administered via i.p.
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 24 mg/mL (68.89 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
体内 1% DMSO+30% polyethylene glycol+1% Tween 80 30 mg/mL

* <1 mg/mlは製品が微弱に溶解する或いは溶解しないことを示します。
* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。

化学情報

分子量 348.36
化学式

C19H16N4O3

CAS No. 371935-74-9
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

マス 濃度 ボリューム 分子量

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

PI3K信号経路図

PI3K Inhibitors with Unique Features

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Tags: PI-103を買う | PI-103 ic50 | PI-103供給者 | PI-103を購入する | PI-103費用 | PI-103生産者 | オーダーPI-103 | PI-103化学構造 | PI-103分子量 | PI-103代理店
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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID