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。

サイズ 価格 在庫  
JPY 19294.39 あり
JPY 21166.23 あり
JPY 38876.76 あり
JPY 53275.56 あり

カスタマーフィードバック(5)

  • (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.

    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.
ターゲット
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
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SK-N-BE MmPRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYj1OHhtOC16IN88US=> NFnLToUzPC92OD:3NkBp MWTpcoR2[2W|IITpcYUuKGGwZDDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCrbnjpZol1cW:wIH;uJG5DKGOnbHyg[5Jwf3Sq NHLpepQzPjJ{NE[4NS=>
SH-SY5Y M1m4RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jqUFAuQCEQvF2= Mn3oNlQwPDhxN{KgbC=> M2LpcIlv\HWlZYOgeIlu\S1iYX7kJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IHnubIljcXSrb36gc44hVkJiY3XscEBoem:5dHi= NITQWIIzPjJ{NE[4NS=>
SH-SY5Y  NVnUWmFySXCxcITvd4l{KEG|c3H5 MmXaNUDPxE1? NU\sT5puOC53LUK0JIg> MoPzd4Vve2m2aYrld{Bv\XW{b3LsZZN1d22jIHPlcIx{KHSxIHTvfI9zfWKrY3nuMYlv\HWlZXSgZZBweHSxc3nz MlvGNlYzOjR4OEG=
G 35 SC MmDtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHHRWoxNjB3LUKwJO69VQ>? MofZNlQwPzJiaB?= NYn1Z|lYTE2VTx?= NUPWcZNWcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= NXjlXG5HOjZzMkGyOVE>
G 38 SC NY\QPYZOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7sNE4xPS1{MDFOwG0> NXTlS2g1OjRxN{KgbC=> MX7EUXNQ NGjLeZBqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 NF\4OnkzPjF{MUK1NS=>
G 40 SC Mn7SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXne2d{OC5yNT2yNEDPxE1? NVvndJBxOjRxN{KgbC=> M1z0O2ROW09? NHfMWoZqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 MlGyNlYyOjF{NUG=
G 35 DC NYDwR25OT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVGwMlA2NTJyIN88US=> Ml;lNlQwPzJiaB?= NVqyTWRZTE2VTx?= Mn6xbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBidmRidHnt[UBl\XCnbnTlcpRtgQ>? M{PSTVI3OTJzMkWx
G 38 DC M1;oeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofTNE4xPS1{MDFOwG0> MYWyOE84OiCq MlzsSG1UVw>? MXvpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueIx6 NFHJVIQzPjF{MUK1NS=>
G 40 DC M1P1Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1Lq[lAvODVvMkCg{txO NWnqTGpxOjRxN{KgbC=> MXLEUXNQ M335XIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? NH;HRpMzPjF{MUK1NS=>
RD MX;BdI9xfG:|aYOgRZN{[Xl? NYfwfIJPOS9zLkWvNkDPxE1? MUC3NkBp NETHPZhqdmS3Y3XzJIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIFfBUnQ3OQ>? MWqyOVc1QTN5OB?=
TE381.T M4fP[GFxd3C2b4Ppd{BCe3OjeR?= NF;Q[4MyNzFwNT:yJO69VQ>? MofQO|IhcA>? MV;pcoR2[2W|IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKEeDTmS2NS=> NGjHTYgzPTd2OUO3PC=>
RMS13 M3\DUmFxd3C2b4Ppd{BCe3OjeR?= NUfXRZV2OS9zLkWvNkDPxE1? NVLHPIQzPzJiaB?= M2XUWIlv\HWlZYOgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiR1HOWFYy M4LzdFI2PzR7M{e4
RH30  MXvBdI9xfG:|aYOgRZN{[Xl? MXyxM|EvPS9{IN88US=> NWrXcI9LPzJiaB?= MXvpcoR2[2W|IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKEeDTmS2NS=> NUTvZmpQOjV5NEmzO|g>
VJ NV:1NWRiSXCxcITvd4l{KEG|c3H5 M3zHNVEwOS53L{Kg{txO NYruUVc5PzJiaB?= MV3pcoR2[2W|IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKEeDTmS2NS=> NVTaN49KOjV5NEmzO|g>
HS578T NYfDNZpGS2WubDDWbYFjcWyrdImgRZN{[Xl? NILVWGIxNTNizszN MVe3NkBp M3jtZYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NWfZVoxKOjV5MkG0NVk>
BT549 MWDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> Mlz5NE0{KM7:TR?= M1HHT|czKGh? NV\3[3lJcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= M4rqelI2PzJzNEG5
MDA-MB-231 NIflcmpE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MYWwMVMh|ryP MV23NkBp MlLqbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NVX3V|hEOjV5MkG0NVk>
MDA-MB-468 MX3D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MoPZNE0{KM7:TR?= NGOxOI84OiCq M1zoNolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MmqyNlU4OjF2MUm=
MDA-MB-436 MWHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NF3yZVgxNTNizszN NWXT[2E{PzJiaB?= MmXmbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? Mn\INlU4OjF2MUm=
SUM149PT NX3KXotqS2WubDDWbYFjcWyrdImgRZN{[Xl? NEXXRWkxNTNizszN Mn:0O|IhcA>? MkPubY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? M3O2eFI2PzJzNEG5
MDA-MB-468 NYLTd|dxTnWwY4Tpc44hSXO|YYm= NIr4R24xNjBzLUGwJO69VQ>? MUGyOEBp MYLkc5dvemWpdXzheIV{KHSqZTDs[ZZmdHNib3[g{tIuXHKFUEGsJIMuVXmlIHHu[EBkgWOuaX6gSUBxem:2ZXnud:Kh NU\McVl{OjV5MkG0NVk>
MDA-MB-231 MVXGeY5kfGmxbjDBd5NigQ>? NGP3UVAxNjBzLUGwJO69VQ>? MXqyOEBp NGi1VW5ld3ewcnXneYxifGW|IITo[UBt\X[nbIOgc4Yh|rJvVILDVFEtKGNvTYnjJIFv\CCleXPsbY4hTSCycn;0[Ylve8Li NHXI[HYzPTd{MUSxPS=>
HS578T NXnDbWtUTnWwY4Tpc44hSXO|YYm= MkDBNE4xOS1zMDFOwG0> NF3x[W0zPCCq NX;Dfpdy\G:5boLl[5Vt[XSnczD0bIUhdGW4ZXzzJI9nKM7{LWTyR3AyNCClLV35Z{BidmRiY4njcIlvKEVicILveIVqdnQEoB?= MoDrNlU4OjF2MUm=
SW872 NGnQcXFHfW6ldHnvckBCe3OjeR?= NF7PNnkxNjBzLUCuOUDPxE1? M4TGZ|I1KGh? MoHUdoVlfWOnczDBT3QheGixc4Doc5J6dGG2aX;uJEhxSUuWKTDhcoQhPEWEUEGgdIhwe3Cqb4L5cIF1cW:wIDjwOGVDWDFrIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{wrC= M1LNfFI1Pjl3NkOy
SW982 MoTsSpVv[3Srb36gRZN{[Xl? NVW2c|JOOC5yMT2wMlUh|ryP MVuyOEBp NEPvcWdz\WS3Y3XzJGFMXCCyaH;zdIhwenmuYYTpc44hMHCDS2SpJIFv\CB2RVLQNUBxcG:|cHjvdplt[XSrb36gLJA1TUKSMTmgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYNCpC=> NG\vZ5ozPDZ7NU[zNi=>
SW872 MoTwRZBweHSxc3nzJGF{e2G7 NXLOZ5JzOC5yMT2wMlUh|ryP NYHBXnZtPDhiaB?= MWDpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MV[yOFY6PTZ|Mh?=
SW982 MnnsRZBweHSxc3nzJGF{e2G7 M3r6NFAvODFvMD61JO69VQ>? MlflOFghcA>? NUTORXNkcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NXHtWGdHOjR4OUW2N|I>
AGS HG M4O1bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLpTWM2OD1yLk[4JOKyKDBwMEOxJO69VQ>? NFnWV5MzPDV7N{S3PC=>
AGS LG MkTiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTBwMEWgxtEhOC5yMEGg{txO NXvNe4l2OjR3OUe0O|g>
HGC27 HG NHH1ZWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPpRmVKSzVyPUCuN|ghyrFiMD6wNlIh|ryP NX3EfXA2OjR3OUe0O|g>
HGC27 LG NEnhPYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1W4UGlEPTB;MD6wNkDDuSByLkCwOEDPxE1? MnTlNlQ2QTd2N{i=
MKN45 HG NFvRcpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLYTWM2OD1zLkCxJOKyKDBwMEWxJO69VQ>? NGLTUHEzPDV7N{S3PC=>
MKN45 LG NXj3ZnZ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HN[GlEPTB;MD64O{DDuSByLkCzNEDPxE1? NWXJUHFmOjR3OUe0O|g>
NUGC4 HG NXvodpFDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFz2XZFKSzVyPUG0MlAhyrFiMz65NVMh|ryP MmDmNlQ2QTd2N{i=
NUGC4 LG M{nnd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPTTWM2OD1zND6wJOKyKDVwM{KxJO69VQ>? NHLOUXIzPDV7N{S3PC=>
A549 NH;vV4RHfW6ldHnvckBCe3OjeR?= NWT1e4o2OC5{NT:wMlUwOSEQvF2= MoTUNlQhcA>? MWLpcohq[mm2czDBb5QheGixc4Doc5J6dGG2aX;uJJNtcWeqdHz5 NIXleW8zPDN3MUSyOS=>
H460 MlfESpVv[3Srb36gRZN{[Xl? MnrFNE4zPS9yLkWvNUDPxE1? NEH1TmgzPCCq MV\pcohq[mm2czDBb5QheGixc4Doc5J6dGG2aX;uJJNtcWeqdHz5 NGnRdZozPDN3MUSyOS=>
H661 MXXGeY5kfGmxbjDBd5NigQ>? NUfITVhEOC5{NT:wMlUwOSEQvF2= MkTSNlQhcA>? Mn3ubY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7 M1HDXlI1OzVzNEK1
SAS M1TDXWZ2dmO2aX;uJGF{e2G7 MkPWNE4zPS9yLkWvNUDPxE1? MWeyOEBp MnfGbY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7 NYHuOm5VOjR|NUG0NlU>
UT5 M2KxdGZ2dmO2aX;uJGF{e2G7 MVSwMlI2NzBwNT:xJO69VQ>? MV:yOEBp M17j[olvcGmkaYTzJGFsfCCyaH;zdIhwenmuYYTpc44he2mpbnnmbYNidnSueR?= NUOxUpM5OjR|NUG0NlU>
FaDu MXHGeY5kfGmxbjDBd5NigQ>? M2D0e|AvOjVxMD61M|Eh|ryP MofxNlQhcA>? NVvoSIJ1cW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|aXfubYZq[2GwdHz5 M{fKd|I1OzVzNEK1
RD M2fIS2Fxd3C2b4Ppd{BCe3OjeR?= MoLCNU8yNjVxMjFOwG0> MVm3NkBp NG\xO5ZFVVOR NVLGSHlDcW6mdXPld{Bk[XOyYYPlMYRmeGWwZHXueEBieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDVU|EzPg>? NIi4dVUzOzZ6NEmyOS=>
TE671 NHv2VJVCeG:ydH;zbZMhSXO|YYm= MnfkNU8yNjVxMjFOwG0> NXnpSYh4PzJiaB?= NX\uT3ZDTE2VTx?= M{HNSIlv\HWlZYOgZ4F{eGG|ZT3k[ZBmdmSnboSgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiVV:xNlY> NXTaR|RWOjN4OES5NlU>
RH30  MofNRZBweHSxc3nzJGF{e2G7 MX2xM|EvPS9{IN88US=> MU[3NkBp NHHTN3hFVVOR M4jDZ4lv\HWlZYOgZ4F{eGG|ZT3k[ZBmdmSnboSgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiVV:xNlY> MWSyN|Y5PDl{NR?=
RMS13 MnrTRZBweHSxc3nzJGF{e2G7 NV\yS3l6OS9zLkWvNkDPxE1? M3nyUlczKGh? M2jETWROW09? NF;Lb4VqdmS3Y3XzJINie3Cjc3Wt[IVx\W6mZX70JIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIGXPNVI3 Ml[5NlM3QDR7MkW=
SUM149PT NFnQZmNE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NVPpS2JCOC5|IN88US=> MkH5O|IhcA>? NIXzRpJmdmijbnPld{BkgXSxdH;4bYMh\W[oZXP0d{Bw\iCSSUPLM2FMXCCyYYToe4F6KGmwaHnibZRwenN? M3jBSVI{PjBzMEe0
MDA-MB-468 Mlu2R4VtdCCYaXHibYxqfHliQYPzZZk> MoTCNE4{KM7:TR?= M{\Od|czKGh? M3fL[oVvcGGwY3XzJIN6fG:2b4jpZ{Bm\m[nY4TzJI9nKFCLM1uvRWtVKHCjdHj3ZZkhcW6qaXLpeI9zew>? NIHjflAzOzZyMUC3OC=>
MDA-MB-231 NFXPT4RE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NXLId5NsOC5|IN88US=> Mmm5O|IhcA>? NXfEOJBs\W6qYX7j[ZMh[3m2b4TvfIlkKGWoZnXjeJMhd2ZiUFmzT{9CU1RicHH0bJdigSCrbnjpZol1d3K| MkXTNlM3ODFyN{S=
SY5Y MXzGeY5kfGmxbjDBd5NigQ>? NHewcGUyNjVxMj61M|Uh|ryP NGXWdGQzPCCq NIS4[IhqdmS3Y3XzJGcyyqClZXzsMYN6[2ynIHHydoV{fCCjbnSgZZBweHSxc3nz NIXxcGczOzN5OEO0NS=>
SKNBE(2c) M4\ENmZ2dmO2aX;uJGF{e2G7 MWqxMlUwOi53L{Wg{txO MmLkNlQhcA>? M{LERYlv\HWlZYOgS|HDqGOnbHytZ5lkdGViYYLy[ZN1KGGwZDDhdI9xfG:|aYO= NInaO3czOzN5OEO0NS=>
RD M2e3e2Fxd3C2b4Ppd{BCe3OjeR?= M{TCXlMhyrWP MoSxNVIhcA>? NWT2[GpJTE2VTx?= NH\s[2l{\W6|aYTpfoV{KFKGIHPlcIx{KHSxIFTPXE1qdmS3Y3XkJIFxd3C2b4Ppdy=> NUfDOFRxOjN|MEC4NFk>
TP5014 NELjSlJCeG:ydH;zbZMhSXO|YYm= NEDZNpo{KML3TR?= MX2xNkBp NE\Yb25FVVOR MWHz[Y5{cXSrenXzJHJFKGOnbHzzJJRwKESRWD3pcoR2[2WmIHHwc5B1d3Orcx?= NFHiUmszOzNyMEiwPS=>
HT1080 M4T6R2Fxd3C2b4Ppd{BCe3OjeR?= Ml3pN{DDvU1? MWSxNkBp NFS2eHdFVVOR NYLjVGs3e2Wwc3n0bZpmeyCURDDj[YxteyC2bzDEU3gucW6mdXPl[EBieG:ydH;zbZM> M2HjUVI{OzByOEC5
A549 Mlu1SpVv[3Srb36gRZN{[Xl? M{LBW|AuOy5|IN88US=> NULKb5dzPzJiaB?= NYnLVVhFcW6mdXPld{Bkd22ybHX0[UBld3ewcnXneYxifGmxbjDv[kBxSUuW NYrabJdTOjN{NUm1PVE>
HCC827 MWXGeY5kfGmxbjDBd5NigQ>? M4noNFAuOy5|IN88US=> MnXSO|IhcA>? NGPaR45qdmS3Y3XzJINwdXCuZYTlJIRwf26{ZXf1cIF1cW:wIH;mJJBCU1R? M1[5NlI{OjV7NUmx
H3122 M2rCfmZ2dmO2aX;uJGF{e2G7 MVGwMVMvOyEQvF2= NFv2RpQ4OiCq NYj5cGhqcW6mdXPld{Bkd22ybHX0[UBld3ewcnXneYxifGmxbjDv[kBxSUuW MlrENlMzPTl3OUG=
TALL-1 M4X4dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXmx5qCK|ryP M2PwV|ch\A>? MmTC[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 NVzDcZAzOjNyM{iyO|M>
HPB-ALL NFL5U29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3XNgKBkc7:TR?= MVO3JIQ> Mlvl[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 M2jae|I{ODN6Mkez
DND41 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUmx5qCK|ryP M3nJSlch\A>? NXT0XWd6\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 NXrMc2lOOjNyM{iyO|M>
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MOLT-16 M{[wR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PVelHjiIoQvF2= NGjyb4M4KGR? NUnhdpBO\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 M3jobVI{ODN6Mkez
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NCI-H929 M2L3ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlu3NE0zKM7:TR?= M{i2OVI1KGh? MmTJTWM2OD1yLkK1JO69VQ>? NVPu[pNjOjJ6MkmyN|Q>
KMS12-BM  NHK2dmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWe2bnN{OC1{IN88US=> MmDRNlQhcA>? NE\TcFJKSzVy78{eNkDPxE1? MWOyNlgzQTJ|NB?=
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518A2 Mn;nSpVv[3Srb36gRZN{[Xl? MXSwMlAxOeLCk{JihKnPxE1? MmH1NlQhcA>? NYXvZ5h3e3WycILld5NmeyCyaH;zdIhwenmuYYTpc44hd2ZicHjvd5Bp[XSrZInsJIlvd3OrdH;sJFMuc2mwYYPlJIRwf26|dILlZY0hfGG{Z3X0dy=> MXmyNVA1QDd6NR?=
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多くの細胞株試験データを見る場合、クリックしてください

体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[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.
細胞試験: [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)
動物試験:[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 Insoluble
Ethanol Insoluble
体内 順序で溶剤を入れること:
1% DMSO+30% polyethylene glycol+1% Tween 80
30 mg/mL

* 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

相関PI3K製品

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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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID