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(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
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SH-SY5Y MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHENE05KM7:TR?= NWPSXolqOjRxNEivO|IhcA>? NUHRbJlxcW6mdXPld{B1cW2nLTDhcoQh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgbY5pcWKrdHnvckBwdiCQQjDj[YxtKGe{b4f0bC=> MYqyOlIzPDZ6MR?=
SH-SY5Y  MVjBdI9xfG:|aYOgRZN{[Xl? NEHscJoyKM7:TR?= MXewMlUuOjRiaB?= Mm\Gd4Vve2m2aYrld{Bv\XW{b3LsZZN1d22jIHPlcIx{KHSxIHTvfI9zfWKrY3nuMYlv\HWlZXSgZZBweHSxc3nz MX[yOlIzPDZ6MR?=
G 35 SC MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3S1flAvODVvMkCg{txO MU[yOE84OiCq NW\kRmhCTE2VTx?= NFTJ[YZqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 M3rqd|I3OTJzMkWx
G 38 SC NIrjdJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M331elAvODVvMkCg{txO MV:yOE84OiCq NWjiPXVpTE2VTx?= M3;KfIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? NWXNXnhXOjZzMkGyOVE>
G 40 SC MnfiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HWbVAvODVvMkCg{txO MY[yOE84OiCq NH\xdIFFVVOR MWPpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueIx6 M4jjT|I3OTJzMkWx
G 35 DC NVvHV3pxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2P5UVAvODVvMkCg{txO M4DscVI1Nzd{IHi= NGXLOJBFVVOR M{K3XolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? NHvVSlMzPjF{MUK1NS=>
G 38 DC M3rFbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXZTVkxNjB3LUKwJO69VQ>? Mnn6NlQwPzJiaB?= MVvEUXNQ MWDpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueIx6 M3jXPFI3OTJzMkWx
G 40 DC MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV:wMlA2NTJyIN88US=> NYDCbYluOjRxN{KgbC=> MXvEUXNQ NEjGbXlqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 NUjMUVVyOjZzMkGyOVE>
RD M{jiRmFxd3C2b4Ppd{BCe3OjeR?= NV7ZT5F7OS9zLkWvNkDPxE1? NEO5OlY4OiCq MmTjbY5lfWOnczDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCJQV7UOlE> NFLD[pczPTd2OUO3PC=>
TE381.T NYmxbnJ[SXCxcITvd4l{KEG|c3H5 NVPjcFNVOS9zLkWvNkDPxE1? NGHl[I44OiCq MnXWbY5lfWOnczDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCJQV7UOlE> MoPmNlU4PDl|N{i=
RMS13 NYDlZXg2SXCxcITvd4l{KEG|c3H5 M1fUN|EwOS53L{Kg{txO NEPpTW04OiCq M37mNIlv\HWlZYOgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiR1HOWFYy NWT4V5NJOjV5NEmzO|g>
RH30  M3\KeGFxd3C2b4Ppd{BCe3OjeR?= MX:xM|EvPS9{IN88US=> MXy3NkBp NXTT[ZMzcW6mdXPld{BieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDHRW5VPjF? MYCyOVc1QTN5OB?=
VJ NYruUYZvSXCxcITvd4l{KEG|c3H5 M13rOFEwOS53L{Kg{txO NHrWd5o4OiCq M{ezXYlv\HWlZYOgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiR1HOWFYy M1LFbVI2PzR7M{e4
HS578T MmH6R4VtdCCYaXHibYxqfHliQYPzZZk> NWLDR5ZDOC1|IN88US=> NFL6SZk4OiCq M4DCd4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MnvhNlU4OjF2MUm=
BT549 M17OOWNmdGxiVnnhZoltcXS7IFHzd4F6 MUCwMVMh|ryP MmPYO|IhcA>? NH\yOFNqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MVeyOVczOTRzOR?=
MDA-MB-231 MXPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M3rSTFAuOyEQvF2= MVK3NkBp M2rNSYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NV31d4hjOjV5MkG0NVk>
MDA-MB-468 MkT4R4VtdCCYaXHibYxqfHliQYPzZZk> NE\HWIIxNTNizszN MYq3NkBp NWjTc3hbcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MnPKNlU4OjF2MUm=
MDA-MB-436 MoTtR4VtdCCYaXHibYxqfHliQYPzZZk> NVHifpp3OC1|IN88US=> NWXjeIh7PzJiaB?= NUHuTlQ{cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NHrreIUzPTd{MUSxPS=>
SUM149PT MkLNR4VtdCCYaXHibYxqfHliQYPzZZk> NFPh[3IxNTNizszN MUC3NkBp NEjmWJFqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NEH1PJIzPTd{MUSxPS=>
MDA-MB-468 NIDKbG5HfW6ldHnvckBCe3OjeR?= NGXhOnoxNjBzLUGwJO69VQ>? MlLGNlQhcA>? MVHkc5dvemWpdXzheIV{KHSqZTDs[ZZmdHNib3[g{tIuXHKFUEGsJIMuVXmlIHHu[EBkgWOuaX6gSUBxem:2ZXnud:Kh NVrJ[5NDOjV5MkG0NVk>
MDA-MB-231 Mkj4SpVv[3Srb36gRZN{[Xl? NFvxeHYxNjBzLUGwJO69VQ>? Mn;ONlQhcA>? NY\KXVU2\G:5boLl[5Vt[XSnczD0bIUhdGW4ZXzzJI9nKM7{LWTyR3AyNCClLV35Z{BidmRiY4njcIlvKEVicILveIVqdnQEoB?= M{KybFI2PzJzNEG5
HS578T NUm3UGVyTnWwY4Tpc44hSXO|YYm= NHnm[GgxNjBzLUGwJO69VQ>? NEXZTVIzPCCq MkPr[I94dnKnZ4XsZZRmeyC2aHWgcIV3\Wy|IH;mJO6zNVS{Q2CxMEBkNU27YzDhcoQh[3mlbHnuJGUheHKxdHXpcpPDqA>? MlrsNlU4OjF2MUm=
SW872 NXfMSnRMTnWwY4Tpc44hSXO|YYm= NV22OIYzOC5yMT2wMlUh|ryP NF;rZ|czPCCq MoDJdoVlfWOnczDBT3QheGixc4Doc5J6dGG2aX;uJEhxSUuWKTDhcoQhPEWEUEGgdIhwe3Cqb4L5cIF1cW:wIDjwOGVDWDFrIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{wrC= M3\3WlI1Pjl3NkOy
SW982 MXXGeY5kfGmxbjDBd5NigQ>? MUmwMlAyNTBwNTFOwG0> NVSzdmtSOjRiaB?= MoHPdoVlfWOnczDBT3QheGixc4Doc5J6dGG2aX;uJEhxSUuWKTDhcoQhPEWEUEGgdIhwe3Cqb4L5cIF1cW:wIDjwOGVDWDFrIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{wrC= M1nL[|I1Pjl3NkOy
SW872 NUjCbFd3SXCxcITvd4l{KEG|c3H5 NHL4flMxNjBzLUCuOUDPxE1? NIW3U5Y1QCCq MWPpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NVG0Znk5OjR4OUW2N|I>
SW982 MmXVRZBweHSxc3nzJGF{e2G7 MoXONE4xOS1yLkWg{txO NVXFVm5[PDhiaB?= NH;KUFhqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 MUiyOFY6PTZ|Mh?=
AGS HG NUHvWIp2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DLWGlEPTB;MD62PEDDuSByLkCzNUDPxE1? NH;ndmczPDV7N{S3PC=>
AGS LG MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXhTWM2OD1yLkC1JOKyKDBwMECxJO69VQ>? NX\NUJN4OjR3OUe0O|g>
HGC27 HG NHvBPJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfUW|VKSzVyPUCuN|ghyrFiMD6wNlIh|ryP MlnFNlQ2QTd2N{i=
HGC27 LG NU\Z[JJoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlvyTWM2OD1yLkCyJOKyKDBwMEC0JO69VQ>? MnnRNlQ2QTd2N{i=
MKN45 HG M1;NbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTFwMEGgxtEhOC5yNUGg{txO NWC5PJQyOjR3OUe0O|g>
MKN45 LG MoPkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rD[WlEPTB;MD64O{DDuSByLkCzNEDPxE1? MUGyOFU6PzR5OB?=
NUGC4 HG Mnv3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXqdVBKSzVyPUG0MlAhyrFiMz65NVMh|ryP M3fhXlI1PTl5NEe4
NUGC4 LG NULKUoJbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjSeW9KSzVyPUG0MlAhyrFiNT6zNlEh|ryP MXiyOFU6PzR5OB?=
A549 NGHFZ4FHfW6ldHnvckBCe3OjeR?= M1q4S|AvOjVxMD61M|Eh|ryP NHjVWmEzPCCq NUfOeXNncW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|bHnnbJRtgQ>? Mki0NlQ{PTF2MkW=
H460 NITaRoNHfW6ldHnvckBCe3OjeR?= MXmwMlI2NzBwNT:xJO69VQ>? M1jNUVI1KGh? MVfpcohq[mm2czDBb5QheGixc4Doc5J6dGG2aX;uJJNtcWeqdHz5 MneyNlQ{PTF2MkW=
H661 MVzGeY5kfGmxbjDBd5NigQ>? M{ftVlAvOjVxMD61M|Eh|ryP M4KweFI1KGh? MkDqbY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7 M3zsNlI1OzVzNEK1
SAS Mo\pSpVv[3Srb36gRZN{[Xl? NGq1bIgxNjJ3L{CuOU8yKM7:TR?= MXiyOEBp MonlbY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7 NX3nVFZJOjR|NUG0NlU>
UT5 MoPESpVv[3Srb36gRZN{[Xl? MnTRNE4zPS9yLkWvNUDPxE1? NXzCU4pyOjRiaB?= NWLyb21RcW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|aXfubYZq[2GwdHz5 NXvyb3RNOjR|NUG0NlU>
FaDu M4XMNWZ2dmO2aX;uJGF{e2G7 NHHGOIYxNjJ3L{CuOU8yKM7:TR?= MkTpNlQhcA>? MYTpcohq[mm2czDBb5QheGixc4Doc5J6dGG2aX;uJJNq\26rZnnjZY51dHl? M2\GXVI1OzVzNEK1
RD MnjGRZBweHSxc3nzJGF{e2G7 Ml3INU8yNjVxMjFOwG0> MkPrO|IhcA>? MVvEUXNQ M125eYlv\HWlZYOgZ4F{eGG|ZT3k[ZBmdmSnboSgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiVV:xNlY> M{foe|I{Pjh2OUK1
TE671 M1rrbmFxd3C2b4Ppd{BCe3OjeR?= M37MZlEwOS53L{Kg{txO MkDpO|IhcA>? NFHEUJlFVVOR M4fhbYlv\HWlZYOgZ4F{eGG|ZT3k[ZBmdmSnboSgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiVV:xNlY> NVHY[YdsOjN4OES5NlU>
RH30  M2\kdmFxd3C2b4Ppd{BCe3OjeR?= NXe1dmh6OS9zLkWvNkDPxE1? NGmyUIk4OiCq NFvjS5hFVVOR M2nscolv\HWlZYOgZ4F{eGG|ZT3k[ZBmdmSnboSgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiVV:xNlY> MViyN|Y5PDl{NR?=
RMS13 NVfyR5ZxSXCxcITvd4l{KEG|c3H5 Ml7DNU8yNjVxMjFOwG0> NYjhOYt1PzJiaB?= M1nkfmROW09? NVjYT41xcW6mdXPld{Bk[XOyYYPlMYRmeGWwZHXueEBieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDVU|EzPg>? NE[1ZVkzOzZ6NEmyOS=>
SUM149PT M{C5WGNmdGxiVnnhZoltcXS7IFHzd4F6 M2XQPVAvOyEQvF2= M3LyUVczKGh? M2nLR4VvcGGwY3XzJIN6fG:2b4jpZ{Bm\m[nY4TzJI9nKFCLM1uvRWtVKHCjdHj3ZZkhcW6qaXLpeI9zew>? NIHnNHczOzZyMUC3OC=>
MDA-MB-468 NUDD[HFTS2WubDDWbYFjcWyrdImgRZN{[Xl? MmW4NE4{KM7:TR?= NGm2NIg4OiCq MUHlcohidmOnczDjfZRwfG:6aXOg[YZn\WO2czDv[kBRUTONL1HLWEBx[XSqd3H5JIlvcGmkaYTvdpM> MoWzNlM3ODFyN{S=
MDA-MB-231 M2PwVWNmdGxiVnnhZoltcXS7IFHzd4F6 MkHxNE4{KM7:TR?= NEDnZW44OiCq MWLlcohidmOnczDjfZRwfG:6aXOg[YZn\WO2czDv[kBRUTONL1HLWEBx[XSqd3H5JIlvcGmkaYTvdpM> NX3oW3BoOjN4MEGwO|Q>
SY5Y NUTjfXlrTnWwY4Tpc44hSXO|YYm= M2O5Z|EvPS9{LkWvOUDPxE1? M3noRlI1KGh? MUnpcoR2[2W|IFexxsBk\WyuLXP5Z4xmKGG{cnXzeEBidmRiYYDvdJRwe2m| M4jwNFI{Ozd6M{Sx
SKNBE(2c) MWDGeY5kfGmxbjDBd5NigQ>? NWrIVnlNOS53L{KuOU82KM7:TR?= NEjCWHQzPCCq NWjHSZZCcW6mdXPld{BIOcLiY3XscE1kgWOuZTDhdpJme3RiYX7kJIFxd3C2b4Ppdy=> MUmyN|M4QDN2MR?=
RD M3e2ZmFxd3C2b4Ppd{BCe3OjeR?= M1;oflMhyrWP MYixNkBp M13kdWROW09? MkfHd4Vve2m2aYrld{BTTCClZXzsd{B1dyCGT2itbY5lfWOnZDDhdI9xfG:|aYO= MUKyN|MxODhyOR?=
TP5014 MnH1RZBweHSxc3nzJGF{e2G7 MV:zJOK2VQ>? NF[3dXQyOiCq Mk\jSG1UVw>? NHPtWml{\W6|aYTpfoV{KFKGIHPlcIx{KHSxIFTPXE1qdmS3Y3XkJIFxd3C2b4Ppdy=> NEm2PJozOzNyMEiwPS=>
HT1080 MYHBdI9xfG:|aYOgRZN{[Xl? MkLxN{DDvU1? NWjZXlBYOTJiaB?= MVfEUXNQ MkGwd4Vve2m2aYrld{BTTCClZXzsd{B1dyCGT2itbY5lfWOnZDDhdI9xfG:|aYO= NF;xR3UzOzNyMEiwPS=>
A549 NX7RUI9WTnWwY4Tpc44hSXO|YYm= MlXuNE0{NjNizszN MV63NkBp NF7XUHVqdmS3Y3XzJINwdXCuZYTlJIRwf26{ZXf1cIF1cW:wIH;mJJBCU1R? NVvGT|M5OjN{NUm1PVE>
HCC827 MXPGeY5kfGmxbjDBd5NigQ>? MW[wMVMvOyEQvF2= MYi3NkBp NWTDO4Q4cW6mdXPld{Bkd22ybHX0[UBld3ewcnXneYxifGmxbjDv[kBxSUuW NULwRox[OjN{NUm1PVE>
H3122 NHvmdlFHfW6ldHnvckBCe3OjeR?= MnLrNE0{NjNizszN NGD2flE4OiCq MXfpcoR2[2W|IHPvcZBt\XSnIHTve45z\We3bHH0bY9vKG:oIIDBT3Q> M4TjTVI{OjV7NUmx
TALL-1 M4LTNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXBNgKBkc7:TR?= MlHxO{Bl MXTk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> Mn\VNlMxOzh{N{O=
HPB-ALL NW\SWHFxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGSyW|Iy6oDLzszN MoLlO{Bl M{Pz[oRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? MYOyN|A{QDJ5Mx?=
DND41 MlXqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\SSXYy6oDLzszN MnO4O{Bl NYLJNJl3\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 M3HaPVI{ODN6Mkez
SUP-T1 NGXX[4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHzNgKBkc7:TR?= NETseWs4KGR? MWPk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> MV[yN|A{QDJ5Mx?=
PEER MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfNRXZ[OeLCid88US=> NYLxe|d3PyCm NIfYbVNl\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? Ml\6NlMxOzh{N{O=
ALL-SIL NF\RNFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTYNgKBkc7:TR?= NXv6[lJ3PyCm MYjk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> Mn3lNlMxOzh{N{O=
KE37 NGDiOGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvGT4cy6oDLzszN NEfjbo44KGR? MoPy[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 M4\uSFI{ODN6Mkez
Karpas-45 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nYdVHjiIoQvF2= MX23JIQ> Mn6w[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 MkX6NlMxOzh{N{O=
RPMI-8402 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnKbVky6oDLzszN NH7Xd484KGR? MUXk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> NIWyPGQzOzB|OEK3Ny=>
Jurkat Moe0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoC0NgKBkc7:TR?= MnjNO{Bl NX3CV|R4\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 MVeyN|A{QDJ5Mx?=
MOLT-4 M1fqXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULTfVhnOeLCid88US=> MX:3JIQ> Mojx[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 NI\qe4MzOzB|OEK3Ny=>
PF-382 NX3tcGh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LON|HjiIoQvF2= NF7ae4k4KGR? MYnk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> M3PFcFI{ODN6Mkez
CCRF-CEM MkPOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXOOoQy6oDLzszN NGPneHc4KGR? NEi4OYNl\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? NHXYV3UzOzB|OEK3Ny=>
LOUCY M1e3ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XHblHjiIoQvF2= M2XUN|ch\A>? M2\3eIRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? NEjQUlgzOzB|OEK3Ny=>
MOLT-16 NWLTTY1DT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVmx5qCK|ryP MX:3JIQ> NVvPUJhZ\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 MUKyN|A{QDJ5Mx?=
MM1S NXPXNG53T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHNdYoxNTJizszN NX\2SFk{OjRiaB?= MYPJR|UxRTBwNTFOwG0> M{DzW|IzQDJ7MkO0
NCI-H929 MlLBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVP6[4RZOC1{IN88US=> M{LPNFI1KGh? NV74V|c4UUN3ME2wMlI2KM7:TR?= MY[yNlgzQTJ|NB?=
KMS12-BM  NIDa[WFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFP4WVgxNTJizszN Mm\uNlQhcA>? MUjJR|Ux97zgMjFOwG0> NVjOfJUyOjJ6MkmyN|Q>
MDA-MB-436 MlfQSpVv[3Srb36gRZN{[Xl? MYmxJO69VQ>? Mon5NlQhcA>? M{TrO5Jm\HWlZYOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2S= MlTUNlI1QDh3OUC=
SUM149PT M{nXW2Z2dmO2aX;uJGF{e2G7 M3znU|Eh|ryP NXq1U5RlOjRiaB?= MofUdoVlfWOnczD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVB?= NXy0XmF5OjJ2OEi1PVA>
SUM1315MO2 NUC1RZMyTnWwY4Tpc44hSXO|YYm= NHLTWmIyKM7:TR?= MV[yOEBp MlPndoVlfWOnczD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVB?= Mkn4NlI1QDh3OUC=
HCC1937 MonBSpVv[3Srb36gRZN{[Xl? NV7v[nl1OSEQvF2= NXLZN3RqOjRiaB?= MWXy[YR2[2W|IITo[UBxcG:|cHjvdplt[XSrb36gc4YhSUuW MmTmNlI1QDh3OUC=
HCC827 M4K4RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXiwMVMh|ryP NVHwZm1PPzJiaB?= MnrXTWM2OD1yLkOg{txO M{LnOVIyOjJyNEe0
PC-9  M{nN[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPje2oxNTNizszN MkDZO|IhcA>? NEXHUJpKSzVyPUCuPEDPxE1? MmPHNlEzOjB2N{S=
LN229 MnW5SpVv[3Srb36gRZN{[Xl? M2D6fVEh|ryP MonhOFghcA>? NUPFb4NVcW6mdXPld{BifXSxcHjh[49{d22nIH\vdo1ifGmxbh?= NGLBV4IzOTB4Mkm5Ny=>
U87 NFzzNpNHfW6ldHnvckBCe3OjeR?= M4S4c|Eh|ryP NF7YUYs1QCCq NVfXRmxMcW6mdXPld{BifXSxcHjh[49{d22nIH\vdo1ifGmxbh?= MWCyNVA3Ojl7Mx?=
U373 M2jYb2Z2dmO2aX;uJGF{e2G7 NX7Ie|JxOSEQvF2= MYO0PEBp M3\jbIlv\HWlZYOgZZV1d3CqYXfvd49u\SCob4LtZZRqd25? NWLqdVRWOjFyNkK5PVM>
SF767 MkCwSpVv[3Srb36gRZN{[Xl? MonnNUDPxE1? MUG0PEBp NGjFWGJqdmS3Y3XzJIF2fG:yaHHnc5NwdWViZn;ycYF1cW:w NGnTepkzOTB4Mkm5Ny=>
Mel-Juso NVjSTGxuS2WubDDWbYFjcWyrdImgRZN{[Xl? MoHGNE4xOeLCk{Gw5qCK|ryP MlvVO|IhcA>? NYf0eHpHcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MknnNlExPDh5OEW=
518A2  MlnMR4VtdCCYaXHibYxqfHliQYPzZZk> NF3LSZoxNjBz4pETNVDjiIoQvF2= NUDibmloPzJiaB?= MlLobY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MnqyNlExPDh5OEW=
Mel-Juso  NWK0NVFVTnWwY4Tpc44hSXO|YYm= NUKzVohNOC5yMEJihLMy6oDLzszN M2\nUlI1KGh? MYPzeZBxemW|c3XzJJBpd3OyaH;yfYxifGmxbjDv[kBxcG:|cHjheIllgWxiaX7vd4l1d2xiMz3rbY5ie2ViZH;3cpN1emWjbTD0ZZJo\XS| MUCyNVA1QDd6NR?=
518A2 NFKx[4pHfW6ldHnvckBCe3OjeR?= NYPIe5oyOC5yMEJihLMy6oDLzszN NX;DTnlUOjRiaB?= MlXwd5VxeHKnc4Pld{BxcG:|cHjvdplt[XSrb36gc4YheGixc4DoZZRq\HmuIHnuc5NqfG:uIEOtb4lv[XOnIHTve45{fHKnYX2geIFz\2W2cx?= MXSyNVA1QDd6NR?=
PC3  M{DtTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHRR2pqOjSq NEfxcWdIUTVywrC9JFExOCCwTR?= NYXTR2tJOjB3NUGwOlE>
U87MG NGexVYlHfW6ldHnvckBCe3OjeR?= NI[ycowxNjFvMTFOwG0> NXXxNJhEOjUkgJnoxsA> NIHSenhFVVOR NXLtdJRxcW6qaXLpeJMhWEl|Sz3t[YRq[XSnZDDzbYdv[Wyrbne= NHj2cHkyQTZ|M{[4Ny=>
U138MG Mn[xSpVv[3Srb36gRZN{[Xl? M3T1O|AvOS1zIN88US=> MlXoNlTjiImqwrC= M{fHbWROW09? NHrNRlRqdmirYnn0d{BRUTONLX3l[IlifGWmIIPp[45idGmwZx?= NH\aTpIyQTZ|M{[4Ny=>
U118MG M{XOTmZ2dmO2aX;uJGF{e2G7 M4fKV|AvOS1zIN88US=> MWmyOQKBkWkEoB?= Mo\RSG1UVw>? MXzpcohq[mm2czDQTVNMNW2nZHnheIVlKHOrZ37hcIlv\w>? NIf4d4MyQTZ|M{[4Ny=>
U87MG MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37EPGlEPTB;MD6xOEDPxE1? NEPB[YsyQTV6NEKyOy=>
IGROV-1 M{GyeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTBwME[g{txO NYHidodzOTl3OESyNlc>
DETROIT562 NELteHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTBwMUOg{txO MYCxPVU5PDJ{Nx?=
PC3  NIq1dFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfTfHdKSzVyPUCuNVAh|ryP Mm\1NVk2QDR{Mke=
SKOV-3 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnPUYxKSzVyPUCuNVIh|ryP Mm\tNVk2QDR{Mke=
HUVEC Ml7sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTzTWM2OD1yLkC4JO69VQ>? MmX2NVk2QDR{Mke=
UCH-1  M{CxNGZ2dmO2aX;uJGF{e2G7 M3v2RVAuPSEQvF2= M{PIZolvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiYn;0bEBCU1RiYX7kJI1VV1JiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MYmxPVUzQDR2MR?=
UCH-1  M1;PfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjse|lnOC5yMT2xNEDPxE1? MlXuOkBl NWq4dowxcW6qaXLpeJMheHKxbHnm[ZJifGmxbjDkc5NmKGSncHXu[IVvfGy7 MYCxPVUzQDR2MR?=
UCH-1  M4HoVWFxd3C2b4Ppd{BCe3OjeR?= NV6xfJZ1OC5zLUGwJO69VQ>? MkG4NlQhcA>? MlvKSG1UVw>? NXP1WFBZcW6mdXPld{BieG:ydH;zbZM> NGW3UFQyQTV{OES0NS=>

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 slightly soluble or insoluble
Ethanol slightly soluble or 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