PI-103

For research use only. Not for use in humans.

目录号:S1038

PI-103 Chemical Structure

CAS No. 371935-74-9

PI-103 是一种多靶点 PI3K 抑制剂,在无细胞试验中作用于p110α/β/δ/γIC50为 2 nM/3 nM/3 nM/15 nM,对 mTOR/DNA-PK的作用较小,IC50为30 nM/23 nM。PI-103 可诱导小鼠T细胞淋巴瘤的凋亡。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1103.62 现货
RMB 1211.49 现货
RMB 2226.16 现货
RMB 3023.41 现货
RMB 4832.1 现货
RMB 6470.64 现货
RMB 11220.3 现货
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客户使用Selleck生产的PI-103发表文献81篇:

产品安全说明书

PI3K抑制剂选择性比较

生物活性

产品描述 PI-103 是一种多靶点 PI3K 抑制剂,在无细胞试验中作用于p110α/β/δ/γIC50为 2 nM/3 nM/3 nM/15 nM,对 mTOR/DNA-PK的作用较小,IC50为30 nM/23 nM。PI-103 可诱导小鼠T细胞淋巴瘤的凋亡。
特性 PI-103是第一个有效合成的mTOR抑制剂。
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
体外研究

PI-103有效抑制蛋白激酶mTOR的对apamycin敏感的(mTORC1)和对rapamycin不敏感的(mTORC2)复合物。PI-103是第三大多靶点PI3K抑制剂。[1]PI-103抑制组成型和生长因子诱导的PI3K/Akt和mTORC1激活。在胚细胞中,尤其在白血病干细胞中,PI-103抑制白血病细胞增殖和白血病前体细胞形成集落,且诱导线粒体细胞凋亡。PI-103抑制p110α的效果比抑制p110β强200倍以上。PI-103也有效抑制脂肪细胞中的PI(3,4)P2和PIP3,及肌管中的PIP3。与LY294002抑制Akt磷酸化的IC50值相比,PI-103抑制Akt磷酸化的IC50值要低到100倍。PI-103保护动物使其免受胰岛素刺激而导致的血糖降低。PI-103和etoposide联用作用于胚细胞和不成熟的白血病细胞有增强凋亡的功效。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
UCH-1  MVvBdI9xfG:|aYOgRZN{[Xl? MmPkNE4yNTFyIN88US=> NEPOSYIzPCCq MoraSG1UVw>? NX3zdlRYcW6mdXPld{BieG:ydH;zbZM> NFuweGk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUWyPFQ1OSd-MUm1Nlg1PDF:L3G+
UCH-1  M1L5Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfzbZM1OC5yMT2xNEDPxE1? M2PFSVYh\A>? NYDqWHh3cW6qaXLpeJMheHKxbHnm[ZJifGmxbjDkc5NmKGSncHXu[IVvfGy7 NGPNZ5U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUWyPFQ1OSd-MUm1Nlg1PDF:L3G+
UCH-1  MV;GeY5kfGmxbjDBd5NigQ>? NULTPIo4OC13IN88US=> MYLpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKGKxdHigRWtVKGGwZDDtWG9TKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NE\hRYM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUWyPFQ1OSd-MUm1Nlg1PDF:L3G+
HUVEC M{TQWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTBwMEig{txO NWXNNnkzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm1PFQzOjdpPkG5OVg1OjJ5PD;hQi=>
SKOV-3 M3\rWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfKV4NKSzVyPUCuNVIh|ryP NXTtdGRERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm1PFQzOjdpPkG5OVg1OjJ5PD;hQi=>
PC3  MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4j6cWlEPTB;MD6xNEDPxE1? NY\rSot6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm1PFQzOjdpPkG5OVg1OjJ5PD;hQi=>
DETROIT562 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjDTWM2OD1yLkGzJO69VQ>? NV\NT5R7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm1PFQzOjdpPkG5OVg1OjJ5PD;hQi=>
IGROV-1 M4TtdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPoVnhKSzVyPUCuNFYh|ryP MmfEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl3OESyNlcoRjF7NUi0NlI4RC:jPh?=
U87MG NWTKbnpIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTBwMUSg{txO NH3VOII9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUW4OFIzPyd-MUm1PFQzOjd:L3G+
U118MG M1nKbmZ2dmO2aX;uJGF{e2G7 NUPuPYpqOC5zLUGg{txO MUCyOQKBkWkEoB?= NYfufWN3TE2VTx?= NH[zRlRqdmirYnn0d{BRUTONLX3l[IlifGWmIIPp[45idGmwZx?= MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTZ|M{[4N{c,OTl4M{O2PFM9N2F-
U138MG MmfQSpVv[3Srb36gRZN{[Xl? MX6wMlEuOSEQvF2= MmrzNlTjiImqwrC= NF75XVBFVVOR NGPZcGxqdmirYnn0d{BRUTONLX3l[IlifGWmIIPp[45idGmwZx?= M3LFPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7NkOzOlg{Lz5zOU[zN|Y5OzxxYU6=
U87MG MmrtSpVv[3Srb36gRZN{[Xl? NIXjVVYxNjFvMTFOwG0> M2LPXlI16oDLaNMg M1f5T2ROW09? NGPoOYxqdmirYnn0d{BRUTONLX3l[IlifGWmIIPp[45idGmwZx?= MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTZ|M{[4N{c,OTl4M{O2PFM9N2F-
PC3  NWDIc3c6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MViyOIg> NIKzZlhIUTVywrC9JFExOCCwTR?= MnjEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB3NUGwOlEoRjJyNUWxNFYyRC:jPh?=
518A2 Ml7MSpVv[3Srb36gRZN{[Xl? NITjW2oxNjByMfMAl|HjiIoQvF2= MoTONlQhcA>? Mmfnd5VxeHKnc4Pld{BxcG:|cHjvdplt[XSrb36gc4YheGixc4DoZZRq\HmuIHnuc5NqfG:uIEOtb4lv[XOnIHTve45{fHKnYX2geIFz\2W2cx?= NV;1bW5oRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGwOFg4QDVpPkKxNFQ5Pzh3PD;hQi=>
Mel-Juso  NH[3e2FHfW6ldHnvckBCe3OjeR?= MoDWNE4xODIkgKOx5qCK|ryP MUOyOEBp NFnKZYh{fXCycnXzd4V{KHCqb4PwbI9zgWyjdHnvckBw\iCyaH;zdIhifGmmeXygbY5we2m2b3ygN{1scW6jc3Wg[I94dnO2cnXhcUB1[XKpZYTz MorkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjFyNEi3PFUoRjJzMES4O|g2RC:jPh?=
518A2  NIDOdGVE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M3vsdlAvODIkgKOxNQKBkc7:TR?= NGX4WIg4OiCq NFq4NYlqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NXjxWXY2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGwOFg4QDVpPkKxNFQ5Pzh3PD;hQi=>
Mel-Juso NVG2XmVJS2WubDDWbYFjcWyrdImgRZN{[Xl? MonQNE4xOeLCk{Gw5qCK|ryP NVjZT|JNPzJiaB?= NF;zXFhqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 M{PjOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzMES4O|g2Lz5{MUC0PFc5PTxxYU6=
SF767 MWLGeY5kfGmxbjDBd5NigQ>? MkfrNUDPxE1? M1TLbFQ5KGh? NHvQVFFqdmS3Y3XzJIF2fG:yaHHnc5NwdWViZn;ycYF1cW:w MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTB4Mkm5N{c,OjFyNkK5PVM9N2F-
U373 M3HJeWZ2dmO2aX;uJGF{e2G7 MX6xJO69VQ>? NF3FTXU1QCCq NF3rNlJqdmS3Y3XzJIF2fG:yaHHnc5NwdWViZn;ycYF1cW:w MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTB4Mkm5N{c,OjFyNkK5PVM9N2F-
U87 MkPRSpVv[3Srb36gRZN{[Xl? M2XReFEh|ryP NHGzOYY1QCCq NF;4e4lqdmS3Y3XzJIF2fG:yaHHnc5NwdWViZn;ycYF1cW:w M2LqOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzME[yPVk{Lz5{MUC2Nlk6OzxxYU6=
LN229 Mm\5SpVv[3Srb36gRZN{[Xl? MUmxJO69VQ>? NWnIT2FQPDhiaB?= Mke3bY5lfWOnczDheZRweGijZ3;zc41mKG[xcn3heIlwdg>? M{m4WlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzME[yPVk{Lz5{MUC2Nlk6OzxxYU6=
PC-9  Ml3tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTlZ28xNTNizszN MnrRO|IhcA>? MV\JR|UxRTBwODFOwG0> MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTJ{MES3OEc,OjF{MkC0O|Q9N2F-
HCC827 NEXCNllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWqwMVMh|ryP MnjuO|IhcA>? M1S1VWlEPTB;MD6zJO69VQ>? M1PSXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzMkKwOFc1Lz5{MUKyNFQ4PDxxYU6=
HCC1937 MVHGeY5kfGmxbjDBd5NigQ>? MWOxJO69VQ>? NVrk[JQ2OjRiaB?= MYjy[YR2[2W|IITo[UBxcG:|cHjvdplt[XSrb36gc4YhSUuW NHPJZ4c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkS4PFU6OCd-MkK0PFg2QTB:L3G+
SUM1315MO2 Mk[1SpVv[3Srb36gRZN{[Xl? NVnJe|JsOSEQvF2= M4LWXVI1KGh? NEXrRmtz\WS3Y3XzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvU MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjR6OEW5NEc,OjJ2OEi1PVA9N2F-
SUM149PT M4jQ[mZ2dmO2aX;uJGF{e2G7 MX2xJO69VQ>? M3r5R|I1KGh? M4PBUZJm\HWlZYOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2S= MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjR6OEW5NEc,OjJ2OEi1PVA9N2F-
MDA-MB-436 MVrGeY5kfGmxbjDBd5NigQ>? M1P3e|Eh|ryP NX7McnhiOjRiaB?= NV7rdXlSemWmdXPld{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWC=> MlrHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ2OEi1PVAoRjJ{NEi4OVkxRC:jPh?=
KMS12-BM  M1Hkemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDqOWMxNTJizszN Mnz6NlQhcA>? Ml;qTWM2OO,:nkKg{txO NIrJTWc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkiyPVI{PCd-MkK4NlkzOzR:L3G+
NCI-H929 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4f3S|AuOiEQvF2= Mme5NlQhcA>? M3T2eWlEPTB;MD6yOUDPxE1? M4jjVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OEK5NlM1Lz5{MkiyPVI{PDxxYU6=
MM1S M3X1eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjGdnpIOC1{IN88US=> MWKyOEBp NXX4[pdOUUN3ME2wMlUh|ryP NFrrN4E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkiyPVI{PCd-MkK4NlkzOzR:L3G+
MOLT-16 M4jJT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVztfWh[OeLCid88US=> NYe4V3QxPyCm MY\k[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> MlHrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyM{iyO|MoRjJ|MEO4Nlc{RC:jPh?=
LOUCY M{fTTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLlNgKBkc7:TR?= MXu3JIQ> NHyxOIdl\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? M4O1elxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MEO4Nlc{Lz5{M{CzPFI4OzxxYU6=
CCRF-CEM MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX22bZVGOeLCid88US=> MXe3JIQ> MlnF[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzB|OEK3N{c,OjNyM{iyO|M9N2F-
PF-382 NIraeHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnt[lVlOeLCid88US=> MnTuO{Bl NV3nTFlS\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 MmrTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyM{iyO|MoRjJ|MEO4Nlc{RC:jPh?=
MOLT-4 MmjTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfoNgKBkc7:TR?= M1rBOVch\A>? M1\jboRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? MofFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyM{iyO|MoRjJ|MEO4Nlc{RC:jPh?=
Jurkat MmewS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnxcm12OeLCid88US=> MofvO{Bl Mm\j[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 NHjmW5k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{CzPFI4Oyd-MkOwN|gzPzN:L3G+
RPMI-8402 NWT2bJZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXGx5qCK|ryP M3TvUVch\A>? NYK5d21O\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 M3\PSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MEO4Nlc{Lz5{M{CzPFI4OzxxYU6=
Karpas-45 NXLXdpFGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjwdJoy6oDLzszN M3q2cVch\A>? Mlfa[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 M4[zdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MEO4Nlc{Lz5{M{CzPFI4OzxxYU6=
KE37 Mnj4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzXNgKBkc7:TR?= MYC3JIQ> Mo\B[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 Mor6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyM{iyO|MoRjJ|MEO4Nlc{RC:jPh?=
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MG 63 (6-TG R) M4DjbJFJXFNiYYPzZZk> Mmf3dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE2JIE[zJEg3NVSJIGKpJINmdGy| M2f3fFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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A673 NETmOYRyUFSVIHHzd4F6 NXG0cYlveUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhSTZ5MzDj[Yxteyl? NXLUZpdvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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SJ-GBM2 MlX4dWhVWyCjc4PhfS=> NYfzUFQ1eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhW0pvR1LNNkBk\Wyucx?= MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
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Saos-2 MXrxTHRUKGG|c3H5 NVzNbVhueUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhW2Gxcz2yJINmdGy| MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
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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
体内研究 当肿瘤达到50-100 mm3时, 动物随机分组,用PI-103处理,及空白对照处理。PI-103具有明显活性,处理18天后,使肿瘤平均尺寸降低4倍。用PI-103处理的鼠在发病前或验尸时没有明显毒性现象(根据体重,食物和水摄取情况,活动性, 及常规检查)。处理的肿瘤Akt和S6磷酸化水平明显降低,伴随着p110α和mTOR被抑制。PI-103处理神经胶质移植瘤,抑制生长。[2]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
- 合并

p110激酶实验:

加入含10 μCi γ-32P-ATP 的ATP开始反应,终浓度为10 或100 μM,在室温下进行20分钟。用于分析 TLC,加入105 μL 1 N HCl,然后加入160μL CHCl3:MeOH (1:1),反应终止。涡旋两相混合物,简单离心,使用CHCl3预包被的凝胶上样吸头将有机相转移到新的试管中。TLC板上染色提取物,然后在n-丙醇:1 M乙酸的溶液中进行3到4小时。然后烘干TLC板, 然后用感光成像系统处理,再进行量化。测定PI-103,用10-12种浓度从实验所用最高浓度(100 μM)稀释2倍的抑制剂进行激酶活性测定。测定IC50重复进行2到4次,取几次独立测量的平均值。
细胞实验:[2]
- 合并
  • Cell lines: U87MG细胞
  • Concentrations: 0.5 μM
  • Incubation Time: 24小时
  • Method: 评估细胞死亡,用PI-103处理U87MG细胞24小时。通过LDH活性的比色测定,用细胞毒性检测试剂盒测量细胞死亡。按公式:[(实验值-低对照值)/(高对照值-低对照值)×100]计算死亡百分率(3个12孔板每个实验点的平均值),低对照细胞用DMSO处理的,高对照细胞用1% Triton X-100在37oC下处理30分钟。
    (Only for Reference)
动物实验:[2]
- 合并
  • Animal Models: 左前肢末端皮下注射U87MG:106个ΔEGFR 细胞的6到12周大Balbc nu/nu鼠
  • Dosages: 5 mg/kg
  • Administration: 腹腔注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 24 mg/mL (68.89 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
5%DMSO+40%PEG300+5%Tween80+50%ddH2O
1 mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 348.36
化学式

C19H16N4O3

CAS号 371935-74-9
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID