PI-103
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/γ的IC50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。
PI-103 Chemical Structure
CAS: 371935-74-9
客户使用Selleck的PI-103发表文献97篇
产品质控
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PI-103相关产品
| 相关靶点 | p110α p110β p110δ p110γ C2β Vps34 | 点击展开 |
|---|---|---|
| 相关化合物库 | 激酶抑制剂库 PI3K/Akt 抑制剂库 凋亡分子化合物库 细胞周期化合物库 NF-κB信号通路库 | 点击展开 |
相关信号通路图
PI3K抑制剂选择性比较
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| RH30 | Apoptosis Assay | 1/1.5/2 μM | 72 h | induces caspase-dependent apoptosis combined with UO126 | 23684925 |
| RMS13 | Apoptosis Assay | 1/1.5/2 μM | 72 h | induces caspase-dependent apoptosis combined with UO126 | 23684925 |
| SUM149PT | Cell Viability Assay | 0.3 μM | 72 h | enhances cytotoxic effects of PI3K/AKT pathway inhibitors | 23601074 |
| MDA-MB-468 | Cell Viability Assay | 0.3 μM | 72 h | enhances cytotoxic effects of PI3K/AKT pathway inhibitors | 23601074 |
| MDA-MB-231 | Cell Viability Assay | 0.3 μM | 72 h | enhances cytotoxic effects of PI3K/AKT pathway inhibitors | 23601074 |
| SY5Y | Function Assay | 1.5/2.5/5 μM | 24 h | induces G1 cell-cycle arrest and apoptosis | 23378341 |
| SKNBE(2c) | Function Assay | 1.5/2.5/5 μM | 24 h | induces G1 cell-cycle arrest and apoptosis | 23378341 |
| RD | Apoptosis Assay | 3 µM | 12 h | sensitizes RD cells to DOX-induced apoptosis | 23300809 |
| TP5014 | Apoptosis Assay | 3 µM | 12 h | sensitizes RD cells to DOX-induced apoptosis | 23300809 |
| HT1080 | Apoptosis Assay | 3 µM | 12 h | sensitizes RD cells to DOX-induced apoptosis | 23300809 |
| A549 | Function Assay | 0-3.3 μM | 72 h | induces complete downregulation of pAKT | 23259591 |
| HCC827 | Function Assay | 0-3.3 μM | 72 h | induces complete downregulation of pAKT | 23259591 |
| H3122 | Function Assay | 0-3.3 μM | 72 h | induces complete downregulation of pAKT | 23259591 |
| TALL-1 | Growth Inhibition Assay | 1 μM | 7 d | decreases the cell number significantly | 23038273 |
| HPB-ALL | Growth Inhibition Assay | 1 μM | 7 d | decreases the cell number significantly | 23038273 |
| DND41 | Growth Inhibition Assay | 1 μM | 7 d | decreases the cell number significantly | 23038273 |
| SUP-T1 | Growth Inhibition Assay | 1 μM | 7 d | decreases the cell number significantly | 23038273 |
| PEER | Growth Inhibition Assay | 1 μM | 7 d | decreases the cell number significantly | 23038273 |
| ALL-SIL | Growth Inhibition Assay | 1 μM | 7 d | decreases the cell number significantly | 23038273 |
| KE37 | Growth Inhibition Assay | 1 μM | 7 d | decreases the cell number significantly | 23038273 |
| Karpas-45 | Growth Inhibition Assay | 1 μM | 7 d | decreases the cell number significantly | 23038273 |
| RPMI-8402 | Growth Inhibition Assay | 1 μM | 7 d | decreases the cell number significantly | 23038273 |
| Jurkat | Growth Inhibition Assay | 1 μM | 7 d | decreases the cell number significantly | 23038273 |
| MOLT-4 | Growth Inhibition Assay | 1 μM | 7 d | decreases the cell number significantly | 23038273 |
| PF-382 | Growth Inhibition Assay | 1 μM | 7 d | decreases the cell number significantly | 23038273 |
| CCRF-CEM | Growth Inhibition Assay | 1 μM | 7 d | decreases the cell number significantly | 23038273 |
| LOUCY | Growth Inhibition Assay | 1 μM | 7 d | decreases the cell number significantly | 23038273 |
| MOLT-16 | Growth Inhibition Assay | 1 μM | 7 d | decreases the cell number significantly | 23038273 |
| MM1S | Growth Inhibition Assay | 0-2 μM | 24 h | IC50=0.5 μM | 22829234 |
| NCI-H929 | Growth Inhibition Assay | 0-2 μM | 24 h | IC50=0.25 μM | 22829234 |
| KMS12-BM | Growth Inhibition Assay | 0-2 μM | 24 h | IC50＞2 μM | 22829234 |
| MDA-MB-436 | Function Assay | 1 μM | 24 h | reduces the phosphorylation of AKT | 22488590 |
| SUM149PT | Function Assay | 1 μM | 24 h | reduces the phosphorylation of AKT | 22488590 |
| SUM1315MO2 | Function Assay | 1 μM | 24 h | reduces the phosphorylation of AKT | 22488590 |
| HCC1937 | Function Assay | 1 μM | 24 h | reduces the phosphorylation of AKT | 22488590 |
| HCC827 | Growth Inhibition Assay | 0-3 μM | 72 h | IC50=0.3 μM | 21220474 |
| PC-9 | Growth Inhibition Assay | 0-3 μM | 72 h | IC50=0.8 μM | 21220474 |
| LN229 | Function Assay | 1 μM | 48 h | induces autophagosome formation | 21062993 |
| U87 | Function Assay | 1 μM | 48 h | induces autophagosome formation | 21062993 |
| U373 | Function Assay | 1 μM | 48 h | induces autophagosome formation | 21062993 |
| SF767 | Function Assay | 1 μM | 48 h | induces autophagosome formation | 21062993 |
| Mel-Juso | Cell Viability Assay | 0.01–10 μM | 72 h | inhibits cell viability dose dependently | 21048785 |
| 518A2 | Cell Viability Assay | 0.01–10 μM | 72 h | inhibits cell viability dose dependently | 21048785 |
| Mel-Juso | Function Assay | 0.001–1 μM | 24 h | suppresses phosphorylation of phosphatidyl inositol 3-kinase downstream targets | 21048785 |
| 518A2 | Function Assay | 0.001–1 μM | 24 h | suppresses phosphorylation of phosphatidyl inositol 3-kinase downstream targets | 21048785 |
| U87MG | Function Assay | 0.1-1 μM | 24 h | inhibits PI3K-mediated signaling | 19633683 |
| U138MG | Function Assay | 0.1-1 μM | 24 h | inhibits PI3K-mediated signaling | 19633683 |
| U118MG | Function Assay | 0.1-1 μM | 24 h | inhibits PI3K-mediated signaling | 19633683 |
| UCH-1 | Growth Inhibition Assay | 0.01-10 μM | 6 d | inhibits proliferation dose dependently | 19528441 |
| UCH-1 | Apoptosis Assay | 0.1-10 μM | 24 h | induces apoptosis | 19528441 |
| TE671 | Apoptosis Assay | 1/1.5/2 μM | 72 h | induces caspase-dependent apoptosis combined with UO126 | 23684925 |
| RD | Apoptosis Assay | 1/1.5/2 μM | 72 h | induces caspase-dependent apoptosis combined with UO126 | 23684925 |
| FaDu | Function Assay | 0.25/0.5/1 μM | 24 h | inhibits Akt phosphorylation significantly | 24351425 |
| UT5 | Function Assay | 0.25/0.5/1 μM | 24 h | inhibits Akt phosphorylation significantly | 24351425 |
| SAS | Function Assay | 0.25/0.5/1 μM | 24 h | inhibits Akt phosphorylation significantly | 24351425 |
| H661 | Function Assay | 0.25/0.5/1 μM | 24 h | inhibits Akt phosphorylation significantly | 24351425 |
| H460 | Function Assay | 0.25/0.5/1 μM | 24 h | inhibits Akt phosphorylation slightly | 24351425 |
| A549 | Function Assay | 0.25/0.5/1 μM | 24 h | inhibits Akt phosphorylation slightly | 24351425 |
| SW982 | Apoptosis Assay | 0.01-0.5 μM | 48 h | induces apoptosis dose dependently | 24695632 |
| SW872 | Apoptosis Assay | 0.01-0.5 μM | 48 h | induces apoptosis dose dependently | 24695632 |
| SW982 | Function Assay | 0.01-0.5 μM | 24 h | reduces AKT phosphorylation (pAKT) and 4EBP1 phosphorylation (p4EBP1) in a dose-dependent manner | 24695632 |
| SW872 | Function Assay | 0.01-0.5 μM | 24 h | reduces AKT phosphorylation (pAKT) and 4EBP1 phosphorylation (p4EBP1) in a dose-dependent manner | 24695632 |
| HS578T | Function Assay | 0.01-10 μM | 24 h | downregulates the levels of β-TrCP1, c-Myc and cyclin E proteins | 25721419 |
| MDA-MB-231 | Function Assay | 0.01-10 μM | 24 h | downregulates the levels of β-TrCP1, c-Myc and cyclin E proteins | 25721419 |
| MDA-MB-468 | Function Assay | 0.01-10 μM | 24 h | downregulates the levels of β-TrCP1, c-Myc and cyclin E proteins | 25721419 |
| SUM149PT | Cell Viability Assay | 0-3 μM | 72 h | inhibits cell viability dose dependently | 25721419 |
| MDA-MB-436 | Cell Viability Assay | 0-3 μM | 72 h | inhibits cell viability dose dependently | 25721419 |
| MDA-MB-468 | Cell Viability Assay | 0-3 μM | 72 h | inhibits cell viability dose dependently | 25721419 |
| MDA-MB-231 | Cell Viability Assay | 0-3 μM | 72 h | inhibits cell viability dose dependently | 25721419 |
| BT549 | Cell Viability Assay | 0-3 μM | 72 h | inhibits cell viability dose dependently | 25721419 |
| HS578T | Cell Viability Assay | 0-3 μM | 72 h | inhibits cell viability dose dependently | 25721419 |
| VJ | Apoptosis Assay | 1/1.5/2 μM | 72 h | induces apoptosis combined with GANT61 | 25749378 |
| RH30 | Apoptosis Assay | 1/1.5/2 μM | 72 h | induces apoptosis combined with GANT61 | 25749378 |
| RMS13 | Apoptosis Assay | 1/1.5/2 μM | 72 h | induces apoptosis combined with GANT61 | 25749378 |
| TE381.T | Apoptosis Assay | 1/1.5/2 μM | 72 h | induces apoptosis combined with GANT61 | 25749378 |
| RD | Apoptosis Assay | 1/1.5/2 μM | 72 h | induces apoptosis combined with GANT61 | 25749378 |
| G 40 DC | Growth Inhibition Assay | 0.05-20 μM | 24/72 h | inhibits cell viability dose and time dependently | 26121251 |
| G 38 DC | Growth Inhibition Assay | 0.05-20 μM | 24/72 h | inhibits cell viability dose and time dependently | 26121251 |
| G 35 DC | Growth Inhibition Assay | 0.05-20 μM | 24/72 h | inhibits cell viability dose and time dependently | 26121251 |
| G 40 SC | Growth Inhibition Assay | 0.05-20 μM | 24/72 h | inhibits cell viability dose and time dependently | 26121251 |
| G 38 SC | Growth Inhibition Assay | 0.05-20 μM | 24/72 h | inhibits cell viability dose and time dependently | 26121251 |
| G 35 SC | Growth Inhibition Assay | 0.05-20 μM | 24/72 h | inhibits cell viability dose and time dependently | 26121251 |
| SH-SY5Y | Apoptosis Assay | 1 μM | 0.5-24 h | sensitizes neuroblastoma cells to doxorubicin-induced apoptosis | 26224681 |
| SH-SY5Y | Growth Inhibition Assay | 0-8 μM | 24/48/72 h | induces time- and concentration-dependent inhibition on NB cell growth | 26224681 |
| SK-N-BE | Growth Inhibition Assay | 0-8 μM | 24/48/72 h | induces time- and concentration-dependent inhibition on NB cell growth | 26224681 |
| U87 | Antiproliferative assay | 0.04 to 10 uM | 72 hrs | Antiproliferative activity against human U87 cells harboring mutations in PI(3)K pathway components at 0.04 to 10 uM after 72 hrs by fluorescence assay | 18849971 |
| LN229 | Antiproliferative assay | 0.04 to 10 uM | 72 hrs | Antiproliferative activity against human LN229 cells harboring mutations in PI(3)K pathway components at 0.04 to 10 uM after 72 hrs by fluorescence assay | 18849971 |
| U87 | Cell cycle assay | 2.5 uM | 24 hrs | Cell cycle arrest in human U87 cells assessed as accumulation at G0/G1 phase at 2.5 uM after 24 hrs by FACS analysis | 18849971 |
| LN229 | Cell cycle assay | 2.5 uM | 24 hrs | Cell cycle arrest in human LN229 cells assessed as accumulation at G0/G1 phase at 2.5 uM after 24 hrs by FACS analysis | 18849971 |
| SEG1 | Cell cycle assay | 2.5 uM | 24 hrs | Cell cycle arrest in human SEG1 cells assessed as accumulation at G0/G1 phase at 2.5 uM after 24 hrs by FACS analysis | 18849971 |
| TT | Function assay | 0.04 to 10 uM | 2 hrs | Inhibition of S6K autophosphorylation in human TT cells at 0.04 to 10 uM after 2 hrs by Western blot analysis | 18849971 |
| K562 | Cell cycle assay | 2.5 uM | 24 hrs | Cell cycle arrest in human K562 cells harboring Bcr/Abl gene assessed as accumulation at G0/G1 phase at 2.5 uM after 24 hrs by FACS analysis | 18849971 |
| K562 | Cell cycle assay | 2.5 uM | 24 hrs | Cell cycle arrest in human K562 cells harboring Bcr/Abl T315I mutant gene assessed as accumulation at G0/G1 phase at 2.5 uM after 24 hrs by FACS analysis | 18849971 |
| BA/F3 | Cell cycle assay | 2.5 uM | 24 hrs | Cell cycle arrest in mouse BA/F3 cells harboring Bcr/Abl gene assessed as accumulation at G0/G1 phase at 2.5 uM after 24 hrs by FACS analysis | 18849971 |
| BA/F3 | Cell cycle assay | 2.5 uM | 24 hrs | Cell cycle arrest in mouse BA/F3 cells harboring Bcr/Abl T315I mutant gene assessed as accumulation at G0/G1 phase at 2.5 uM after 24 hrs by FACS analysis | 18849971 |
| UCH-1 | Function Assay | 0-5 μM | inhibits the phosphorylation of both AKT and mTOR in a dose-dependent manner | 19528441 | |
| HEK293 | Function assay | 0.5uM | Inhibition of PKB-S473 phosphorylation in IGF-1 treated HEK293 cells at 0.5uM | 17850214 | |
| Rh30 | Cell cycle assay | 1 to 10 uM | Cell cycle arrest in human Rh30 cells assessed as increase in G1 cell population at 1 to 10 uM by flow cytometric analysis | 22130133 | |
| PC3 | Growth Inhibition Assay | 24h | GI50 = 100 nM | 20551061 | |
| TT | Antiproliferative assay | 13 days | Antiproliferative activity against human TT cells after 13 days by fluorescence assay, IC50=0.0022μM. | 18849971 | |
| Sf9 | Function assay | 30 mins | Inhibition of N-terminal His-6-tagged full length human PI3Kalpha expressed in baculovirus-infected sf9 cells after 30 mins by TR-FRET assay, IC50=0.0179μM. | 24900786 | |
| HEK293T | Function assay | 15 mins | Inhibition of mTORC1 (unknown origin) expressed in HEK293T cells after 15 mins in presence of gamma-[32]P-ATP by high-throughput screening assay, IC50=0.02μM. | 29211480 | |
| Sf9 | Function assay | 30 mins | Inhibition of GST-tagged full length human PI3Kalpha D810A mutant expressed in baculovirus-infected sf9 cells after 30 mins by TR-FRET assay, IC50=0.074μM. | 24900786 | |
| Sf9 | Function assay | 30 mins | Inhibition of GST-tagged full length human PI3Kalpha Y836A mutant expressed in baculovirus-infected sf9 cells after 30 mins by TR-FRET assay, IC50=0.7963μM. | 24900786 | |
| Caco2 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human Caco2 cells after 48 hrs by Hoechst 33342 staining-based assay, IC50=0.8μM. | 30655216 | |
| Caco2 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human Caco2 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay, IC50=0.9μM. | 23063566 | |
| HCT116 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HCT116 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay, IC50=1μM. | 23063566 | |
| Sf9 | Function assay | 30 mins | Inhibition of GST-tagged full length human PI3Kalpha M772A mutant expressed in baculovirus-infected sf9 cells after 30 mins by TR-FRET assay, IC50=1.0344μM. | 24900786 | |
| PC3 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human PC3 cells after 48 hrs by Hoechst 33342 staining-based assay, IC50=1.2μM. | 30655216 | |
| HuH7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HuH7 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay, IC50=1.5μM. | 23063566 | |
| PC3 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human PC3 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay, IC50=1.5μM. | 23063566 | |
| Caco2 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human Caco2 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay, IC50=2μM. | 28214231 | |
| HaCaT | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HaCaT cells after 48 hrs by Hoechst 33342 staining-based assay, IC50=2μM. | 30655216 | |
| NCI-H727 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human NCI-H727 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay, IC50=3μM. | 23063566 | |
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 cells measured after 48 hrs by MTT assay, IC50=3μM. | 28011424 | |
| HCT116 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HCT116 cells after 48 hrs by Hoechst 33342 staining-based assay, IC50=3μM. | 30655216 | |
| HaCaT | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HaCaT cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay, IC50=3.5μM. | 28214231 | |
| HCT116 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HCT116 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay, IC50=3.9μM. | 28214231 | |
| A549 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human A549 cells measured after 48 hrs by MTT assay, IC50=4μM. | 28011424 | |
| MIAPaCa2 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MIAPaCa2 cells measured after 48 hrs by MTT assay, IC50=6μM. | 28011424 | |
| HuH7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HuH7 cells after 48 hrs by Hoechst 33342 staining-based assay, IC50=6μM. | 30655216 | |
| PC3 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human PC3 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay, IC50=7.6μM. | 28214231 | |
| HepG2 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HepG2 cells measured after 48 hrs by MTT assay, IC50=8μM. | 28011424 | |
| MDA-MB-231 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by Hoechst 33342 staining-based assay, IC50=8μM. | 30655216 | |
| MDA-MB-231 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay, IC50=15μM. | 23063566 | |
| U87MG | Growth Inhibition Assay | IC50=0.14 μM | 19584227 | ||
| IGROV-1 | Growth Inhibition Assay | IC50=0.06 μM | 19584227 | ||
| DETROIT562 | Growth Inhibition Assay | IC50=0.13 μM | 19584227 | ||
| PC3 | Growth Inhibition Assay | IC50=0.10 μM | 19584227 | ||
| SKOV-3 | Growth Inhibition Assay | IC50=0.12 μM | 19584227 | ||
| HUVEC | Growth Inhibition Assay | IC50=0.08 μM | 19584227 | ||
| NUGC4 LG | Growth Inhibition Assay | IC50=14.0 ± 5.321 μM | 24597478 | ||
| NUGC4 HG | Growth Inhibition Assay | IC50=14.0 ± 3.913 μM | 24597478 | ||
| MKN45 LG | Growth Inhibition Assay | IC50=0.87 ± 0.030 μM | 24597478 | ||
| MKN45 HG | Growth Inhibition Assay | IC50=1.01 ± 0.051 μM | 24597478 | ||
| HGC27 LG | Growth Inhibition Assay | IC50=0.02 ± 0.004 μM | 24597478 | ||
| HGC27 HG | Growth Inhibition Assay | IC50=0.38 ± 0.022 μM | 24597478 | ||
| AGS LG | Growth Inhibition Assay | IC50=0.05 ± 0.001 μM | 24597478 | ||
| AGS HG | Growth Inhibition Assay | IC50=0.68 ± 0.031 μM | 24597478 | ||
| ECV304 | Antiproliferative assay | Antiproliferative activity against human ECV304 cells, IC50=6.3μM. | 22130133 | ||
| Bel7404 | Antiproliferative assay | Antiproliferative activity against human Bel7404 cells, IC50=7μM. | 22130133 | ||
| MCF7 | Antiproliferative assay | Antiproliferative activity against human MCF7 cells, IC50=22.4μM. | 22130133 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 29435139 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 29435139 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 29435139 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 29435139 | ||
| Caco2 | Cell cycle assay | Cell cycle arrest in human Caco2 cells assessed as accumulation at G1/S phase by Hoechst staining based fluorescence assay | 28214231 | ||
| HCT116 | Cell cycle assay | Cell cycle arrest in human HCT116 cells assessed as accumulation at G2/M phase by Hoechst staining based fluorescence assay | 28214231 | ||
| PC3 | Cell cycle assay | Cell cycle arrest in human PC3 cells assessed as accumulation at G1/S phase by Hoechst staining based fluorescence assay | 28214231 | ||
| HaCaT | Cell cycle assay | Cell cycle arrest in human HaCaT cells assessed as accumulation at G1/S phase by Hoechst staining based fluorescence assay | 28214231 | ||
| 点击查看更多细胞系数据 | |||||
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/γ的IC50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。 | |||||||||||
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| 特性 | PI-103是第一个有效合成的mTOR抑制剂。 | |||||||||||
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | 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] | |||
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| 激酶实验 | 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 | 细胞系 | U87MG细胞 | ||
| 浓度 | 0.5 μM | |||
| 孵育时间 | 24小时 | |||
| 方法 | 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。 | |||
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p-AKT / AKT / p-S6K / S6K / p-S6 / S6 / p-p38 / p38 p-GSK3 / GSK3 / p-BAD / BAD / p-MDM2 / MDM2 / p-p27 / p27 β-TrCP1 / p-mTOR |
|
18922908 | |
| Immunofluorescence | autophagosomes / autolysosomes |
|
26814436 | |
| Growth inhibition assay | Cell viability |
|
25721419 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | 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] | |
|---|---|---|
| 动物实验 | 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 | |
化学信息&溶解度
| 分子量 | 348.36 | 分子式 | C19H16N4O3 |
| CAS号 | 371935-74-9 | SDF | Download PI-103 SDF |
| Smiles | C1COCCN1C2=NC(=NC3=C2OC4=C3C=CC=N4)C5=CC(=CC=C5)O | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 24 mg/mL ( (68.89 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
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）
mg/kg
g
μL
只
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
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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