Home PI3K/Akt/mTOR PI3K Inhibitor PI-103

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PI-103 PI3K Inhibitor

Kat.-Nr.S1038

PI-103 ist ein Multi-Target-PI3K-Inhibitor für p110α/β/δ/γ mit IC50 von 2 nM/3 nM/3 nM/15 nM in zellfreien Assays, weniger potent gegenüber mTOR/DNA-PK mit IC50 von 30 nM/23 nM. Diese Verbindung induziert Apoptose in murinem T-Zell-Lymphom.
PI-103 PI3K Inhibitor Chemical Structure

Chemische Struktur

Molekulargewicht: 348.36

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Qualitätskontrolle

Charge: Reinheit: 99.59%
99.59

Zellkultur, Behandlung & Arbeitskonzentration

Zelllinien Assay-Typ Konzentration Inkubationszeit Formulierung Aktivitätsbeschreibung PMID
UCH-1  Apoptosis Assay 0.1-10 μM 24 h DMSO induces apoptosis 19528441
UCH-1  Growth Inhibition Assay 0.01-10 μM 6 d inhibits proliferation dose dependently 19528441
UCH-1  Function Assay 0-5 μM inhibits the phosphorylation of both AKT and mTOR in a dose-dependent manner 19528441
HUVEC Growth Inhibition Assay IC50=0.08 μM 19584227
SKOV-3 Growth Inhibition Assay IC50=0.12 μM 19584227
PC3  Growth Inhibition Assay IC50=0.10 μM 19584227
DETROIT562 Growth Inhibition Assay IC50=0.13 μM 19584227
IGROV-1 Growth Inhibition Assay IC50=0.06 μM 19584227
U87MG Growth Inhibition Assay IC50=0.14 μM 19584227
U118MG Function Assay 0.1-1 μM 24 h  DMSO inhibits PI3K-mediated signaling 19633683
U138MG Function Assay 0.1-1 μM 24 h  DMSO inhibits PI3K-mediated signaling 19633683
U87MG Function Assay 0.1-1 μM 24 h  DMSO inhibits PI3K-mediated signaling 19633683
PC3  Growth Inhibition Assay 24h GI50 = 100 nM 20551061
518A2 Function Assay 0.001–1 μM 24 h suppresses phosphorylation of phosphatidyl inositol 3-kinase downstream targets 21048785
Mel-Juso  Function Assay 0.001–1 μM 24 h suppresses phosphorylation of phosphatidyl inositol 3-kinase downstream targets 21048785
518A2  Cell Viability Assay 0.01–10 μM 72 h inhibits cell viability dose dependently 21048785
Mel-Juso Cell Viability Assay 0.01–10 μM 72 h inhibits cell viability dose dependently 21048785
SF767 Function Assay 1 μM 48 h induces autophagosome formation 21062993
U373 Function Assay 1 μM 48 h induces autophagosome formation 21062993
U87 Function Assay 1 μM 48 h induces autophagosome formation 21062993
LN229 Function Assay 1 μM 48 h induces autophagosome formation 21062993
PC-9  Growth Inhibition Assay 0-3 μM 72 h IC50=0.8 μM 21220474
HCC827 Growth Inhibition Assay 0-3 μM 72 h IC50=0.3 μM 21220474
HCC1937 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
SUM149PT Function Assay 1 μM 24 h reduces the phosphorylation of AKT 22488590
MDA-MB-436 Function Assay 1 μM 24 h reduces the phosphorylation of AKT 22488590
KMS12-BM  Growth Inhibition Assay 0-2 μM 24 h IC50＞2 μM 22829234
NCI-H929 Growth Inhibition Assay 0-2 μM 24 h IC50=0.25 μM 22829234
MM1S Growth Inhibition Assay 0-2 μM 24 h IC50=0.5 μM 22829234
MOLT-16 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
CCRF-CEM 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
MOLT-4 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
RPMI-8402 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
KE37 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
PEER 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
DND41 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
TALL-1 Growth Inhibition Assay 1 μM 7 d decreases the cell number significantly 23038273
H3122 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
A549 Function Assay 0-3.3 μM 72 h induces complete downregulation of pAKT 23259591
HT1080 Apoptosis Assay 3 µM 12 h DMSO sensitizes RD cells to DOX-induced apoptosis 23300809
TP5014 Apoptosis Assay 3 µM 12 h DMSO sensitizes RD cells to DOX-induced apoptosis 23300809
RD Apoptosis Assay 3 µM 12 h DMSO sensitizes RD cells to DOX-induced apoptosis 23300809
SKNBE(2c) Function Assay 1.5/2.5/5 μM 24 h induces G1 cell-cycle arrest and apoptosis 23378341
SY5Y Function Assay 1.5/2.5/5 μM 24 h induces G1 cell-cycle arrest and apoptosis 23378341
MDA-MB-231 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
SUM149PT Cell Viability Assay 0.3 μM 72 h enhances cytotoxic effects of PI3K/AKT pathway inhibitors 23601074
RMS13 Apoptosis Assay 1/1.5/2 μM 72 h DMSO induces caspase-dependent apoptosis combined with UO126 23684925
RH30  Apoptosis Assay 1/1.5/2 μM 72 h DMSO induces caspase-dependent apoptosis combined with UO126 23684925
TE671 Apoptosis Assay 1/1.5/2 μM 72 h DMSO induces caspase-dependent apoptosis combined with UO126 23684925
RD Apoptosis Assay 1/1.5/2 μM 72 h DMSO 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
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
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 DMSO inhibits cell viability dose and time dependently 26121251
G 38 DC Growth Inhibition Assay 0.05-20 μM 24/72 h DMSO inhibits cell viability dose and time dependently 26121251
G 35 DC Growth Inhibition Assay 0.05-20 μM 24/72 h DMSO inhibits cell viability dose and time dependently 26121251
G 40 SC Growth Inhibition Assay 0.05-20 μM 24/72 h DMSO inhibits cell viability dose and time dependently 26121251
G 38 SC Growth Inhibition Assay 0.05-20 μM 24/72 h DMSO inhibits cell viability dose and time dependently 26121251
G 35 SC Growth Inhibition Assay 0.05-20 μM 24/72 h DMSO 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
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
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
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
MCF7 Antiproliferative assay Antiproliferative activity against human MCF7 cells, IC50=22.4μM. 22130133
HEK293 Function assay 0.5uM Inhibition of PKB-S473 phosphorylation in IGF-1 treated HEK293 cells at 0.5uM 17850214
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
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
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
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Chemische Informationen, Lagerung & Stabilität

Molekulargewicht 348.36 Formel

C19H16N4O3

 Lagerung (Ab dem Eingangsdatum)
CAS-Nr. 371935-74-9 SDF herunterladen Lagerung von Stammlösungen

Synonyme N/A Smiles C1COCCN1C2=NC(=NC3=C2OC4=C3C=CC=N4)C5=CC(=CC=C5)O

Löslichkeit

In vitro
Charge:

DMSO : 24 mg/mL (68.89 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molaritätsrechner

Masse Konzentration Volumen Molekulargewicht
Verdünnungsrechner Molekulargewichtsrechner

In vivo
Charge:

In-vivo-Formulierungsrechner (Klare Lösung)

Schritt 1: Geben Sie die untenstehenden Informationen ein (Empfohlen: Ein zusätzliches Tier zur Berücksichtigung von Verlusten während des Experiments)

mg/kg g μL

Schritt 2: Geben Sie die In-vivo-Formulierung ein (Dies ist nur der Rechner, keine Formulierung. Bitte kontaktieren Sie uns zuerst, wenn es im Abschnitt "Löslichkeit" keine In-vivo-Formulierung gibt.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Berechnungsergebnisse:

Arbeitskonzentration: mg/ml;

Methode zur Herstellung der DMSO-Stammlösung: mg Wirkstoff vorgelöst in μL DMSO ( Konzentration der Stammlösung mg/mL, Bitte kontaktieren Sie uns zuerst, wenn die Konzentration die DMSO-Löslichkeit der Wirkstoffcharge überschreitet. )

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügenμL PEG300, mischen und klären, dann hinzufügenμL Tween 80, mischen und klären, dann hinzufügen μL ddH2O, mischen und klären.

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügen μL Maisöl, mischen und klären.

Hinweis: 1. Bitte stellen Sie sicher, dass die Flüssigkeit klar ist, bevor Sie das nächste Lösungsmittel hinzufügen.
2. Achten Sie darauf, das/die Lösungsmittel der Reihe nach hinzuzufügen. Sie müssen sicherstellen, dass die bei der vorherigen Zugabe erhaltene Lösung eine klare Lösung ist, bevor Sie mit der Zugabe des nächsten Lösungsmittels fortfahren. Physikalische Methoden wie Vortex, Ultraschall oder ein heißes Wasserbad können zur Unterstützung des Lösens verwendet werden.

Wirkmechanismus

Merkmale
The first potent, synthetic mTOR inhibitor.
Targets/IC50/Ki
p110α
(Cell-free assay)
2 nM
p110β
(Cell-free assay)
3 nM
p110δ
(Cell-free assay)
3 nM
p110γ
(Cell-free assay)
15 nM
DNA-PK
(Cell-free assay)
23 nM
mTOR
(Cell-free assay)
30 nM
In vitro

PI-103 hemmt potent sowohl die Rapamycin-sensitiven (mTORC1) als auch die Rapamycin-insensitiven (mTORC2) Komplexe der Proteinkinase mTOR. Diese Verbindung hemmt die konstitutive und Wachstumsfaktor-induzierte PI3K/Akt- sowie die mTORC1-Aktivierung. In Blasten hemmt sie die leukämische Proliferation, die Klonogenität leukämischer Vorläuferzellen und induziert mitochondriale Apoptose, insbesondere im Kompartiment, das leukämische Stammzellen enthält. Diese Chemikalie hemmt p110α >200-fach potenter als p110β. Sie blockiert auch potent die Produktion von PI(3,4)P2 und PIP3 in Adipozyten und PIP3 in Myotubes. Diese Verbindung hemmt die Phosphorylierung von Akt mit einem IC95-Wert, der 100-fach niedriger ist als der für LY294002. Auffallend ist, dass sie Tiere vollständig vor einem stimulierten Abfall des Blutzuckers schützt. Sie hat additive proapoptotische Effekte in Blasten und in unreifen leukämischen Zellen.

Kinase-Assay
Enzym-Assays
Die Phosphatidylinositid-3-Kinase-Hemmungsaktivität wurde unter Verwendung eines Szintillationsnäherungsassays in Anwesenheit von 1 μmol/L ATP bestimmt. Die Hemmung der mTOR-Proteinkinase wurde unter Verwendung einer TR-FRET-basierten LanthaScreen-Methode von Invitrogen bestimmt. Diese Verbindung wurde bei einer maximalen Konzentration von 10 μmol/L in Anwesenheit von 1 μmol/L ATP getestet, und die IC50-Werte wurden unter Verwendung der GraphPad Prism-Software bestimmt.
In vivo

Wenn die Tumoren 50-100 mm3 erreichen, werden die Tiere randomisiert und mit Vehikel oder PI-103 behandelt. Diese Verbindung zeigt eine signifikante Aktivität und verringert die durchschnittliche Tumorgröße nach 18 Tagen um das 4-fache. Mäuse, die mit dieser Chemikalie behandelt wurden, zeigen keine offensichtlichen Anzeichen von präexistenter Toxizität (basierend auf Körpergewicht, Nahrungs- und Wasseraufnahme, Aktivität und allgemeiner Untersuchung) oder bei der Nekropsie. Behandelte Tumoren zeigen verringerte Spiegel von phosphoryliertem Akt und S6, was mit der Blockade von p110α und mTOR übereinstimmt. Diese Behandlung ist zytostatisch für Gliom-Xenotransplantate.

Literatur

Anwendungen

Methoden Biomarker Bilder PMID
Western blot β-TrCP1 / p-mTOR p-GSK3 / GSK3 / p-BAD / BAD / p-MDM2 / MDM2 / p-p27 / p27 p-AKT / AKT / p-S6K / S6K / p-S6 / S6 / p-p38 / p38
S1038-WB3
25721419
Immunofluorescence autophagosomes / autolysosomes
S1038-IF1
26814436
Growth inhibition assay Cell viability
S1038-viability1
25721419

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