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PI-103 PI3K inibitore

N. Cat.S1038

PI-103 è un inibitore di PI3K multi-bersaglio per p110α/β/δ/γ con IC50 di 2 nM/3 nM/3 nM/15 nM in saggi senza cellule, meno potente verso mTOR/DNA-PK con IC50 di 30 nM/23 nM. Questo composto induce l'apoptosi nel linfoma murino a cellule T.
PI-103 PI3K inibitore Chemical Structure

Struttura chimica

Peso molecolare: 348.36

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Controllo Qualità

Lotto: Purezza: 99.59%
99.59

Coltura cellulare, trattamento e concentrazione di lavoro

Linee cellulari Tipo di saggio Concentrazione Tempo di incubazione Formulazione Descrizione dellattività 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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Informazioni chimiche, conservazione e stabilità

Peso molecolare 348.36 Formula

C19H16N4O3

 Conservazione (Dalla data di ricezione)
N. CAS 371935-74-9 Scarica SDF Conservazione delle soluzioni stock

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

Solubilità

In vitro
Lotto:

DMSO : 24 mg/mL (68.89 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Water : Insoluble

Ethanol : Insoluble

Calcolatore di Molarità

Massa Concentrazione Volume Peso molecolare
Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo
Lotto:

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante lesperimento)

mg/kg g μL

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non cè una formulazione in vivo nella sezione Solubilità.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Risultati del calcolo:

Concentrazione di lavoro: mg/ml;

Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH2O, mescolare e chiarire.

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.

Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nellaggiunta precedente, sia una soluzione limpida prima di procedere allaggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno dacqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo dazione

Caratteristiche
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 inibisce potentemente sia i complessi sensibili (mTORC1) che insensibili (mTORC2) alla rapamicina della proteina chinasi mTOR. Questo composto inibisce l'attivazione costitutiva e indotta da fattori di crescita di PI3K/Akt, nonché l'attivazione di mTORC1. Nelle cellule blastiche, inibisce la proliferazione leucemica, la clonogenicità dei progenitori leucemici e induce l'apoptosi mitocondriale, specialmente nel compartimento contenente le cellule staminali leucemiche. Questa sostanza chimica inibisce p110α >200 volte più potentemente di p110β. Blocca anche potentemente la produzione di PI(3,4)P2 e PIP3 negli adipociti e PIP3 nei miotubi. Questo composto inibisce la fosforilazione di Akt con un IC95 100 volte inferiore rispetto a quello per LY294002. Sorprendentemente, protegge completamente gli animali dal declino stimolato della glicemia. Ha effetti proapoptotici additivi nelle cellule blastiche e nelle cellule leucemiche immature.

Saggio chinasico
Saggi enzimatici
L'attività inibitoria della fosfatidilinositide 3-chinasi è stata determinata utilizzando un saggio di prossimità per scintillazione in presenza di 1 μmol/L di ATP. L'inibizione della proteina chinasi mTOR è stata determinata utilizzando un metodo LanthaScreen basato su TR-FRET di Invitrogen. Questo composto è stato saggiato a una concentrazione massima di 10 μmol/L in presenza di 1 μmol/L di ATP e i valori di IC50 sono stati determinati utilizzando il software GraphPad Prism.
In vivo

Quando i tumori raggiungono 50-100 mm3, gli animali vengono randomizzati e trattati con veicolo o PI-103. Questo composto mostra un'attività significativa, diminuendo la dimensione media del tumore di 4 volte dopo 18 giorni. I topi trattati con questa sostanza chimica non mostrano segni evidenti di tossicità premorbosa (basata sul peso corporeo, sull'assunzione di cibo e acqua, sull'attività e sull'esame generale) o all'autopsia. I tumori trattati mostrano livelli diminuiti di Akt e S6 fosforilati, coerentemente con il blocco di p110α e mTOR. Questo trattamento è citostatico per gli xenotrapianti di glioma.

Riferimenti

Applicazioni

Metodi Biomarcatori Immagini 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

Supporto tecnico

Istruzioni per la manipolazione

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