Home PI3K/Akt/mTOR PI3K Inhibitor Buparlisib (BKM120)

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Buparlisib (BKM120) PI3K-Inhibitor

Kat.-Nr.S2247

Buparlisib (BKM120, NVP-BKM120) ist ein selektiver PI3K-Inhibitor von p110α/β/δ/γ mit einer IC50 von 52 nM/166 nM/116 nM/262 nM in zellfreien Assays. Reduzierte Wirksamkeit gegen VPS34, mTOR, DNAPK, mit geringer Aktivität gegenüber PI4Kβ. Buparlisib induziert Apoptose. Phase 2.
Buparlisib (BKM120) PI3K Inhibitor Chemical Structure

Chemische Struktur

Molekulargewicht: 410.39

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Qualitätskontrolle

Charge: Reinheit: 99.94%
99.94

Zellkultur, Behandlung & Arbeitskonzentration

Zelllinien Assay-Typ Konzentration Inkubationszeit Formulierung Aktivitätsbeschreibung PMID
glioma cell lines Growth Inhibition Assay 72h IC50=1-2μM 22065080
U87 Apoptosis Assay 2μM 72h induces cell apoptosis and cleaved PARP and caspase-3 22065080
SNU-601 Growth Inhibition Assay 72h DMSO IC50=0.816±0.063μM 22159814
SNU-1 Growth Inhibition Assay 72h DMSO IC50=1.082±0.028μM 22159814
SNU-668 Growth Inhibition Assay 72h DMSO IC50=1.579±0.074μM 22159814
AGS Growth Inhibition Assay 72h DMSO IC50=1.714±0.117μM 22159814
SNU-216 Growth Inhibition Assay 72h DMSO IC50=2.692±0.082μM 22159814
SNU-5 Growth Inhibition Assay 72h DMSO IC50=1.351±0.091μM 22159814
SNU-638 Growth Inhibition Assay 72h DMSO IC50=2.282±0.053μM 22159814
SNU-16 Growth Inhibition Assay 72h DMSO IC50=1.573±0.001μM 22159814
SNU-484 Growth Inhibition Assay 72h DMSO IC50=1.728±0.045μM 22159814
SNU-620 Growth Inhibition Assay 72h DMSO IC50=2.939±0.001μM 22159814
SNU-719 Growth Inhibition Assay 72h DMSO IC50=3.037±0.032μM 22159814
MM cell lines Growth Inhibition Assay 10μM 24h DMSO IC50 varies among different cell lines in time and dose dependence 22207485
ARP-1 Apoptosis Assay 10μM 24h DMSO induces MM cell apoptosis through caspase activation 22207485
colon cancer cell lines Growth Inhibition Assay 0-10μM 72h DMSO IC50=1μM 22543857
gastric cancer cell lines Growth Inhibition Assay 0-10μM 72h DMSO IC50=2-5μM 22543857
HCT-116/HT-29/MKN-45 Apoptosis Assay 2μM 48h shift in G2 phase 22543857
HT-29 and HCT-116 Caspase assay 5μM 24h induces caspase activity 22543857
PIK3CA-mutant MCF7 Growth Inhibition Assay GI50=160±91nM，LD50=980±273nM 72h GI50=160±91nM，LD50=980±273nM 22653967
PIK3CA-mutant MCF7 Kinase Assay IC50=114±3nM 72h IC50=114±3nM in reducing Akt phosphorylation levels 22653967
MCF7-myr-Akt Growth Inhibition Assay GI50=299±68nM，LD50＞10,000nM 72h GI50=299±68nM，LD50＞10,000nM 22653967
Y1 cell line Growth Inhibition Assay 0.1μM/1μM 24h DMSO inhibits 60％ cell viability in Myc-Sctr-transfected cells 22692904
human NSCLC Growth Inhibition Assay 0.5-2μM 72h IC50=1μM 22781393
human NSCLC Kinase Assay 1μM 24h inhibits the Akt/mTOR signaling pathway at 3h after treatment 22781393
JVM2 Cytotoxicity assay 0.2-20μM 72h DMSO IC50=0.9μM 23238639
EHEB Cytotoxicity assay 0.2-20μM 72h DMSO IC50=0.7μM 23238639
MEC2 Cytotoxicity assay 0.2-20μM 72h DMSO IC50=0.7μM 23238639
primary B-CLL lymphocytes Apoptosis Assay IC50 for each primary cell line 24h DMSO IC50＜3μM for all patients 23238639
primary B-CLL lymphocytes Kinase Assay IC50 for each primary cell line 24h inhibits p70S6K & 4E-BP1 expression 23238639
SK-HEP1 Growth Inhibition Assay 1-20μM 72h DMSO IC50＜1μM 23479136
786-0 Growth Inhibition Assay 1-20μM 72h DMSO IC50＜1μM 23479136
human HCC cell lines Cell viability assay 0.005-1μM 48h IC50=1μM 23489999
Huh7 Kinase Assay 1μM 48h significantly reduces phosphorylation of Akt 23489999
human NSCLC cell lines Apoptosis Assay 0.125-4μM 24h DMSO IC50s ranges from 0.4-2μM 23562472
Primary CLL cells Apoptosis Assay 1-10μM 48h induces apoptosis in CLL cells independent of prognostic markers 23850807
Primary CLL cells Kinase Assay 2μM 30min decreased PI3K activity 23850807
Primary CLL cells Cytotoxic Assay 2μM 24h induces cell cytotoxicity 23850807
LC-1/SQSF Function Assay 3μM 24h DMSO decrease NRF2 protein level 23980093
BCR-ABL Growth Inhibition Assay 0.25-10μM 4d significantly inhibit cell proliferation 24244612
T-ALL Apoptosis Assay between 1.4 and 5.3 mM at 24h and 0.9 and 5.5 mM at 48h in different cell line 24 or 48h DMSO affects the PI3K pathway in T-ALL cell lines 24310736
H1975 Growth Inhibition Assay 0.3-9.6μM 72h DMSO IC50=1.385μM 24337846
H1975 Apoptosis Assay 2μM 24h DMSO increases apoptosis rate significantly 24337846
BON Growth Inhibition Assay 1-5μM 72h decreases cell proliferation 24443523
BON Apoptosis Assay 1-5μM 24h increases apoptosis 24443523
GBM Apoptosis Assay 2μM 48h DMSO induced higher levels of apoptosis, and decreased cell viability 24500492
FaDu Function Assay 5 μM 24 h DMSO Reduces oxygen consumption 24631147
EMT6 Function Assay 5 μM 24 h DMSO Reduces oxygen consumption 24631147
HCT116 Function Assay 5 μM 24 h DMSO Reduces oxygen consumption 24631147
U87 Function Assay 5 μM 24 h DMSO Reduces oxygen consumption 24631147
Saos-2 Function Assay 50 μM 48 h Inhibits cell invasion 24727660
MG-63 Function Assay 50 μM 48 h Inhibits cell invasion 24727660
SJSA-1 Function Assay 50 μM 48 h Inhibits cell invasion 24727660
Saos-2 Function Assay 50 μM 48 h Inhibits matrix metalloproteinase-2 expression 24727660
MG-63 Function Assay 50 μM 48 h Inhibits matrix metalloproteinase-2 expression 24727660
SJSA-1 Function Assay 50 μM 48 h Inhibits matrix metalloproteinase-2 expression 24727660
Saos-2 Growth Inhibition Assay 50 μM 48 h Inhibits cell viability 24727660
MG-63 Growth Inhibition Assay 50 μM 48 h Inhibits cell viability 24727660
SJSA-1 Growth Inhibition Assay 50 μM 48 h Inhibits cell viability 24727660
LN18 Growth Inhibition Assay 20 μM 72 h DMSO IC50<5 μM 24741074
LN229 Growth Inhibition Assay 20 μM 72 h DMSO IC50<5 μM 24741074
LNZ308 Growth Inhibition Assay 20 μM 72 h DMSO IC50<5 μM 24741074
T98G Growth Inhibition Assay 20 μM 72 h DMSO IC50<5 μM 24741074
U87 Growth Inhibition Assay 20 μM 72 h DMSO IC50<5 μM 24741074
LN18 Function Assay 5 μM 24 h DMSO Inhibits phosphorylation of AKT 24741074
LNZ308 Function Assay 5 μM 24 h DMSO Inhibits phosphorylation of AKT 24741074
MDA-MB-175 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
MDA-MB-134 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
HCC1500 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
EFM-19 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
ZR-75-30 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
MDA-MB-361 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
T-47D Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
SK-BR-3 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
UACC-732 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
BT-474 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
HCC202 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
MCF7 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
MDA-MB-415 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
MDA-MB-453 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
ZR-75-1 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
HCC38 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
HCC1419 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
UACC-812 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
HCC1187 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
KPL-1 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
SUM-225 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
EFM-192A Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
JIMT-1 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
HCC1143 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
HCC2218 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
MDA-MB-468 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
BT-20 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
MDA-MB-435 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
BT-549 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
HCC1806 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
HCC1937 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
Hs578T Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
MCF7 Cytotoxic Assay 72 h DMSO Cytotoxicity against human MCF7 cells expressing PI3Kalpha E545K mutant with GI50 of 0.000158 μM 24900266
DU145 Cytotoxic Assay 72 h DMSO Cytotoxicity against human DU145 cells expressing LKB1 mutant with GI50 of 0.000435 μM 24900266
A2780 Cytotoxic Assay 72 h DMSO Cytotoxicity against PTEN-deficient human A2780 cells with GI50 of 0.000635 μM 24900266
U87MG Cytotoxic Assay 72 h DMSO Cytotoxicity against PTEN-deficient human U87MG cells with GI50 of 0.000698 μM 24900266
A2780 Function Assay 1 h DMSO Inhibition of PI3K-mediated AKT Ser473 phosphorylation with EC50 of 0.055 μM 24900266
DU145 Function Assay 1 h DMSO Inhibition of PI3K-mediated AKT Ser473 phosphorylation in human DU145 cells harboring LKB1 mutation with EC50 of 0.073 μM 24900266
A2780 Function Assay 1 h DMSO Inhibition of PI3K-mediated AKT Ser473 phosphorylation in PTEN-deficient human A2780 cells with EC50 of 0.074 μM 24900266
MCF7 Function Assay 1 h DMSO Inhibition of PI3Kalpha E545K mutant-mediated AKT Ser473 phosphorylation with EC50 of 0.1 μM 24900266
U87MG Function Assay 1 h DMSO Inhibition of PI3K-mediated AKT Ser473 phosphorylation in PTEN-deficient human U87MG cells with EC50 of 0.13 μM 24900266
A2780 Growth Inhibition Assay 72 h DMSO EC50=0.52 μM 24900266
Huh7 Function Assay 1 μM 1 h DMSO Inhibits phosphorylation of AKT at Ser474 25004403
BNL Function Assay 1 μM 1 h DMSO Inhibits phosphorylation of S6 25004403
BON-1 Growth Inhibition Assay 500 nM 10 d DMSO Inhibits cell growth 25026292
BON-1 Function Assay 500 nM 4 h DMSO Inhibits phosphorylation of AKT at Thr308 and Ser473 25026292
QGP-1 Function Assay 500 nM 4 h DMSO Inhibits phosphorylation of AKT at Thr308 and Ser473 25026292
HCT-15 Apotosis Assay 10 μM 48 h DMSO Induces apoptosis in HCT-15 cells harbouring PIK3CA hotspot mutation 25152245
HCT-116 Apotosis Assay 10 μM 48 h DMSO Induces apoptosis in HCT-116 cells harbouring PIK3CA hotspot mutation 25152245
NCI-H460 Apotosis Assay 10 μM 48 h DMSO Induces apoptosis in NCI-H460 cells harbouring PIK3CA hotspot mutation 25152245
SKOV-3 Apotosis Assay 10 μM 48 h DMSO Induces apoptosis in SKOV-3 cells harbouring PIK3CA hotspot mutation 25152245
BSY-1 Apotosis Assay 10 μM 48 h DMSO Induces apoptosis in BSY-1 cells harbouring PIK3CA hotspot mutation 25152245
MKN-1 Apotosis Assay 10 μM 48 h DMSO Induces apoptosis in MKN-1 cells harbouring PIK3CA hotspot mutation 25152245
NCI-H522 Apotosis Assay 10 μM 48 h DMSO Induces apoptosis 25152245
OVCAR-3 Apotosis Assay 10 μM 48 h DMSO Induces apoptosis 25152245
HBC-5 Apotosis Assay 10 μM 48 h DMSO Induces apoptosis 25152245
RXF-631L Apotosis Assay 10 μM 48 h DMSO Induces apoptosis 25152245
MKN-45 Apotosis Assay 10 μM 48 h DMSO Induces apoptosis 25152245
LNCaP Function Assay 1 μM Suppresses p-AKT levels 25360799
LNCaP95 Function Assay 1 μM Suppresses p-AKT levels 25360799
A549 Function Assay 500 nM 48 h DMSO Inhibits Akt activation 25937299
A549 Growth Inhibition Assay 1 μM 72 h DMSO Inhibits cell growth 25937299
H522 Growth Inhibition Assay 1 μM 72 h DMSO Inhibits cell growth 25937299
SKMES-1 Cytotoxic Assay 1 μM 72 h Induces cell death 26013318
H596 Function Assay 1 μM Impairs cell migration 26013318
HCC2450 Function Assay 1 μM Impairs cell invasion 26013318
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 0.48 μM. 25765909
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 1 μM. 25765909
U87MG Antiproliferative assay 72 hrs Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay, IC50 = 1.64 μM. 25765909
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50 = 2.07 μM. 25765909
HeLa Antiproliferative assay 72 hrs Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay, IC50 = 4.34 μM. 25765909
HCT116 Function assay 10 uM 1 hr Inhibition of PI3K/Akt in human HCT116 cells assessed as Akt phosphorylation at 10 uM after 1 hr by Western blotting analysis 25765909
A2058 melanoma Cell cycle assay 5 uM 24 hrs Cell cycle arrest in human A2058 melanoma cells assessed as accumulation at SubG1 phase at 5 uM after 24 hrs by propidium iodide staining based FACS analysis 28829592
A2058 melanoma Cell cycle assay 5 uM 24 hrs Cell cycle arrest in human A2058 melanoma cells assessed as accumulation at G2/M phase at 5 uM after 24 hrs by propidium iodide staining based FACS analysis 28829592
SKOV3 Cell cycle assay 2 uM 24 hrs Cell cycle arrest in human SKOV3 cells assessed as accumulation at G2/M phase at 2 uM after 24 hrs by propidium iodide staining based FACS analysis 28829592
SKOV3 Cell cycle assay 2 uM 24 hrs Cell cycle arrest in human SKOV3 cells assessed as accumulation at SubG1 phase at 2 uM after 24 hrs by propidium iodide staining based FACS analysis 28829592
MDA-MB-231 Cytotoxicity assay 72 hrs Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50 = 1.88 μM. 29107429
PC3 Cytotoxicity assay 72 hrs Cytotoxicity against human PC3 cells after 72 hrs by MTT assay, IC50 = 5.34 μM. 29107429
T47D Cytotoxicity assay 72 hrs Cytotoxicity against human T47D cells after 72 hrs by MTT assay, IC50 = 6.92 μM. 29107429
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 11.05 μM. 29107429
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY 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
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD 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
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 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
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 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
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
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 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
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD 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
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
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 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
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
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
insect Function assay Inhibition of recombinant human His-tagged p85alpha/p110alpha E545K mutant expressed in insect cells, IC50 = 0.011 μM. 30034607
insect Function assay Inhibition of recombinant human His-tagged p85alpha/p110alpha E542K mutant expressed in insect cells, IC50 = 0.029 μM. 30034607
Sf21 Function assay 1 hr Inhibition of recombinant human full-length N-terminal His6-tagged p110delta/recombinant human full length p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate measured after 1 hr by Alexa633 Tracer-based fluorescence polar, IC50 = 0.125 μM. 30034607
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells harboring PIK3CA E545K mutant after 72 hrs by MTT assay, IC50 = 0.206 μM. 30034607
Sf21 Function assay 1 hr Inhibition of recombinant human full-length N-terminal His6-tagged p110beta/recombinant human full length p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate measured after 1 hr by Alexa633 Tracer-based fluorescence polari, IC50 = 0.234 μM. 30034607
T47D Antiproliferative assay 72 hrs Antiproliferative activity against human T47D cells harboring PI3KCA H1047R mutant after 72 hrs by MTT assay, IC50 = 0.286 μM. 30034607
PC3 Function assay 2 hrs Inhibition of PI3K in human PC3 cells assessed as reduction in AKT phosphorylation at Ser473 measured after 2 hrs by fluorescence assay, IC50 = 0.365 μM. 30034607
HT-29 Cell cycle assay 0.111 to 3 uM 24 hrs Cell cycle arrest in human HT-29 cells assessed as accumulation at G2/M phase at 0.111 to 3 uM after 24 hrs by propidium iodide staining based flow cytometry 30034607
A2058 Function assay 1 hr Inhibition of TORC2 in human A2058 cells assessed as decrease in PKB/Akt phosphorylation at Ser473 after 1 hr by Western blot analysis, IC50 = 0.416 μM. 30359003
A2058 Function assay 1 hr Inhibition of TORC1 in human A2058 cells assessed as decrease in S6 phosphorylation at Ser235/236 after 1 hr by Western blot analysis, IC50 = 0.553 μM. 30359003
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Chemische Informationen, Lagerung & Stabilität

Molekulargewicht 410.39 Formel

C18H21F3N6O2

 Lagerung (Ab dem Eingangsdatum)
CAS-Nr. 944396-07-0 SDF herunterladen Lagerung von Stammlösungen

Synonyme NVP-BKM120 Smiles C1COCCN1C2=NC(=NC(=C2)C3=CN=C(C=C3C(F)(F)F)N)N4CCOCC4

Löslichkeit

In vitro
Charge:

DMSO : 82 mg/mL (199.8 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Ethanol : 25 mg/mL

Water : 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

Targets/IC50/Ki
p110α
(Cell-free assay)
52 nM
p110δ
(Cell-free assay)
116 nM
p110β
(Cell-free assay)
166 nM
p110γ
(Cell-free assay)
262 nM
Vps34
(Cell-free assay)
2.4 μM
mTOR
(Cell-free assay)
4.6 μM
In vitro
Buparlisib (BKM120) ist nicht empfindlich gegenüber PI3K der Klasse III und Klasse IV oder PI4K. Es zeigt eine große Antiproliferationsaktivität gegenüber PI3K-deregulierten Zelllinien einschließlich A2780, U87MG, MCF7 und DU145 mit einem GI50 von 0,1-0,7 nM. Diese Verbindung induziert die Apoptosis von multiplen Myelomzellen (ARP1, ARK, MM.1S, MM1.R und U266), was zu einer Zunahme der Zellen in der G1-Phase und einer Abnahme der Zellen in der S-Phase führt. Es induzierte auch die Apoptosis von CD138+ primären MM-Zellen und weist eine signifikant geringere Zytotoxizität gegenüber CD138- Stromazellen auf. Seine Exposition könnte eine Hochregulierung von BimS und eine Herunterregulierung von XIAP verursachen. BKM120 zeigt antiproliferative Aktivität in menschlichen Magenkrebszelllinien durch die Verringerung der mTOR-Downstream-Signalübertragung. Es könnte entweder p-ERK oder p-STAT3 in KRAS-mutierten Magenkrebszellen erhöhen. In Kombination mit einer STAT3-Blockade zeigt es einen Synergismus in Zellen, die mutiertes KRAS aufweisen, durch Induktion von Apoptosis, aber nicht in KRAS-Wildtyp-Zellen. Eine aktuelle Studie zeigt, dass es differentiale Formen des Zelltods auf der Grundlage des p53-Status der Zellen aufweist, wobei p53-Wildtyp-Zellen einen apoptotischen Zelltod durchlaufen und p53-mutierte/deletierte Zellen einen mitotischen Katastrophen-Zelltod haben. Es vermittelt die mitotische Katastrophe hauptsächlich durch die Aurora B Kinase.
Kinase-Assay
PI3K biochemischer Assay (ATP-Depletionsassay)
Buparlisib (BKM120) wird in DMSO gelöst und direkt in eine schwarze 384-Well-Platte mit 1,25 µL pro Well verteilt. Um die Reaktion zu starten, werden 25 µL 10 nM PI3 kinase und 5 µg/mL 1-α-Phosphatidylinositol (PI) in Assay-Puffer (10 mM Tris pH 7.5, 5 mM MgCl2, 20 mM NaCl, 1 mM DTT und 0.05% CHAPS) zu jedem Well gegeben, gefolgt von 25 µL 2 µM ATP in Assay-Puffer. Die Reaktion wird durchgeführt, bis ca. 50% des ATPs verbraucht sind, und dann durch Zugabe von 25 µL KinaseGlo-Lösung gestoppt. Die gestoppte Reaktion wird 5 Minuten inkubiert und das verbleibende ATP wird dann über Lumineszenz nachgewiesen.
In vivo
Buparlisib (BKM120) hemmt pAktser473 in A2780-Xenograft-Tumoren bei Dosen von 30, 60 bzw. 100 mg/kg vollständig und zeigt auch Antitumoraktivität gegen das U87MG-Gliom-Modell bei Dosen von 30 und 60 mg/kg. Die Behandlung mit dieser Verbindung führt zu einem signifikant reduzierten Tumorvolumen und einem geringeren Spiegel der zirkulierenden menschlichen Kappa-Kette bei 5 μM/kg/Tag−1 im ARP1-SCID-Mausmodell, mit verlängertem Überleben.
Literatur
  • [4] https://pubmed.ncbi.nlm.nih.gov/22065080/

Anwendungen

Methoden Biomarker Bilder PMID
Western blot p-MET / MET p-STAT3 / STAT3 / p-ERK / ERK / p-S6 p-ERK / ERK / LC3 Nuclear NF-κB p65 / NF-κB p65 p-FOXO3a (S253) / FOXO3a p-AKT (T308) / p-AKT (S473) / AKT
S2247-WB6
29928341
Immunofluorescence FOXO3a
S2247-IF1
28036259
Growth inhibition assay Cell viability
S2247-viability1
26673665

Klinische Studieninformationen

(Daten von https://clinicaltrials.gov, aktualisiert am 2024-05-22)

NCT-Nummer Rekrutierung Erkrankungen Sponsor/Kooperationspartner Startdatum Phasen
NCT04338399 Active not recruiting
Head and Neck Cancer
Adlai Nortye Biopharma Co. Ltd.
 December 12 2020 Phase 3
NCT02614508 Terminated
Recurrent Chronic Lymphocytic Leukemia|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia|Refractory Small Lymphocytic Lymphoma
Emory University|Novartis
 January 2016 Phase 1
NCT01613677 Withdrawn
Treatment for Metastatic or Locally Advanced Cervical Cancer
Novartis Pharmaceuticals|Novartis
 November 2015 Phase 2

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