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Buparlisib (BKM120) PI3K-remmer

Name: Buparlisib (BKM120)
Brand: Selleck Chemicals
SKU: S2247
Rating: 5 (287 reviews)

Cat.nr.S2247

Buparlisib (BKM120, NVP-BKM120) is een selectieve PI3K-remmer van p110α/β/δ/γ met respectievelijk een IC50 van 52 nM/166 nM/116 nM/262 nM in celvrije assays. Verminderde potentie tegen VPS34, mTOR, DNAPK, met weinig activiteit tegen PI4Kβ. Buparlisib induceert apoptose. Fase 2.

Buparlisib (BKM120) PI3K remmer Chemical Structure

Chemische structuur

Molecuulgewicht: 410.39

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Batch: Zuiverheid: 99.94%

99.94

Gerelateerde doelwitten	Akt mTOR GSK-3 ATM/ATR DNA-PK AMPK PDPK1 PTEN PP2A PDK
Overig PI3K Inhibitoren	GDC-0077 (Inavolisib) SAR405 Quercetin (Sophoretin) LY294002 XL147 analogue Tersolisib (STX-478) 740 Y-P (PDGFR 740Y-P) GO-203 TFA Eganelisib (IPI-549) Paxalisib (GDC-0084)

Celkweek, behandeling & werkzame concentratie

Cellijnen	Assaytype	Concentratie	Incubatietijd	Formulering	Activiteitsbeschrijving	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 informatie, opslag en stabiliteit

Molecuulgewicht	410.39	Formule	C₁₈H₂₁F₃N₆O₂	Opslag (vanaf de datum van ontvangst)	3 jaar-20°Cpoeder
CAS-nr.	944396-07-0	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	NVP-BKM120			Smiles	C1COCCN1C2=NC(=NC(=C2)C3=CN=C(C=C3C(F)(F)F)N)N4CCOCC4

Oplosbaarheid

In vitro
Batch:

DMSO : 82 mg/mL (199.8 mM)
(Met vocht verontreinigd DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Ethanol : 25 mg/mL

Water : Insoluble

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Massa	Concentratie	Volume	Molecuulgewicht
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In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	4.100mg/ml (9.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 82 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	0.300mg/ml (0.73mM)	Taking the 1 mL working solution as an example, add 50 μL of 6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo formulatiecalculator (heldere oplossing)

Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in de sectie oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-moedervloeistof: mg geneesmiddel vooropgelost in μL DMSO ( Concentratie moedervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de batch van het geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH₂O, mengen en verhelderen.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme

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) is niet gevoelig voor Klasse III en Klasse IV PI3K's of PI4K. Het vertoont een grote antiproliferatieve activiteit tegen PI3K-gedereguleerde cellijnen, waaronder A2780, U87MG, MCF7 en DU145 met een GI50 van 0,1-0,7 nM. Deze verbinding induceert apoptose van multipel myeloomcellen (ARP1, ARK, MM.1S, MM1.R en U266), wat resulteert in een toename van G1-fasecellen en een afname van S-fasecellen. Het induceerde ook CD138+ primaire MM-celapoptose en heeft een significant lagere cytotoxiciteit tegen CD138− stromale cellen. Blootstelling eraan kan opregulatie van BimS en downregulatie van XIAP veroorzaken. BKM120 toont antiproliferatieve activiteit in menselijke maagkankercellijnen door mTOR-downstream signalering te verminderen. Het kan p-ERK of p-STAT3 verhogen in KRAS-mutante maagkankercellen. Combinatie met STAT3-blokkade toont een synergisme in cellen die gemuteerd KRAS bevatten door apoptose te induceren, maar niet in KRAS wild-type cellen. Een recente studie toont aan dat het differentiële vormen van celdood vertoont op basis van de p53-status van de cellen, waarbij p53 wild-type cellen apoptotische celdood ondergaan en p53 mutante/gedeleteerde cellen mitotische catastrofe celdood hebben. Het medieert mitotische catastrofe voornamelijk via Aurora B-kinase.
Kinase Assay	PI3K biochemische assay (ATP-depletie assay)
Kinase Assay	Buparlisib (BKM120) wordt opgelost in DMSO en direct gedistribueerd in een zwarte 384-wells plaat met 1,25 µL per well. Om de reactie te starten, wordt 25 µL van 10 nM PI3 kinase en 5 µg/mL 1-α-fosfatidylinositol (PI) in assaybuffer (10 mM Tris pH 7,5, 5 mM MgCl₂, 20 mM NaCl, 1 mM DTT en 0,05% CHAPS) aan elk well toegevoegd, gevolgd door 25 µL van 2 µM ATP in assaybuffer. De reactie wordt uitgevoerd totdat ongeveer 50% van de ATP is uitgeput en vervolgens gestopt door de toevoeging van 25 µL KinaseGlo-oplossing. De gestopte reactie wordt 5 minuten geïncubeerd en de resterende ATP wordt vervolgens gedetecteerd via luminescentie.
In vivo	Buparlisib (BKM120) remt pAktser473 volledig in A2780 xenograft-tumoren bij doses van respectievelijk 30, 60 of 100 mg/kg, en vertoont ook antitumoractiviteit tegen het U87MG glioommodel bij doses van 30 en 60 mg/kg. Deze behandeling met de verbinding resulteert in significant verminderd tumorvolume en niveau van circulerende menselijke kappa-keten bij 5 μM/kg/dag−1 in het ARP1 SCID-muismodel, met een verlengde overleving.
Referenties	[1] http://pubs.acs.org/doi/abs/10.1021/ml200156t [2] https://pubmed.ncbi.nlm.nih.gov/22207485/ [3] https://pubmed.ncbi.nlm.nih.gov/22159814/ [4] https://pubmed.ncbi.nlm.nih.gov/22065080/

Toepassingen

Methoden	Biomarkers	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	29928341
Immunofluorescence	FOXO3a	28036259
Growth inhibition assay	Cell viability	26673665

Informatie over klinische proeven

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)

NCT-nummer	Werving	Aandoeningen	Sponsor/medewerkers	Startdatum	Fasen
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

Technische ondersteuning

Gebruiksaanwijzing

Tel: +1-832-582-8158 Ext:3

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