Cat. No.: HY-70063

Buparlisib

(Synonyms: BKM120; NVP-BKM120)

90 Cited Publications

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Based on 90 publication(s) in Google Scholar

Buparlisib (BKM120; NVP-BKM120) is a pan-class I PI3K inhibitor, with blood-brain barrier permeability. Buparlisib has IC₅₀s of 52, 166, 116 and 262 nM for p110α, p110β, p110δ and p110γ, respectively.

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Pureté: 99.82%
CAS No.: 944396-07-0
Formule: C₁₈H₂₁F₃N₆O₂
Masse moléculaire:410.39

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Buparlisib Chemical Structure

CAS No.: 944396-07-0

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (90)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

p110α

52 nM (IC₅₀)

p110α-H1047R

58 nM (IC₅₀)

p110α-E545K

99 nM (IC₅₀)

p110δ

116 nM (IC₅₀)

p110β

166 nM (IC₅₀)

p110γ

262 nM (IC₅₀)

Vps34

2.4 μM (IC₅₀)

mTOR

4.6 μM (IC₅₀)

Voir tous les produits spécifiques à Isoform PI3K :

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	EC₅₀	0.055 μM Compound: 15, NVP-BKM120	Inhibition of PI3K-mediated AKT Ser473 phosphorylation in human A2780 cells after 1 hr Inhibition of PI3K-mediated AKT Ser473 phosphorylation in human A2780 cells after 1 hr	[PMID: 24900266]
A2780	EC₅₀	0.074 μM Compound: 15, NVP-BKM120	Inhibition of PI3K-mediated AKT Ser473 phosphorylation in PTEN-deficient human A2780 cells after 1 hr Inhibition of PI3K-mediated AKT Ser473 phosphorylation in PTEN-deficient human A2780 cells after 1 hr	[PMID: 24900266]
A2780	EC₅₀	0.52 μM Compound: 15, NVP-BKM120	Antiproliferative activity against human A2780 cells after 3 days by CellTiter-Glo assay Antiproliferative activity against human A2780 cells after 3 days by CellTiter-Glo assay	[PMID: 24900266]
A2780	GI₅₀	0.635 nM Compound: 15, NVP-BKM120	Cytotoxicity against PTEN-deficient human A2780 cells after 3 days by CellTiterGlo assay Cytotoxicity against PTEN-deficient human A2780 cells after 3 days by CellTiterGlo assay	[PMID: 24900266]
A-431	IC₅₀	1.03 μM Compound: 5a	Antiproliferative activity against human A431 cells after 72 hrs by CCK8 assay Antiproliferative activity against human A431 cells after 72 hrs by CCK8 assay	[PMID: 27427973]
A549	IC₅₀	1.51 μM Compound: 5a	Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay	[PMID: 27427973]
A549	IC₅₀	2.07 μM Compound: BKM120	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 25765909]
A549	IC₅₀	9.75 μM Compound: BKM120	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth by MTT assay	[PMID: 37689214]
BaF3	IC₅₀	4.8 μM Compound: BKM120	Antiproliferative activity against mouse BaF3 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 38048697]
Bel-7402	IC₅₀	1.92 μM Compound: 5a	Antiproliferative activity against human Bel7402 cells after 72 hrs by CCK8 assay Antiproliferative activity against human Bel7402 cells after 72 hrs by CCK8 assay	[PMID: 27427973]
Bel-7402	IC₅₀	13 μM Compound: 4; BKM120	Antiproliferative activity against human Bel7402 cells after 96 hrs by MTT assay Antiproliferative activity against human Bel7402 cells after 96 hrs by MTT assay	[PMID: 31117517]
BGC-823	IC₅₀	1.43 μM Compound: 5a	Antiproliferative activity against human BGC823 cells after 72 hrs by CCK8 assay Antiproliferative activity against human BGC823 cells after 72 hrs by CCK8 assay	[PMID: 27427973]
Capan-2	IC₅₀	42 μM Compound: 4; BKM120	Antiproliferative activity against human Capan2 cells after 96 hrs by MTT assay Antiproliferative activity against human Capan2 cells after 96 hrs by MTT assay	[PMID: 31117517]
Ca-Ski	IC₅₀	0.74 μM Compound: BKM120	Antiproliferative activity against human Ca-Ski cells assessed as cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human Ca-Ski cells assessed as cell viability incubated for 48 hrs by MTT assay	[PMID: 38636129]
D283 Med	IC₅₀	0.279 μM Compound: BKM120	Cytotoxicity against human D283 Med cells assessed as reduction in cell viability incubated for 48 hrs by Cell TiterGlo luminescent assay Cytotoxicity against human D283 Med cells assessed as reduction in cell viability incubated for 48 hrs by Cell TiterGlo luminescent assay	[PMID: 33636537]
Daoy	IC₅₀	0.279 μM Compound: BKM120	Cytotoxicity against human Daoy cells assessed as reduction in cell viability incubated for 48 hrs by Cell TiterGlo luminescent assay Cytotoxicity against human Daoy cells assessed as reduction in cell viability incubated for 48 hrs by Cell TiterGlo luminescent assay	[PMID: 33636537]
DOHH-2	IC₅₀	1.4 μM Compound: BKM120	Antiproliferative activity against human DOHH-2 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human DOHH-2 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 38048697]
DU-145	EC₅₀	0.073 μM Compound: 15, NVP-BKM120	Inhibition of PI3K-mediated AKT Ser473 phosphorylation in human DU145 cells harboring LKB1 mutation after 1 hr Inhibition of PI3K-mediated AKT Ser473 phosphorylation in human DU145 cells harboring LKB1 mutation after 1 hr	[PMID: 24900266]
DU-145	GI₅₀	0.435 nM Compound: 15, NVP-BKM120	Cytotoxicity against human DU145 cells expressing LKB1 mutant Cytotoxicity against human DU145 cells expressing LKB1 mutant	[PMID: 24900266]
DU-145	IC₅₀	0.91 μM Compound: 5a	Antiproliferative activity against human DU145 cells after 72 hrs by CCK8 assay Antiproliferative activity against human DU145 cells after 72 hrs by CCK8 assay	[PMID: 27427973]
DU-145	IC₅₀	45 μM Compound: 4; BKM120	Antiproliferative activity against human DU145 cells after 96 hrs by MTT assay Antiproliferative activity against human DU145 cells after 96 hrs by MTT assay	[PMID: 31117517]
EL4	IC₅₀	0.86 μM Compound: BKM120	Antiproliferative activity against mouse EL4 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse EL4 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 38048697]
Friend leukemia cell line	IC₅₀	0.81 μM Compound: BKM120	Antiproliferative activity against mouse Friend leukemia cell line assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse Friend leukemia cell line assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 38048697]
HCT-116	IC₅₀	0.48 μM Compound: BKM120	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 25765909]
HCT-116	IC₅₀	1.3 μM Compound: 4; BKM120	Antiproliferative activity against human HCT116 cells after 96 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 96 hrs by MTT assay	[PMID: 31117517]
HCT-116	IC₅₀	3.73 μM Compound: BKM120	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth by MTT assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth by MTT assay	[PMID: 37689214]
HCT-8	IC₅₀	1.7 μM Compound: 4; BKM120	Antiproliferative activity against human HCT8 cells after 96 hrs by MTT assay Antiproliferative activity against human HCT8 cells after 96 hrs by MTT assay	[PMID: 31117517]
HEK-293T	IC₅₀	6.11 μM Compound: BKM120	Cytotoxicity against human HEK293T cells assessed as cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human HEK293T cells assessed as cell viability incubated for 48 hrs by MTT assay	[PMID: 38636129]
HeLa	IC₅₀	1.17 μM Compound: 5a	Antiproliferative activity against human HeLa cells after 72 hrs by CCK8 assay Antiproliferative activity against human HeLa cells after 72 hrs by CCK8 assay	[PMID: 27427973]
HeLa	IC₅₀	4.34 μM Compound: BKM120	Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay	[PMID: 25765909]
HeLa	IC₅₀	9.06 μM Compound: BKM120	Antiproliferative activity against human HeLa cells assessed as cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as cell viability incubated for 48 hrs by MTT assay	[PMID: 38636129]
HepG2	IC₅₀	23.57 μM Compound: BKM120	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth by MTT assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth by MTT assay	[PMID: 37689214]
HepG2	IC₅₀	3.2 μM Compound: 4; BKM120	Antiproliferative activity against human HepG2 cells after 96 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 96 hrs by MTT assay	[PMID: 31117517]
HGC-27	IC₅₀	0.99 μM Compound: 4; BKM120	Antiproliferative activity against human HGC27 cells after 96 hrs by MTT assay Antiproliferative activity against human HGC27 cells after 96 hrs by MTT assay	[PMID: 31117517]
HL-60	IC₅₀	1.2 μM Compound: BKM120	Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 38048697]
HL-60	IC₅₀	1.51 μM Compound: BKM120	Antiproliferative activity against human HL-60 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Antiproliferative activity against human HL-60 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 36272186]
HT-1080	IC₅₀	2.08 μM Compound: 5a	Antiproliferative activity against human HT1080 cells after 72 hrs by CCK8 assay Antiproliferative activity against human HT1080 cells after 72 hrs by CCK8 assay	[PMID: 27427973]
Huh-7	IC₅₀	1.51 μM Compound: 5a	Antiproliferative activity against human HuH7 cells after 72 hrs by CCK8 assay Antiproliferative activity against human HuH7 cells after 72 hrs by CCK8 assay	[PMID: 27427973]
Huh-7	IC₅₀	2 μM Compound: 4; BKM120	Antiproliferative activity against human HuH7 cells after 96 hrs by MTT assay Antiproliferative activity against human HuH7 cells after 96 hrs by MTT assay	[PMID: 31117517]
HUVEC	IC₅₀	0.886 μM Compound: NVP-BKM120; BKM	Cytotoxicity against HUVEC after 72 hrs by MTT assay Cytotoxicity against HUVEC after 72 hrs by MTT assay	[PMID: 30034607]
K562	IC₅₀	0.73 μM Compound: BKM120	Antiproliferative activity against human K562 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Antiproliferative activity against human K562 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 36272186]
K562	IC₅₀	1.1 μM Compound: 5a	Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay	[PMID: 27427973]
K562	IC₅₀	7.9 μM Compound: 4; BKM120	Antiproliferative activity against human K562 cells after 96 hrs by MTT assay Antiproliferative activity against human K562 cells after 96 hrs by MTT assay	[PMID: 31117517]
L02	IC₅₀	59.16 μM Compound: BKM120	Cytotoxicity against human L02 cells assessed as cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human L02 cells assessed as cell viability incubated for 48 hrs by MTT assay	[PMID: 38636129]
L1210	IC₅₀	0.37 μM Compound: BKM120	Antiproliferative activity against mouse L1210 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse L1210 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 38048697]
MCF7	EC₅₀	<0.1 μM Compound: 15, NVP-BKM120	Inhibition of PI3Kalpha E545K mutant-mediated AKT Ser473 phosphorylation in human MCF7 cells after 1 hr Inhibition of PI3Kalpha E545K mutant-mediated AKT Ser473 phosphorylation in human MCF7 cells after 1 hr	[PMID: 24900266]
MCF7	GI₅₀	0.158 nM Compound: 15, NVP-BKM120	Cytotoxicity against human MCF7 cells expressing PI3Kalpha E545K mutant Cytotoxicity against human MCF7 cells expressing PI3Kalpha E545K mutant	[PMID: 24900266]
MCF7	IC₅₀	0.206 μM Compound: NVP-BKM120; BKM	Antiproliferative activity against human MCF7 cells harboring PIK3CA E545K mutant after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells harboring PIK3CA E545K mutant after 72 hrs by MTT assay	[PMID: 30034607]
MCF7	IC₅₀	1 μM Compound: BKM120	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 25765909]
MCF7	IC₅₀	1.5 μM Compound: 5a	Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay	[PMID: 27427973]
MCF7	IC₅₀	11.05 μM Compound: Buparlisib	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 29107429]
MCF7	IC₅₀	16.43 μM Compound: BKM120	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth by MTT assay	[PMID: 37689214]
MCF7	IC₅₀	5.7 μM Compound: 4; BKM120	Antiproliferative activity against human MCF7 cells after 96 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 96 hrs by MTT assay	[PMID: 31117517]
MDA-MB-231	IC₅₀	1.88 μM Compound: Buparlisib	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 29107429]
MDA-MB-453	IC₅₀	0.37 μM Compound: 4; BKM120	Antiproliferative activity against human MDA-MB-453 cells after 96 hrs by MTT assay Antiproliferative activity against human MDA-MB-453 cells after 96 hrs by MTT assay	[PMID: 31117517]
MDA-MB-468	IC₅₀	3.97 μM Compound: BKM120	Antiproliferative activity against human MDA-MB-468 cells measured after 7 days by Celltiter-glo assay Antiproliferative activity against human MDA-MB-468 cells measured after 7 days by Celltiter-glo assay	[PMID: 33309164]
MOLT-4	IC₅₀	0.8 μM Compound: 5a	Antiproliferative activity against human MOLT4 cells after 72 hrs by CCK8 assay Antiproliferative activity against human MOLT4 cells after 72 hrs by CCK8 assay	[PMID: 27427973]
MV4-11	IC₅₀	0.56 μM Compound: BKM120	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 38048697]
MV4-11	IC₅₀	0.73 μM Compound: BKM120	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 36272186]
NB-4	IC₅₀	0.75 μM Compound: BKM120	Antiproliferative activity against human NB4 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human NB4 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 38048697]
NCI-H1299	IC₅₀	3.6 μM Compound: 4; BKM120	Antiproliferative activity against human NCI-H1299 cells after 96 hrs by MTT assay Antiproliferative activity against human NCI-H1299 cells after 96 hrs by MTT assay	[PMID: 31117517]
NCI-H460	IC₅₀	3.2 μM Compound: 4; BKM120	Antiproliferative activity against human NCI-H460 cells after 96 hrs by MTT assay Antiproliferative activity against human NCI-H460 cells after 96 hrs by MTT assay	[PMID: 31117517]
NCI-N87	IC₅₀	0.66 μM Compound: 5a	Antiproliferative activity against human NCI-N87 cells after 72 hrs by CCK8 assay Antiproliferative activity against human NCI-N87 cells after 72 hrs by CCK8 assay	[PMID: 27427973]
PANC-1	IC₅₀	1.83 μM Compound: 5a	Antiproliferative activity against human PANC1 cells after 72 hrs by CCK8 assay Antiproliferative activity against human PANC1 cells after 72 hrs by CCK8 assay	[PMID: 27427973]
PC-3	IC₅₀	12.06 μM Compound: BKM120	Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth by MTT assay Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth by MTT assay	[PMID: 37689214]
PC-3	IC₅₀	5.34 μM Compound: Buparlisib	Cytotoxicity against human PC3 cells after 72 hrs by MTT assay Cytotoxicity against human PC3 cells after 72 hrs by MTT assay	[PMID: 29107429]
Raji	IC₅₀	0.99 μM Compound: BKM120	Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 38048697]
Ramos	IC₅₀	5.4 μM Compound: BKM120	Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 38048697]
SGC-7901	IC₅₀	1.24 μM Compound: 5a	Antiproliferative activity against human SGC7901 cells after 72 hrs by CCK8 assay Antiproliferative activity against human SGC7901 cells after 72 hrs by CCK8 assay	[PMID: 27427973]
SiHa	IC₅₀	11.87 μM Compound: BKM120	Antiproliferative activity against human SiHa cells assessed as cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human SiHa cells assessed as cell viability incubated for 48 hrs by MTT assay	[PMID: 38636129]
SiHa	IC₅₀	7.18 μM Compound: BKM120	Antiproliferative activity against human SiHa cells assessed as inhibition of cell growth by MTT assay Antiproliferative activity against human SiHa cells assessed as inhibition of cell growth by MTT assay	[PMID: 37689214]
SW1990	IC₅₀	1.3 μM Compound: 4; BKM120	Antiproliferative activity against human SW1990 cells after 96 hrs by MTT assay Antiproliferative activity against human SW1990 cells after 96 hrs by MTT assay	[PMID: 31117517]
T47D	IC₅₀	0.286 μM Compound: NVP-BKM120; BKM	Antiproliferative activity against human T47D cells harboring PI3KCA H1047R mutant after 72 hrs by MTT assay Antiproliferative activity against human T47D cells harboring PI3KCA H1047R mutant after 72 hrs by MTT assay	[PMID: 30034607]
T47D	IC₅₀	6.92 μM Compound: Buparlisib	Cytotoxicity against human T47D cells after 72 hrs by MTT assay Cytotoxicity against human T47D cells after 72 hrs by MTT assay	[PMID: 29107429]
THP-1	IC₅₀	12 μM Compound: 4; BKM120	Antiproliferative activity against human THP1 cells after 96 hrs by MTT assay Antiproliferative activity against human THP1 cells after 96 hrs by MTT assay	[PMID: 31117517]
U-87MG ATCC	EC₅₀	0.13 μM Compound: 15, NVP-BKM120	Inhibition of PI3K-mediated AKT Ser473 phosphorylation in PTEN-deficient human U87MG cells after 1 hr Inhibition of PI3K-mediated AKT Ser473 phosphorylation in PTEN-deficient human U87MG cells after 1 hr	[PMID: 24900266]
U-87MG ATCC	GI₅₀	0.698 nM Compound: 15, NVP-BKM120	Cytotoxicity against PTEN-deficient human U87MG cells Cytotoxicity against PTEN-deficient human U87MG cells	[PMID: 24900266]
U-87MG ATCC	IC₅₀	1.64 μM Compound: BKM120	Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay	[PMID: 25765909]
U-87MG ATCC	IC₅₀	4.8 μM Compound: 4; BKM120	Antiproliferative activity against human U87 cells after 96 hrs by MTT assay Antiproliferative activity against human U87 cells after 96 hrs by MTT assay	[PMID: 31117517]
U-937	IC₅₀	0.58 μM Compound: 5a	Antiproliferative activity against human U937 cells after 72 hrs by CCK8 assay Antiproliferative activity against human U937 cells after 72 hrs by CCK8 assay	[PMID: 27427973]

In Vitro

Buparlisib (NVP-BKM120) exhibits activity of 50–300 nM against class I PI3K (including the most common p110α mutant). In addition, NVP-BKM120 shows lower potency against class III and IV PI3K, with biochemical activities of 2, 5, >5 and >25 μM observed, respectively, for the inhibition of VPS34, mTOR, DNAPK and PI4K^[1].
Buparlisib (≥10 μM, 24 h) induces apoptosis in multiple myeloma (MM) cells in a dose- and time-dependent manner^[1].
Buparlisib (10 μM, 24 h) causes dose-dependent growth inhibition in all tested MM cell lines, with IC₅₀ values ??between 1 and 10 μM for ARP-1, ARK, and MM.1R, while the IC50 value for MM.1S was <1 μM and for U266 it was between 10 and 100 μM^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

In A2780 xenograft tumors, oral dosing of Buparlisib (NVP-BKM120) at 3, 10, 30, 60, and 100 mg/kg results in a dose dependent modulation of pAKT^Ser473. Partial inhibition of pAKT^Ser473 is observed at 3 and 10 mg/kg, and near complete inhibition is observed at doses of 30, 60, or 100 mg/kg, respectively. Inhibition of pAKT (normalized to total AKT) tracked well with both plasma and tumor drug exposure^[1].
Mice receiving Buparlisib (NVP-BKM120) (5 μM per kg per day for 15 days) treatment has significantly smaller tumor burdens as compare with control mice, which are measured as tumor volume (P<0.05) and level of circulating human kappa chain. In addition, NVP-BKM120 treatment significantly prolongs the survival of tumor-bearing mice (P<0.05)^[2].
Buparlisib has an excellent brain penetration that is unaffected by efflux transporters at the blood-brain barrier^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 944396-07-0
Appearance Solid
Masse moléculaire 410.39
Formule C₁₈H₂₁F₃N₆O₂
Color White to off-white
SMILES

FC(F)(C1=C(C2=CC(N3CCOCC3)=NC(N4CCOCC4)=N2)C=NC(N)=C1)F
Synonyms

BKM120; NVP-BKM120
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (90)

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Nature

Short-term post-fast refeeding enhances intestinal stemness via polyamines. [Abstract]

2024 Sep;633(8031):895-904. PMID: 39169180
Nature

Ras drives malignancy through stem cell crosstalk with the microenvironment. [Abstract]

2022 Dec;612(7940):555-563. PMID: 36450983
Nature

Suppression of insulin feedback enhances the efficacy of PI3K inhibitors. [Abstract]

2018 Aug;560(7719):499-503. PMID: 30051890
Nat Med

Combination inhibition of PI3K and mTORC1 yields durable remissions in mice bearing orthotopic patient-derived xenografts of HER2-positive breast cancer brain metastases. [Abstract]

2016 Jul;22(7):723-6. PMID: 27270588

Buparlisib purchased from MedChemExpress. Usage Cited in: Nat Med. 2016 Jul;22(7):723-6. [Abstract]

Selective response of HER2-positive PDX DF-BM355 to the combination of BKM120/RAD001. Western blot analysis of lysates from vehicle-treated or BKM120-treated DF-BM355 in vivo.
Science

Direct sensing of dietary ω-6 linoleic acid through FABP5-mTORC1 signaling. [Abstract]

2025 Mar 14;387(6739):eadm9805. PMID: 40080571
Cell

RNA Pol II inhibition activates cell death independently from the loss of transcription. [Abstract]

2025 Oct 30;188(22):6301-6316.e29. PMID: 40818455
Cell

Microbiome metabolism of dietary phytochemicals controls the anticancer activity of PI3K inhibitors. [Abstract]

2025 May 29;188(11):3065-3080.e21. PMID: 40393457
Cancer Discov

The INPP4B Tumor Suppressor Modulates EGFR Trafficking and Promotes Triple-Negative Breast Cancer. [Abstract]

2020 Aug;10(8):1226-1239. PMID: 32513774
Cancer Discov

PTEN Methylation by NSD2 Controls Cellular Sensitivity to DNA Damage. [Abstract]

2019 Sep;9(9):1306-1323. PMID: 31217297
Cancer Discov

Identifying and Targeting Sporadic Oncogenic Genetic Aberrations in Mouse Models of Triple-Negative Breast Cancer. [Abstract]

2018 Mar;8(3):354-369. PMID: 29203461
Cancer Commun (Lond)

Aberrant translation regulated by METTL1/WDR4-mediated tRNA N7-methylguanosine modification drives head and neck squamous cell carcinoma progression. [Abstract]

2022 Mar;42(3):223-244. PMID: 35179319
Nat Cancer

A first-in-class selective inhibitor of EGFR and PI3K offers a single-molecule approach to targeting adaptive resistance. [Abstract]

2024 Aug;5(8):1250-1266. PMID: 38992135
Nat Biomed Eng

TLR7/8-agonist-loaded nanoparticles promote the polarization of tumour-associated macrophages to enhance cancer immunotherapy. [Abstract]

2018 Aug;2(8):578-588. PMID: 31015631
Cancer Res

GOT2 Silencing Promotes Reprogramming of Glutamine Metabolism and Sensitizes Hepatocellular Carcinoma to Glutaminase Inhibitors. [Abstract]

2022 Sep 16;82(18):3223-3235. PMID: 35895805
Autophagy

Lysosomal targetomics of ghr KO mice shows chaperone-mediated autophagy degrades nucleocytosolic acetyl-coA enzymes. [Abstract]

2022 Jul;18(7):1551-1571. PMID: 34704522
Nat Commun

Proteomic characterization of gastric cancer response to chemotherapy and targeted therapy reveals new therapeutic strategies. [Abstract]

2022 Sep 29;13(1):5723. PMID: 36175412
Nat Commun

PRMT5-mediated arginine methylation activates AKT kinase to govern tumorigenesis. [Abstract]

2021 Jun 8;12(1):3444. PMID: 34103528
Nat Commun

SH3RF3 promotes breast cancer stem-like properties via JNK activation and PTX3 upregulation. [Abstract]

2020 May 19;11(1):2487. PMID: 32427938
Sci Transl Med

Obesity promotes breast epithelium DNA damage in women carrying a germline mutation in BRCA1 or BRCA2. [Abstract]

2023 Feb 22;15(684):eade1857. PMID: 36812344
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Sci Adv

BRD9 functions as a methylarginine reader to regulate AKT-EZH2 signaling. [Abstract]

2025 Apr 25;11(17):eads6385. PMID: 40279411
Sci Adv

Fasting improves therapeutic response in hepatocellular carcinoma through p53-dependent metabolic synergism. [Abstract]

2022 Jan 21;8(3):eabh2635. PMID: 35061544
Cancer Lett

Inhibition of BTF3 sensitizes luminal breast cancer cells to PI3Kα inhibition through the transcriptional regulation of ERα. [Abstract]

2019 Jan:440-441:54-63. PMID: 30315845

Buparlisib purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2019 Jan:440-441:54-63. [Abstract]

The cells are transfected with either the negative control (siNC) or BTF3 siRNA for 12 hours followed by BKM-120 or AZD-6482 treatment for 48 hours. The protein abundance is determined by an immunoblotting analysis.
J Exp Med

MYC is a clinically significant driver of mTOR inhibitor resistance in breast cancer. [Abstract]

2023 Nov 6;220(11):e20211743. PMID: 37642941
Cell Commun Signal

MIIP inhibits the growth of prostate cancer via interaction with PP1α and negative modulation of AKT signaling. [Abstract]

2019 May 15;17(1):44. PMID: 31092266
Diabetologia

Saturated fatty acids entrap PDX1 in stress granules and impede islet beta cell function. [Abstract]

2021 May;64(5):1144-1157. PMID: 33569632
J Transl Med

SLC38A5 suppresses ferroptosis through glutamine-mediated activation of the PI3K/AKT/mTOR signaling in osteosarcoma. [Abstract]

2024 Nov 7;22(1):1004. PMID: 39511570
Proc Natl Acad Sci U S A

Role for ERK1/2-dependent activation of FCHSD2 in cancer cell-selective regulation of clathrin-mediated endocytosis. [Abstract]

2018 Oct 9;115(41):E9570-E9579. PMID: 30249660
Dev Cell

Tumor-intrinsic FDFT1 determines coordinated macrophage anti-tumor immunity. [Abstract]

2026 Apr 29:S1534-5807(26)00150-4. PMID: 42061405
Oncogene

Targeting glutamine metabolism network for the treatment of therapy-resistant prostate cancer. [Abstract]

2022 Feb;41(8):1140-1154. PMID: 35046532
Oncogene

PI3K-p110α mediates resistance to HER2-targeted therapy in HER2+, PTEN-deficient breast cancers. [Abstract]

2016 Jul 7;35(27):3607-12. PMID: 26500061

Buparlisib purchased from MedChemExpress. Usage Cited in: Oncogene. 2016 Jul 7;35(27):3607-12. [Abstract]

(A) Immunoblot analyses in HCC1569 cells treated with BYL719, KIN193 (MedChemexpress) or BKM120 (μM). (B, C) Immunoblot analyses in BT474 and BT474-shPTEN cells treated as indicated in (A).
NPJ Breast Cancer

SIMD: Synergistic integration mutualistic platform based on single-cell and proteotranscriptomics for drug repositioning. [Abstract]

2025 Dec 24;12(1):4. PMID: 41444222
ACS Appl Mater Interfaces

Micellar Formulation of Talazoparib and Buparlisib for Enhanced DNA Damage in Breast Cancer Chemoradiotherapy. [Abstract]

2019 Apr 3;11(13):12342-12356. PMID: 30860347
Cell Rep

Adipocyte PI3K links adipostasis with baseline insulin secretion at fasting through an adipoincretin effect. [Abstract]

2024 Apr 23;43(5):114132. PMID: 38656871
World J Gastroenterol

Roles of phosphatidylinositol-3-kinases signaling pathway in inflammation-related cancer: Impact of rs10889677 variant and buparlisib in colitis-associated cancer. [Abstract]

2023 Oct 28;29(40):5543-5556. PMID: 37970476
Cell Rep

Divergent Roles of PI3K Isoforms in PTEN-Deficient Glioblastomas. [Abstract]

2020 Sep 29;32(13):108196. PMID: 32997991
Cell Syst

Torin2 Exploits Replication and Checkpoint Vulnerabilities to Cause Death of PI3K-Activated Triple-Negative Breast Cancer Cells. [Abstract]

2020 Jan 22;10(1):66-81.e11. PMID: 31812693
Cancer Cell Int

Breast cancer organoids from a patient with giant papillary carcinoma as a high-fidelity model. [Abstract]

2020 Mar 18;20:86. PMID: 32206037
Sci Signal

KRASG12C inhibition produces a driver-limited state revealing collateral dependencies. [Abstract]

2019 May 28;12(583). pii: eaaw9450. PMID: 31138768
JCI Insight

YAP/TAZ mediates resistance to KRAS inhibitors through inhibiting proapoptosis and activating the SLC7A5/mTOR axis. [Abstract]

2024 Dec 20;9(24):e178535. PMID: 39704172
Oncoimmunology

Inhibition of PI3K pathway increases immune infiltrate in muscle-invasive bladder cancer. [Abstract]

2019 Mar 16;8(5):e1581556. PMID: 31069145
J Cell Biol

PTEN is both an activator and a substrate of chaperone-mediated autophagy. [Abstract]

2023 Sep 4;222(9):e202208150. PMID: 37418003
J Cell Biol

Inhibition of class I PI3K enhances chaperone-mediated autophagy. [Abstract]

2020 Dec 7;219(12):e202001031. PMID: 33048163
Hepatol Commun

Murine Liver Organoids as a Genetically Flexible System to Study Liver Cancer In Vivo and In Vitro. [Abstract]

2019 Feb 5;3(3):423-436. PMID: 30859153
Cancer Immunol Immunother

Dual roles of HK3 in regulating the network between tumor cells and tumor-associated macrophages in neuroblastoma. [Abstract]

2024 May 7;73(7):122. PMID: 38714539
Eur J Pharmacol

BKM120 inhibits malignant rhabdoid tumor of the kidney through induction of apoptosis and G0/G1 phase arrest. [Abstract]

2023 Jul 15:951:175747. PMID: 37142086
J Clin Endocrinol Metab

Targeting Corticotroph HDAC and PI3-Kinase in Cushing Disease. [Abstract]

2021 Jan 1;106(1):e232-e246. PMID: 33000123
Molecules

In Vitro and in Vivo Activity of mTOR Kinase and PI3K Inhibitors Against Leishmania donovani and Trypanosoma brucei. [Abstract]

2020 Apr 23;25(8):1980. PMID: 32340370
Sci Rep

Establishment of novel cholangiocarcinoma cell lines with ARID1A deficiency and preclinical validation of synthetic lethality therapies. [Abstract]

2025 Nov 18;15(1):40619. PMID: 41254205
Sci Rep

Solid stress-induced migration is mediated by GDF15 through Akt pathway activation in pancreatic cancer cells. [Abstract]

2019 Jan 30;9(1):978. PMID: 30700740
Cancers (Basel)

Evaluation of Combined Chemotherapy and Genomic-Driven Targeted Therapy in Patient-Derived Xenografts Identifies New Therapeutic Approaches in Squamous Non-Small-Cell Lung Cancer Patients. [Abstract]

2024 Aug 7;16(16):2785. PMID: 39199558
Cancers (Basel)

Combined Targeting of Pathogenetic Mechanisms in Pancreatic Neuroendocrine Tumors Elicits Synergistic Antitumor Effects. [Abstract]

2022 Nov 8;14(22):5481. PMID: 36428573
Cell Signal

RNF130 inhibits the proliferation, migration and invasion of osteosarcoma through DAB1 mediated suppression of the PI3K/AKT signaling pathway. [Abstract]

2026 Mar 31:144:112506. PMID: 41933674
Oncol Rep

Depleting HIF‑1α attenuates the progression of osteosarcoma, but tumorigenicity is sustained through HIF‑independent pathways. [Abstract]

2026 May;55(5):94. PMID: 41823542
Cell Signal

ABLIM1 promotes the proliferation, migration and invasion of osteosarcoma through DCC mediated activation of PI3K/AKT signaling pathway. [Abstract]

2025 Nov:135:112077. PMID: 40846275
Cell Signal

IRF2BPL inhibits proliferation, migration and invasion of osteosarcoma cells by inhibiting FOSL2-mediated PI3K/AKT pathway activation. [Abstract]

2025 Nov:135:112068. PMID: 40834975
Biomedicines

A Drug Screening Reveals Minocycline Hydrochloride as a Therapeutic Option to Prevent Breast Cancer Cells Extravasation across the Blood-Brain Barrier. [Abstract]

2022 Aug 16;10(8):1988. PMID: 36009536
J Endocr Soc

Thyroid Hormone Receptor Beta Inhibits PI3K-Akt-mTOR Signaling Axis in Anaplastic Thyroid Cancer via Genomic Mechanisms. [Abstract]

2021 Jun 1;5(8):bvab102. PMID: 34258492
J Biol Chem

The E3 ligase β-TRCP1 earmarks OTUD3 for destruction to fine-tune cGAS activation. [Abstract]

2026 Jun;302(6):111461. PMID: 41999888
J Cell Sci

Tumor acidosis supports cancer cell lipid uptake via a rapid transporter-independent mechanism. [Abstract]

2025 Apr 7:jcs.263688. PMID: 40190115
Carcinogenesis

HECTD3 E3 ligase mediates ubiquitination of AKT-phosphorylated CMTM3 in HER2-overexpressed breast cancer cells. [Abstract]

2025 Aug 21:bgaf048. PMID: 40836897
Endocrinology

TRβ Agonism Induces Tumor Suppression and Enhances Drug Efficacy in Anaplastic Thyroid Cancer in Female Mice. [Abstract]

2023 Aug 28;164(10):bqad135. PMID: 37702560
Analyst

Quantification of buparlisib in human liver microsomes employing an ultra-fast, sensitive UPLC-MS/MS method: in vitro and in silico metabolic stability evaluation. [Abstract]

2026 Feb 16;151(4):1058-1070. PMID: 41589698
Mol Carcinog

Four and a half LIM domains 2 (FHL2) attenuates tumorigenesis of gastrointestinal stromal tumors (GISTs) by negatively regulating KIT signaling. [Abstract]

2024 Jul;63(7):1334-1348. PMID: 38629424
Mol Carcinog

Epidermal growth factor receptor signaling in precancerous keratinocytes promotes neighboring head and neck cancer squamous cell carcinoma cancer stem cell-like properties and phosphoinositide 3-kinase inhibitor insensitivity. [Abstract]

2022 Jul;61(7):664-676. PMID: 35417043
BMC Anesthesiol

The expression of kappa-opioid receptor promotes the migration of breast cancer cells in vitro. [Abstract]

2021 Aug 30;21(1):210. PMID: 34461834
Brain Behav

Protective effect of docosahexaenoic acid on lipotoxicity-mediated cell death in Schwann cells: Implication of PI3K/AKT and mTORC2 pathways. [Abstract]

2018 Nov;8(11):e01123. PMID: 30264903

Buparlisib purchased from MedChemExpress. Usage Cited in: Brain Behav. 2018 Nov;8(11):e01123. [Abstract]

The effect of BKM120 on AKT phosphorylation is examined by Western blot.
PLoS One

PIK3CA missense mutations promote glioblastoma pathogenesis, but do not enhance targeted PI3K inhibition. [Abstract]

2018 Jul 5;13(7):e0200014. PMID: 29975751

Buparlisib purchased from MedChemExpress. Usage Cited in: PLoS One. 2018 Jul 5;13(7):e0200014. [Abstract]

Representative immunoblots of control and NHA^RAS treated with Buparlisib for 24 h.
PLoS One

Targeting the mTOR Complex by Everolimus in NRAS Mutant Neuroblastoma. [Abstract]

2016 Jan 28;11(1):e0147682. PMID: 26821351
Prostate

GOLM1 promotes prostate cancer progression through activating PI3K-AKT-mTOR signaling. [Abstract]

2018 Feb;78(3):166-177. PMID: 29181846

Buparlisib purchased from MedChemExpress. Usage Cited in: Prostate. 2018 Feb;78(3):166-177. [Abstract]

Western blot analysis of p-AKT (Ser473) in stable cell lines (Vector-DU145 and GOLM1-DU145) treated with 200 nM, 500 nM or 1 μM BKM120.
Clin Med Insights Oncol

Exploring the Clinical Implications of RPL3 Presence in BRCA-Associated Cancers: Unraveling the Interplay With Cancer Immunity. [Abstract]

2024 Oct 16:18:11795549241285387. PMID: 39429685
Mol Genet Genomics

Buparlisib induces eukaryotic elongation factor-2 expression to cause treatment failure for lung cancer cells. [Abstract]

2026 Jan 31;301(1):26. PMID: 41619002
In Vitro Cell Dev Biol Anim

Breast cancer organoids from malignant pleural effusion-derived tumor cells as an individualized medicine platform. [Abstract]

2021 May;57(5):510-518. PMID: 33950403
Am J Transl Res

PIK3CA mutations contribute to fulvestrant resistance in ER-positive breast cancer. [Abstract]

2019 Sep 15;11(9):6055-6065. PMID: 31632573
Anticancer Res

Broad-spectrum Preclinical Antitumor Activity of Eribulin (Halaven®): Combination with Anticancer Agents of Differing Mechanisms. [Abstract]

2018 Jun;38(6):3375-3385. PMID: 29848686
bioRxiv

Genome-wide profiling identifies the genetic dependencies of cell death following EGFR inhibition. [Abstract]

2025 Apr 9:2025.04.04.647273. PMID: 40291701
bioRxiv

2025 February 23.
bioRxiv

Pol II degradation activates cell death independently from the loss of transcription. [Abstract]

2024 Dec 10:2024.12.09.627542. PMID: 39713309
Biomed Pharmacother

Buparlisib and ponatinib inhibit aggressiveness of cholangiocarcinoma cells via suppression of IRS1-related pathway by targeting oxidative stress resistance. [Abstract]

2024 Nov:180:117569. PMID: 39418964
bioRxiv

2022 Aug 02.
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Endocytic vesicles act as vehicles for glucose uptake in response to growth factor stimulation. [Abstract]

2023 Jul 24:2023.07.23.550235. PMID: 37546742
University of Gothenburg

2023 Jun 27.
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Post-fast refeeding enhances intestinal stem cell-mediated regeneration and tumourigenesis through mTORC1-dependent polyamine synthesis. [Abstract]

2023 Jan 10:rs.3.rs-2320717. PMID: 36711807
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November 7th, 2022
Medizinische Hochschule Hannover

2020 Oct.
Universidad de Granada

2020 Sep.
Cold Spring Harb Mol Case Stud

Case report for an adolescent with germline RET mutation and alveolar rhabdomyosarcoma. [Abstract]

2020 Jun 12;6(3):a004853. PMID: 32532875
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Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (243.67 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4367 mL

12.1835 mL

24.3671 mL

5 mM

0.4873 mL

2.4367 mL

4.8734 mL

10 mM

0.2437 mL

1.2184 mL

2.4367 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline