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BKM120 (NVP-BKM120, Buparlisib)

(CAS No:944396-07-0)

Buparlisib (BKM120, NVP-BKM120) is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM in cell-free assays, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ. Phase 2.

CAS No:944396-07-0

Molecular Weight(MW):410.39

Purity:98%+

Specification:500mg;1g;5g;10g;50g;100g

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QC Documents

COA	MSDS	HPLC	NMR

ChemicalInfomation

CAS No:	944396-07-0
Molecular formula(MF)	C₁₈H₂₁F₃N₆O₂
Molecular Weight(MW):	410.39
Alias	NVP-BKM-120

Solubility

In vitro	DMSO	82 mg/mL (199.8 mM)
	Ethanol	2 mg/mL (4.87 mM)
	Water	<1 mg/mL
In vivo	0.5% CMC Na	6 mg/mL

Biological Activity

Description

Buparlisib (BKM120, NVP-BKM120) is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM in cell-free assays, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ. Phase 2.

Targets

p110α ^[1] (Cell-free assay)	p110δ ^[1] (Cell-free assay)	p110β ^[1] (Cell-free assay)	p110γ ^[1] (Cell-free assay)	Vps34 ^[1] (Cell-free assay)	View More
52 nM	116 nM	166 nM	262 nM	2.4 μM	View More

In vitro

BKM120 is not sensitive to Class III and Class IV PI3K's or PI4K. NVP-BKM120 shows great antiproliferation activity to PI3K deregulated cell lines including A2780, U87MG, MCF7 and DU145 with GI50 of 0.1-0.7 nM. ^[1] BKM120 induces multiple myeloma cells (ARP1, ARK, MM.1S, MM1.R and U266) apoptosis, which results in increased G1-phase cells and decreased S-phase cells. BKM120 induced CD138+ primary MM cell apoptosis and has significant lower cytotoxicity toward CD138− stromal cells. BKM120 exposure could cause upregulation of BimS and downregulation of XIAP. ^[2] BKM120 demonstrates antiproliferative activity in human gastric cancer cell lines by decreasing mTOR downstream signaling. BKM120 could increase either p-ERK or p-STAT3 in KRAS mutant gastric cancer cells. Combination with STAT3 blockade, BKM120 shows a synergism in cells harboring mutated KRAS by inducing apoptosis, but not in KRAS wild-type cells. ^[3] A recent study shows that BKM120 shows differential forms of cell death on the basis of p53 status of the cells with p53 wild-type cells undergoing apoptotic cell death and p53 mutant/deleted cells having a mitotic catastrophe cell death. BKM120 mediates mitotic catastrophe mainly through Aurora B kinase. ^[4]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
MCF7	Cytotoxic Assay		72 h	DMSO	Cytotoxicity against human MCF7 cells expressing PI3Kalpha E545K mutant with GI50 of 0.000158 Î¼M	24900266
DU145	Cytotoxic Assay		72 h	DMSO	Cytotoxicity against human DU145 cells expressing LKB1 mutant with GI50 of 0.000435 Î¼M	24900266
A2780	Cytotoxic Assay		72 h	DMSO	Cytotoxicity against PTEN-deficient human A2780 cells with GI50 of 0.000635 Î¼M	24900266
U87MG	Cytotoxic Assay		72 h	DMSO	Cytotoxicity against PTEN-deficient human U87MG cells with GI50 of 0.000698 Î¼M	24900266
A2780	Function Assay		1 h	DMSO	Inhibition of PI3K-mediated AKT Ser473 phosphorylation with EC50 of 0.055 Î¼M	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 Î¼M	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 Î¼M	24900266
MCF7	Function Assay		1 h	DMSO	Inhibition of PI3Kalpha E545K mutant-mediated AKT Ser473 phosphorylation with EC50 of 0.1 Î¼M	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 Î¼M	24900266
A2780	Growth Inhibition Assay		72 h	DMSO	EC50=0.52 Î¼M	24900266
SKMES-1	Cytotoxic Assay	1 Î¼M	72 h		Induces cell death	26013318
H596	Function Assay	1 Î¼M			Impairs cell migration	26013318
HCC2450	Function Assay	1 Î¼M			Impairs cell invasion	26013318
A549	Function Assay	500 nM	48 h	DMSO	Inhibits Akt activation	25937299
A549	Growth Inhibition Assay	1 Î¼M	72 h	DMSO	Inhibits cell growth	25937299
H522	Growth Inhibition Assay	1 Î¼M	72 h	DMSO	Inhibits cell growth	25937299
LNCaP	Function Assay	1 Î¼M			Suppresses p-AKT levels	25360799
LNCaP95	Function Assay	1 Î¼M			Suppresses p-AKT levels	25360799
HCT-15	Apotosis Assay	10 Î¼M	48 h	DMSO	Induces apoptosis in HCT-15 cells harbouring PIK3CA hotspot mutation	25152245
HCT-116	Apotosis Assay	10 Î¼M	48 h	DMSO	Induces apoptosis in HCT-116 cells harbouring PIK3CA hotspot mutation	25152245
NCI-H460	Apotosis Assay	10 Î¼M	48 h	DMSO	Induces apoptosis in NCI-H460 cells harbouring PIK3CA hotspot mutation	25152245
SKOV-3	Apotosis Assay	10 Î¼M	48 h	DMSO	Induces apoptosis in SKOV-3 cells harbouring PIK3CA hotspot mutation	25152245
BSY-1	Apotosis Assay	10 Î¼M	48 h	DMSO	Induces apoptosis in BSY-1 cells harbouring PIK3CA hotspot mutation	25152245
MKN-1	Apotosis Assay	10 Î¼M	48 h	DMSO	Induces apoptosis in MKN-1 cells harbouring PIK3CA hotspot mutation	25152245
NCI-H522	Apotosis Assay	10 Î¼M	48 h	DMSO	Induces apoptosis	25152245
OVCAR-3	Apotosis Assay	10 Î¼M	48 h	DMSO	Induces apoptosis	25152245
HBC-5	Apotosis Assay	10 Î¼M	48 h	DMSO	Induces apoptosis	25152245
RXF-631L	Apotosis Assay	10 Î¼M	48 h	DMSO	Induces apoptosis	25152245
MKN-45	Apotosis Assay	10 Î¼M	48 h	DMSO	Induces apoptosis	25152245
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
Huh7	Function Assay	1 Î¼M	1 h	DMSO	Inhibits phosphorylation of AKT at Ser474	25004403
BNL	Function Assay	1 Î¼M	1 h	DMSO	Inhibits phosphorylation of S6	25004403
MDA-MB-175	Growth Inhibition Assay	1 Î¼M	5 d	DMSO	IC50<1 Î¼M	24879796
MDA-MB-134	Growth Inhibition Assay	1 Î¼M	5 d	DMSO	IC50<1 Î¼M	24879796
HCC1500	Growth Inhibition Assay	1 Î¼M	5 d	DMSO	IC50<1 Î¼M	24879796
EFM-19	Growth Inhibition Assay	1 Î¼M	5 d	DMSO	IC50<1 Î¼M	24879796
ZR-75-30	Growth Inhibition Assay	1 Î¼M	5 d	DMSO	IC50<1 Î¼M	24879796
MDA-MB-361	Growth Inhibition Assay	1 Î¼M	5 d	DMSO	IC50<1 Î¼M	24879796
T-47D	Growth Inhibition Assay	1 Î¼M	5 d	DMSO	IC50<1 Î¼M	24879796
SK-BR-3	Growth Inhibition Assay	1 Î¼M	5 d	DMSO	IC50<1 Î¼M	24879796
UACC-732	Growth Inhibition Assay	1 Î¼M	5 d	DMSO	IC50<1 Î¼M	24879796
BT-474	Growth Inhibition Assay	1 Î¼M	5 d	DMSO	IC50<1 Î¼M	24879796
HCC202	Growth Inhibition Assay	1 Î¼M	5 d	DMSO	IC50<1 Î¼M	24879796
MCF7	Growth Inhibition Assay	1 Î¼M	5 d	DMSO	IC50<1 Î¼M	24879796
MDA-MB-415	Growth Inhibition Assay	1 Î¼M	5 d	DMSO	IC50<1 Î¼M	24879796
MDA-MB-453	Growth Inhibition Assay	1 Î¼M	5 d	DMSO	IC50<1 Î¼M	24879796
ZR-75-1	Growth Inhibition Assay	1 Î¼M	5 d	DMSO	IC50<1 Î¼M	24879796
HCC38	Growth Inhibition Assay	1 Î¼M	5 d	DMSO	IC50<1 Î¼M	24879796
HCC1419	Growth Inhibition Assay	1 Î¼M	5 d	DMSO	IC50<1 Î¼M	24879796
UACC-812	Growth Inhibition Assay	1 Î¼M	5 d	DMSO	IC50<1 Î¼M	24879796
HCC1187	Growth Inhibition Assay	1 Î¼M	5 d	DMSO	IC50<1 Î¼M	24879796
KPL-1	Growth Inhibition Assay	1 Î¼M	5 d	DMSO	IC50<1 Î¼M	24879796
SUM-225	Growth Inhibition Assay	1 Î¼M	5 d	DMSO	IC50<1 Î¼M	24879796
EFM-192A	Growth Inhibition Assay	1 Î¼M	5 d	DMSO	IC50<1 Î¼M	24879796
JIMT-1	Growth Inhibition Assay	1 Î¼M	5 d	DMSO	IC50<1 Î¼M	24879796
HCC1143	Growth Inhibition Assay	1 Î¼M	5 d	DMSO	IC50<1 Î¼M	24879796
HCC2218	Growth Inhibition Assay	1 Î¼M	5 d	DMSO	IC50<1 Î¼M	24879796
MDA-MB-468	Growth Inhibition Assay	1 Î¼M	5 d	DMSO	IC50<1 Î¼M	24879796
BT-20	Growth Inhibition Assay	1 Î¼M	5 d	DMSO	IC50<1 Î¼M	24879796
MDA-MB-435	Growth Inhibition Assay	1 Î¼M	5 d	DMSO	IC50<1 Î¼M	24879796
BT-549	Growth Inhibition Assay	1 Î¼M	5 d	DMSO	IC50<1 Î¼M	24879796
HCC1806	Growth Inhibition Assay	1 Î¼M	5 d	DMSO	IC50<1 Î¼M	24879796
HCC1937	Growth Inhibition Assay	1 Î¼M	5 d	DMSO	IC50<1 Î¼M	24879796
Hs578T	Growth Inhibition Assay	1 Î¼M	5 d	DMSO	IC50<1 Î¼M	24879796
LN18	Growth Inhibition Assay	20 Î¼M	72 h	DMSO	IC50<5 Î¼M	24741074
LN229	Growth Inhibition Assay	20 Î¼M	72 h	DMSO	IC50<5 Î¼M	24741074
LNZ308	Growth Inhibition Assay	20 Î¼M	72 h	DMSO	IC50<5 Î¼M	24741074
T98G	Growth Inhibition Assay	20 Î¼M	72 h	DMSO	IC50<5 Î¼M	24741074
U87	Growth Inhibition Assay	20 Î¼M	72 h	DMSO	IC50<5 Î¼M	24741074
LN18	Function Assay	5 Î¼M	24 h	DMSO	Inhibits phosphorylation of AKT	24741074
LNZ308	Function Assay	5 Î¼M	24 h	DMSO	Inhibits phosphorylation of AKT	24741074
Saos-2	Function Assay	50 Î¼M	48 h		Inhibits cell invasion	24727660
MG-63	Function Assay	50 Î¼M	48 h		Inhibits cell invasion	24727660
SJSA-1	Function Assay	50 Î¼M	48 h		Inhibits cell invasion	24727660
Saos-2	Function Assay	50 Î¼M	48 h		Inhibits matrix metalloproteinase-2 expression	24727660
MG-63	Function Assay	50 Î¼M	48 h		Inhibits matrix metalloproteinase-2 expression	24727660
SJSA-1	Function Assay	50 Î¼M	48 h		Inhibits matrix metalloproteinase-2 expression	24727660
Saos-2	Growth Inhibition Assay	50 Î¼M	48 h		Inhibits cell viability	24727660
MG-63	Growth Inhibition Assay	50 Î¼M	48 h		Inhibits cell viability	24727660
SJSA-1	Growth Inhibition Assay	50 Î¼M	48 h		Inhibits cell viability	24727660
FaDu	Function Assay	5 Î¼M	24 h	DMSO	Reduces oxygen consumption	24631147
EMT6	Function Assay	5 Î¼M	24 h	DMSO	Reduces oxygen consumption	24631147
HCT116	Function Assay	5 Î¼M	24 h	DMSO	Reduces oxygen consumption	24631147
U87	Function Assay	5 Î¼M	24 h	DMSO	Reduces oxygen consumption	24631147
GBM	Apoptosis Assay	2Î¼M	48h	DMSO	induced higher levels of apoptosis, and decreased cell viability	24500492
BON	Growth Inhibition Assay	1-5Î¼M	72h		decreases cell proliferation	24443523
BON	Apoptosis Assay	1-5Î¼M	24h		increases apoptosis	24443523
H1975	Growth Inhibition Assay	0.3-9.6Î¼M	72h	DMSO	IC50=1.385Î¼M	24337846
H1975	Apoptosis Assay	2Î¼M	24h	DMSO	increases apoptosis rate significantly	24337846
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
BCR-ABL	Growth Inhibition Assay	0.25-10Î¼M	4d		significantly inhibit cell proliferation	24244612
LC-1/SQSF	Function Assay	3Î¼M	24h	DMSO	decrease NRF2 protein level	23980093
Primary CLL cells	Apoptosis Assay	1-10Î¼M	48h		induces apoptosis in CLL cells independent of prognostic markers	23850807
Primary CLL cells	Kinase Assay	2Î¼M	30min		decreased PI3K activity	23850807
Primary CLL cells	Cytotoxic Assay	2Î¼M	24h		induces cell cytotoxicity	23850807
human NSCLC cell lines	Apoptosis Assay	0.125-4Î¼M	24h	DMSO	IC50s ranges from 0.4-2Î¼M	23562472
human HCC cell lines	Cell viability assay	0.005-1Î¼M	48h		IC50=1Î¼M	23489999
Huh7	Kinase Assay	1Î¼M	48h		signiï¬cantly reduces phosphorylation of Akt	23489999
SK-HEP1	Growth Inhibition Assay	1-20Î¼M	72h	DMSO	IC50ï¼1Î¼M	23479136
786-0	Growth Inhibition Assay	1-20Î¼M	72h	DMSO	IC50ï¼1Î¼M	23479136
JVM2	Cytotoxicity assay	0.2-20Î¼M	72h	DMSO	IC50=0.9Î¼M	23238639
EHEB	Cytotoxicity assay	0.2-20Î¼M	72h	DMSO	IC50=0.7Î¼M	23238639
MEC2	Cytotoxicity assay	0.2-20Î¼M	72h	DMSO	IC50=0.7Î¼M	23238639
primary B-CLL lymphocytes	Apoptosis Assay	IC50 for each primary cell line	24h	DMSO	IC50ï¼3Î¼M for all patients	23238639
primary B-CLL lymphocytes	Kinase Assay	IC50 for each primary cell line	24h		inhibits p70S6K & 4E-BP1 expression	23238639
human NSCLC	Growth Inhibition Assay	0.5-2Î¼M	72h		IC50=1Î¼M	22781393
human NSCLC	Kinase Assay	1Î¼M	24h		inhibits the Akt/mTOR signaling pathway at 3h after treatment	22781393
Y1 cell line	Growth Inhibition Assay	0.1Î¼M/1Î¼M	24h	DMSO	inhibits 60ï¼ cell viability in Myc-Sctr-transfected cells	22692904
PIK3CA-mutant MCF7	Growth Inhibition Assay	GI50=160Â±91nMï¼LD50=980Â±273nM	72h		GI50=160Â±91nMï¼LD50=980Â±273nM	22653967
PIK3CA-mutant MCF7	Kinase Assay	IC50=114Â±3nM	72h		IC50=114Â±3nM in reducing Akt phosphorylation levels	22653967
MCF7-myr-Akt	Growth Inhibition Assay	GI50=299Â±68nMï¼LD50ï¼10,000nM	72h		GI50=299Â±68nMï¼LD50ï¼10,000nM	22653967
colon cancer cell lines	Growth Inhibition Assay	0-10Î¼M	72h	DMSO	IC50=1Î¼M	22543857
gastric cancer cell lines	Growth Inhibition Assay	0-10Î¼M	72h	DMSO	IC50=2-5Î¼M	22543857
HCT-116/HT-29/MKN-45	Apoptosis Assay	2Î¼M	48h		shift in G2 phase	22543857
HT-29 and HCT-116	Caspase assay	5Î¼M	24h		induces caspase activity	22543857
MM cell lines	Growth Inhibition Assay	10Î¼M	24h	DMSO	IC50 varies among different cell lines in time and dose dependence	22207485
ARP-1	Apoptosis Assay	10Î¼M	24h	DMSO	induces MM cell apoptosis through caspase activation	22207485
SNU-601	Growth Inhibition Assay		72h	DMSO	IC50=0.816Â±0.063Î¼M	22159814
SNU-1	Growth Inhibition Assay		72h	DMSO	IC50=1.082Â±0.028Î¼M	22159814
SNU-668	Growth Inhibition Assay		72h	DMSO	IC50=1.579Â±0.074Î¼M	22159814
AGS	Growth Inhibition Assay		72h	DMSO	IC50=1.714Â±0.117Î¼M	22159814
SNU-216	Growth Inhibition Assay		72h	DMSO	IC50=2.692Â±0.082Î¼M	22159814
SNU-5	Growth Inhibition Assay		72h	DMSO	IC50=1.351Â±0.091Î¼M	22159814
SNU-638	Growth Inhibition Assay		72h	DMSO	IC50=2.282Â±0.053Î¼M	22159814
SNU-16	Growth Inhibition Assay		72h	DMSO	IC50=1.573Â±0.001Î¼M	22159814
SNU-484	Growth Inhibition Assay		72h	DMSO	IC50=1.728Â±0.045Î¼M	22159814
SNU-620	Growth Inhibition Assay		72h	DMSO	IC50=2.939Â±0.001Î¼M	22159814
SNU-719	Growth Inhibition Assay		72h	DMSO	IC50=3.037Â±0.032Î¼M	22159814
glioma cell lines	Growth Inhibition Assay		72h		IC50=1-2Î¼M	22065080
U87	Apoptosis Assay	2Î¼M	72h		induces cell apoptosis and cleaved PARP and caspase-3	22065080

... Click to View More Cell Line Experimental Data

In vivo

BKM120 completely inhibits pAktser473 in A2780 xenograft tumors at doses of 30, 60, or 100 mg/kg, respectively. BKM120 also shows antitumor activity against U87MG glioma model at doses of 30 and 60 mg/kg. ^[1] BKM120 treatment results in significantly reduced tumor volume and level of circulating human kappa chain at 5 μM/kg/day−1in ARP1 SCID mouse model, with prolonged survival. ^[2]