Buparlisib (BKM120, NVP-BKM120)

Catalog No.S2247

Molecular Weight(MW): 410.39

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.

Cited by 135 Publications

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Nature, 2016, 529(7586):413-417

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Biochem Biophys Res Commun, 2019, 513(3):546-552

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Leuk Lymphoma, 2019, 10.1080/10428194.2019.1594211

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Cancer Lett, 2018, 439:56-65

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University Gattingen, 2013, Elisabeth Hand

PubMed: ( click the link to review the publication )

Purity & Quality Control

Choose Selective PI3K Inhibitors

Biological Activity

Description

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	M2KyfWN6fG:2b4jpZ{BCe3OjeR?=		NXLNeGtMPzJiaB?=	MlLsSG1UVw>?	NIDS[4ZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0Z5IHPlcIx{KGW6cILld5NqdmdiUFmzT4FteGijIFW1OFVMKG23dHHueEB4cXSqIFfJOVAhd2ZiMD6wNFAyPThizszN	MXeyOFkxODJ4Nh?=
DU145	NFfaeJVEgXSxdH;4bYMhSXO\|YYm=		MnzRO\|IhcA>?	NYrxSYl1TE2VTx?=	NX;UTlFZS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hTFVzNEWgZ4VtdHNiZYjwdoV{e2mwZzDMT2IyKG23dHHueEB4cXSqIFfJOVAhd2ZiMD6wNFA1OzVizszN	M{\5clI1QTByMk[2
A2780	NGm2WXJEgXSxdH;4bYMhSXO\|YYm=		MlvjO\|IhcA>?	NFXIZo1FVVOR	NInrTXVEgXSxdH;4bYNqfHliYXfhbY5{fCCSVFXOMYRm\mmlaXXueEBpfW2jbjDBNlc5OCClZXzsd{B4cXSqIFfJOVAhd2ZiMD6wNFA3OzVizszN	NFi0R4szPDlyMEK2Oi=>
U87MG	Mn7PR5l1d3SxeHnjJGF{e2G7		Mn;EO\|IhcA>?	NUfybYhpTE2VTx?=	NYTkcFR6S3m2b4TvfIlkcXS7IHHnZYlve3RiUGTFUk1l\W[rY3nlcpQhcHWvYX6gWVg4VUdiY3XscJMhf2m2aDDHTVUxKG:oIECuNFAxPjl6IN88US=>	Mkj5NlQ6ODB{Nk[=
A2780	NGDJb4tHfW6ldHnvckBCe3OjeR?=		M3fOPFEhcA>?	MXrEUXNQ	NEO2eJJKdmirYnn0bY9vKG:oIGDJN2sudWWmaXH0[YQhSUuWIGPldlQ4OyCyaH;zdIhwenmuYYTpc44hf2m2aDDFR\|UxKG:oIECuNFU2KM7:TR?=	MYOyOFkxODJ4Nh?=
DU145	NGq4SVZHfW6ldHnvckBCe3OjeR?=		MmTVNUBp	NX3TU\|k1TE2VTx?=	NEWwVGNKdmirYnn0bY9vKG:oIGDJN2sudWWmaXH0[YQhSUuWIGPldlQ4OyCyaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hTFVzNEWgZ4VtdHNiaHHyZo9zcW6pIFzLRlEhdXW2YYTpc44hf2m2aDDFR\|UxKG:oIECuNFc{KM7:TR?=	MXmyOFkxODJ4Nh?=
A2780	M3H1cWZ2dmO2aX;uJGF{e2G7		M3;IXlEhcA>?	MlrYSG1UVw>?	NVvwbYVUUW6qaXLpeIlwdiCxZjDQTVNMNW2nZHnheIVlKEGNVDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKGmwIGDUSW4u\GWoaXPp[Y51KGi3bXHuJGEzPzhyIHPlcIx{KHerdHigSWM2OCCxZjCwMlA4PCEQvF2=	M2rVflI1QTByMk[2
MCF7	NVfEXGdtTnWwY4Tpc44hSXO\|YYm=		M3TjOVEhcA>?	MU\EUXNQ	NWOwfpE3UW6qaXLpeIlwdiCxZjDQTVNM[WyyaHGgSVU1PUtibYX0ZY51NW2nZHnheIVlKEGNVDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKHerdHigSWM2OCCxZjCwMlEh\|ryP	NXOyToh6OjR7MECyOlY>
U87MG	MU\GeY5kfGmxbjDBd5NigQ>?		NGHjSo0yKGh?	NGPDclNFVVOR	NH3wSoxKdmirYnn0bY9vKG:oIGDJN2sudWWmaXH0[YQhSUuWIGPldlQ4OyCyaH;zdIhwenmuYYTpc44hcW5iUGTFUk1l\W[rY3nlcpQhcHWvYX6gWVg4VUdiY3XscJMhf2m2aDDFR\|UxKG:oIECuNVMh\|ryP	NGmxXWYzPDlyMEK2Oi=>
A2780	NVjUVmpyT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		M3HCcFczKGh?	NGfkOmRFVVOR	M3Ox[GVEPTB;MD61NkDPxE1?	M1PFUFI1QTByMk[2
SKMES-1	MoTLR5l1d3SxeHnjJGF{e2G7	M3\UVFEh\|ryP	M1nlPFczKGh?		M2LENGlv\HWlZYOgZ4VtdCCmZXH0bC=>	MmfZNlYxOTN\|MUi=
H596	NEXQUnBHfW6ldHnvckBCe3OjeR?=	NWj4XXppOSEQvF2=			NVvzRopiUW2yYXnyd{Bk\WyuIH3p[5JifGmxbh?=	MnmyNlYxOTN\|MUi=
HCC2450	M4Pl[2Z2dmO2aX;uJGF{e2G7	MYmxJO69VQ>?			M4\xWWlueGGrcoOgZ4VtdCCrbo\hd4lwdg>?	M1zoWVI3ODF\|M{G4
A549	NFT0NGZHfW6ldHnvckBCe3OjeR?=	NI\IbFQ2ODBibl2=	NGHYSWE1QCCq	M1fzWGROW09?	MWfJcohq[mm2czDBb5Qh[WO2aY\heIlwdg>?	MorXNlU6Ozd{OUm=
A549	MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MXexJO69VQ>?	NFPwZXM4OiCq	MULEUXNQ	NULocZg4UW6qaXLpeJMh[2WubDDndo94fGh?	Mn;DNlU6Ozd{OUm=
H522	NVLhUWlZT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M2TKdlEh\|ryP	M3\xSVczKGh?	MWPEUXNQ	NGnKdXlKdmirYnn0d{Bk\WyuIHfyc5d1cA>?	NIrCTYEzPTl\|N{K5PS=>
LNCaP	M1HLNmZ2dmO2aX;uJGF{e2G7	M4rGfVEh\|ryP			NFXvTZZUfXCycnXzd4V{KHBvQVvUJIxmfmWucx?=	NY[xbox[OjV\|NkC3PVk>
LNCaP95	MoTmSpVv[3Srb36gRZN{[Xl?	NWL2dXFbOSEQvF2=			MkjXV5VxeHKnc4Pld{BxNUGNVDDs[ZZmdHN?	M3e2PFI2OzZyN{m5
HCT-15	MWfBdI91d3OrczDBd5NigQ>?	MWqxNEDPxE1?	NX3TPXlQPDhiaB?=	MoDoSG1UVw>?	Ml;YTY5lfWOnczDhdI9xfG:\|aYOgbY4hUEOWLUG1JINmdGy\|IHjhdoJwfXKrbnegVGlMO0ODIHjveJNxd3RibYX0ZZRqd25?	NWnOeoVbOjVzNUKyOFU>
HCT-116	NGLJfFVCeG:2b4Ppd{BCe3OjeR?=	NHfVVGkyOCEQvF2=	NFHOcJY1QCCq	MYLEUXNQ	M13rW2lv\HWlZYOgZZBweHSxc3nzJIlvKEiFVD2xNVYh[2WubIOgbIFz[m:3cnnu[{BRUUt\|Q1GgbI91e3CxdDDteZRifGmxbh?=	NHHaem0zPTF3MkK0OS=>
NCI-H460	M3XTeGFxd3Sxc3nzJGF{e2G7	NGH3eVkyOCEQvF2=	NETSOWY1QCCq	NGWyZZRFVVOR	NITEfYJKdmS3Y3XzJIFxd3C2b4Ppd{BqdiCQQ1mtTFQ3OCClZXzsd{Bp[XKkb4XybY5oKFCLS{PDRUBpd3S\|cH;0JI12fGG2aX;u	NFu2WIYzPTF3MkK0OS=>
SKOV-3	Mn\0RZBwfG:\|aYOgRZN{[Xl?	MnvvNVAh\|ryP	NYfJd5JFPDhiaB?=	NGPYTlVFVVOR	MkOxTY5lfWOnczDhdI9xfG:\|aYOgbY4hW0uRVj2zJINmdGy\|IHjhdoJwfXKrbnegVGlMO0ODIHjveJNxd3RibYX0ZZRqd25?	NX;rZ5BwOjVzNUKyOFU>
BSY-1	NFr4[3hCeG:2b4Ppd{BCe3OjeR?=	M4fZdVExKM7:TR?=	Mo\jOFghcA>?	MlX5SG1UVw>?	NX7JN\|lLUW6mdXPld{BieG:ydH;zbZMhcW5iQmPZMVEh[2WubIOgbIFz[m:3cnnu[{BRUUt\|Q1GgbI91e3CxdDDteZRifGmxbh?=	M4\aTVI2OTV{MkS1
MKN-1	MmfIRZBwfG:\|aYOgRZN{[Xl?	M3nSd\|ExKM7:TR?=	NEW4NmY1QCCq	MY\EUXNQ	NF\1eZpKdmS3Y3XzJIFxd3C2b4Ppd{BqdiCPS16tNUBk\WyuczDoZZJjd3W{aX7nJHBKUzOFQTDoc5R{eG:2IH31eIF1cW:w	NYLGcGNXOjVzNUKyOFU>
NCI-H522	Mn3NRZBwfG:\|aYOgRZN{[Xl?	NVHETmFDOTBizszN	NGHvW3c1QCCq	NVHrOlgyTE2VTx?=	M{PjcGlv\HWlZYOgZZBweHSxc3nz	NFfVS4EzPTF3MkK0OS=>
OVCAR-3	M3m1ZWFxd3Sxc3nzJGF{e2G7	M2fHbFExKM7:TR?=	NVjRe5ZqPDhiaB?=	M4XhbWROW09?	MWrJcoR2[2W\|IHHwc5B1d3Orcx?=	NVK5TGJtOjVzNUKyOFU>
HBC-5	MYrBdI91d3OrczDBd5NigQ>?	NFi3c\|EyOCEQvF2=	MnPyOFghcA>?	NIPqTnNFVVOR	NWTUVYg5UW6mdXPld{BieG:ydH;zbZM>	NUHaR2V2OjVzNUKyOFU>
RXF-631L	MWPBdI91d3OrczDBd5NigQ>?	NEnB[pUyOCEQvF2=	NV\jUYxyPDhiaB?=	M{DuVGROW09?	NUHhNnB5UW6mdXPld{BieG:ydH;zbZM>	MmPuNlUyPTJ{NEW=
MKN-45	NFe5V4NCeG:2b4Ppd{BCe3OjeR?=	MUOxNEDPxE1?	NU\zPY53PDhiaB?=	NVe2ZpF4TE2VTx?=	MlPCTY5lfWOnczDhdI9xfG:\|aYO=	NYXhPXZZOjVzNUKyOFU>
BON-1	MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M1\QT\|UxOCCwTR?=	MXmxNEBl	MU\EUXNQ	M2XoVGlvcGmkaYTzJINmdGxiZ4Lve5Rp	M3PvZ\|I2ODJ4Mkmy
BON-1	M4\wSGZ2dmO2aX;uJGF{e2G7	MWK1NFAhdk1?	NFK1eG81KGh?	MVnEUXNQ	MVPJcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRWtVKGG2IGTodlMxQCCjbnSgV4VzPDd\|	MoDONlUxOjZ{OUK=
QGP-1	NU\VboFPTnWwY4Tpc44hSXO\|YYm=	M3HRXFUxOCCwTR?=	NI\5THY1KGh?	NUTFO\|F[TE2VTx?=	NHX1THNKdmirYnn0d{BxcG:\|cHjvdplt[XSrb36gc4YhSUuWIHH0JHRpejNyODDhcoQhW2W{NEez	NH\WUZAzPTB{NkK5Ni=>
Huh7	MV7GeY5kfGmxbjDBd5NigQ>?	M33yPVEh\|ryP	MVmxJIg>	M4GydWROW09?	MYDJcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRWtVKGG2IGPldlQ4PA>?	MUmyOVAxPDRyMx?=
BNL	MXHGeY5kfGmxbjDBd5NigQ>?	NVz0dWJtOSEQvF2=	MmDZNUBp	NHzofGZFVVOR	MnfFTY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJHM3	MUKyOVAxPDRyMx?=
MDA-MB-175	NV;0WmpUT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MXGxJO69VQ>?	MnnwOUBl	MYTEUXNQ	NHvaXGlKSzVyPEGg{txO	MWiyOFg4QTd7Nh?=
MDA-MB-134	MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M3\Cc\|Eh\|ryP	NHvvXHU2KGR?	NX3se3dzTE2VTx?=	MWXJR\|UxRDFizszN	MWiyOFg4QTd7Nh?=
HCC1500	MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M3HSSVEh\|ryP	M4TvNFUh\A>?	NXT4dZB4TE2VTx?=	MmfLTWM2ODxzIN88US=>	NEDXbHIzPDh5OUe5Oi=>
EFM-19	NUjGTZNST3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NYXtWJVLOSEQvF2=	NVf1PHhYPSCm	MoTDSG1UVw>?	MV7JR\|UxRDFizszN	NULRUlM2OjR6N{m3PVY>
ZR-75-30	M3GyWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MmPpNUDPxE1?	NGjFSIo2KGR?	NGjHXXhFVVOR	M176ZmlEPTB:MTFOwG0>	M4nnXVI1QDd7N{m2
MDA-MB-361	M{Ht[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NF7WSXoyKM7:TR?=	NU\DOFkzPSCm	NV73XWc6TE2VTx?=	M{XpZmlEPTB:MTFOwG0>	MUKyOFg4QTd7Nh?=
T-47D	NVTQUFdWT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NUDzelJtOSEQvF2=	NHHyWVI2KGR?	MlX6SG1UVw>?	M{\EdmlEPTB:MTFOwG0>	NGDFblgzPDh5OUe5Oi=>
SK-BR-3	M1u2emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NVryUoVlOSEQvF2=	M3\0NFUh\A>?	NIPT[HFFVVOR	MnqyTWM2ODxzIN88US=>	NFTBPZgzPDh5OUe5Oi=>
UACC-732	M4rtbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	Ml3DNUDPxE1?	NIXRRYQ2KGR?	MnXsSG1UVw>?	Mn3tTWM2ODxzIN88US=>	MViyOFg4QTd7Nh?=
BT-474	NFvFUXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NFnJcXgyKM7:TR?=	NV3jbnpnPSCm	MYLEUXNQ	M3zUU2lEPTB:MTFOwG0>	M2X5OFI1QDd7N{m2
HCC202	MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NVjCZo1iOSEQvF2=	NV6zTINWPSCm	M1H2fGROW09?	NXTnOXZ4UUN3MEyxJO69VQ>?	M1r4RlI1QDd7N{m2
MCF7	NU\Wd403T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NHXYZ\|MyKM7:TR?=	NUDPVm1bPSCm	NEHTTJpFVVOR	MXLJR\|UxRDFizszN	MlX2NlQ5Pzl5OU[=
MDA-MB-415	NF3jdXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MVWxJO69VQ>?	M3[4SFUh\A>?	MWfEUXNQ	MYLJR\|UxRDFizszN	NIDEenIzPDh5OUe5Oi=>
MDA-MB-453	MlzBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M{DyWlEh\|ryP	M2SweVUh\A>?	M1TVSmROW09?	NGTOWHpKSzVyPEGg{txO	M2rZNFI1QDd7N{m2
ZR-75-1	NIjMdZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	Ml;yNUDPxE1?	MXm1JIQ>	NHfrTolFVVOR	MWjJR\|UxRDFizszN	M4S3RlI1QDd7N{m2
HCC38	Mkm0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M{naUFEh\|ryP	M{nFTFUh\A>?	M4PXWWROW09?	NEfKPWpKSzVyPEGg{txO	NHz5WVkzPDh5OUe5Oi=>
HCC1419	MlmyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NITCOnUyKM7:TR?=	NVnjS5I5PSCm	NGTYOGpFVVOR	MYHJR\|UxRDFizszN	NYfQRXpyOjR6N{m3PVY>
UACC-812	MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NX3QUlg3OSEQvF2=	MnXHOUBl	NICzXZpFVVOR	NFnRV2JKSzVyPEGg{txO	M4DEflI1QDd7N{m2
HCC1187	MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MkDtNUDPxE1?	M3zsNFUh\A>?	NYqzS\|JLTE2VTx?=	MXnJR\|UxRDFizszN	NXP4PYlYOjR6N{m3PVY>
KPL-1	M3PWeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M3LRflEh\|ryP	MkDOOUBl	NYDMUZlTTE2VTx?=	NWPQ[4ZPUUN3MEyxJO69VQ>?	MV6yOFg4QTd7Nh?=
SUM-225	NF[1T4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NF[5eVYyKM7:TR?=	Mo\5OUBl	MWrEUXNQ	NE\GR5RKSzVyPEGg{txO	M3LUc\|I1QDd7N{m2
EFM-192A	M{TZNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NUfueHpuOSEQvF2=	NG\wXYg2KGR?	MkLpSG1UVw>?	Mn\ZTWM2ODxzIN88US=>	Mom0NlQ5Pzl5OU[=
JIMT-1	MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NYO3TW0{OSEQvF2=	M{LZOVUh\A>?	NUWySmVWTE2VTx?=	MYLJR\|UxRDFizszN	MYqyOFg4QTd7Nh?=
HCC1143	MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MXSxJO69VQ>?	M4rz[lUh\A>?	MVTEUXNQ	M1i5SmlEPTB:MTFOwG0>	Mn\PNlQ5Pzl5OU[=
HCC2218	NVjUSW1MT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NVOxSWxqOSEQvF2=	NWLYWpp6PSCm	MYfEUXNQ	MYXJR\|UxRDFizszN	M4DrdlI1QDd7N{m2
MDA-MB-468	NHXYWFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MV6xJO69VQ>?	NVnYOXhEPSCm	NH;kWlRFVVOR	NF3wenlKSzVyPEGg{txO	M2HQcVI1QDd7N{m2
BT-20	MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NYjUc3R4OSEQvF2=	M{jacVUh\A>?	NUnCW4h{TE2VTx?=	M2\UbWlEPTB:MTFOwG0>	MXuyOFg4QTd7Nh?=
MDA-MB-435	MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MmPGNUDPxE1?	NIXMOHc2KGR?	NGK1UFFFVVOR	M13ZfGlEPTB:MTFOwG0>	M4fMdlI1QDd7N{m2
BT-549	NYPEbXo4T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M2nX[FEh\|ryP	NGHrXoY2KGR?	NYPRXoJITE2VTx?=	NEfpe3lKSzVyPEGg{txO	MWCyOFg4QTd7Nh?=
HCC1806	NVzVbZJtT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NF;5bJEyKM7:TR?=	MYK1JIQ>	MnnWSG1UVw>?	NW\UZVA4UUN3MEyxJO69VQ>?	NH3WeGozPDh5OUe5Oi=>
HCC1937	NEfvdmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MVKxJO69VQ>?	NV\yVFN5PSCm	MlnqSG1UVw>?	MYLJR\|UxRDFizszN	MmezNlQ5Pzl5OU[=
Hs578T	M3zC[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MlW0NUDPxE1?	MkXwOUBl	NEOzV5JFVVOR	MV\JR\|UxRDFizszN	NFfveIozPDh5OUe5Oi=>
LN18	NFq1OmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NYPGbXVDOjBizszN	M3v4VlczKGh?	NYnqN3ptTE2VTx?=	NWXIT\|VDUUN3MEy1JO69VQ>?	M3\LdVI1PzRzMEe0
LN229	NVXqW3ZZT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NHzxZnczOCEQvF2=	NETpSnk4OiCq	M3vEbWROW09?	MkG1TWM2ODx3IN88US=>	Mke3NlQ4PDFyN{S=
LNZ308	NVTvfmxUT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NX30S\|Z6OjBizszN	NEPGSFY4OiCq	NUfPdHFKTE2VTx?=	MYrJR\|UxRDVizszN	M4n0SFI1PzRzMEe0
T98G	NIL4ZmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MWOyNEDPxE1?	M3GwVVczKGh?	NYjm[mIzTE2VTx?=	NVPGT2RiUUN3MEy1JO69VQ>?	NELUdo8zPDd2MUC3OC=>
U87	NYfoPGJ3T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MYOyNEDPxE1?	MoDQO\|IhcA>?	NYCyPGZETE2VTx?=	NYXwPGltUUN3MEy1JO69VQ>?	NYnhS\|NzOjR5NEGwO\|Q>
LN18	MXzGeY5kfGmxbjDBd5NigQ>?	MUG1JO69VQ>?	NXu1eHdHOjRiaB?=	M4jwRmROW09?	MVfJcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRWtV	NVz1SGpvOjR5NEGwO\|Q>
LNZ308	M3TGUWZ2dmO2aX;uJGF{e2G7	M3LhVVUh\|ryP	M{DXSVI1KGh?	NVfWeFFDTE2VTx?=	MXnJcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRWtV	M1fxbVI1PzRzMEe0
Saos-2	MXXGeY5kfGmxbjDBd5NigQ>?	MkPZOVAh\|ryP	NX3jd3B4PDhiaB?=		MXrJcohq[mm2czDj[YxtKGmwdnHzbY9v	NGDKSnozPDd{N{[2NC=>
MG-63	Mk\kSpVv[3Srb36gRZN{[Xl?	NF;tTm82OCEQvF2=	NUfudGFxPDhiaB?=		MlTBTY5pcWKrdIOgZ4VtdCCrbo\hd4lwdg>?	MlTmNlQ4Ojd4NkC=
SJSA-1	NWDvbGtiTnWwY4Tpc44hSXO\|YYm=	MX[1NEDPxE1?	NF;lU\|k1QCCq		MoLjTY5pcWKrdIOgZ4VtdCCrbo\hd4lwdg>?	Ml2wNlQ4Ojd4NkC=
Saos-2	M2n2UmZ2dmO2aX;uJGF{e2G7	NYfxXpFOPTBizszN	NIPzboE1QCCq		M4n2eWlvcGmkaYTzJI1ifHKreDDt[ZRidGyxcILveIVqdmG\|ZT2yJIV5eHKnc4Ppc44>	MoeyNlQ4Ojd4NkC=
MG-63	MnfvSpVv[3Srb36gRZN{[Xl?	MX[1NEDPxE1?	MXS0PEBp		M4i3RWlvcGmkaYTzJI1ifHKreDDt[ZRidGyxcILveIVqdmG\|ZT2yJIV5eHKnc4Ppc44>	NH:wVokzPDd{N{[2NC=>
SJSA-1	NXfBOVJWTnWwY4Tpc44hSXO\|YYm=	MoL2OVAh\|ryP	MYe0PEBp		NXv2R3gyUW6qaXLpeJMhdWG2cnn4JI1mfGGubH;wdo91\WmwYYPlMVIh\XiycnXzd4lwdg>?	NXzGZ5JGOjR5Mke2OlA>
Saos-2	Moj3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NXXYbVNLPTBizszN	MV:0PEBp		M3XoUWlvcGmkaYTzJINmdGxidnnhZoltcXS7	NEPm[5EzPDd{N{[2NC=>
MG-63	M2rBeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M4nqUFUxKM7:TR?=	MXu0PEBp		MUjJcohq[mm2czDj[YxtKH[rYXLpcIl1gQ>?	NHXGZpIzPDd{N{[2NC=>
SJSA-1	NUHXZVcxT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MnLmOVAh\|ryP	NULx[mVYPDhiaB?=		MX\Jcohq[mm2czDj[YxtKH[rYXLpcIl1gQ>?	NHvabowzPDd{N{[2NC=>
FaDu	M3LwbmZ2dmO2aX;uJGF{e2G7	NEGzZ4k2KM7:TR?=	NYHDUpJbOjRiaB?=	NHzGdZFFVVOR	NFrKdJFT\WS3Y3XzJI95gWenbjDjc45{fW2ydHnvci=>	NWDCRVNwOjR4M{GxOFc>
EMT6	NVX2cZpVTnWwY4Tpc44hSXO\|YYm=	M4PrV\|Uh\|ryP	MXSyOEBp	MoKySG1UVw>?	MkLxVoVlfWOnczDvfJlo\W5iY3;ud5VueHSrb36=	NYfaRpBZOjR4M{GxOFc>
HCT116	M3Lr[GZ2dmO2aX;uJGF{e2G7	MWK1JO69VQ>?	MX[yOEBp	MUDEUXNQ	NIfSW49T\WS3Y3XzJI95gWenbjDjc45{fW2ydHnvci=>	MoLaNlQ3OzFzNEe=
U87	MmezSpVv[3Srb36gRZN{[Xl?	NGSxPWk2KM7:TR?=	MWOyOEBp	M3y0ZWROW09?	MYfS[YR2[2W\|IH;4fYdmdiClb37zeY1xfGmxbh?=	M1ryRVI1PjNzMUS3
GBM	NVX0OVZpSXCxcITvd4l{KEG\|c3H5	MV[y{txO	MkWwOFhp	NFrUPJlFVVOR	NX7LSpRrcW6mdXPl[EBpcWeqZYKgcIV3\Wy\|IH;mJIFxd3C2b4Ppd{wh[W6mIHTlZ5Jm[XOnZDDj[YxtKH[rYXLpcIl1gQ>?	NFvr[VgzPDVyMES5Ni=>
BON	Ml3BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NXnt[WV2OS13zszN	MVO3Nog>		NH7hblll\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9v	NH3KU5EzPDR2M{WyNy=>
BON	NFThbWNCeG:ydH;zbZMhSXO\|YYm=	M36zSFEuPc7:TR?=	NWW2dFNZOjSq		MojrbY5kemWjc3XzJIFxd3C2b4Ppdy=>	NVzIR4RwOjR2NEO1NlM>
H1975	MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M4rtcFAvOy17LkdOwG0>	MoPIO\|Jp	NY\2WllbTE2VTx?=	MUDJR\|UxRTFwM{i1{txO	NXfkcmRrOjR\|M{e4OFY>
H1975	M2TSUWFxd3C2b4Ppd{BCe3OjeR?=	M1zoeFLPxE1?	M2XqUlI1cA>?	NFO0eHNFVVOR	NFzJNodqdmO{ZXHz[ZMh[XCxcITvd4l{KHKjdHWgd4lodmmoaXPhcpRtgQ>?	M2XtO\|I1OzN5OES2
T-ALL	MUjBdI9xfG:\|aYOgRZN{[Xl?	M3PZfIJmfHenZX6gNU41KGGwZDC1MlMhdU1iYYSgNlRpKGGwZDCwMlkh[W6mIEWuOUBuVSCjdDC0PIghcW5iZHnm[oVz\W62IHPlcIwhdGmwZR?=	NI\LfmYzPCCxcjC0PIg>	M3nnfmROW09?	MXvh[oZm[3S\|IITo[UBRUTONIIDheIh4[XliaX6gWE1CVExiY3XscEBtcW6ncx?=	MorwNlQ{OTB5M{[=
BCR-ABL	NYLlN5pNT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MkfONE4zPS1zMN88US=>	M2LQNlRl		Mk[2d4lodmmoaXPhcpRtgSCrbnjpZol1KGOnbHygdJJwdGmoZYLheIlwdg>?	NFHKSFkzPDJ2NE[xNi=>
LC-1/SQSF	MXLGeY5kfGmxbjDBd5NigQ>?	M1O3bVPPxE1?	MYmyOIg>	NWTGV41NTE2VTx?=	MUHk[YNz\WG\|ZTDOVmYzKHC{b4TlbY4hdGW4ZXy=	NX3mTplWOjN7OECwPVM>
Primary CLL cells	MkfyRZBweHSxc3nzJGF{e2G7	MoLhNU0yOM7:TR?=	MWG0PIg>		NWXPclB5cW6mdXPld{BieG:ydH;zbZMhcW5iQ1zMJINmdGy\|IHnu[IVx\W6mZX70JI9nKHC{b3fuc5N1cWNibXHyb4Vzew>?	M{n1U\|I{QDVyOEC3
Primary CLL cells	MY\LbY5ie2ViQYPzZZk>	M1m5SlLPxE1?	NU\5dWoxOzCvaX6=		Mkmz[IVkemWjc3XkJHBKO0tiYXP0bZZqfHl?	NIXjUIQzOzh3MEiwOy=>
Primary CLL cells	NHLw[VBEgXSxdH;4bYMhSXO\|YYm=	NVjxeGNpOs7:TR?=	MlHTNlRp		MnTUbY5lfWOnczDj[YxtKGO7dH;0c5hq[2m2eR?=	NYrBSJRNOjN6NUC4NFc>
human NSCLC cell lines	MmPXRZBweHSxc3nzJGF{e2G7	MmjZNE4yOjVvNN88US=>	MUOyOIg>	NFPl[o5FVVOR	MYHJR\|UxeyC{YX7n[ZMh\nKxbTCwMlQuOs7:TR?=	M{C2WFI{PTZ{NEey
human HCC cell lines	Mn;tR4VtdCC4aXHibYxqfHliYYPzZZk>	MUmwMlAxPS1zzszN	M33O[FQ5cA>?		MXrJR\|UxRTIQvF2=	NEDUWJkzOzR6OUm5PS=>
Huh7	NIHuXnZMcW6jc3WgRZN{[Xl?	Ml;ZNe69VQ>?	NH7ESFU1QGh?		MULzbYdvce,ugXPhcpRtgSC{ZXT1Z4V{KHCqb4PwbI9zgWyjdHnvckBw\iCDa4S=	MoDwNlM1QDl7OUm=
SK-HEP1	NIPZUY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NV\z[lZsOS1{MN88US=>	NVzDPYR1PzKq	M{jVTWROW09?	M3fBVWlEPTExvKyx{txO	NYPDZlJZOjN2N{mxN\|Y>
786-0	NYPQO3FFT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NEXJRVMyNTJyzszN	NFnq[W04Omh?	M36wXmROW09?	NEC3TnVKSzVy78{cNe69VQ>?	MWqyN\|Q4QTF\|Nh?=
JVM2	M3Kxd2N6fG:2b4jpZ4l1gSCjc4PhfS=>	M4K1fVAvOi1{MN88US=>	M2XTVVczcA>?	MWXEUXNQ	M{TLbGlEPTB;MD65{txO	Mk\ENlMzOzh4M{m=
EHEB	MlXwR5l1d3SxeHnjbZR6KGG\|c3H5	NH2zNI8xNjJvMkFOwG0>	NVjmNZZZPzKq	MYLEUXNQ	NWeydXAzUUN3ME2wMlfPxE1?	M4DVOVI{OjN6NkO5
MEC2	M3LGNGN6fG:2b4jpZ4l1gSCjc4PhfS=>	NFq5[5QxNjJvMkFOwG0>	M4jtU\|czcA>?	Mn7jSG1UVw>?	NV22[5VHUUN3ME2wMlfPxE1?	MoOwNlMzOzh4M{m=
primary B-CLL lymphocytes	MYDBdI9xfG:\|aYOgRZN{[Xl?	M3HocGlEPTBiZn;yJIVi[2hicILpcYFzgSClZXzsJIxqdmV?	M{TOR\|I1cA>?	M2XVemROW09?	MmHMTWM2OO,:nEROwG0h\m:{IHHscEBx[XSrZX70dy=>	NHm0XXUzOzJ\|OE[zPS=>
primary B-CLL lymphocytes	NYrIZZVxU2mwYYPlJGF{e2G7	NVnNWpdHUUN3MDDmc5Ih\WGlaDDwdolu[XK7IHPlcIwhdGmwZR?=	NUjsRphwOjSq		MX3pcohq[mm2czDwO\|BUPktiJjC0SU1DWDFiZYjwdoV{e2mxbh?=	NHrEdmMzOzJ\|OE[zPS=>
human NSCLC	NVnPWnhCT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M1HDWVAvPS1{zszN	NXLxO2dXPzKq		MVTJR\|UxRTIQvF2=	NFrLWJYzOjd6MUO5Ny=>
human NSCLC	NFniSIpMcW6jc3WgRZN{[Xl?	MWix{txO	M2n2TVI1cA>?		NI[0TJdqdmirYnn0d{B1cGViQXv0M41VV1Jic3nncoFtcW6pIIDheIh4[XliYYSgN4gh[W[2ZYKgeJJm[XSvZX70	NUDxVHl1OjJ5OEGzPVM>
Y1 cell line	NUPIdo1pT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NE\ScW0xNjIQvF2vNe69VQ>?	M2fxNVI1cA>?	NVi5[FliTE2VTx?=	M{S5ZYlvcGmkaYTzJFYx97zHIHPlcIwhfmmjYnnsbZR6KGmwIF35Z{1U[3S{LYTyZY5{\mWldHXkJINmdGy\|	MVGyNlY6OjlyNB?=
PIK3CA-mutant MCF7	MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NX\VVpI6T0l3ME2xOlDDuTlzbl5vwKxNTDVyPUm4NOKyOjd\|bl2=	MlHGO\|Jp		MorBS2k2OD1zNkFCtVkydk4xvJzMSFUxRTl6MNMxNlc{dk1?	M3\DOFIzPjV\|OU[3
PIK3CA-mutant MCF7	M3PhNmtqdmG\|ZTDBd5NigQ>?	M3PCOmlEPTB;MUG0xtE{dk1?	MXK3Nog>		NXG4XndRUUN3ME2xNVTDuTOwTTDpckBz\WS3Y3nu[{BCc3RicHjvd5Bpd3K7bHH0bY9vKGyndnXsdy=>	M4i1cFIzPjV\|OU[3
MCF7-myr-Akt	M1\L[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MnPPS2k2OD1{OUpCtVY5dk4xvJzMSFUx97zgMUCsNFAxdk1?	NF75OlY4Omh?		Mmm0S2k2OD1{OUpCtVY5dk4xvJzMSFUx97zgMUCsNFAxdk1?	NWDTZYFpOjJ4NUO5Olc>
colon cancer cell lines	NG\YO\|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NUPTZmFWOC1zMN88US=>	MXm3Nog>	MWHEUXNQ	NUnhVFZtUUN3ME2x{txO	NWPVZ3FkOjJ3NEO4OVc>
gastric cancer cell lines	NITod4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NFzPPW0xNTFyzszN	Mn3hO\|Jp	MYrEUXNQ	MXXJR\|UxRTJvNd88US=>	NYjFSY1ROjJ3NEO4OVc>
HCT-116/HT-29/MKN-45	M1G3U2Fxd3C2b4Ppd{BCe3OjeR?=	MmHGNu69VQ>?	MV20PIg>		M{C5cJNpcW[2IHnuJGczKHCqYYPl	NFjmT\|MzOjV2M{i1Oy=>
HT-29 and HCT-116	NYOzdFE3S2G\|cHHz[UBie3OjeR?=	M{TwdlXPxE1?	M1nz[FI1cA>?		MoXhbY5lfWOnczDjZZNx[XOnIHHjeIl3cXS7	M4fhZ\|IzPTR\|OEW3
MM cell lines	Mnu5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MYixNO69VQ>?	NYf2Xnp2OjSq	NUHaelh2TE2VTx?=	NFe1OWZKSzVyII\hdolmeyCjbX;u[{BlcW[oZYLlcpQh[2WubDDsbY5meyCrbjD0bY1mKGGwZDDkc5NmKGSncHXu[IVv[2V?	MXmyNlIxPzR6NR?=
ARP-1	MnPORZBweHSxc3nzJGF{e2G7	NXPoPJpHOTEQvF2=	MkjBNlRp	NHjxXZZFVVOR	MWTpcoR2[2W\|IF3NJINmdGxiYYDvdJRwe2m\|IITodo92\2hiY3HzdIF{\SCjY4TpeoF1cW:w	MUmyNlIxPzR6NR?=
SNU-601	MlfwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NXzmR4hEPzKq	NVvSdJlCTE2VTx?=	M1jPemlEPTB;MD64NVbDuTBwME[z{txO	NEH0c\|QzOjF3OUixOC=>
SNU-1	NYO4N5Y1T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		M2rPWVczcA>?	NVmwfGxGTE2VTx?=	MoroTWM2OD1zLkC4NuKyOC5yMklOwG0>	MlPRNlIyPTl6MUS=
SNU-668	NXi1SoU5T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MWS3Nog>	M4jMSWROW09?	MW\JR\|UxRTFwNUe5xtExNjB5NN88US=>	M13nWVIzOTV7OEG0
AGS	M2DoOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MmOxO\|Jp	MojpSG1UVw>?	MWTJR\|UxRTFwN{G0xtExNjFzN988US=>	MX6yNlE2QThzNB?=
SNU-216	MnHQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		M4Wy[VczcA>?	M362VmROW09?	MmTaTWM2OD1{Lk[5NuKyOC5yOENOwG0>	Mnv3NlIyPTl6MUS=
SNU-5	M1mzWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NFm2OIM4Omh?	MmTESG1UVw>?	NGfZbXdKSzVyPUGuN\|UyyrFyLkC5Ne69VQ>?	NEnocFUzOjF3OUixOC=>
SNU-638	NYThRVlLT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NFfZeZM4Omh?	NGjaVmRFVVOR	M3Lxd2lEPTB;Mj6yPFLDuTBwMEWz{txO	MoTPNlIyPTl6MUS=
SNU-16	NX7xb\|RzT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NEDtdY04Omh?	MkXMSG1UVw>?	MXXJR\|UxRTFwNUezxtExNjByMd88US=>	M{PQdFIzOTV7OEG0
SNU-484	MmHLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NE\ETo44Omh?	MlvsSG1UVw>?	M{XsU2lEPTB;MT63NljDuTBwMES1{txO	M{nUPVIzOTV7OEG0
SNU-620	MlzyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		M{HmfVczcA>?	MkLjSG1UVw>?	MUHJR\|UxRTJwOUO5xtExNjByMd88US=>	MY[yNlE2QThzNB?=
SNU-719	NUXsUYNrT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MUW3Nog>	NXvZZXNjTE2VTx?=	MUTJR\|UxRTNwMEO3xtExNjB\|Mt88US=>	M3uxZ\|IzOTV7OEG0
glioma cell lines	MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		M1LDO\|czcA>?		MWPJR\|UxRTFvMt88US=>	MnK5NlIxPjVyOEC=
U87	M1\n[mFxd3C2b4Ppd{BCe3OjeR?=	M3nXd\|LPxE1?	Mm\4O\|Jp		NGXLNo5qdmS3Y3XzJINmdGxiYYDvdJRwe2m\|IHHu[EBkdGWjdnXkJHBCWlBiYX7kJINie3Cjc3WtNy=>	MoHYNlIxPjVyOEC=

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	p-AKT (T308) / p-AKT (S473) / AKT; PubMed: 27283525 J Neurooncol Left western blots showing levels of pAkt (T308), pAkt (S473) and total Akt in U87 cells exposed to buparlisib for 72 h. Right densitometric assessment of western blots, showing relative changes in phosphorylation. p-FOXO3a (S253) / FOXO3a; PubMed: 28036259 Oncotarget Cells were treated with 0.5 μM BKM120 for 24 h and cell lysates were immunoblotted with the indicated antibodies. Actin was used as the loading control. Nuclear NF-κB p65 / NF-κB p65; PubMed: 26673665 Cell Death Dis Western blots show BKM120 downregulating pAKT, nuclear NF-κB p65 and total NF-κB p65 in MDR and their parental cells. β-actin was used as a loading control for pAKT, AKT and total NF-κB p65. Lamin B was used as a loading control for nuclear NF-κB p65. p-ERK / ERK / LC3; PubMed: 27572309 Oncotarget The indicated cell lines were exposed to different concentrations of BKM120 as indicated for 8 h A. or with 2 μM BKM120 for the indicated times B. The cells were then harvested for preparation of whole-cell protein lysates and subsequent Western blot analysis to detect the given proteins. p-STAT3 / STAT3 / p-ERK / ERK / p-S6; PubMed: 29928341 Oncol Lett Western blot analysis of H460 and H2126 cell lysates using specific antibodies to phosphorylated or total proteins of STAT3, ERK1/2, AKT, S6 or GAPDH (loading control). The cells were treated with increasing concentrations of BKM120 for 24 h. p-MET / MET; PubMed: 29928341 Oncol Lett The expression of phosphorylated or total forms of MET protein was analyzed by western blotting.	27283525 28036259 26673665 27572309 29928341
Immunofluorescence	FOXO3a; PubMed: 28036259 Oncotarget Cells were cultured on coverslips to approximately 60% confluency and then treated with 1 μM BKM120 for an additional 24 h. Immunofluorescence staining was performed using an anti-FOXO3a antibody and the nuclei were stained with DAPI. Scale bar, 20 μm.	28036259
Growth inhibition assay	Cell viability; PubMed: 26673665 Cell Death Dis Dose-response curves were used to calculate the IC50 of BKM120 for MCs of MCF-7/A02 cells (upper) and CALDOX cells (lower).	26673665

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]

Protocol

Kinase Assay:^[1]	- Collapse PI3K biochemical assay (ATP depletion assay): BKM120 is dissolved in DMSO and directly distributed into a black 384-well plate at 1.25 µL per well. To start the reaction, 25 µL of 10 nM PI3 kinase and 5 µg/mL 1-α-phosphatidylinositol (PI) in assay buffer (10 mM Tris pH 7.5, 5 mM MgCl₂, 20 mM NaCl, 1 mM DTT and 0.05% CHAPS) are added into each well followed by 25 µL of 2 µM ATP in assay buffer. The reaction is performed until approx 50% of the ATP is depleted and then stopped by the addition of 25 µL of KinaseGlo solution. The stopped reaction is incubated for 5 minutes and the remaining ATP is then detected via luminescence.
Cell Research:^[1]	- Collapse Cell lines: A2780 cells. Concentrations: 0-6.6 μM Incubation Time: 3 days. Method: A2780 cells are cultured in DMEM supplemented with 10% FBS, L-glutamine, sodium pyruvate, and antibiotics. Cells are plated in the same medium at a density of 10³ cells per well, 100 μL per well into black-walled-clear-bottom plates and incubated for 3-5 hours. BKM120 supplied in DMSO (20 mM) is diluted. The diluted BKM120 solution (2 μL), is then added to cell medium (500 μL) cell medium (concentration from 0-6.6 μM). Equal volumes of this solution (100 μL) are added to the cells in 96 well plates and incubated at 37 °C for 3 days and developed using Cell Titer Glo. Inhibition of cell proliferation is determined by luminescence read using Trilux. (Only for Reference)
Animal Research:^[1]	- Collapse Animal Models: U87MG and A2780 xenografts are established in female nu/nu mice. Formulation: In 15% Captisol. Dosages: ~60 mg/kg. Administration: Dosed orally daily (q.d.). (Only for Reference)

References

[4] Koul D, et al. Clin Cancer Res, 2012, 18(1), 184-195.

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Solubility (25°C)

In vitro	DMSO	82 mg/mL (199.8 mM)
	Ethanol	2 mg/mL (4.87 mM)
	Water	Insoluble
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 5% DMSO+30% PEG 300+ddH2O For best results, use promptly after mixing.	15mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download Buparlisib (BKM120, NVP-BKM120) SDF

Molecular Weight	410.39
Formula	C₁₈H₂₁F₃N₆O₂
CAS No.	944396-07-0
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	N/A

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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2019-10-14)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02614508	Terminated	Drug: Buparlisib\|Drug: Ibrutinib\|Biological: Ofatumumab	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	Drug: BKM120	Treatment for Metastatic or Locally Advanced Cervical Cancer	Novartis Pharmaceuticals\|Novartis	November 2015	Phase 2
NCT01953445	Withdrawn	Drug: paclitaxel\|Drug: BKM120	Breast Neoplasms	Washington University School of Medicine	August 2014	Phase 2

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Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Also blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays.
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Buparlisib (BKM120, NVP-BKM120)

Cited by 135 Publications

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Chemical Information Download Buparlisib (BKM120, NVP-BKM120) SDF

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PI3K Inhibitors with Unique Features

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Buparlisib (BKM120, NVP-BKM120)

Cited by 135 Publications

Purity & Quality Control

Choose Selective PI3K Inhibitors

Biological Activity

Protocol

References

Solubility (25°C)

Chemical Information Download Buparlisib (BKM120, NVP-BKM120) SDF

Bio Calculators

Molarity Calculator

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

Dilution Calculator

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

The Serial Dilution Calculator Equation

Serial Dilutions

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Molecular Weight Calculator

Total Molecular Weight: g/mol

Instructions to calculate molar mass (molecular weight) of a chemical compound:

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2019-10-14)

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PI3K Signaling Pathway Map

PI3K Inhibitors with Unique Features

Related PI3K Products

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