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 105 Publications

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

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Nat Med, 2015, 10.1038/nm.3855

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Mol Cell, 2017, 67(3):512-527

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J Transl Med, 2016, 14:56

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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	NFPSZWNEgXSxdH;4bYMhSXO\|YYm=		MV:3NkBp	NUT1[mZMTE2VTx?=	M4K5PGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh\XiycnXzd4lv\yCSSUPLZYxxcGFiRUW0OWshdXW2YX70JJdqfGhiR1m1NEBw\iByLkCwNFE2QCEQvF2=	MYKyOFkxODJ4Nh?=
DU145	NInSeFJEgXSxdH;4bYMhSXO\|YYm=		NYrmZYprPzJiaB?=	Mme1SG1UVw>?	NXr0bmY4S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hTFVzNEWgZ4VtdHNiZYjwdoV{e2mwZzDMT2IyKG23dHHueEB4cXSqIFfJOVAhd2ZiMD6wNFA1OzVizszN	M1\hTFI1QTByMk[2
A2780	NUmzZ5RXS3m2b4TvfIlkKEG\|c3H5		NIW3WmY4OiCq	MlG0SG1UVw>?	MoXER5l1d3SxeHnjbZR6KGGpYXnud5QhWFSHTj3k[YZq[2mnboSgbJVu[W5iQUK3PFAh[2WubIOge4l1cCCJSUWwJI9nKDBwMECwOlM2KM7:TR?=	MlvoNlQ6ODB{Nk[=
U87MG	MknpR5l1d3SxeHnjJGF{e2G7		NEfYZZA4OiCq	MUXEUXNQ	Mmq0R5l1d3SxeHnjbZR6KGGpYXnud5QhWFSHTj3k[YZq[2mnboSgbJVu[W5iVUi3UWch[2WubIOge4l1cCCJSUWwJI9nKDBwMECwOlk5KM7:TR?=	M4HHclI1QTByMk[2
A2780	M3fmXWZ2dmO2aX;uJGF{e2G7		NU\kTVhsOSCq	NHXFNGpFVVOR	Mn;OTY5pcWKrdHnvckBw\iCSSUPLMY1m\GmjdHXkJGFMXCCVZYK0O\|MheGixc4Doc5J6dGG2aX;uJJdqfGhiRVO1NEBw\iByLkC1OUDPxE1?	NWTOdnc{OjR7MECyOlY>
DU145	NV7QfmlQTnWwY4Tpc44hSXO\|YYm=		NGnJbJkyKGh?	M{LGeGROW09?	MXnJcohq[mm2aX;uJI9nKFCLM1utcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:\|cHjvdplt[XSrb36gbY4hcHWvYX6gSHUyPDViY3XscJMhcGG{Yn;ybY5oKEyNQkGgcZV1[XSrb36ge4l1cCCHQ{WwJI9nKDBwMEezJO69VQ>?	Ml;4NlQ6ODB{Nk[=
A2780	NXTUdVdlTnWwY4Tpc44hSXO\|YYm=		NFPJ[XQyKGh?	M1LYWGROW09?	MWrJcohq[mm2aX;uJI9nKFCLM1utcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:\|cHjvdplt[XSrb36gbY4hWFSHTj3k[YZq[2mnboSgbJVu[W5iQUK3PFAh[2WubIOge4l1cCCHQ{WwJI9nKDBwMEe0JO69VQ>?	NW[3Um1HOjR7MECyOlY>
MCF7	MU\GeY5kfGmxbjDBd5NigQ>?		MWCxJIg>	NETFfZhFVVOR	NFXQZZFKdmirYnn0bY9vKG:oIGDJN2tidHCqYTDFOVQ2UyCvdYThcpQudWWmaXH0[YQhSUuWIGPldlQ4OyCyaH;zdIhwenmuYYTpc44hf2m2aDDFR\|UxKG:oIECuNUDPxE1?	MkiwNlQ6ODB{Nk[=
U87MG	MUfGeY5kfGmxbjDBd5NigQ>?		NYP3SllxOSCq	MWjEUXNQ	MWLJcohq[mm2aX;uJI9nKFCLM1utcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:\|cHjvdplt[XSrb36gbY4hWFSHTj3k[YZq[2mnboSgbJVu[W5iVUi3UWch[2WubIOge4l1cCCHQ{WwJI9nKDBwMUOg{txO	MX2yOFkxODJ4Nh?=
A2780	NE\nemhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		M{XCelczKGh?	MUjEUXNQ	NEe4N\|dGSzVyPUCuOVIh\|ryP	M13JWVI1QTByMk[2
SKMES-1	MV\DfZRwfG:6aXOgRZN{[Xl?	NVTD[otvOSEQvF2=	NGOwb3Q4OiCq		NFPIc2RKdmS3Y3XzJINmdGxiZHXheIg>	NHjNSIUzPjBzM{OxPC=>
H596	NFvy[I1HfW6ldHnvckBCe3OjeR?=	MmG2NUDPxE1?			NWHVUoJGUW2yYXnyd{Bk\WyuIH3p[5JifGmxbh?=	MljTNlYxOTN\|MUi=
HCC2450	NFy3ZXZHfW6ldHnvckBCe3OjeR?=	MWexJO69VQ>?			MYLJcZBicXK\|IHPlcIwhcW64YYPpc44>	MWOyOlAyOzNzOB?=
A549	NHrPSldHfW6ldHnvckBCe3OjeR?=	MoPnOVAxKG6P	MUG0PEBp	MXXEUXNQ	M2LueWlvcGmkaYTzJGFsfCCjY4TpeoF1cW:w	MlzXNlU6Ozd{OUm=
A549	M{Wwfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MkGzNUDPxE1?	NELoOXg4OiCq	MXvEUXNQ	NWjWUpZXUW6qaXLpeJMh[2WubDDndo94fGh?	MkjmNlU6Ozd{OUm=
H522	Mn;FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NIWxWIYyKM7:TR?=	M3y5RlczKGh?	MnPLSG1UVw>?	NHPBW4hKdmirYnn0d{Bk\WyuIHfyc5d1cA>?	MVqyOVk{PzJ7OR?=
LNCaP	M4X2eWZ2dmO2aX;uJGF{e2G7	MXyxJO69VQ>?			NV;0O4tNW3WycILld5NmeyCyLVHLWEBt\X[nbIO=	M1\EPVI2OzZyN{m5
LNCaP95	Mli4SpVv[3Srb36gRZN{[Xl?	Mm\uNUDPxE1?			MlLRV5VxeHKnc4Pld{BxNUGNVDDs[ZZmdHN?	MXyyOVM3ODd7OR?=
HCT-15	M3jFTmFxd3Sxc3nzJGF{e2G7	NVPQVY1lOTBizszN	NGLDVok1QCCq	NXHBUFhLTE2VTx?=	MW\JcoR2[2W\|IHHwc5B1d3OrczDpckBJS1RvMUWgZ4VtdHNiaHHyZo92emmwZzDQTWs{S0FiaH;0d5BwfCCvdYTheIlwdg>?	NVHvfo81OjVzNUKyOFU>
HCT-116	MmDKRZBwfG:\|aYOgRZN{[Xl?	NGHOeXcyOCEQvF2=	NHrsSGI1QCCq	MoH1SG1UVw>?	NHHqc4RKdmS3Y3XzJIFxd3C2b4Ppd{BqdiCKQ2StNVE3KGOnbHzzJIhiemKxdYLpcochWEmNM1PBJIhwfHOyb4SgcZV1[XSrb36=	M2O5dlI2OTV{MkS1
NCI-H460	MnnPRZBwfG:\|aYOgRZN{[Xl?	NGLCW4wyOCEQvF2=	NHvt[Yw1QCCq	Mn\BSG1UVw>?	NGHKR4FKdmS3Y3XzJIFxd3C2b4Ppd{BqdiCQQ1mtTFQ3OCClZXzsd{Bp[XKkb4XybY5oKFCLS{PDRUBpd3S\|cH;0JI12fGG2aX;u	NWjHNmtOOjVzNUKyOFU>
SKOV-3	NXGydVFZSXCxdH;zbZMhSXO\|YYm=	MVSxNEDPxE1?	Mme4OFghcA>?	NW[5OFRZTE2VTx?=	MojXTY5lfWOnczDhdI9xfG:\|aYOgbY4hW0uRVj2zJINmdGy\|IHjhdoJwfXKrbnegVGlMO0ODIHjveJNxd3RibYX0ZZRqd25?	NGfrTGkzPTF3MkK0OS=>
BSY-1	Mn7nRZBwfG:\|aYOgRZN{[Xl?	NIrTWmEyOCEQvF2=	MnXkOFghcA>?	MXfEUXNQ	MkewTY5lfWOnczDhdI9xfG:\|aYOgbY4hSlO\LUGgZ4VtdHNiaHHyZo92emmwZzDQTWs{S0FiaH;0d5BwfCCvdYTheIlwdg>?	MYSyOVE2OjJ2NR?=
MKN-1	Mn;4RZBwfG:\|aYOgRZN{[Xl?	M1nSRlExKM7:TR?=	NVzFTY8{PDhiaB?=	MUjEUXNQ	MlTRTY5lfWOnczDhdI9xfG:\|aYOgbY4hVUuQLUGgZ4VtdHNiaHHyZo92emmwZzDQTWs{S0FiaH;0d5BwfCCvdYTheIlwdg>?	MnX3NlUyPTJ{NEW=
NCI-H522	M2T6[mFxd3Sxc3nzJGF{e2G7	NXPPSWRSOTBizszN	MYW0PEBp	NFS2bY1FVVOR	NETYOmlKdmS3Y3XzJIFxd3C2b4Ppdy=>	MXqyOVE2OjJ2NR?=
OVCAR-3	MkPzRZBwfG:\|aYOgRZN{[Xl?	NXziXVFEOTBizszN	NHvXRVM1QCCq	M{XmO2ROW09?	M1z0PGlv\HWlZYOgZZBweHSxc3nz	MoXhNlUyPTJ{NEW=
HBC-5	NHHNfWJCeG:2b4Ppd{BCe3OjeR?=	M2LGcVExKM7:TR?=	MUm0PEBp	M3HaVmROW09?	NVH0bFZtUW6mdXPld{BieG:ydH;zbZM>	NFS0VZIzPTF3MkK0OS=>
RXF-631L	NIXoOWFCeG:2b4Ppd{BCe3OjeR?=	MXmxNEDPxE1?	NXvpeWp2PDhiaB?=	MofWSG1UVw>?	M1n6RWlv\HWlZYOgZZBweHSxc3nz	M3ziTlI2OTV{MkS1
MKN-45	MoXrRZBwfG:\|aYOgRZN{[Xl?	MkHZNVAh\|ryP	MWW0PEBp	NHrZXGxFVVOR	MkKzTY5lfWOnczDhdI9xfG:\|aYO=	NIH2OZYzPTF3MkK0OS=>
BON-1	MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NHvlXpE2ODBibl2=	MXqxNEBl	Mk[zSG1UVw>?	NEHX[odKdmirYnn0d{Bk\WyuIHfyc5d1cA>?	MnP3NlUxOjZ{OUK=
BON-1	NEHtUVRHfW6ldHnvckBCe3OjeR?=	NV\RXpdyPTByIH7N	MYq0JIg>	NG\vVHhFVVOR	Ml\MTY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXCCjdDDUbJI{ODhiYX7kJHNmejR5Mx?=	NH6yfYUzPTB{NkK5Ni=>
QGP-1	M4rBOGZ2dmO2aX;uJGF{e2G7	NGi2XWU2ODBibl2=	NFrTT5U1KGh?	MVvEUXNQ	MlzxTY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXCCjdDDUbJI{ODhiYX7kJHNmejR5Mx?=	MVyyOVAzPjJ7Mh?=
Huh7	NVvvUnpOTnWwY4Tpc44hSXO\|YYm=	NG\0N5gyKM7:TR?=	NYjYSXIyOSCq	NEXh[4ZFVVOR	NULGbGNNUW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEGNVDDheEBU\XJ2N{S=	M3rxXVI2ODB2NECz
BNL	MnHQSpVv[3Srb36gRZN{[Xl?	NVvlcGZbOSEQvF2=	NYnOOJdqOSCq	M3OzZmROW09?	MWnJcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gV\|Y>	NFLFcmIzPTByNESwNy=>
MDA-MB-175	M2LrNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NWL2RnVUOSEQvF2=	NULy[5dpPSCm	NYHCbFlTTE2VTx?=	NFHJdYRKSzVyPEGg{txO	NV2yVpg3OjR6N{m3PVY>
MDA-MB-134	NFi0SYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MkC0NUDPxE1?	MlfyOUBl	M4nNW2ROW09?	NFnEd4RKSzVyPEGg{txO	NF7jOm0zPDh5OUe5Oi=>
HCC1500	NVSwOG9MT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NVHyUGVCOSEQvF2=	M3LISlUh\A>?	M1niR2ROW09?	NX\iRppsUUN3MEyxJO69VQ>?	MlS2NlQ5Pzl5OU[=
EFM-19	NV:yPYdvT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NI\hU4EyKM7:TR?=	M1jwPFUh\A>?	M2XYTWROW09?	NGTBWY1KSzVyPEGg{txO	Mn;CNlQ5Pzl5OU[=
ZR-75-30	MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MkHWNUDPxE1?	MoXSOUBl	NFfHfGJFVVOR	NVrHOmtXUUN3MEyxJO69VQ>?	Ml;CNlQ5Pzl5OU[=
MDA-MB-361	NYfJeFJ4T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NFTK[ngyKM7:TR?=	NV3De44{PSCm	NVzvTYVYTE2VTx?=	NEn3d\|RKSzVyPEGg{txO	NHvFcJczPDh5OUe5Oi=>
T-47D	Mmf6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NHLy[HkyKM7:TR?=	Mo\1OUBl	MYfEUXNQ	MlvWTWM2ODxzIN88US=>	NXXMN3RXOjR6N{m3PVY>
SK-BR-3	M1X2e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NGfB[okyKM7:TR?=	MUi1JIQ>	NX\OWI1KTE2VTx?=	NEHYeVBKSzVyPEGg{txO	M3;pT\|I1QDd7N{m2
UACC-732	NY\iTJFZT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MWixJO69VQ>?	Mnm2OUBl	NHXkVW5FVVOR	MnvNTWM2ODxzIN88US=>	MVmyOFg4QTd7Nh?=
BT-474	MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M3nPZVEh\|ryP	NVK1W4pPPSCm	NWjId4cxTE2VTx?=	MkXoTWM2ODxzIN88US=>	NF3CfW0zPDh5OUe5Oi=>
HCC202	MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NGPFeokyKM7:TR?=	MnLiOUBl	MnrVSG1UVw>?	MnHoTWM2ODxzIN88US=>	Mnu5NlQ5Pzl5OU[=
MCF7	NW[4WW9pT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NIHvWnUyKM7:TR?=	NUTJO2V7PSCm	NUnwUmVJTE2VTx?=	MWjJR\|UxRDFizszN	NVXiPGRbOjR6N{m3PVY>
MDA-MB-415	MlLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NFzhNW4yKM7:TR?=	NXrIeWs6PSCm	NF\DZlJFVVOR	NXjEVo84UUN3MEyxJO69VQ>?	NX;3cmZNOjR6N{m3PVY>
MDA-MB-453	M4jkVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NF;pNFEyKM7:TR?=	M4fIZlUh\A>?	M3\NSGROW09?	MXTJR\|UxRDFizszN	NHvIVngzPDh5OUe5Oi=>
ZR-75-1	M1LyN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MUmxJO69VQ>?	MWe1JIQ>	MV;EUXNQ	MXXJR\|UxRDFizszN	M4HkcFI1QDd7N{m2
HCC38	M3\xfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	Mo[1NUDPxE1?	MV21JIQ>	MnrYSG1UVw>?	MlX3TWM2ODxzIN88US=>	MVKyOFg4QTd7Nh?=
HCC1419	MmLQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MlLENUDPxE1?	NU[zcWVkPSCm	NETC[GJFVVOR	M2nsdWlEPTB:MTFOwG0>	M3y5WlI1QDd7N{m2
UACC-812	NUjWeIozT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M2XpV\|Eh\|ryP	NHnUUmY2KGR?	NXzxO\|c{TE2VTx?=	M{DrVGlEPTB:MTFOwG0>	Mn\0NlQ5Pzl5OU[=
HCC1187	NEf4WlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MoTLNUDPxE1?	MWG1JIQ>	NVnuVJNqTE2VTx?=	MXjJR\|UxRDFizszN	MViyOFg4QTd7Nh?=
KPL-1	M4Lqcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M4LZWVEh\|ryP	MofnOUBl	NVHpblR[TE2VTx?=	NEnvRY5KSzVyPEGg{txO	MW[yOFg4QTd7Nh?=
SUM-225	NGDZN4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MofjNUDPxE1?	NX7jOopQPSCm	M3Lod2ROW09?	NFXBNpBKSzVyPEGg{txO	NFrDd3AzPDh5OUe5Oi=>
EFM-192A	Ml7WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M4XmSlEh\|ryP	MXS1JIQ>	NGfI[2tFVVOR	NYThR3F[UUN3MEyxJO69VQ>?	Ml;TNlQ5Pzl5OU[=
JIMT-1	MkLVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MVSxJO69VQ>?	NY[0R45TPSCm	NF7qTYJFVVOR	NFPPR2RKSzVyPEGg{txO	NHOxSmQzPDh5OUe5Oi=>
HCC1143	Mnv0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MYOxJO69VQ>?	M4XyXlUh\A>?	NYi2dIZyTE2VTx?=	NWjGdYl{UUN3MEyxJO69VQ>?	MmTjNlQ5Pzl5OU[=
HCC2218	NV\ZeW01T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MXKxJO69VQ>?	MYm1JIQ>	MVfEUXNQ	M{LXdmlEPTB:MTFOwG0>	NFf2SmgzPDh5OUe5Oi=>
MDA-MB-468	NEL0OmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M362SlEh\|ryP	NY\XXGVVPSCm	NELPPWNFVVOR	MkHmTWM2ODxzIN88US=>	NXnHSVh4OjR6N{m3PVY>
BT-20	MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NEPJUJgyKM7:TR?=	MlLYOUBl	NWfyPI9UTE2VTx?=	NIX5XIJKSzVyPEGg{txO	M2rnRVI1QDd7N{m2
MDA-MB-435	NH3FVFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M1W4d\|Eh\|ryP	NH;ZUVA2KGR?	NFXHd3ZFVVOR	Mnn0TWM2ODxzIN88US=>	MlKxNlQ5Pzl5OU[=
BT-549	NWXKT\|gzT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MnHzNUDPxE1?	MUi1JIQ>	M1Th[GROW09?	MkjjTWM2ODxzIN88US=>	M1u4PVI1QDd7N{m2
HCC1806	NG\oc2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M1vFZlEh\|ryP	MXW1JIQ>	Mly4SG1UVw>?	NHjURmRKSzVyPEGg{txO	M{O3bVI1QDd7N{m2
HCC1937	NF;IdldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M2nIRlEh\|ryP	NIPIXIc2KGR?	NHW1WHRFVVOR	MXfJR\|UxRDFizszN	NV;iRllzOjR6N{m3PVY>
Hs578T	MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NF\DdmkyKM7:TR?=	MmPROUBl	M1K1UmROW09?	M1OyVmlEPTB:MTFOwG0>	NFzOZ28zPDh5OUe5Oi=>
LN18	NYD4NHV5T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M1LvdVIxKM7:TR?=	NFHD[oc4OiCq	NFTpcVlFVVOR	MmexTWM2ODx3IN88US=>	M1LqNFI1PzRzMEe0
LN229	NH;iTXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MorJNlAh\|ryP	NIrxSpc4OiCq	NWDiWZR6TE2VTx?=	NXHWZZA{UUN3MEy1JO69VQ>?	NWThSpFrOjR5NEGwO\|Q>
LNZ308	M1nvRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M2nFNFIxKM7:TR?=	M1LhclczKGh?	M3;odWROW09?	NHu3[pFKSzVyPEWg{txO	Mn7DNlQ4PDFyN{S=
T98G	NGPOfZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M{CyfFIxKM7:TR?=	NH\WeWw4OiCq	MXTEUXNQ	Mn;STWM2ODx3IN88US=>	MYeyOFc1OTB5NB?=
U87	M2LSbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NUPGbGluOjBizszN	MnrPO\|IhcA>?	M1TuUmROW09?	M2PMOGlEPTB:NTFOwG0>	MUeyOFc1OTB5NB?=
LN18	MV7GeY5kfGmxbjDBd5NigQ>?	NGLjbpQ2KM7:TR?=	MWqyOEBp	NHr5fo9FVVOR	MlGzTY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXA>?	MUCyOFc1OTB5NB?=
LNZ308	NU\HdYE2TnWwY4Tpc44hSXO\|YYm=	MlT0OUDPxE1?	NFPSN24zPCCq	NVz4XI1VTE2VTx?=	M4\kUmlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBCU1R?	MkjVNlQ4PDFyN{S=
Saos-2	NF3NNXBHfW6ldHnvckBCe3OjeR?=	NYnQfVZFPTBizszN	M120OlQ5KGh?		M4fFZ2lvcGmkaYTzJINmdGxiaX72ZZNqd25?	NGLCbVYzPDd{N{[2NC=>
MG-63	M1Xie2Z2dmO2aX;uJGF{e2G7	NFXxRVk2OCEQvF2=	M4fzOVQ5KGh?		M3yx[GlvcGmkaYTzJINmdGxiaX72ZZNqd25?	NGTiRpQzPDd{N{[2NC=>
SJSA-1	NF;iTGJHfW6ldHnvckBCe3OjeR?=	M3nCeVUxKM7:TR?=	NH;vRXo1QCCq		M1K3bmlvcGmkaYTzJINmdGxiaX72ZZNqd25?	NFPlW4UzPDd{N{[2NC=>
Saos-2	MnHZSpVv[3Srb36gRZN{[Xl?	MnzKOVAh\|ryP	MUG0PEBp		NICyUZpKdmirYnn0d{Bu[XS{aYigcYV1[Wyub4Dyc5RmcW6jc3WtNkBmgHC{ZYPzbY9v	NF62d4IzPDd{N{[2NC=>
MG-63	NX6wc4o{TnWwY4Tpc44hSXO\|YYm=	M2HDRVUxKM7:TR?=	M4XzcVQ5KGh?		NX7RW3V5UW6qaXLpeJMhdWG2cnn4JI1mfGGubH;wdo91\WmwYYPlMVIh\XiycnXzd4lwdg>?	NVPzcW1ROjR5Mke2OlA>
SJSA-1	MnzySpVv[3Srb36gRZN{[Xl?	MlTNOVAh\|ryP	MYO0PEBp		MUjJcohq[mm2czDtZZRzcXhibXX0ZYxtd3C{b4TlbY5ie2VvMjDlfJBz\XO\|aX;u	MYKyOFczPzZ4MB?=
Saos-2	NYfmeGRHT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	Mk[2OVAh\|ryP	MmjBOFghcA>?		MWDJcohq[mm2czDj[YxtKH[rYXLpcIl1gQ>?	MX2yOFczPzZ4MB?=
MG-63	MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NUK5bJg1PTBizszN	NFLpdnA1QCCq		MXHJcohq[mm2czDj[YxtKH[rYXLpcIl1gQ>?	M3;NOFI1PzJ5Nk[w
SJSA-1	MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MkfNOVAh\|ryP	MlXBOFghcA>?		NGTMTXhKdmirYnn0d{Bk\WyuII\pZYJqdGm2eR?=	NH61UHUzPDd{N{[2NC=>
FaDu	NX30Unh2TnWwY4Tpc44hSXO\|YYm=	M2f5XVUh\|ryP	M4f6RlI1KGh?	NH33bJJFVVOR	NXLtfo83WmWmdXPld{BwgHmpZX6gZ49ve3WvcITpc44>	Ml;TNlQ3OzFzNEe=
EMT6	M1vrSmZ2dmO2aX;uJGF{e2G7	NEjCRZk2KM7:TR?=	NEPaUGIzPCCq	Ml7HSG1UVw>?	NFPkeoZT\WS3Y3XzJI95gWenbjDjc45{fW2ydHnvci=>	MW[yOFY{OTF2Nx?=
HCT116	MmDWSpVv[3Srb36gRZN{[Xl?	NETzUGs2KM7:TR?=	NUjDOHFWOjRiaB?=	M4LqdWROW09?	M4D2fXJm\HWlZYOgc5h6\2WwIHPvcpN2dXC2aX;u	NYTlUYtsOjR4M{GxOFc>
U87	M4DCRWZ2dmO2aX;uJGF{e2G7	MmDmOUDPxE1?	M{O2bFI1KGh?	MYTEUXNQ	M1nkRXJm\HWlZYOgc5h6\2WwIHPvcpN2dXC2aX;u	M3HzWlI1PjNzMUS3
GBM	NVrOTZBQSXCxcITvd4l{KEG\|c3H5	NYDaR5RKOs7:TR?=	NH3ONJE1QGh?	M1jXeGROW09?	NY\Xe\|dVcW6mdXPl[EBpcWeqZYKgcIV3\Wy\|IH;mJIFxd3C2b4Ppd{wh[W6mIHTlZ5Jm[XOnZDDj[YxtKH[rYXLpcIl1gQ>?	NEXWTnczPDVyMES5Ni=>
BON	M3PaTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MnGwNU02\|ryP	NX3afol5PzKq		MmPT[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvci=>	NVXic2loOjR2NEO1NlM>
BON	MWHBdI9xfG:\|aYOgRZN{[Xl?	NXT0XlJLOS13zszN	M{TQXlI1cA>?		MWHpcoNz\WG\|ZYOgZZBweHSxc3nz	NEfJc5ozPDR2M{WyNy=>
H1975	MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NGnxe\|cxNjNvOT62{txO	NFrFZ2c4Omh?	NFLpc4ZFVVOR	M3vKT2lEPTB;MT6zPFXPxE1?	NX\FPJozOjR\|M{e4OFY>
H1975	NX7GfVIxSXCxcITvd4l{KEG\|c3H5	M4LCVFLPxE1?	MVeyOIg>	NUDucHBVTE2VTx?=	Mlf0bY5kemWjc3XzJIFxd3C2b4Ppd{Bz[XSnIIPp[45q\mmlYX70cJk>	NELUTHEzPDN\|N{i0Oi=>
T-ALL	NYjQbplGSXCxcITvd4l{KEG\|c3H5	M3;lSYJmfHenZX6gNU41KGGwZDC1MlMhdU1iYYSgNlRpKGGwZDCwMlkh[W6mIEWuOUBuVSCjdDC0PIghcW5iZHnm[oVz\W62IHPlcIwhdGmwZR?=	NEH0UVEzPCCxcjC0PIg>	NYTSW2tMTE2VTx?=	M4DO[IFn\mWldIOgeIhmKFCLM1ugdIF1cHejeTDpckBVNUGOTDDj[YxtKGyrbnXz	MVWyOFMyODd\|Nh?=
BCR-ABL	NYDU[nFzT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NFG0clkxNjJ3LUGw{txO	NEC3U3M1\A>?		NIDUZYd{cWewaX\pZ4FvfGy7IHnubIljcXRiY3XscEBxem:uaX\ldoF1cW:w	MUmyOFI1PDZzMh?=
LC-1/SQSF	NVji[nJSTnWwY4Tpc44hSXO\|YYm=	MVKz{txO	M17WdVI1cA>?	M3H6O2ROW09?	MoP5[IVkemWjc3WgUnJHOiCycn;0[YlvKGyndnXs	MXuyN\|k5ODB7Mx?=
Primary CLL cells	M4ixZ2Fxd3C2b4Ppd{BCe3OjeR?=	NWPpb2xlOS1zMN88US=>	M{fqfVQ5cA>?		NW\qR5Z6cW6mdXPld{BieG:ydH;zbZMhcW5iQ1zMJINmdGy\|IHnu[IVx\W6mZX70JI9nKHC{b3fuc5N1cWNibXHyb4Vzew>?	NYDvPZc1OjN6NUC4NFc>
Primary CLL cells	NX;a[4tnU2mwYYPlJGF{e2G7	NVzJS5l[Os7:TR?=	NEPzS\|E{OG2rbh?=		MXTk[YNz\WG\|ZXSgVGk{UyCjY4Tpeol1gQ>?	MUCyN\|g2ODhyNx?=
Primary CLL cells	MVnDfZRwfG:6aXOgRZN{[Xl?	M{nJfVLPxE1?	NH:4SXczPGh?		NInlNXZqdmS3Y3XzJINmdGxiY4n0c5RwgGmlaYT5	M1fJVlI{QDVyOEC3
human NSCLC cell lines	NWfWd3RSSXCxcITvd4l{KEG\|c3H5	NGHnXYkxNjF{NT20{txO	NFzuTFczPGh?	MX7EUXNQ	MVHJR\|UxeyC{YX7n[ZMh\nKxbTCwMlQuOs7:TR?=	NFL6U4gzOzV4MkS3Ni=>
human HCC cell lines	M3W3UmNmdGxidnnhZoltcXS7IHHzd4F6	M{PaPVAvODB3LUJOwG0>	NYHEOplJPDiq		MXfJR\|UxRTIQvF2=	NXLHRXZMOjN2OEm5PVk>
Huh7	MUPLbY5ie2ViQYPzZZk>	MlzyNe69VQ>?	MWW0PIg>		M3rFVZNq\26r77{BZ4FvfGy7IILl[JVk\XNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=>	MmnKNlM1QDl7OUm=
SK-HEP1	MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M1nhb\|EuOjEQvF2=	M3;zSlczcA>?	NUfUdnROTE2VTx?=	NUKyUHRpUUN3MP-8oFHPxE1?	MlLXNlM1PzlzM{[=
786-0	NGnxVFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MVexMVIx\|ryP	NXrO[\|F7PzKq	NIXUS4lFVVOR	NIHDcJBKSzVy78{cNe69VQ>?	MkL2NlM1PzlzM{[=
JVM2	M1XqR2N6fG:2b4jpZ4l1gSCjc4PhfS=>	NET5W4oxNjJvMkFOwG0>	NHfIWoE4Omh?	M4flRmROW09?	MVrJR\|UxRTBwOd88US=>	NWXy[JE6OjN{M{i2N\|k>
EHEB	NYDQepZ3S3m2b4TvfIlkcXS7IHHzd4F6	MUewMlIuOjEQvF2=	M3X3ZVczcA>?	NIXhPVVFVVOR	M{nVbWlEPTB;MD63{txO	NYTqSYpEOjN{M{i2N\|k>
MEC2	MYjDfZRwfG:6aXPpeJkh[XO\|YYm=	NWHYV2VWOC5{LUKw{txO	NX33NYwyPzKq	M{\J[2ROW09?	M3XTbGlEPTB;MD63{txO	MnTJNlMzOzh4M{m=
primary B-CLL lymphocytes	NXe0bnZpSXCxcITvd4l{KEG\|c3H5	MYjJR\|UxKG[xcjDlZYNpKHC{aX3hdpkh[2WubDDsbY5m	NWj0ZXJyOjSq	M1TkVmROW09?	M2\sW2lEPTExvKyz{txOKG[xcjDhcIwheGG2aXXueJM>	NVfIc4lnOjN{M{i2N\|k>
primary B-CLL lymphocytes	MVzLbY5ie2ViQYPzZZk>	M4e0N2lEPTBiZn;yJIVi[2hicILpcYFzgSClZXzsJIxqdmV?	NUfUdIpyOjSq		M{T4bYlvcGmkaYTzJJA4OFN4SzCmJFRGNUKSMTDlfJBz\XO\|aX;u	NEXJeVgzOzJ\|OE[zPS=>
human NSCLC	NECzOHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MV2wMlUuOs7:TR?=	M3fmPFczcA>?		MnSyTWM2OD1zzszN	M3S0dVIzPzhzM{mz
human NSCLC	MXjLbY5ie2ViQYPzZZk>	M{DadlHPxE1?	NWPBfFFMOjSq		MYDpcohq[mm2czD0bIUhSWu2L33UU3Ihe2mpbnHsbY5oKHCjdHj3ZZkh[XRiM3igZYZ1\XJidILlZZRu\W62	NEXScIMzOjd6MUO5Ny=>
Y1 cell line	MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MVSwMlHPxE1xMd88US=>	NYj3cJVuOjSq	M3nsbGROW09?	NEjndGRqdmirYnn0d{A3OO,:hTDj[YxtKH[rYXLpcIl1gSCrbjDNfYMuW2O2cj30doFve2[nY4Tl[EBk\Wyucx?=	M1zldVIzPjl{OUC0
PIK3CA-mutant MCF7	NESxZlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	Ml;hS2k2OD1zNkFCtVkydk4xvJzMSFUxRTl6MNMxNlc{dk1?	M1vsSVczcA>?		M1nGemdKPTB;MU[wxtE6OW6P78{MUGQ2OD17OEFCtVI4O26P	NHrtZWgzOjZ3M{m2Oy=>
PIK3CA-mutant MCF7	MYDLbY5ie2ViQYPzZZk>	MXfJR\|UxRTFzNNMxN45O	NXfI[WdCPzKq		NVrQbW4yUUN3ME2xNVTDuTOwTTDpckBz\WS3Y3nu[{BCc3RicHjvd5Bpd3K7bHH0bY9vKGyndnXsdy=>	M1;meVIzPjV\|OU[3
MCF7-myr-Akt	MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MXrHTVUxRTJ7OdMxOlhvVe,:jFzEOVDwxJ5zMDywNFBvVQ>?	MXq3Nog>		MWXHTVUxRTJ7OdMxOlhvVe,:jFzEOVDwxJ5zMDywNFBvVQ>?	M1GwPFIzPjV\|OU[3
colon cancer cell lines	M2rMS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MYiwMVEx\|ryP	NGTBTIo4Omh?	MY\EUXNQ	MWDJR\|UxRTIQvF2=	MYSyNlU1Ozh3Nx?=
gastric cancer cell lines	NXfZd2RET3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NF;lZWUxNTFyzszN	NUe4cnVqPzKq	NFPrVldFVVOR	NX63elY1UUN3ME2yMVXPxE1?	MUWyNlU1Ozh3Nx?=
HCT-116/HT-29/MKN-45	NXXjR5JjSXCxcITvd4l{KEG\|c3H5	MXmy{txO	NILTVpc1QGh?		M3[0WZNpcW[2IHnuJGczKHCqYYPl	M3O1eVIzPTR\|OEW3
HT-29 and HCT-116	MVHDZZNx[XOnIHHzd4F6	NV7JflhxPc7:TR?=	MkHONlRp		NXG0cYI6cW6mdXPld{Bk[XOyYYPlJIFkfGm4aYT5	M1nGSlIzPTR\|OEW3
MM cell lines	M3XjPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NF;CSGIyOM7:TR?=	NU\vRldVOjSq	NIr6ZW9FVVOR	NVX6NJVNUUN3MDD2ZZJq\XNiYX3vcoch\GmoZnXy[Y51KGOnbHygcIlv\XNiaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdmOn	MVKyNlIxPzR6NR?=
ARP-1	MnnwRZBweHSxc3nzJGF{e2G7	NGPkNnUyOM7:TR?=	MnvHNlRp	NV3IN45XTE2VTx?=	MWnpcoR2[2W\|IF3NJINmdGxiYYDvdJRwe2m\|IITodo92\2hiY3HzdIF{\SCjY4TpeoF1cW:w	MmTqNlIzODd2OEW=
SNU-601	NUX4SINKT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NX3Ld4lJPzKq	M4LhO2ROW09?	MlT0TWM2OD1yLkixOuKyOC5yNkROwG0>	MYWyNlE2QThzNB?=
SNU-1	M4Xnd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7		M{OyR\|czcA>?	MWrEUXNQ	M4q1UmlEPTB;MT6wPFLDuTBwMEK4{txO	M2q4SlIzOTV7OEG0
SNU-668	MoXsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		M2\pRlczcA>?	MnLOSG1UVw>?	NHrI[lRKSzVyPUGuOVc6yrFyLkC3OO69VQ>?	NXfh[ZZqOjJzNUm4NVQ>
AGS	Mkj6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MlH2O\|Jp	M1z6cmROW09?	MmDFTWM2OD1zLkexOOKyOC5zMUhOwG0>	M1njVVIzOTV7OEG0
SNU-216	MlrLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NXzDUlBUPzKq	MkHaSG1UVw>?	MUHJR\|UxRTJwNkmyxtExNjB6Mt88US=>	M4jHN\|IzOTV7OEG0
SNU-5	M2jjc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NXPoRZZMPzKq	Mmi4SG1UVw>?	NH[1ZYVKSzVyPUGuN\|UyyrFyLkC5Ne69VQ>?	MWGyNlE2QThzNB?=
SNU-638	M3za[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		M3fJS\|czcA>?	NEDFZlRFVVOR	MWjJR\|UxRTJwMkiyxtExNjB3M988US=>	MmG5NlIyPTl6MUS=
SNU-16	M4WwXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MWC3Nog>	M4DDT2ROW09?	MkfHTWM2OD1zLkW3N:KyOC5yMEJOwG0>	NVG1VJRJOjJzNUm4NVQ>
SNU-484	NYHVfnZjT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NFqwTFk4Omh?	NFPJV\|ZFVVOR	MY\JR\|UxRTFwN{K4xtExNjB2Nd88US=>	NGnMfGwzOjF3OUixOC=>
SNU-620	NFq5fYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MYi3Nog>	MnHNSG1UVw>?	MV3JR\|UxRTJwOUO5xtExNjByMd88US=>	NETJUXczOjF3OUixOC=>
SNU-719	NEfPbW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MYi3Nog>	M3HmbWROW09?	Ml3HTWM2OD1\|LkCzO:KyOC5yM{NOwG0>	MlmwNlIyPTl6MUS=
glioma cell lines	NX;0[ZZLT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		M2nBW\|czcA>?		M{PqWGlEPTB;MT2y{txO	MVSyNlA3PTB6MB?=
U87	M32zU2Fxd3C2b4Ppd{BCe3OjeR?=	Mom3Nu69VQ>?	MXS3Nog>		NUP5flhxcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDhcoQh[2ynYY\l[EBRSVKSIHHu[EBk[XOyYYPlMVM>	M{H5PFIzODZ3MEiw

... 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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PI3K Signaling Pathway Map

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Wortmannin

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 105 Publications

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

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

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PI3K Signaling Pathway Map

PI3K Inhibitors with Unique Features

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Buparlisib (BKM120, NVP-BKM120)

Cited by 105 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

Computed Result

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)

Tech Support

PI3K Signaling Pathway Map

PI3K Inhibitors with Unique Features

Related PI3K Products

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