Buparlisib (BKM120, NVP-BKM120)

Catalog No.S2247

Buparlisib (BKM120, NVP-BKM120) Chemical Structure

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.

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Cited by 105 Publications

Purity & Quality Control

Choose Selective PI3K Inhibitors

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)
52 nM 116 nM 166 nM 262 nM 2.4 μM
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     


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     


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     


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     


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     


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     


The expression of phosphorylated or total forms of MET protein was analyzed by western blotting. 

27283525 28036259 26673665 27572309 29928341
Immunofluorescence
FOXO3a; 

PubMed: 28036259     


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     


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]
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  • 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)

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

Molecular Weight 410.39
Formula

C18H21F3N6O2

CAS No. 944396-07-0
Storage powder
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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The Serial Dilution Calculator Equation

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    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

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

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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

If you have any other enquiries, please leave a message.

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PI3K Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID