Buparlisib (BKM120)

For research use only.

Catalog No.S2247 Synonyms: NVP-BKM120

151 publications

Buparlisib (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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Selleck's Buparlisib (BKM120) has been cited by 151 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 MVvDfZRwfG:6aXOgRZN{[Xl? NVrCd45ZPzJiaB?= MV\EUXNQ MYDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIV5eHKnc4PpcochWEl|S3HsdIhiKEV3NEXLJI12fGGwdDD3bZRpKEeLNUCgc4YhOC5yMECxOVgh|ryP MkPUNlQ6ODB{Nk[=
DU145 MYrDfZRwfG:6aXOgRZN{[Xl? NUnjcFB6PzJiaB?= NYTKd5VTTE2VTx?= MXfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDEWVE1PSClZXzsd{BmgHC{ZYPzbY5oKEyNQkGgcZV1[W62IIfpeIghT0l3MDDv[kAxNjByMESzOUDPxE1? MXOyOFkxODJ4Nh?=
A2780 NYLqR5lHS3m2b4TvfIlkKEG|c3H5 NI[5TYs4OiCq M3nLUWROW09? NIe1VlFEgXSxdH;4bYNqfHliYXfhbY5{fCCSVFXOMYRm\mmlaXXueEBpfW2jbjDBNlc5OCClZXzsd{B4cXSqIFfJOVAhd2ZiMD6wNFA3OzVizszN NW[xcHJbOjR7MECyOlY>
U87MG MnPVR5l1d3SxeHnjJGF{e2G7 MoDmO|IhcA>? M3PXOWROW09? M2\SXWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KFCWRV6t[IVncWOrZX70JIh2dWGwIGW4O21IKGOnbHzzJJdqfGhiR1m1NEBw\iByLkCwNFY6QCEQvF2= MXuyOFkxODJ4Nh?=
A2780 M{PpcGZ2dmO2aX;uJGF{e2G7 NFz4dIIyKGh? M2HRR2ROW09? MWXJcohq[mm2aX;uJI9nKFCLM1utcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:|cHjvdplt[XSrb36ge4l1cCCHQ{WwJI9nKDBwMEW1JO69VQ>? MXWyOFkxODJ4Nh?=
DU145 MU\GeY5kfGmxbjDBd5NigQ>? NGPNc4IyKGh? NEjL[m5FVVOR M3\vU2lvcGmkaYTpc44hd2ZiUFmzT{1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBFXTF2NTDj[YxteyCqYYLic5JqdmdiTFvCNUBufXSjdHnvckB4cXSqIFXDOVAhd2ZiMD6wO|Mh|ryP M3jLd|I1QTByMk[2
A2780 Mn3YSpVv[3Srb36gRZN{[Xl? M2DkeFEhcA>? NX\yOI9lTE2VTx?= MY\Jcohq[mm2aX;uJI9nKFCLM1utcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:|cHjvdplt[XSrb36gbY4hWFSHTj3k[YZq[2mnboSgbJVu[W5iQUK3PFAh[2WubIOge4l1cCCHQ{WwJI9nKDBwMEe0JO69VQ>? NUfvfJFMOjR7MECyOlY>
MCF7 NFryOFVHfW6ldHnvckBCe3OjeR?= NHvVRlQyKGh? M1u0UGROW09? MojFTY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiRUW0OWshdXW2YX70MY1m\GmjdHXkJGFMXCCVZYK0O|MheGixc4Doc5J6dGG2aX;uJJdqfGhiRVO1NEBw\iByLkGg{txO M3XKTVI1QTByMk[2
U87MG NXvRS4h3TnWwY4Tpc44hSXO|YYm= NUHkW5BnOSCq M13BTGROW09? MXPJcohq[mm2aX;uJI9nKFCLM1utcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:|cHjvdplt[XSrb36gbY4hWFSHTj3k[YZq[2mnboSgbJVu[W5iVUi3UWch[2WubIOge4l1cCCHQ{WwJI9nKDBwMUOg{txO MknxNlQ6ODB{Nk[=
A2780 NVHwTmNZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHrfo84OiCq NGCySHNFVVOR NX3Vb|dYTUN3ME2wMlUzKM7:TR?= MWGyOFkxODJ4Nh?=
SKMES-1 MlLBR5l1d3SxeHnjJGF{e2G7 NH\5WVYyKM7:TR?= MUe3NkBp M1rQbWlv\HWlZYOgZ4VtdCCmZXH0bC=> NEDhUZczPjBzM{OxPC=>
H596 NWHyeFF[TnWwY4Tpc44hSXO|YYm= MYOxJO69VQ>? NGW5UYRKdXCjaYLzJINmdGxibXnndoF1cW:w NITvOHAzPjBzM{OxPC=>
HCC2450 NHTlWlBHfW6ldHnvckBCe3OjeR?= MmDJNUDPxE1? MorZTY1x[Wm{czDj[YxtKGmwdnHzbY9v M3rCXFI3ODF|M{G4
A549 MXLGeY5kfGmxbjDBd5NigQ>? MYG1NFAhdk1? M{C1SFQ5KGh? NVK5e|dsTE2VTx?= NEX4UHNKdmirYnn0d{BCc3RiYXP0bZZifGmxbh?= Mmj6NlU6Ozd{OUm=
A549 MkKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYq4VnBvOSEQvF2= M4TX[FczKGh? MojLSG1UVw>? M13xfGlvcGmkaYTzJINmdGxiZ4Lve5Rp NHzXUpYzPTl|N{K5PS=>
H522 NVHmT4R1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml65NUDPxE1? NXfnVFBGPzJiaB?= NUPoeWFxTE2VTx?= NGjKOXhKdmirYnn0d{Bk\WyuIHfyc5d1cA>? MX[yOVk{PzJ7OR?=
LNCaP MWLGeY5kfGmxbjDBd5NigQ>? NXHXZ3BVOSEQvF2= MUfTeZBxemW|c3XzJJAuSUuWIHzleoVtew>? NXjpT3Z5OjV|NkC3PVk>
LNCaP95 NWDpe496TnWwY4Tpc44hSXO|YYm= M2HaZVEh|ryP M2H4WHN2eHC{ZYPz[ZMheC2DS2SgcIV3\Wy| NV3pemszOjV|NkC3PVk>
HCT-15 MoHNRZBwfG:|aYOgRZN{[Xl? NG\OZYMyOCEQvF2= NH\K[W41QCCq NFfySotFVVOR MY\JcoR2[2W|IHHwc5B1d3OrczDpckBJS1RvMUWgZ4VtdHNiaHHyZo92emmwZzDQTWs{S0FiaH;0d5BwfCCvdYTheIlwdg>? NWjKT5duOjVzNUKyOFU>
HCT-116 NV\ScVdZSXCxdH;zbZMhSXO|YYm= NUnY[ZdnOTBizszN MXu0PEBp NFX0dnhFVVOR M{G0[mlv\HWlZYOgZZBweHSxc3nzJIlvKEiFVD2xNVYh[2WubIOgbIFz[m:3cnnu[{BRUUt|Q1GgbI91e3CxdDDteZRifGmxbh?= MnH1NlUyPTJ{NEW=
NCI-H460 MWnBdI91d3OrczDBd5NigQ>? MVqxNEDPxE1? MVq0PEBp MoiySG1UVw>? NVjFdWlXUW6mdXPld{BieG:ydH;zbZMhcW5iTlPJMWg1PjBiY3XscJMhcGG{Yn;1dolv\yCSSVuzR2EhcG:2c4DveEBufXSjdHnvci=> NVPjTZFOOjVzNUKyOFU>
SKOV-3 MojMRZBwfG:|aYOgRZN{[Xl? NGHr[pEyOCEQvF2= MVi0PEBp MYrEUXNQ MUnJcoR2[2W|IHHwc5B1d3OrczDpckBUU0:YLUOgZ4VtdHNiaHHyZo92emmwZzDQTWs{S0FiaH;0d5BwfCCvdYTheIlwdg>? M3jDeVI2OTV{MkS1
BSY-1 NF3Mc3BCeG:2b4Ppd{BCe3OjeR?= NFHWeZAyOCEQvF2= MVm0PEBp M{[4dWROW09? NU\MTVN[UW6mdXPld{BieG:ydH;zbZMhcW5iQmPZMVEh[2WubIOgbIFz[m:3cnnu[{BRUUt|Q1GgbI91e3CxdDDteZRifGmxbh?= Mom3NlUyPTJ{NEW=
MKN-1 MV7BdI91d3OrczDBd5NigQ>? NGDGZpoyOCEQvF2= NX\ifnJEPDhiaB?= MmDQSG1UVw>? MkXLTY5lfWOnczDhdI9xfG:|aYOgbY4hVUuQLUGgZ4VtdHNiaHHyZo92emmwZzDQTWs{S0FiaH;0d5BwfCCvdYTheIlwdg>? M4XXSlI2OTV{MkS1
NCI-H522 NGPMdJhCeG:2b4Ppd{BCe3OjeR?= NGfUd|UyOCEQvF2= NXz4PIhtPDhiaB?= NU\mS3BCTE2VTx?= MnT6TY5lfWOnczDhdI9xfG:|aYO= NU\kbYpoOjVzNUKyOFU>
OVCAR-3 NVzlWmo4SXCxdH;zbZMhSXO|YYm= MVOxNEDPxE1? M1HEO|Q5KGh? MWrEUXNQ NYHPU2EyUW6mdXPld{BieG:ydH;zbZM> M1H6WlI2OTV{MkS1
HBC-5 NETUfXNCeG:2b4Ppd{BCe3OjeR?= M3\KTFExKM7:TR?= M3jJ[lQ5KGh? MoLlSG1UVw>? MmfYTY5lfWOnczDhdI9xfG:|aYO= NHvZUpkzPTF3MkK0OS=>
RXF-631L NEPa[lZCeG:2b4Ppd{BCe3OjeR?= NHToO4cyOCEQvF2= MmrMOFghcA>? NYGweVFWTE2VTx?= MV7JcoR2[2W|IHHwc5B1d3Orcx?= M4rq[|I2OTV{MkS1
MKN-45 MV\BdI91d3OrczDBd5NigQ>? MYexNEDPxE1? MU[0PEBp NUDFfppUTE2VTx?= MWjJcoR2[2W|IHHwc5B1d3Orcx?= M3XycFI2OTV{MkS1
BON-1 M3[0SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\zRVUxOCCwTR?= MkjONVAh\A>? MV3EUXNQ NFjXclJKdmirYnn0d{Bk\WyuIHfyc5d1cA>? NY\XN|cyOjVyMk[yPVI>
BON-1 M3vtZ2Z2dmO2aX;uJGF{e2G7 MVy1NFAhdk1? MYG0JIg> MYLEUXNQ NXeyPJdWUW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEGNVDDheEBVcHJ|MEigZY5lKFOnckS3Ny=> MmLjNlUxOjZ{OUK=
QGP-1 NYTCdG8zTnWwY4Tpc44hSXO|YYm= NYnqd4RKPTByIH7N MYq0JIg> NGLTUppFVVOR NHPOWYhKdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhSUuWIHH0JHRpejNyODDhcoQhW2W{NEez M1Lob|I2ODJ4Mkmy
Huh7 M4rxN2Z2dmO2aX;uJGF{e2G7 NWDYfHIzOSEQvF2= NVjOSms6OSCq M4n0fWROW09? MUfJcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRWtVKGG2IGPldlQ4PA>? NVTCNI5LOjVyMES0NFM>
BNL MkDXSpVv[3Srb36gRZN{[Xl? NIHQPG4yKM7:TR?= NFTD[JkyKGh? Ml;ESG1UVw>? NHvlWoJKdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhWzZ? NFPDTJYzPTByNESwNy=>
MDA-MB-175 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELRN|EyKM7:TR?= MlXROUBl Mo\ISG1UVw>? NVz4UYFUUUN3MEyxJO69VQ>? M2DvTFI1QDd7N{m2
MDA-MB-134 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYOxJO69VQ>? MXS1JIQ> MmLGSG1UVw>? M4\1UmlEPTB:MTFOwG0> NInaVYwzPDh5OUe5Oi=>
HCC1500 M4r1Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHxfpkyKM7:TR?= MmXMOUBl MYnEUXNQ NVzET2FsUUN3MEyxJO69VQ>? MoXBNlQ5Pzl5OU[=
EFM-19 MkHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUKxJO69VQ>? M4O2PVUh\A>? NUe3TWRJTE2VTx?= M3XhT2lEPTB:MTFOwG0> NU\TXVJWOjR6N{m3PVY>
ZR-75-30 NWL0[|BUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXDVoMyKM7:TR?= NImzc4c2KGR? NVztV45XTE2VTx?= NETs[WJKSzVyPEGg{txO MnziNlQ5Pzl5OU[=
MDA-MB-361 Mn3uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPm[nAyKM7:TR?= MXG1JIQ> M1PiNWROW09? M1fQVWlEPTB:MTFOwG0> NITaeXkzPDh5OUe5Oi=>
T-47D M1XWVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXSxJO69VQ>? NELtWmY2KGR? M3LsPGROW09? NW[wRXExUUN3MEyxJO69VQ>? MkPzNlQ5Pzl5OU[=
SK-BR-3 M4PieWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWWxJO69VQ>? NYTVfHZNPSCm NHixU|dFVVOR MlfRTWM2ODxzIN88US=> NI\hXFUzPDh5OUe5Oi=>
UACC-732 NELwZ4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzoToIyKM7:TR?= NXn1SYV{PSCm NGnjUpBFVVOR NVv6cppyUUN3MEyxJO69VQ>? MUKyOFg4QTd7Nh?=
BT-474 MofwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYn4TVRkOSEQvF2= NEnKe282KGR? M1rUfGROW09? MULJR|UxRDFizszN NULhdIdEOjR6N{m3PVY>
HCC202 NGrUdWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmD3NUDPxE1? M{Dze|Uh\A>? MVPEUXNQ MUXJR|UxRDFizszN MV6yOFg4QTd7Nh?=
MCF7 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TYOlEh|ryP MlXuOUBl NHLZR2lFVVOR MmHNTWM2ODxzIN88US=> M1\peFI1QDd7N{m2
MDA-MB-415 NWPS[2hXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWSxJO69VQ>? NH7BUmc2KGR? NUfQcYo6TE2VTx?= M1TEXWlEPTB:MTFOwG0> Mn\DNlQ5Pzl5OU[=
MDA-MB-453 M2fScGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIr3epMyKM7:TR?= NUP5VoUxPSCm M2HhfmROW09? M2DxXWlEPTB:MTFOwG0> MV:yOFg4QTd7Nh?=
ZR-75-1 MofoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXHXYFMOSEQvF2= Ml\nOUBl NFXTVWdFVVOR MUfJR|UxRDFizszN NWP1bINqOjR6N{m3PVY>
HCC38 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHG0eYMyKM7:TR?= MofQOUBl MV7EUXNQ MWjJR|UxRDFizszN NE\oOHAzPDh5OUe5Oi=>
HCC1419 MmPaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEG5bGkyKM7:TR?= Mm\FOUBl NIXiXZNFVVOR Mnv4TWM2ODxzIN88US=> MnLyNlQ5Pzl5OU[=
UACC-812 NFrp[3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVOxJO69VQ>? M1mwVlUh\A>? MYPEUXNQ MnnSTWM2ODxzIN88US=> NEjuUZYzPDh5OUe5Oi=>
HCC1187 M{\lVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLZfWlWOSEQvF2= M33kUlUh\A>? MnOySG1UVw>? M1LHfGlEPTB:MTFOwG0> M2LuWlI1QDd7N{m2
KPL-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTVeIpSOSEQvF2= MWK1JIQ> MVvEUXNQ MWnJR|UxRDFizszN M1zBbFI1QDd7N{m2
SUM-225 NY\1VpFKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWGxJO69VQ>? NF\6XoU2KGR? NVnYT4lUTE2VTx?= NWPvPZY2UUN3MEyxJO69VQ>? NXHoWIV7OjR6N{m3PVY>
EFM-192A NWr0c2t1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjGd25YOSEQvF2= M1zPN|Uh\A>? NU\WeI9mTE2VTx?= NFi0ZWJKSzVyPEGg{txO MWeyOFg4QTd7Nh?=
JIMT-1 NILM[WNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPERoN6OSEQvF2= MVi1JIQ> NInmcmZFVVOR Ml;vTWM2ODxzIN88US=> M2XRbFI1QDd7N{m2
HCC1143 NHLHO4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDqPJYyKM7:TR?= NX75fY9LPSCm NWrHNmlzTE2VTx?= M3XhXmlEPTB:MTFOwG0> MVyyOFg4QTd7Nh?=
HCC2218 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\1NUDPxE1? M1TTeFUh\A>? NYLyd3N3TE2VTx?= M3fHeGlEPTB:MTFOwG0> MkTzNlQ5Pzl5OU[=
MDA-MB-468 MmjzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjQPWsyKM7:TR?= MVe1JIQ> MV7EUXNQ M1H5PWlEPTB:MTFOwG0> MUeyOFg4QTd7Nh?=
BT-20 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXmxJO69VQ>? NEj1T2U2KGR? NUDuVYNWTE2VTx?= M4DUN2lEPTB:MTFOwG0> MUKyOFg4QTd7Nh?=
MDA-MB-435 M4D5T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUexJO69VQ>? MX21JIQ> NH\ifVZFVVOR MlS4TWM2ODxzIN88US=> NUjmUI9EOjR6N{m3PVY>
BT-549 M1nIe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWKxJO69VQ>? NI\JO4g2KGR? M4XHc2ROW09? NGr0cFZKSzVyPEGg{txO MWWyOFg4QTd7Nh?=
HCC1806 MlizS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHP3dIQyKM7:TR?= MkPnOUBl MVrEUXNQ M13OOWlEPTB:MTFOwG0> M4O0TFI1QDd7N{m2
HCC1937 M4fDeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1u3R|Eh|ryP M3;QcFUh\A>? MoHTSG1UVw>? MVzJR|UxRDFizszN M1WwUFI1QDd7N{m2
Hs578T NXzSUHh3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nYWFEh|ryP M{T6ZlUh\A>? MmLFSG1UVw>? Ml:5TWM2ODxzIN88US=> MlrJNlQ5Pzl5OU[=
LN18 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHyTJo6OjBizszN MnfaO|IhcA>? NYewc2doTE2VTx?= NFX1WFVKSzVyPEWg{txO NHWwXpAzPDd2MUC3OC=>
LN229 M1m4e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TMN|IxKM7:TR?= NXvaU5dEPzJiaB?= NVvwTI84TE2VTx?= M1LkNmlEPTB:NTFOwG0> MVeyOFc1OTB5NB?=
LNZ308 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjQNlAh|ryP MnnVO|IhcA>? NHXiN3BFVVOR NUfDNIw2UUN3MEy1JO69VQ>? MYOyOFc1OTB5NB?=
T98G M4LoOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\5N|IxKM7:TR?= MYS3NkBp MVjEUXNQ NI[xOFhKSzVyPEWg{txO NVPDPZNWOjR5NEGwO|Q>
U87 MmWyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV6yNEDPxE1? M3fWflczKGh? Mn\qSG1UVw>? NVGxdlhvUUN3MEy1JO69VQ>? MX[yOFc1OTB5NB?=
LN18 NGLVXmxHfW6ldHnvckBCe3OjeR?= MX21JO69VQ>? MVOyOEBp M{fGdWROW09? NUi4WnNvUW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEGNVB?= Ml;aNlQ4PDFyN{S=
LNZ308 MoexSpVv[3Srb36gRZN{[Xl? MlzuOUDPxE1? M1zY[FI1KGh? M{LtS2ROW09? M{DBc2lvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBCU1R? NX7rR|ZyOjR5NEGwO|Q>
Saos-2 MlHHSpVv[3Srb36gRZN{[Xl? NITtdnc2OCEQvF2= MoTKOFghcA>? NIX5RnVKdmirYnn0d{Bk\WyuIHnueoF{cW:w MXGyOFczPzZ4MB?=
MG-63 MoT4SpVv[3Srb36gRZN{[Xl? Moi1OVAh|ryP M3;hSlQ5KGh? M1rtZmlvcGmkaYTzJINmdGxiaX72ZZNqd25? M1\FclI1PzJ5Nk[w
SJSA-1 MnrkSpVv[3Srb36gRZN{[Xl? NXLOUWNnPTBizszN M1PlNFQ5KGh? NX\sXVZGUW6qaXLpeJMh[2WubDDpcpZie2mxbh?= MVqyOFczPzZ4MB?=
Saos-2 NWHiPHhiTnWwY4Tpc44hSXO|YYm= M174elUxKM7:TR?= NFe3VIY1QCCq M4DPNGlvcGmkaYTzJI1ifHKreDDt[ZRidGyxcILveIVqdmG|ZT2yJIV5eHKnc4Ppc44> MlG1NlQ4Ojd4NkC=
MG-63 NWq5N3RzTnWwY4Tpc44hSXO|YYm= MU[1NEDPxE1? MkjGOFghcA>? NVm0XIs4UW6qaXLpeJMhdWG2cnn4JI1mfGGubH;wdo91\WmwYYPlMVIh\XiycnXzd4lwdg>? NHTZNoozPDd{N{[2NC=>
SJSA-1 NXXSR2loTnWwY4Tpc44hSXO|YYm= MXO1NEDPxE1? NG\4O2Q1QCCq MV\Jcohq[mm2czDtZZRzcXhibXX0ZYxtd3C{b4TlbY5ie2VvMjDlfJBz\XO|aX;u M17hU|I1PzJ5Nk[w
Saos-2 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHWOVAh|ryP M4T1SFQ5KGh? NF7IT4JKdmirYnn0d{Bk\WyuII\pZYJqdGm2eR?= NUGyVIRHOjR5Mke2OlA>
MG-63 M1jEW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jre|UxKM7:TR?= M1;NU|Q5KGh? MmjUTY5pcWKrdIOgZ4VtdCC4aXHibYxqfHl? MkPDNlQ4Ojd4NkC=
SJSA-1 M1qx[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjjfpY2OCEQvF2= M2nEXVQ5KGh? M4LqeGlvcGmkaYTzJINmdGxidnnhZoltcXS7 Mkn3NlQ4Ojd4NkC=
FaDu M{\QXGZ2dmO2aX;uJGF{e2G7 MUC1JO69VQ>? NYPEZmZ[OjRiaB?= NHPFTGRFVVOR MofXVoVlfWOnczDvfJlo\W5iY3;ud5VueHSrb36= M4LJSFI1PjNzMUS3
EMT6 NEC1NohHfW6ldHnvckBCe3OjeR?= M{DIRlUh|ryP MVWyOEBp MXXEUXNQ NV;xe|BHWmWmdXPld{BwgHmpZX6gZ49ve3WvcITpc44> M2fOT|I1PjNzMUS3
HCT116 MoXUSpVv[3Srb36gRZN{[Xl? NUe0[otqPSEQvF2= MXGyOEBp NYTQOWdITE2VTx?= MmfvVoVlfWOnczDvfJlo\W5iY3;ud5VueHSrb36= MnP0NlQ3OzFzNEe=
U87 MkPKSpVv[3Srb36gRZN{[Xl? NEK4dVI2KM7:TR?= MX2yOEBp NF60e4dFVVOR M4naZnJm\HWlZYOgc5h6\2WwIHPvcpN2dXC2aX;u Mnq4NlQ3OzFzNEe=
GBM NYjNN4FJSXCxcITvd4l{KEG|c3H5 NITRUXEz|ryP NUDB[oZ4PDiq NXP1XlNiTE2VTx?= NHfnSWNqdmS3Y3XkJIhq\2incjDs[ZZmdHNib3[gZZBweHSxc3nzMEBidmRiZHXjdoVie2WmIHPlcIwhfmmjYnnsbZR6 NEfrbXgzPDVyMES5Ni=>
BON MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWixMVXPxE1? NIjCPIM4Omh? MoLh[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvci=> MUWyOFQ1OzV{Mx?=
BON MVvBdI9xfG:|aYOgRZN{[Xl? NEG1NmcyNTYQvF2= M2K5RVI1cA>? MXnpcoNz\WG|ZYOgZZBweHSxc3nz Mon3NlQ1PDN3MkO=
H1975 NGOyfFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWi2SpQ{OC5|LUmuOu69VQ>? MkS0O|Jp MVnEUXNQ NYft[YpyUUN3ME2xMlM5Pc7:TR?= MkTGNlQ{Ozd6NE[=
H1975 MorGRZBweHSxc3nzJGF{e2G7 MnuyNu69VQ>? M{C2blI1cA>? MXrEUXNQ MV3pcoNz\WG|ZYOgZZBweHSxc3nzJJJifGVic3nncolncWOjboTsfS=> NHvEeFgzPDN|N{i0Oi=>
T-ALL NInUZ5VCeG:ydH;zbZMhSXO|YYm= MUni[ZR4\WWwIEGuOEBidmRiNT6zJI1OKGG2IEK0bEBidmRiMD65JIFv\CB3LkWgcW0h[XRiNEjoJIlvKGSrZn\ldoVvfCClZXzsJIxqdmV? NFzVZYszPCCxcjC0PIg> Mn72SG1UVw>? NUjvRppF[W[oZXP0d{B1cGViUFmzT{Bx[XSqd3H5JIlvKFRvQVzMJINmdGxibHnu[ZM> NHnFVZEzPDNzMEezOi=>
BCR-ABL M1ewUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfDNE4zPS1zMN88US=> NXX6eo5mPGR? NGP6UIF{cWewaX\pZ4FvfGy7IHnubIljcXRiY3XscEBxem:uaX\ldoF1cW:w NEHuZ5QzPDJ2NE[xNi=>
LC-1/SQSF MY\GeY5kfGmxbjDBd5NigQ>? NUK3U|JTO87:TR?= M1TGTVI1cA>? MYLEUXNQ NUnR[lV2\GWlcnXhd4UhVlKIMjDwdo91\WmwIHzleoVt NGfCR4EzOzl6MEC5Ny=>
Primary CLL cells M{O5d2Fxd3C2b4Ppd{BCe3OjeR?= NHvobHIyNTFyzszN NWfPfYNYPDiq NH;uVGdqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCFTFygZ4VtdHNiaX7k[ZBmdmSnboSgc4YheHKxZ37vd5Rq[yCvYYLr[ZJ{ NHfYTnczOzh3MEiwOy=>
Primary CLL cells NX3neJJTU2mwYYPlJGF{e2G7 MnXxNu69VQ>? NUfzPFJJOzCvaX6= NEP4O5dl\WO{ZXHz[YQhWEl|SzDhZ5Rqfmm2eR?= NHO5SI0zOzh3MEiwOy=>
Primary CLL cells M1r2bmN6fG:2b4jpZ{BCe3OjeR?= MlPmNu69VQ>? MVqyOIg> NVTKW3dxcW6mdXPld{Bk\WyuIHP5eI91d3irY3n0fS=> MWOyN|g2ODhyNx?=
human NSCLC cell lines MX7BdI9xfG:|aYOgRZN{[Xl? M1r2[FAvOTJ3LUVOwG0> MkX1NlRp NIfpSnJFVVOR MlnLTWM2OHNicnHu[4V{KG[{b32gNE41NTMQvF2= MWmyN|U3OjR5Mh?=
human HCC cell lines M3npbWNmdGxidnnhZoltcXS7IHHzd4F6 NEixdGsxNjByNT2x{txO M4PjN|Q5cA>? Mkn6TWM2OD1zzszN M2ntV|I{PDh7OUm5
Huh7 M1;TSWtqdmG|ZTDBd5NigQ>? MVWx{txO MVi0PIg> M{jKPZNq\26r77{BZ4FvfGy7IILl[JVk\XNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> NE\aVFQzOzR6OUm5PS=>
SK-HEP1 NFy2XnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYC4TnFkOS1{MN88US=> M4rodlczcA>? MUjEUXNQ MVzJR|Ux97zeMd88US=> M{n0XVI{PDd7MUO2
786-0 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWCxMVIx|ryP NYHmR4xJPzKq MlvoSG1UVw>? NWnS[2NWUUN3MP-8oFHPxE1? M4i5WlI{PDd7MUO2
JVM2 NXfDfmF4S3m2b4TvfIlkcXS7IHHzd4F6 NGrBc4QxNjJvMkFOwG0> NUHvXpM1PzKq M1;IbGROW09? NYPMe4luUUN3ME2wMlnPxE1? MV6yN|I{QDZ|OR?=
EHEB NWO4RZRYS3m2b4TvfIlkcXS7IHHzd4F6 M3fXW|AvOi1{MN88US=> NHnpOnE4Omh? M1fiOmROW09? NHz0SmJKSzVyPUCuO:69VQ>? MY[yN|I{QDZ|OR?=
MEC2 MmnVR5l1d3SxeHnjbZR6KGG|c3H5 NFLXPW8xNjJvMkFOwG0> NISzXWQ4Omh? MmjMSG1UVw>? Mn;qTWM2OD1yLkhOwG0> M2rqb|I{OjN6NkO5
primary B-CLL lymphocytes MlPHRZBweHSxc3nzJGF{e2G7 M4DXZ2lEPTBiZn;yJIVi[2hicILpcYFzgSClZXzsJIxqdmV? NHLj[YkzPGh? NVq5XXRkTE2VTx?= MnnLTWM2OO,:nEROwG0h\m:{IHHscEBx[XSrZX70dy=> NYDOR4IyOjN{M{i2N|k>
primary B-CLL lymphocytes M3:4T2tqdmG|ZTDBd5NigQ>? MnL2TWM2OCCob4Kg[YFkcCCycnntZZJ6KGOnbHygcIlv\Q>? M3OxdlI1cA>? NXjzWWZbcW6qaXLpeJMheDdyU{\LJEYhPEVvQmCxJIV5eHKnc4Ppc44> M3Hje|I{OjN6NkO5
human NSCLC Ml31S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TYRVAvPS1{zszN M2HHT|czcA>? NHeyTZNKSzVyPUJOwG0> NFW1ZmozOjd6MUO5Ny=>
human NSCLC NULHSVZuU2mwYYPlJGF{e2G7 Mn\2Ne69VQ>? NYq1O2FlOjSq MX;pcohq[mm2czD0bIUhSWu2L33UU3Ihe2mpbnHsbY5oKHCjdHj3ZZkh[XRiM3igZYZ1\XJidILlZZRu\W62 NFPmOFMzOjd6MUO5Ny=>
Y1 cell line NHGxVYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfiWFd2OC5zzszNM|HPxE1? MlnxNlRp MnzBSG1UVw>? MXnpcohq[mm2czC2NQ+9jSClZXzsJJZq[WKrbHn0fUBqdiCPeXOtV4N1ei22cnHud4Zm[3SnZDDj[Yxtew>? NXTWVGd7OjJ4OUK5NFQ>
PIK3CA-mutant MCF7 NX\nNVl6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHnZVQ5T0l3ME2xOlDDuTlzbl5vwKxNTDVyPUm4NOKyOjd|bl2= MlnPO|Jp NGjuNoFIUTVyPUG2NOKyQTGwTf-8kGxFPTB;OUiwxtEzPzOwTR?= MmXFNlI3PTN7Nke=
PIK3CA-mutant MCF7 MVzLbY5ie2ViQYPzZZk> M17RdGlEPTB;MUG0xtE{dk1? MnPGO|Jp MXzJR|UxRTFzNNMxN45OKGmwIILl[JVkcW6pIFHreEBxcG:|cHjvdplt[XSrb36gcIV3\Wy| M4nEUlIzPjV|OU[3
MCF7-myr-Akt M2PEd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE[2ZWhIUTVyPUK5PeKyPjiwTf-8kGxFPTExvK6xNEwxODCwTR?= NIjtU2Y4Omh? MYTHTVUxRTJ7OdMxOlhvVe,:jFzEOVDwxJ5zMDywNFBvVQ>? M4f0R|IzPjV|OU[3
colon cancer cell lines MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInaOYwxNTFyzszN NGrrNlA4Omh? NFfTUVRFVVOR MU\JR|UxRTIQvF2= NUHGdId6OjJ3NEO4OVc>
gastric cancer cell lines M1HJUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV:wMVEx|ryP MnW2O|Jp Ml;JSG1UVw>? MUfJR|UxRTJvNd88US=> Mk\ZNlI2PDN6NUe=
HCT-116/HT-29/MKN-45 MUHBdI9xfG:|aYOgRZN{[Xl? NGS4dIIz|ryP MXO0PIg> NXrLVmVbe2irZoSgbY4hTzJicHjhd4U> M{Hpc|IzPTR|OEW3
HT-29 and HCT-116 M2\5T2Nie3Cjc3WgZZN{[Xl? Mn\VOe69VQ>? MUSyOIg> M1fETIlv\HWlZYOgZ4F{eGG|ZTDhZ5Rqfmm2eR?= MmjhNlI2PDN6NUe=
MM cell lines MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHUNVDPxE1? M3n0N|I1cA>? MULEUXNQ MY\JR|UxKH[jcnnld{BidW:wZzDkbYZn\XKnboSgZ4VtdCCuaX7ld{BqdiC2aX3lJIFv\CCmb4PlJIRmeGWwZHXuZ4U> MVyyNlIxPzR6NR?=
ARP-1 Mn33RZBweHSxc3nzJGF{e2G7 NEjRVYoyOM7:TR?= NEHhNGYzPGh? NYfoS4h5TE2VTx?= M2nTNolv\HWlZYOgUW0h[2WubDDhdI9xfG:|aYOgeIhzd3WpaDDjZZNx[XOnIHHjeIl3[XSrb36= NWXLV4RTOjJ{MEe0PFU>
SNU-601 NY\NcJlQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWC3Nog> M4LnTWROW09? Mlm0TWM2OD1yLkixOuKyOC5yNkROwG0> NULLdJBOOjJzNUm4NVQ>
SNU-1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzuUFY4Omh? M1fhTmROW09? NUW3ZXk5UUN3ME2xMlA5OsLzMD6wNljPxE1? NF3PbIozOjF3OUixOC=>
SNU-668 NVjsflU3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{X5WVczcA>? Mo\QSG1UVw>? MkjpTWM2OD1zLkW3PeKyOC5yN{VOwG0> MlnmNlIyPTl6MUS=
AGS MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFny[WQ4Omh? NEXNVFRFVVOR NE[5T4hKSzVyPUGuO|E1yrFyLkGxO:69VQ>? MkHzNlIyPTl6MUS=
SNU-216 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DiS|czcA>? MXzEUXNQ NV7oZpQ{UUN3ME2yMlY6OsLzMD6wPFLPxE1? NYOzN3RNOjJzNUm4NVQ>
SNU-5 NVjCWIF1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILt[XI4Omh? Mn3MSG1UVw>? MnzCTWM2OD1zLkO1NeKyOC5yOUJOwG0> MWmyNlE2QThzNB?=
SNU-638 NHT4VIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkCyO|Jp M3XQOWROW09? NH3ucYpKSzVyPUKuNlgzyrFyLkC1N:69VQ>? NYnTdXFiOjJzNUm4NVQ>
SNU-16 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TINVczcA>? MXrEUXNQ MUfJR|UxRTFwNUezxtExNjByMd88US=> M4KxVFIzOTV7OEG0
SNU-484 MoC5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI[4bZU4Omh? NH;6SZNFVVOR NHi2OGhKSzVyPUGuO|I5yrFyLkC0Oe69VQ>? NV7iUXRWOjJzNUm4NVQ>
SNU-620 M{Lzbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\SV|czcA>? M37mNWROW09? NVfTbo5OUUN3ME2yMlk{QcLzMD6wNFHPxE1? NGLlfIIzOjF3OUixOC=>
SNU-719 NWHEWopST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVf6PJNwPzKq MWDEUXNQ NXnmS3c6UUN3ME2zMlA{P8LzMD6wN|LPxE1? NIPFfYszOjF3OUixOC=>
glioma cell lines MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWK3Nog> NGjCbFZKSzVyPUGtNu69VQ>? NX;rO29DOjJyNkWwPFA>
U87 MV7BdI9xfG:|aYOgRZN{[Xl? NV;nNY5VOs7:TR?= MYi3Nog> MofVbY5lfWOnczDj[YxtKGGyb4D0c5NqeyCjbnSgZ4xm[X[nZDDQRXJRKGGwZDDjZZNx[XOnLUO= MVWyNlA3PTB6MB?=

... 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.
  • 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 NVP-BKM120
Smiles NC1=CC(=C(C=N1)C2=NC(=NC(=C2)N3CCOCC3)N4CCOCC4)C(F)(F)F

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Dilution Calculator

Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

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

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    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
NCT04338399 Not yet recruiting Drug: Buparlisib & Paclitaxel Head and Neck Cancer Adlai Nortye Biopharma Co. Ltd. July 31 2020 Phase 3
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

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID