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 78 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 MXvDfZRwfG:6aXOgRZN{[Xl? M4Tq[VczKGh? NYDOR|JbTE2VTx?= MknIR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{BmgHC{ZYPzbY5oKFCLM1vhcJBp[SCHNUS1T{BufXSjboSge4l1cCCJSUWwJI9nKDBwMECwNVU5KM7:TR?= MVOyOFkxODJ4Nh?=
DU145 NHvHTGREgXSxdH;4bYMhSXO|YYm= NFK4fXU4OiCq NX\V[mhYTE2VTx?= NGjXU5BEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBFXTF2NTDj[YxteyCneIDy[ZN{cW6pIFzLRlEhdXW2YX70JJdqfGhiR1m1NEBw\iByLkCwNFQ{PSEQvF2= MlixNlQ6ODB{Nk[=
A2780 MoToR5l1d3SxeHnjJGF{e2G7 MVq3NkBp MnrtSG1UVw>? MWTDfZRwfG:6aXPpeJkh[WejaX7zeEBRXEWQLXTl[olkcWWwdDDoeY1idiCDMke4NEBk\WyuczD3bZRpKEeLNUCgc4YhOC5yMEC2N|Uh|ryP M2q5PVI1QTByMk[2
U87MG MXHDfZRwfG:6aXOgRZN{[Xl? MkPyO|IhcA>? NX\xc3ZpTE2VTx?= NILCTlhEgXSxdH;4bYNqfHliYXfhbY5{fCCSVFXOMYRm\mmlaXXueEBpfW2jbjDVPFdOTyClZXzsd{B4cXSqIFfJOVAhd2ZiMD6wNFA3QThizszN NGj1UIMzPDlyMEK2Oi=>
A2780 NUXaTplkTnWwY4Tpc44hSXO|YYm= MUWxJIg> M2myVmROW09? NGPIW29KdmirYnn0bY9vKG:oIGDJN2sudWWmaXH0[YQhSUuWIGPldlQ4OyCyaH;zdIhwenmuYYTpc44hf2m2aDDFR|UxKG:oIECuNFU2KM7:TR?= MV[yOFkxODJ4Nh?=
DU145 MVXGeY5kfGmxbjDBd5NigQ>? M{K4SFEhcA>? MVfEUXNQ MXfJcohq[mm2aX;uJI9nKFCLM1utcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gSHUyPDViY3XscJMhcGG{Yn;ybY5oKEyNQkGgcZV1[XSrb36ge4l1cCCHQ{WwJI9nKDBwMEezJO69VQ>? NXvveVVsOjR7MECyOlY>
A2780 M1TnNWZ2dmO2aX;uJGF{e2G7 MV:xJIg> MXHEUXNQ NHnXWnRKdmirYnn0bY9vKG:oIGDJN2sudWWmaXH0[YQhSUuWIGPldlQ4OyCyaH;zdIhwenmuYYTpc44hcW5iUGTFUk1l\W[rY3nlcpQhcHWvYX6gRVI4QDBiY3XscJMhf2m2aDDFR|UxKG:oIECuNFc1KM7:TR?= MVWyOFkxODJ4Nh?=
MCF7 MXTGeY5kfGmxbjDBd5NigQ>? NXLSZndROSCq MU\EUXNQ NFHqTlJKdmirYnn0bY9vKG:oIGDJN2tidHCqYTDFOVQ2UyCvdYThcpQudWWmaXH0[YQhSUuWIGPldlQ4OyCyaH;zdIhwenmuYYTpc44hf2m2aDDFR|UxKG:oIECuNUDPxE1? MXmyOFkxODJ4Nh?=
U87MG MmfZSpVv[3Srb36gRZN{[Xl? NX;ne4ZIOSCq NYDVOmhuTE2VTx?= MkPhTY5pcWKrdHnvckBw\iCSSUPLMY1m\GmjdHXkJGFMXCCVZYK0O|MheGixc4Doc5J6dGG2aX;uJIlvKFCWRV6t[IVncWOrZX70JIh2dWGwIGW4O21IKGOnbHzzJJdqfGhiRVO1NEBw\iByLkGzJO69VQ>? MV:yOFkxODJ4Nh?=
A2780 NIPLPVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;TO|IhcA>? MXzEUXNQ MmrhSWM2OD1yLkWyJO69VQ>? NX20VIs{OjR7MECyOlY>
SKMES-1 MWTDfZRwfG:6aXOgRZN{[Xl? M1nKdFEh|ryP NIfzUVc4OiCq NWfIb45tUW6mdXPld{Bk\WyuIHTlZZRp NIT0VnEzPjBzM{OxPC=>
H596 MnLvSpVv[3Srb36gRZN{[Xl? NYPZVIlKOSEQvF2= NGT0V4JKdXCjaYLzJINmdGxibXnndoF1cW:w NF;rOZAzPjBzM{OxPC=>
HCC2450 NXTjXYRHTnWwY4Tpc44hSXO|YYm= NFv6R3cyKM7:TR?= MmfiTY1x[Wm{czDj[YxtKGmwdnHzbY9v M4WzWVI3ODF|M{G4
A549 Ml\DSpVv[3Srb36gRZN{[Xl? M{nLb|UxOCCwTR?= M3:4eVQ5KGh? MlTLSG1UVw>? NWKxVIl5UW6qaXLpeJMhSWu2IHHjeIl3[XSrb36= MmO5NlU6Ozd{OUm=
A549 NYrHOIRIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\nNm12OSEQvF2= MnvOO|IhcA>? NFO5XnJFVVOR MojSTY5pcWKrdIOgZ4VtdCCpcn;3eIg> MonDNlU6Ozd{OUm=
H522 MoPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PI[FEh|ryP NFzJ[5g4OiCq NXHUNphNTE2VTx?= Mk[xTY5pcWKrdIOgZ4VtdCCpcn;3eIg> M2iyU|I2QTN5Mkm5
LNCaP M{X0W2Z2dmO2aX;uJGF{e2G7 MYixJO69VQ>? NFjhbIRUfXCycnXzd4V{KHBvQVvUJIxmfmWucx?= MUGyOVM3ODd7OR?=
LNCaP95 NYjMdZBuTnWwY4Tpc44hSXO|YYm= MWCxJO69VQ>? MX;TeZBxemW|c3XzJJAuSUuWIHzleoVtew>? M{fOelI2OzZyN{m5
HCT-15 NImzZZVCeG:2b4Ppd{BCe3OjeR?= MmjFNVAh|ryP MlzlOFghcA>? MkCySG1UVw>? MWHJcoR2[2W|IHHwc5B1d3OrczDpckBJS1RvMUWgZ4VtdHNiaHHyZo92emmwZzDQTWs{S0FiaH;0d5BwfCCvdYTheIlwdg>? MmK4NlUyPTJ{NEW=
HCT-116 M1[ySmFxd3Sxc3nzJGF{e2G7 NHSwU|AyOCEQvF2= MVO0PEBp MlzsSG1UVw>? MnfkTY5lfWOnczDhdI9xfG:|aYOgbY4hUEOWLUGxOkBk\WyuczDoZZJjd3W{aX7nJHBKUzOFQTDoc5R{eG:2IH31eIF1cW:w NIPqUpczPTF3MkK0OS=>
NCI-H460 M2LVNmFxd3Sxc3nzJGF{e2G7 MnfrNVAh|ryP MmnlOFghcA>? NH;xdoRFVVOR NHXUXopKdmS3Y3XzJIFxd3C2b4Ppd{BqdiCQQ1mtTFQ3OCClZXzsd{Bp[XKkb4XybY5oKFCLS{PDRUBpd3S|cH;0JI12fGG2aX;u NYP3RopUOjVzNUKyOFU>
SKOV-3 NG[wZVNCeG:2b4Ppd{BCe3OjeR?= NGi3R3AyOCEQvF2= MX:0PEBp MoTrSG1UVw>? MX;JcoR2[2W|IHHwc5B1d3OrczDpckBUU0:YLUOgZ4VtdHNiaHHyZo92emmwZzDQTWs{S0FiaH;0d5BwfCCvdYTheIlwdg>? NWe0R5RPOjVzNUKyOFU>
BSY-1 NGn4c5BCeG:2b4Ppd{BCe3OjeR?= NEHy[lUyOCEQvF2= NX\m[4M5PDhiaB?= NE\PZnBFVVOR MnO3TY5lfWOnczDhdI9xfG:|aYOgbY4hSlO\LUGgZ4VtdHNiaHHyZo92emmwZzDQTWs{S0FiaH;0d5BwfCCvdYTheIlwdg>? MUiyOVE2OjJ2NR?=
MKN-1 NFvjUJdCeG:2b4Ppd{BCe3OjeR?= NEDLT4MyOCEQvF2= NHTabFY1QCCq M3zQWmROW09? NFzoeFBKdmS3Y3XzJIFxd3C2b4Ppd{BqdiCPS16tNUBk\WyuczDoZZJjd3W{aX7nJHBKUzOFQTDoc5R{eG:2IH31eIF1cW:w M4DqdlI2OTV{MkS1
NCI-H522 NEHB[WRCeG:2b4Ppd{BCe3OjeR?= NHLXdIkyOCEQvF2= NW\NdFM{PDhiaB?= NHzOdJZFVVOR NUWxW|c{UW6mdXPld{BieG:ydH;zbZM> MoGzNlUyPTJ{NEW=
OVCAR-3 MVrBdI91d3OrczDBd5NigQ>? Mk\zNVAh|ryP Ml:yOFghcA>? M2DZdGROW09? NHjsNm5KdmS3Y3XzJIFxd3C2b4Ppdy=> MmC5NlUyPTJ{NEW=
HBC-5 NXTrNJhrSXCxdH;zbZMhSXO|YYm= MX[xNEDPxE1? M3uzUlQ5KGh? NWT5c5BCTE2VTx?= M2fifWlv\HWlZYOgZZBweHSxc3nz M3fNT|I2OTV{MkS1
RXF-631L NIXwXHRCeG:2b4Ppd{BCe3OjeR?= NUPvenNQOTBizszN M4PVNlQ5KGh? MWjEUXNQ NWT6cXlHUW6mdXPld{BieG:ydH;zbZM> M3yxUlI2OTV{MkS1
MKN-45 NX32cIVCSXCxdH;zbZMhSXO|YYm= MoW1NVAh|ryP NHjJWHU1QCCq M{\sdGROW09? MV\JcoR2[2W|IHHwc5B1d3Orcx?= M2rvXFI2OTV{MkS1
BON-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljvOVAxKG6P MVuxNEBl MV\EUXNQ NVnmT3EzUW6qaXLpeJMh[2WubDDndo94fGh? MWKyOVAzPjJ7Mh?=
BON-1 NU\6fIhOTnWwY4Tpc44hSXO|YYm= NYj1eVlUPTByIH7N NEDTSmw1KGh? Ml;FSG1UVw>? M3j2eGlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBCU1RiYYSgWIhzOzB6IHHu[EBU\XJ2N{O= MUSyOVAzPjJ7Mh?=
QGP-1 MoPKSpVv[3Srb36gRZN{[Xl? NX7WOmJDPTByIH7N MWi0JIg> NGntOFVFVVOR NFPHV49KdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhSUuWIHH0JHRpejNyODDhcoQhW2W{NEez Mlf1NlUxOjZ{OUK=
Huh7 NHu2WWhHfW6ldHnvckBCe3OjeR?= NUHscnZiOSEQvF2= NVXy[FR4OSCq M1\RVmROW09? MlTBTY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXCCjdDDT[ZI1PzR? MmewNlUxODR2MEO=
BNL MkjMSpVv[3Srb36gRZN{[Xl? NUjoWWxbOSEQvF2= NF;nZVIyKGh? MX\EUXNQ NFr0OGxKdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhWzZ? M2DyPFI2ODB2NECz
MDA-MB-175 NGn4fIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPUNUDPxE1? M2qwfFUh\A>? MmL2SG1UVw>? NFHjRoRKSzVyPEGg{txO NEizemQzPDh5OUe5Oi=>
MDA-MB-134 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\jXG5ZOSEQvF2= MWO1JIQ> NGXlSINFVVOR NGPvPW5KSzVyPEGg{txO NISxVJIzPDh5OUe5Oi=>
HCC1500 M4HnbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vkOFEh|ryP NGn4bmU2KGR? NGnWeoZFVVOR NXq3XoFEUUN3MEyxJO69VQ>? NHvOcpIzPDh5OUe5Oi=>
EFM-19 Mm\vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTP[oFLOSEQvF2= NHrDUXY2KGR? MmPKSG1UVw>? NV\jTpdIUUN3MEyxJO69VQ>? NFjMfnozPDh5OUe5Oi=>
ZR-75-30 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYGxJO69VQ>? MWi1JIQ> Mn3rSG1UVw>? M4W5[mlEPTB:MTFOwG0> MmnpNlQ5Pzl5OU[=
MDA-MB-361 NEn1WnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7xS2MyKM7:TR?= NYrrSFN6PSCm M3X0d2ROW09? NGnIbJBKSzVyPEGg{txO NGr2UXYzPDh5OUe5Oi=>
T-47D MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLKVFNPOSEQvF2= MXK1JIQ> NYTxdnZTTE2VTx?= MY\JR|UxRDFizszN NHrtUoozPDh5OUe5Oi=>
SK-BR-3 NXLrOY85T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XYb|Eh|ryP MmXOOUBl MYTEUXNQ M4TmN2lEPTB:MTFOwG0> NV\IW5BzOjR6N{m3PVY>
UACC-732 NF\scW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nwSVEh|ryP NXHCfGhCPSCm MVHEUXNQ NFLSN3NKSzVyPEGg{txO MVqyOFg4QTd7Nh?=
BT-474 M2ruXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrMV|QyKM7:TR?= NVLjcpljPSCm MmqwSG1UVw>? MoPMTWM2ODxzIN88US=> MnP6NlQ5Pzl5OU[=
HCC202 Mn2zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2qwXFEh|ryP MYm1JIQ> MXnEUXNQ NYDNT|RoUUN3MEyxJO69VQ>? M4i3eFI1QDd7N{m2
MCF7 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV6xJO69VQ>? M3zWTVUh\A>? MljPSG1UVw>? MVfJR|UxRDFizszN NXzkWGtSOjR6N{m3PVY>
MDA-MB-415 MkezS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPrNUDPxE1? MX61JIQ> NI\tVHpFVVOR MV3JR|UxRDFizszN NVzmNnVkOjR6N{m3PVY>
MDA-MB-453 M{\UbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDaNUDPxE1? M{HPWFUh\A>? MVrEUXNQ MkLPTWM2ODxzIN88US=> NGjUeo0zPDh5OUe5Oi=>
ZR-75-1 NVvReIdNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVXicYxkOSEQvF2= M2\tRlUh\A>? NWPrUXdHTE2VTx?= M3u4O2lEPTB:MTFOwG0> M33wW|I1QDd7N{m2
HCC38 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXhOIoyKM7:TR?= MUO1JIQ> MWfEUXNQ NI\1c2pKSzVyPEGg{txO MkPSNlQ5Pzl5OU[=
HCC1419 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvVNUDPxE1? MnXDOUBl MUHEUXNQ MkHpTWM2ODxzIN88US=> MXqyOFg4QTd7Nh?=
UACC-812 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkH2NUDPxE1? MoDXOUBl NFf0eIhFVVOR M{PKSmlEPTB:MTFOwG0> NF7IOmYzPDh5OUe5Oi=>
HCC1187 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLjNUDPxE1? M4K4ZVUh\A>? MmjTSG1UVw>? M3rUZmlEPTB:MTFOwG0> MX[yOFg4QTd7Nh?=
KPL-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\ENUDPxE1? NUHi[29ZPSCm NHPLblBFVVOR NHPuUGdKSzVyPEGg{txO NF:5ZW4zPDh5OUe5Oi=>
SUM-225 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWGxJO69VQ>? MVm1JIQ> MorWSG1UVw>? M2LCemlEPTB:MTFOwG0> Ml7WNlQ5Pzl5OU[=
EFM-192A MnLzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrRNUDPxE1? NGHFTVE2KGR? NGn1ZYlFVVOR M13QcGlEPTB:MTFOwG0> MomzNlQ5Pzl5OU[=
JIMT-1 MoP2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnONUDPxE1? MlXXOUBl M4jLPGROW09? M2LiV2lEPTB:MTFOwG0> M3TyclI1QDd7N{m2
HCC1143 NFfmUHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXWxJO69VQ>? M4KzOlUh\A>? M2W1c2ROW09? MmC1TWM2ODxzIN88US=> M4nQ[FI1QDd7N{m2
HCC2218 NV3ENFJDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYCxJO69VQ>? M4D0XlUh\A>? MXHEUXNQ MXXJR|UxRDFizszN MlvvNlQ5Pzl5OU[=
MDA-MB-468 M2\kWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrhRVEyKM7:TR?= NEjhXVg2KGR? MoXtSG1UVw>? NHfTbGFKSzVyPEGg{txO MWiyOFg4QTd7Nh?=
BT-20 MknsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnBfnEyKM7:TR?= MlK2OUBl NED4S2hFVVOR M3nQSGlEPTB:MTFOwG0> NEDyU|czPDh5OUe5Oi=>
MDA-MB-435 M3WxS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWGxJO69VQ>? NFvmNVU2KGR? NH[0NGxFVVOR M1nCUmlEPTB:MTFOwG0> NXrx[Hp4OjR6N{m3PVY>
BT-549 MmfJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;VPGJ5OSEQvF2= MUS1JIQ> MVrEUXNQ MnfUTWM2ODxzIN88US=> NV\FOnVKOjR6N{m3PVY>
HCC1806 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHXXZZQOSEQvF2= MojjOUBl MmW1SG1UVw>? NIC5cJhKSzVyPEGg{txO MYCyOFg4QTd7Nh?=
HCC1937 NWPT[WJVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvFd|EyKM7:TR?= M1Tv[|Uh\A>? NF;PfVJFVVOR NF;oR|dKSzVyPEGg{txO NH3ITW4zPDh5OUe5Oi=>
Hs578T MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELsNoMyKM7:TR?= NVnCdI1EPSCm NVf1OWlwTE2VTx?= MV7JR|UxRDFizszN NVXhOGc2OjR6N{m3PVY>
LN18 NGK2R5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfxTHMzOCEQvF2= NF3UWpk4OiCq MmrZSG1UVw>? NX:5UmJJUUN3MEy1JO69VQ>? Ml;ONlQ4PDFyN{S=
LN229 M{XiNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDQOVQ6OjBizszN M1fX[FczKGh? MYrEUXNQ NFvTNZlKSzVyPEWg{txO Mk[zNlQ4PDFyN{S=
LNZ308 NXPVVpFYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWCyNEDPxE1? M3;5[FczKGh? M3PjfWROW09? MnHkTWM2ODx3IN88US=> NXTRWZRUOjR5NEGwO|Q>
T98G M1fCXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fsfFIxKM7:TR?= NGrLd5E4OiCq NWX4bVNuTE2VTx?= MULJR|UxRDVizszN Mn3aNlQ4PDFyN{S=
U87 NEjoOI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV6yNEDPxE1? M1e5c|czKGh? MWPEUXNQ NXXz[YZHUUN3MEy1JO69VQ>? MV6yOFc1OTB5NB?=
LN18 M33qTGZ2dmO2aX;uJGF{e2G7 MXq1JO69VQ>? MWCyOEBp NGTSRo9FVVOR MYfJcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRWtV NUHPc253OjR5NEGwO|Q>
LNZ308 M4fCPWZ2dmO2aX;uJGF{e2G7 NEXBdXk2KM7:TR?= NVzCb5NnOjRiaB?= M2fKfWROW09? M{jqV2lvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBCU1R? MnjxNlQ4PDFyN{S=
Saos-2 MnPwSpVv[3Srb36gRZN{[Xl? MoO0OVAh|ryP MkfEOFghcA>? NHvabW9KdmirYnn0d{Bk\WyuIHnueoF{cW:w NGH1PVAzPDd{N{[2NC=>
MG-63 MUHGeY5kfGmxbjDBd5NigQ>? NGH1ZZc2OCEQvF2= NX[xRm82PDhiaB?= NVTxfI9bUW6qaXLpeJMh[2WubDDpcpZie2mxbh?= Mn\uNlQ4Ojd4NkC=
SJSA-1 MU\GeY5kfGmxbjDBd5NigQ>? NY\hdoxkPTBizszN NHvncFE1QCCq MmDaTY5pcWKrdIOgZ4VtdCCrbo\hd4lwdg>? Moq3NlQ4Ojd4NkC=
Saos-2 M2XIOWZ2dmO2aX;uJGF{e2G7 NH\UfnE2OCEQvF2= NGrpSoQ1QCCq M13Q[WlvcGmkaYTzJI1ifHKreDDt[ZRidGyxcILveIVqdmG|ZT2yJIV5eHKnc4Ppc44> NFH0VZEzPDd{N{[2NC=>
MG-63 NHjydVdHfW6ldHnvckBCe3OjeR?= NFmy[2Y2OCEQvF2= M3vQelQ5KGh? MWHJcohq[mm2czDtZZRzcXhibXX0ZYxtd3C{b4TlbY5ie2VvMjDlfJBz\XO|aX;u NXjJW|FQOjR5Mke2OlA>
SJSA-1 NWO0eJdMTnWwY4Tpc44hSXO|YYm= NHHpcIc2OCEQvF2= M1PnPFQ5KGh? M1y2SWlvcGmkaYTzJI1ifHKreDDt[ZRidGyxcILveIVqdmG|ZT2yJIV5eHKnc4Ppc44> MmPkNlQ4Ojd4NkC=
Saos-2 NX6xeVg4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nicFUxKM7:TR?= NUnZXI5oPDhiaB?= NHrxSWRKdmirYnn0d{Bk\WyuII\pZYJqdGm2eR?= NVnWblNHOjR5Mke2OlA>
MG-63 Moi3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUC1NEDPxE1? NYXqS3VHPDhiaB?= MV;Jcohq[mm2czDj[YxtKH[rYXLpcIl1gQ>? M{TJ[FI1PzJ5Nk[w
SJSA-1 NHvldWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fPSFUxKM7:TR?= MVq0PEBp NXjkWlNmUW6qaXLpeJMh[2WubDD2bYFjcWyrdIm= Ml;aNlQ4Ojd4NkC=
FaDu NWfrZ|BUTnWwY4Tpc44hSXO|YYm= NGHjUZo2KM7:TR?= NEnCbnAzPCCq M4PxVmROW09? NGPycWFT\WS3Y3XzJI95gWenbjDjc45{fW2ydHnvci=> MonNNlQ3OzFzNEe=
EMT6 NWTqd2xrTnWwY4Tpc44hSXO|YYm= NIW5U2U2KM7:TR?= NUW3bnY3OjRiaB?= M{PDfGROW09? NXvT[2RvWmWmdXPld{BwgHmpZX6gZ49ve3WvcITpc44> MnrlNlQ3OzFzNEe=
HCT116 M{izWWZ2dmO2aX;uJGF{e2G7 MX[1JO69VQ>? MoPTNlQhcA>? M4jUNWROW09? NEfxZ|RT\WS3Y3XzJI95gWenbjDjc45{fW2ydHnvci=> MnzmNlQ3OzFzNEe=
U87 NFjFT4lHfW6ldHnvckBCe3OjeR?= Ml3lOUDPxE1? NGjy[WUzPCCq MV\EUXNQ NXXrTFBzWmWmdXPld{BwgHmpZX6gZ49ve3WvcITpc44> M1XqZ|I1PjNzMUS3
GBM NEfk[XJCeG:ydH;zbZMhSXO|YYm= NXfNXplCOs7:TR?= MVy0PIg> NEHVelBFVVOR MVfpcoR2[2WmIHjp[4hmeiCuZY\lcJMhd2ZiYYDvdJRwe2m|LDDhcoQh\GWlcnXhd4VlKGOnbHygeoli[mmuaYT5 MWOyOFUxODR7Mh?=
BON NHTMU4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XvTVEuPc7:TR?= M2PuOlczcA>? NX30OFRH\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdg>? MUSyOFQ1OzV{Mx?=
BON NEe3fWtCeG:ydH;zbZMhSXO|YYm= M4TMS|EuPc7:TR?= Mke0NlRp NYnVXFJucW6lcnXhd4V{KGGyb4D0c5Nqew>? MXWyOFQ1OzV{Mx?=
H1975 NU\hUolrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLqNE4{NTlwNt88US=> MlPHO|Jp MWXEUXNQ MWTJR|UxRTFwM{i1{txO Mki5NlQ{Ozd6NE[=
H1975 MnzkRZBweHSxc3nzJGF{e2G7 NFTne|gz|ryP NYSwW5htOjSq MVHEUXNQ MWrpcoNz\WG|ZYOgZZBweHSxc3nzJJJifGVic3nncolncWOjboTsfS=> NHXuUGszPDN|N{i0Oi=>
T-ALL NV;CRo1lSXCxcITvd4l{KEG|c3H5 MUni[ZR4\WWwIEGuOEBidmRiNT6zJI1OKGG2IEK0bEBidmRiMD65JIFv\CB3LkWgcW0h[XRiNEjoJIlvKGSrZn\ldoVvfCClZXzsJIxqdmV? NVvBd4xzOjRib4KgOFhp NWrkSWQ4TE2VTx?= M4jMNYFn\mWldIOgeIhmKFCLM1ugdIF1cHejeTDpckBVNUGOTDDj[YxtKGyrbnXz M4HQd|I1OzFyN{O2
BCR-ABL MmL6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUWwMlI2NTFyzszN NF\SeWw1\A>? MlH6d4lodmmoaXPhcpRtgSCrbnjpZol1KGOnbHygdJJwdGmoZYLheIlwdg>? MYCyOFI1PDZzMh?=
LC-1/SQSF MlfJSpVv[3Srb36gRZN{[Xl? NF\BZ20{|ryP NHW3b28zPGh? NICwTpNFVVOR MXnk[YNz\WG|ZTDOVmYzKHC{b4TlbY4hdGW4ZXy= NVi3R3NYOjN7OECwPVM>
Primary CLL cells NFPyWoFCeG:ydH;zbZMhSXO|YYm= NXLxeox4OS1zMN88US=> MUS0PIg> NH64XVVqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCFTFygZ4VtdHNiaX7k[ZBmdmSnboSgc4YheHKxZ37vd5Rq[yCvYYLr[ZJ{ M4TqOFI{QDVyOEC3
Primary CLL cells M1uwemtqdmG|ZTDBd5NigQ>? M3fz[FLPxE1? NF7TPJM{OG2rbh?= NXLuZXV6\GWlcnXhd4VlKFCLM1ugZYN1cX[rdIm= MWeyN|g2ODhyNx?=
Primary CLL cells MWTDfZRwfG:6aXOgRZN{[Xl? MnL1Nu69VQ>? NWnOdYY5OjSq MlPwbY5lfWOnczDj[YxtKGO7dH;0c5hq[2m2eR?= NYiw[495OjN6NUC4NFc>
human NSCLC cell lines NXfzcJRWSXCxcITvd4l{KEG|c3H5 MmHwNE4yOjVvNN88US=> MWeyOIg> M4jJc2ROW09? MVnJR|UxeyC{YX7n[ZMh\nKxbTCwMlQuOs7:TR?= M3\zb|I{PTZ{NEey
human HCC cell lines MkDPR4VtdCC4aXHibYxqfHliYYPzZZk> NF;YPWMxNjByNT2x{txO NV\PTWQ5PDiq NUnK[5l{UUN3ME2x{txO M1TtbVI{PDh7OUm5
Huh7 NWfBZXNSU2mwYYPlJGF{e2G7 M4LoZ|HPxE1? MVK0PIg> Mn7td4lodmoxrJHjZY51dHlicnXkeYNmeyCyaH;zdIhwenmuYYTpc44hd2ZiQXv0 M{HMbVI{PDh7OUm5
SK-HEP1 MofQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfPTIwyNTJyzszN NF;tVFk4Omh? MmT3SG1UVw>? MnTFTWM2OO,:nEJOwG0> MlL3NlM1PzlzM{[=
786-0 NH6xOGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILNXG8yNTJyzszN M4PRfFczcA>? MlPFSG1UVw>? MYDJR|Ux97zeMd88US=> NXnTOIRDOjN2N{mxN|Y>
JVM2 NXvJWlNXS3m2b4TvfIlkcXS7IHHzd4F6 NIfq[mwxNjJvMkFOwG0> MWG3Nog> NXXMVJU2TE2VTx?= MYfJR|UxRTBwOd88US=> NHjLNJAzOzJ|OE[zPS=>
EHEB MVLDfZRwfG:6aXPpeJkh[XO|YYm= NWLtVpR{OC5{LUKw{txO MVO3Nog> M4\oc2ROW09? MYTJR|UxRTBwN988US=> Mly5NlMzOzh4M{m=
MEC2 M1jmU2N6fG:2b4jpZ4l1gSCjc4PhfS=> NGPycZIxNjJvMkFOwG0> NFTyOFU4Omh? NYrUbW5kTE2VTx?= M{OxWGlEPTB;MD63{txO NULwXVhoOjN{M{i2N|k>
primary B-CLL lymphocytes M3;uVGFxd3C2b4Ppd{BCe3OjeR?= M1jRemlEPTBiZn;yJIVi[2hicILpcYFzgSClZXzsJIxqdmV? NGm4emUzPGh? NXS0XIZYTE2VTx?= MWfJR|Ux97zeM988UUBnd3JiYXzsJJBifGmnboTz MYGyN|I{QDZ|OR?=
primary B-CLL lymphocytes NGPlR4JMcW6jc3WgRZN{[Xl? M2LDV2lEPTBiZn;yJIVi[2hicILpcYFzgSClZXzsJIxqdmV? MXGyOIg> M3LTeYlvcGmkaYTzJJA4OFN4SzCmJFRGNUKSMTDlfJBz\XO|aX;u NXvtW2hPOjN{M{i2N|k>
human NSCLC MnLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXmwMlUuOs7:TR?= MVK3Nog> M{PX[2lEPTB;Md88US=> MUGyNlc5OTN7Mx?=
human NSCLC MojCT4lv[XOnIFHzd4F6 M1LHc|HPxE1? NGD3WFUzPGh? MXnpcohq[mm2czD0bIUhSWu2L33UU3Ihe2mpbnHsbY5oKHCjdHj3ZZkh[XRiM3igZYZ1\XJidILlZZRu\W62 MWOyNlc5OTN7Mx?=
Y1 cell line MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jtW|AvOc7:TT:x{txO NHX6cpUzPGh? NH\CU3FFVVOR NVLJR49QcW6qaXLpeJMhPjExvJWgZ4VtdCC4aXHibYxqfHliaX6gUZlkNVOldIKteJJidnOoZXP0[YQh[2WubIO= M4HhSFIzPjl{OUC0
PIK3CA-mutant MCF7 MlHvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILYOmFIUTVyPUG2NOKyQTGwTf-8kGxFPTB;OUiwxtEzPzOwTR?= MUS3Nog> MljnS2k2OD1zNkFCtVkydk4xvJzMSFUxRTl6MNMxNlc{dk1? NEjLeZczOjZ3M{m2Oy=>
PIK3CA-mutant MCF7 Mkm3T4lv[XOnIFHzd4F6 MlXpTWM2OD1zMUVCtVNvVQ>? NES5SJY4Omh? NEXlOGxKSzVyPUGxOOKyO26PIHnuJJJm\HWlaX7nJGFsfCCyaH;zdIhwenmuYYTpc44hdGW4ZXzz MoL5NlI3PTN7Nke=
MCF7-myr-Akt MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjjW2ZRT0l3ME2yPVnDuTZ6bl5vwKxNTDVy78{eNVAtODBybl2= MU[3Nog> Ml7XS2k2OD1{OUpCtVY5dk4xvJzMSFUx97zgMUCsNFAxdk1? M1iyTVIzPjV|OU[3
colon cancer cell lines M4TaZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mom3NE0yOM7:TR?= M1HwNVczcA>? M{XKXGROW09? NEnWbYJKSzVyPUJOwG0> NWrQb2FWOjJ3NEO4OVc>
gastric cancer cell lines NX[wTlkyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDkNE0yOM7:TR?= M3uwT|czcA>? MmXoSG1UVw>? NXnCXoN6UUN3ME2yMVXPxE1? MmjPNlI2PDN6NUe=
HCT-116/HT-29/MKN-45 MlPPRZBweHSxc3nzJGF{e2G7 M{XFVlLPxE1? NULkUHpsPDiq MU\zbIlnfCCrbjDHNkBxcGG|ZR?= M1L6fVIzPTR|OEW3
HT-29 and HCT-116 NVnObnpUS2G|cHHz[UBie3OjeR?= M{ji[VXPxE1? MYKyOIg> M{Pq[Ylv\HWlZYOgZ4F{eGG|ZTDhZ5Rqfmm2eR?= NWTVT44zOjJ3NEO4OVc>
MM cell lines M3r3fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITwNIsyOM7:TR?= NEi1dngzPGh? MYnEUXNQ NHmxVFhKSzVyII\hdolmeyCjbX;u[{BlcW[oZYLlcpQh[2WubDDsbY5meyCrbjD0bY1mKGGwZDDkc5NmKGSncHXu[IVv[2V? NUjsb4xyOjJ{MEe0PFU>
ARP-1 NWjDPGpQSXCxcITvd4l{KEG|c3H5 MkToNVDPxE1? NVL3e5J3OjSq NXvC[mZVTE2VTx?= NYfUWFZZcW6mdXPld{BOVSClZXzsJIFxd3C2b4Ppd{B1cHKxdXfoJINie3Cjc3WgZYN1cX[jdHnvci=> MoTKNlIzODd2OEW=
SNU-601 NGrRcpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zW[VczcA>? NYPs[IxFTE2VTx?= M2TC[mlEPTB;MD64NVbDuTBwME[z{txO NHLuW|czOjF3OUixOC=>
SNU-1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrxZWZEPzKq MoDnSG1UVw>? MWXJR|UxRTFwMEiyxtExNjB{ON88US=> Mn7DNlIyPTl6MUS=
SNU-668 NWTt[Wg2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPVRpJYPzKq MY\EUXNQ NHjJNVVKSzVyPUGuOVc6yrFyLkC3OO69VQ>? NWjyVIx4OjJzNUm4NVQ>
AGS NYTudFVDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rMUFczcA>? MWPEUXNQ NUHhN4RjUUN3ME2xMlcyPMLzMD6xNVfPxE1? MoPBNlIyPTl6MUS=
SNU-216 NWfoZlZ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV23Nog> M2Pj[mROW09? MUPJR|UxRTJwNkmyxtExNjB6Mt88US=> M2\HZ|IzOTV7OEG0
SNU-5 NGfEeWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXv3[oFoPzKq M4\GWmROW09? MWrJR|UxRTFwM{WxxtExNjB7Md88US=> NFXse3kzOjF3OUixOC=>
SNU-638 NUTLV5lST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFX3cZM4Omh? MnH1SG1UVw>? MV;JR|UxRTJwMkiyxtExNjB3M988US=> MkO3NlIyPTl6MUS=
SNU-16 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXu3Nog> MVnEUXNQ NITsTFJKSzVyPUGuOVc{yrFyLkCwNe69VQ>? NFzjeokzOjF3OUixOC=>
SNU-484 NXn1R4k6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULp[4xvPzKq MVXEUXNQ MlL1TWM2OD1zLkeyPOKyOC5yNEZOwG0> MVqyNlE2QThzNB?=
SNU-620 NIf5OXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmC2O|Jp M1;mRWROW09? MX;JR|UxRTJwOUO5xtExNjByMd88US=> MV[yNlE2QThzNB?=
SNU-719 MnXqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULETI41PzKq MYDEUXNQ NV;aPVk6UUN3ME2zMlA{P8LzMD6wN|LPxE1? MWOyNlE2QThzNB?=
glioma cell lines M4PrSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXO3Nog> MUDJR|UxRTFvMt88US=> NX3wbWVNOjJyNkWwPFA>
U87 M1vNXGFxd3C2b4Ppd{BCe3OjeR?= MlzDNu69VQ>? NXnoS|Y5PzKq MnS0bY5lfWOnczDj[YxtKGGyb4D0c5NqeyCjbnSgZ4xm[X[nZDDQRXJRKGGwZDDjZZNx[XOnLUO= NHToSokzOjB4NUC4NC=>

... 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]
+ Expand

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]
+ Expand
  • 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]
+ Expand
  • 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

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

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    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