Buparlisib (BKM120)

For research use only.

Catalog No.S2247 Synonyms: NVP-BKM120

194 publications

Buparlisib (BKM120) Chemical Structure

CAS No. 944396-07-0

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. Buparlisib induces apoptosis. Phase 2.

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Selleck's Buparlisib (BKM120) has been cited by 194 publications

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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. Buparlisib induces apoptosis. 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
glioma cell lines NV\JVYJ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnBZnp3PzKq M4TyZWlEPTB;MT2y{txO MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjB4NUC4NEc,OjJyNkWwPFA9N2F-
U87 NFnBeXFCeG:ydH;zbZMhSXO|YYm= M1j4[|LPxE1? MUe3Nog> NULEbZFEcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDhcoQh[2ynYY\l[EBRSVKSIHHu[EBk[XOyYYPlMVM> MlHQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJyNkWwPFAoRjJ{ME[1NFgxRC:jPh?=
SNU-601 NELTNW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXm3Nog> MkLHSG1UVw>? NH7wVGpKSzVyPUCuPFE3yrFyLkC2N:69VQ>? NY\FSZY2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKxOVk5OTRpPkKyNVU6QDF2PD;hQi=>
SNU-1 M4PXb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoGxO|Jp Mn;SSG1UVw>? M{P2OmlEPTB;MT6wPFLDuTBwMEK4{txO MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjF3OUixOEc,OjJzNUm4NVQ9N2F-
SNU-668 NUjidXpPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzFdpRlPzKq NETJZ2xFVVOR NH3lTXlKSzVyPUGuOVc6yrFyLkC3OO69VQ>? MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjF3OUixOEc,OjJzNUm4NVQ9N2F-
AGS MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\oSY04Omh? NHf6T4VFVVOR NIXh[WVKSzVyPUGuO|E1yrFyLkGxO:69VQ>? NF;5eI09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG1PVgyPCd-MkKxOVk5OTR:L3G+
SNU-216 NI\k[pFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXe3Nog> M3XsUWROW09? MXHJR|UxRTJwNkmyxtExNjB6Mt88US=> NHTuWpE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG1PVgyPCd-MkKxOVk5OTR:L3G+
SNU-5 MnXuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXaO|Jp NYDVTXl2TE2VTx?= M{fsdmlEPTB;MT6zOVHDuTBwMEmx{txO MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjF3OUixOEc,OjJzNUm4NVQ9N2F-
SNU-638 M2nNNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIC5PYc4Omh? NYLXNI1wTE2VTx?= MlzJTWM2OD1{LkK4NuKyOC5yNUROwG0> NWn0fZQ6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKxOVk5OTRpPkKyNVU6QDF2PD;hQi=>
SNU-16 M4DTVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LMUVczcA>? NXHvVJpkTE2VTx?= NHz5V4JKSzVyPUGuOVc{yrFyLkCwNe69VQ>? NV\UXI9bRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKxOVk5OTRpPkKyNVU6QDF2PD;hQi=>
SNU-484 MkLJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVW3Nog> NEf1TnRFVVOR NY\kbXVmUUN3ME2xMlczQMLzMD6wOFXPxE1? NEfmdVU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG1PVgyPCd-MkKxOVk5OTR:L3G+
SNU-620 NFexfm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPrSGM4Omh? NILEdldFVVOR NULPeItGUUN3ME2yMlk{QcLzMD6wNFHPxE1? M3LEUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MUW5PFE1Lz5{MkG1PVgyPDxxYU6=
SNU-719 M2PSfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{L6XFczcA>? NXO3TIhMTE2VTx?= M3q3R2lEPTB;Mz6wN|fDuTBwMEOy{txO M3TEZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MUW5PFE1Lz5{MkG1PVgyPDxxYU6=
MM cell lines MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU[xNO69VQ>? MXSyOIg> NXTQfWlyTE2VTx?= M3W5N2lEPTBidnHybYV{KGGvb37nJIRq\m[ncnXueEBk\WyuIHzpcoV{KGmwIITpcYUh[W6mIHTvd4Uh\GWyZX7k[Y5k\Q>? MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJyN{S4OUc,OjJ{MEe0PFU9N2F-
ARP-1 NXHS[pc5SXCxcITvd4l{KEG|c3H5 MnT0NVDPxE1? Mk\WNlRp MVnEUXNQ MV;pcoR2[2W|IF3NJINmdGxiYYDvdJRwe2m|IITodo92\2hiY3HzdIF{\SCjY4TpeoF1cW:w NIDYOJM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkKwO|Q5PSd-MkKyNFc1QDV:L3G+
colon cancer cell lines MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2WxdVAuOTEQvF2= MV[3Nog> NFzTN4JFVVOR MnnPTWM2OD1zzszN NWrZPVBvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK1OFM5PTdpPkKyOVQ{QDV5PD;hQi=>
gastric cancer cell lines NYDnW2FXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHPNE0yOM7:TR?= NX7aNGpIPzKq NUC5dFR2TE2VTx?= MoLITWM2OD1{LUZOwG0> NF;FcmI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkW0N|g2Pyd-MkK1OFM5PTd:L3G+
HCT-116/HT-29/MKN-45 NGfOTVRCeG:ydH;zbZMhSXO|YYm= Mn\yNu69VQ>? NY\zZXNYPDiq Mn;Sd4hq\nRiaX6gS|IheGijc3W= MoiyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ3NEO4OVcoRjJ{NUSzPFU4RC:jPh?=
HT-29 and HCT-116 NVnsOmFCS2G|cHHz[UBie3OjeR?= MUi1{txO NWXrOGVvOjSq NVPPdlY1cW6mdXPld{Bk[XOyYYPlJIFkfGm4aYT5 NVnHS4VTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK1OFM5PTdpPkKyOVQ{QDV5PD;hQi=>
PIK3CA-mutant MCF7 NVr0TI5JT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7GS2k2OD1zNkFCtVkydk4xvJzMSFUxRTl6MNMxNlc{dk1? NGjVO3I4Omh? M1;OeGdKPTB;MU[wxtE6OW6P78{MUGQ2OD17OEFCtVI4O26P MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ3M{m2O{c,OjJ4NUO5Olc9N2F-
PIK3CA-mutant MCF7 NUnkb5lOU2mwYYPlJGF{e2G7 NXz0WIMxUUN3ME2xNVTDuTOwTR?= M3GzWlczcA>? M3;pb2lEPTB;MUG0xtE{dk1iaX6gdoVlfWOrbnegRYt1KHCqb4PwbI9zgWyjdHnvckBt\X[nbIO= MoDUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4NUO5OlcoRjJ{NkWzPVY4RC:jPh?=
MCF7-myr-Akt M{jnU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\XXGdKPTB;Mkm5xtE3QG6P78{MUGQ2OO,:nkGwMFAxOG6P MkTkO|Jp MUfHTVUxRTJ7OdMxOlhvVe,:jFzEOVDwxJ5zMDywNFBvVQ>? MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ3M{m2O{c,OjJ4NUO5Olc9N2F-
Y1 cell line NELMOW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFS3VVgxNjIQvF2vNe69VQ>? NGfpUWkzPGh? MVfEUXNQ M{TwNIlvcGmkaYTzJFYx97zHIHPlcIwhfmmjYnnsbZR6KGmwIF35Z{1U[3S{LYTyZY5{\mWldHXkJINmdGy| MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ7MkmwOEc,OjJ4OUK5NFQ9N2F-
human NSCLC MkflS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\mV|AvPS1{zszN MVe3Nog> MXXJR|UxRTIQvF2= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjd6MUO5N{c,OjJ5OEGzPVM9N2F-
human NSCLC MX7LbY5ie2ViQYPzZZk> NETtblQy|ryP NUDESpc5OjSq M2LCdolvcGmkaYTzJJRp\SCDa4SvcXRQWiC|aXfuZYxqdmdicHH0bJdigSCjdDCzbEBi\nSncjD0doVifG2nboS= M{TQVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{N{ixN|k{Lz5{Mke4NVM6OzxxYU6=
JVM2 NHXkRXpEgXSxdH;4bYNqfHliYYPzZZk> M{LjSFAvOi1{MN88US=> NVTrSXR3PzKq Moe1SG1UVw>? NIC1N|hKSzVyPUCuPe69VQ>? M{fhVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MkO4OlM6Lz5{M{KzPFY{QTxxYU6=
EHEB NXLFXGZHS3m2b4TvfIlkcXS7IHHzd4F6 NHnRdFAxNjJvMkFOwG0> NHT4NGs4Omh? MYnEUXNQ NX\4Uo5RUUN3ME2wMlfPxE1? MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzJ|OE[zPUc,OjN{M{i2N|k9N2F-
MEC2 MoHER5l1d3SxeHnjbZR6KGG|c3H5 NXLKd|Q5OC5{LUKw{txO M4S0elczcA>? M{nYXmROW09? M4nyZWlEPTB;MD63{txO NYrMTHl2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyN|g3OzlpPkKzNlM5PjN7PD;hQi=>
primary B-CLL lymphocytes MWPBdI9xfG:|aYOgRZN{[Xl? MnHITWM2OCCob4Kg[YFkcCCycnntZZJ6KGOnbHygcIlv\Q>? NXT0N4FqOjSq NHW0U2FFVVOR MkDRTWM2OO,:nEROwG0h\m:{IHHscEBx[XSrZX70dy=> NGPSUFA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{KzPFY{QSd-MkOyN|g3Ozl:L3G+
primary B-CLL lymphocytes NGjnUVFMcW6jc3WgRZN{[Xl? NFLFRXlKSzVyIH\vdkBm[WOqIIDybY1ienliY3XscEBtcW6n NHXJUXYzPGh? M4nCS4lvcGmkaYTzJJA4OFN4SzCmJFRGNUKSMTDlfJBz\XO|aX;u NHrmb3I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{KzPFY{QSd-MkOyN|g3Ozl:L3G+
SK-HEP1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mkn5NU0zOM7:TR?= NHrmbGE4Omh? MmnCSG1UVw>? M4GzemlEPTExvKyx{txO Ml2wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2N{mxN|YoRjJ|NEe5NVM3RC:jPh?=
786-0 NF;qOpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXmxMVIx|ryP M2WxeVczcA>? M13PR2ROW09? NF[weIdKSzVy78{cNe69VQ>? NHrKcYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S3PVE{Pid-MkO0O|kyOzZ:L3G+
human HCC cell lines NIX0Z5hE\WyuII\pZYJqdGm2eTDhd5NigQ>? NIf5XFExNjByNT2x{txO NGTBeHA1QGh? NWnvN491UUN3ME2x{txO MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR6OUm5PUc,OjN2OEm5PVk9N2F-
Huh7 MnXtT4lv[XOnIFHzd4F6 M1raelHPxE1? NETkVpQ1QGh? MV7zbYdvce,ugXPhcpRtgSC{ZXT1Z4V{KHCqb4PwbI9zgWyjdHnvckBw\iCDa4S= M3HxeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NEi5PVk6Lz5{M{S4PVk6QTxxYU6=
human NSCLC cell lines M1XzdGFxd3C2b4Ppd{BCe3OjeR?= NW\x[IVrOC5zMkWtOO69VQ>? M{D4PVI1cA>? MWTEUXNQ M1rNR2lEPTC|IILhcodmeyCocn;tJFAvPC1{zszN NHzTVZM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{W2NlQ4Oid-MkO1OlI1PzJ:L3G+
Primary CLL cells MWXBdI9xfG:|aYOgRZN{[Xl? MXWxMVEx|ryP MV[0PIg> NF[1XYpqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCFTFygZ4VtdHNiaX7k[ZBmdmSnboSgc4YheHKxZ37vd5Rq[yCvYYLr[ZJ{ NGPG[4k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i1NFgxPyd-MkO4OVA5ODd:L3G+
Primary CLL cells NUDNc3p{U2mwYYPlJGF{e2G7 M3nhXlLPxE1? M365clMxdWmw NHr4bHZl\WO{ZXHz[YQhWEl|SzDhZ5Rqfmm2eR?= MnHpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NUC4NFcoRjJ|OEWwPFA4RC:jPh?=
Primary CLL cells MVXDfZRwfG:6aXOgRZN{[Xl? MkLWNu69VQ>? M3nSN|I1cA>? NF\YZZdqdmS3Y3XzJINmdGxiY4n0c5RwgGmlaYT5 NG\DToc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i1NFgxPyd-MkO4OVA5ODd:L3G+
LC-1/SQSF NVPxe3YzTnWwY4Tpc44hSXO|YYm= Mm\1N:69VQ>? NYfCSW12OjSq NG\TPVJFVVOR NHuxcIJl\WO{ZXHz[UBPWkZ{IIDyc5RmcW5ibHX2[Yw> Mo\YQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7OECwPVMoRjJ|OUiwNFk{RC:jPh?=
BCR-ABL NFXNemxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX2wMlI2NTFyzszN NY\sWXczPGR? MnTVd4lodmmoaXPhcpRtgSCrbnjpZol1KGOnbHygdJJwdGmoZYLheIlwdg>? MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ2NE[xNkc,OjR{NES2NVI9N2F-
T-ALL NHyyR5lCeG:ydH;zbZMhSXO|YYm= M{PHOYJmfHenZX6gNU41KGGwZDC1MlMhdU1iYYSgNlRpKGGwZDCwMlkh[W6mIEWuOUBuVSCjdDC0PIghcW5iZHnm[oVz\W62IHPlcIwhdGmwZR?= MU[yOEBweiB2OHi= MV7EUXNQ NIP3WXhi\m[nY4TzJJRp\SCSSUPLJJBifGi5YYmgbY4hXC2DTFygZ4VtdCCuaX7ldy=> NVK4bIFGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzNVA4OzZpPkK0N|ExPzN4PD;hQi=>
H1975 NFPp[IxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjENE4{NTlwNt88US=> NXXDdGZwPzKq MVrEUXNQ NXW3XZpUUUN3ME2xMlM5Pc7:TR?= NXzVTVFLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzN|c5PDZpPkK0N|M4QDR4PD;hQi=>
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UACC-732 MnrvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPmW2o2OSEQvF2= M1n5ZVUh\A>? M4PHPGROW09? MVTJR|UxRDFizszN MkPqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6N{m3PVYoRjJ2OEe5O|k3RC:jPh?=
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TC32 Mn6xdWhVWyCjc4PhfS=> NYXYOXJLeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGTDN|Ih[2WubIO= MmfRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
A673 MUDxTHRUKGG|c3H5 MUTxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>? NHjVT4U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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Saos-2 NILt[INyUFSVIHHzd4F6 MUHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW2Gxcz2yJINmdGy| NYToS2lyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
BT-37 NX3QUG5EeUiWUzDhd5NigQ>? NF\aPWFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQmStN|ch[2WubIO= NH\OSmc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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BT-12 MnLNdWhVWyCjc4PhfS=> MkDFdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUGyJINmdGy| NXHEWJd4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
MG 63 (6-TG R) NUfhNpdSeUiWUzDhd5NigQ>? NWLpXJZXeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF3HJFY{KCh4LWTHJHIqKGOnbHzz NYjUXmFjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB1643 M1PwNpFJXFNiYYPzZZk> NGLNPXFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKxOlQ{KGOnbHzz Mk\pQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
OHS-50 NEHoT|hyUFSVIHHzd4F6 Mnn3dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE:KUz21NEBk\Wyucx?= MnrnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-SH NUXROG54eUiWUzDhd5NigQ>? M32w[ZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHNMNU5vU1igZ4VtdHN? M1GyRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh41 MojIdWhVWyCjc4PhfS=> Mo\QdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqNEGgZ4VtdHN? M1rBR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
A673 MmDjdWhVWyCjc4PhfS=> NFrYTnVyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBCPjd|IHPlcIx{MQ>? NF:0UFA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh30 NVy4cYdKeUiWUzDhd5NigQ>? M2TaWJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCUaEOwJINmdGy| NU[2OnNxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
MG 63 (6-TG R) M2jNXpFJXFNiYYPzZZk> M2DuOpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJG1IKDZ|IDi2MXRIKFJrIHPlcIx{ NWPlWnFLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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LAN-5 MkTBdWhVWyCjc4PhfS=> Mm[wdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEyDTj21JINmdGy| NV;wbYx5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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insect NG\pbXlHfW6ldHnvckBie3OjeR?= M3vtPGlvcGmkaYTpc44hd2ZicnXjc41jcW6jboSgbJVu[W5iSHnzMZRi\2enZDDwPFVidHCqYT;wNVEx[WyyaHGgSVU1PUtibYX0ZY51KGW6cILld5Nm\CCrbjDpcpNm[3RiY3XscJMtKEmFNUCgQUAxNjBzMTFOwG0v NEHqeok9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MECzOFYxPyd-M{CwN|Q3ODd:L3G+
insect NEO5XJBHfW6ldHnvckBie3OjeR?= M{DSe2lvcGmkaYTpc44hd2ZicnXjc41jcW6jboSgbJVu[W5iSHnzMZRi\2enZDDwPFVidHCqYT;wNVEx[WyyaHGgSVU1OktibYX0ZY51KGW6cILld5Nm\CCrbjDpcpNm[3RiY3XscJMtKEmFNUCgQUAxNjB{OTFOwG0v M2jVSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMEO0OlA4Lz5|MECzOFYxPzxxYU6=
Sf21 NV31d4VUTnWwY4Tpc44h[XO|YYm= NFToU3oyKGi{ MljETY5pcWKrdHnvckBw\iC{ZXPvcYJqdmGwdDDoeY1idiCodXzsMYxmdme2aDDOMZRmem2rbnHsJGhqezZvdHHn[4VlKHBzMUDk[Yx1[S:{ZXPvcYJqdmGwdDDoeY1idiCodXzsJIxmdme2aDDwPFVidHCqYTDlfJBz\XO|ZXSgbY4h[mGldXzveolzfXNiaX7m[YN1\WRiU3[yNUBqdnOnY4SgZ4VtdHNidYPpcochWEmSMjDhd{B{fWK|dILheIUhdWWjc4Xy[YQh[W[2ZYKgNUBpeiCkeTDBcIV5[TZ|MzDUdoFk\XJvYnHz[YQh\my3b4Lld4NmdmOnIIDvcIFzNCCLQ{WwJF0hOC5zMkWg{txONg>? M1y0UlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMEO0OlA4Lz5|MECzOFYxPzxxYU6=
MCF7 MnToRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MUK3NkBpenN? NVfQXmg4SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIhiemKxcnnu[{BRUUt|Q1GgSVU1PUtibYX0ZY51KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUAxNjJyNjFOwG0v NXzRV5lCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwN|Q3ODdpPkOwNFM1PjB5PD;hQi=>
Sf21 MX7GeY5kfGmxbjDhd5NigQ>? MX:xJIhz MnnoTY5pcWKrdHnvckBw\iC{ZXPvcYJqdmGwdDDoeY1idiCodXzsMYxmdme2aDDOMZRmem2rbnHsJGhqezZvdHHn[4VlKHBzMUDi[ZRiN3KnY3;tZolv[W62IHj1cYFvKG[3bHygcIVv\3SqIIC4OYFteGijIHX4dJJme3OnZDDpckBj[WO3bH;2bZJ2eyCrbn\lZ5Rm\CCVZkKxJIlve2WldDDj[YxteyC3c3nu[{BRUVB{IHHzJJN2[nO2cnH0[UBu\WG|dYLl[EBi\nSncjCxJIhzKGK7IFHs[ZhiPjN|IGTyZYNmei2kYYPl[EBndHWxcnXzZ4Vv[2VicH;sZZJqNCCLQ{WwJF0hOC5{M{Sg{txONg>? NV;lO5E{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwN|Q3ODdpPkOwNFM1PjB5PD;hQi=>
T47D MmPFRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NHfiVYo4OiCqcoO= MU\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFR2N1SgZ4VtdHNiaHHyZo9zcW6pIGDJN2tESSCKMUC0O3IhdXW2YX70JIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTBiPTCwMlI5PiEQvF2u Mo\5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByM{S2NFcoRjNyMEO0OlA4RC:jPh?=
PC3 MoTkSpVv[3Srb36gZZN{[Xl? Mk\wNkBpenN? M1nBZ2lvcGmkaYTpc44hd2ZiUFmzT{BqdiCqdX3hckBRSzNiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJGFMXCCyaH;zdIhwenmuYYTpc44h[XRiU3XyOFc{KG2nYYP1doVlKGGodHXyJFIhcHK|IHL5JIZtfW:{ZYPj[Y5k\SCjc4PhfUwhUUN3MDC9JFAvOzZ3IN88UU4> NV3UWXBYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwN|Q3ODdpPkOwNFM1PjB5PD;hQi=>
HT-29 NH\Dd25E\WyuIHP5Z4xmKGG|c3H5 NGi1cocxNjFzMTD0c{A{KHWP MWWyOEBpenN? MVnD[YxtKGO7Y3zlJIFzemW|dDDpckBpfW2jbjDIWE0zQSClZXzsd{Bie3Onc4Pl[EBieyCjY3P1cZVt[XSrb36gZZQhTzJxTTDwbIF{\SCjdDCwMlEyOSC2bzCzJJVOKGGodHXyJFI1KGi{czDifUBxem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nJIJie2WmIH\sc5ch[3m2b33leJJ6 NI\PbJA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MECzOFYxPyd-M{CwN|Q3ODd:L3G+
A2058 MnT2SpVv[3Srb36gZZN{[Xl? NXzkfGt2OSCqch?= NX7iTGxHUW6qaXLpeIlwdiCxZjDUU3JEOiCrbjDoeY1idiCDMkC1PEBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCSS1KvRYt1KHCqb4PwbI9zgWyjdHnvckBifCCVZYK0O|Mh[W[2ZYKgNUBpeiCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZMtKEmFNUCgQUAxNjRzNjFOwG0v M2q1SFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{W5NFA{Lz5|MEO1PVAxOzxxYU6=
A2058 NWTVeot6TnWwY4Tpc44h[XO|YYm= M2TPe|EhcHJ? MVPJcohq[mm2aX;uJI9nKFSRUlOxJIlvKGi3bXHuJGEzODV6IHPlcIx{KGG|c3Xzd4VlKGG|IHTlZ5Jm[XOnIHnuJHM3KHCqb4PwbI9zgWyjdHnvckBifCCVZYKyN|UwOjN4IHHmeIVzKDFiaIKgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m|LDDJR|UxKD1iMD61OVMh|ryPLh?= Mk\XQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB|NUmwNFMoRjNyM{W5NFA{RC:jPh?=

... 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]
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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 C1COCCN1C2=NC(=NC(=C2)C3=CN=C(C=C3C(F)(F)F)N)N4CCOCC4

In vivo Formulation Calculator (Clear solution)

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

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

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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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

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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

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PI3K Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID