Buparlisib (BKM120)

For research use only.

Catalog No.S2247 Synonyms: NVP-BKM120

202 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 202 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 NXu2fmJ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3XiNVczcA>? M4TtcWlEPTB;MT2y{txO MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjB4NUC4NEc,OjJyNkWwPFA9N2F-
U87 MmXGRZBweHSxc3nzJGF{e2G7 MUmy{txO Ml;VO|Jp M{TVWIlv\HWlZYOgZ4VtdCCjcH;weI9{cXNiYX7kJINt\WG4ZXSgVGFTWCCjbnSgZ4F{eGG|ZT2z NGfU[Ys9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkC2OVA5OCd-MkKwOlUxQDB:L3G+
SNU-601 Mon5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVe3Nog> MkLuSG1UVw>? MYDJR|UxRTBwOEG2xtExNjB4M988US=> M1PsO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MUW5PFE1Lz5{MkG1PVgyPDxxYU6=
SNU-1 MoHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTEdmdSPzKq MYnEUXNQ NHT1WoNKSzVyPUGuNFgzyrFyLkCyPO69VQ>? MlvoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNUm4NVQoRjJ{MUW5PFE1RC:jPh?=
SNU-668 Mn3sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPMOZdyPzKq NHjqe3pFVVOR MlezTWM2OD1zLkW3PeKyOC5yN{VOwG0> MmnlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNUm4NVQoRjJ{MUW5PFE1RC:jPh?=
AGS MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1uwdFczcA>? M3yzW2ROW09? MkT3TWM2OD1zLkexOOKyOC5zMUhOwG0> MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjF3OUixOEc,OjJzNUm4NVQ9N2F-
SNU-216 NYrBOYxFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFvaXFM4Omh? MXTEUXNQ M4HJT2lEPTB;Mj62PVLDuTBwMEiy{txO MkPZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNUm4NVQoRjJ{MUW5PFE1RC:jPh?=
SNU-5 NHTaVFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXmxW5ZkPzKq M{DxT2ROW09? M3vWPGlEPTB;MT6zOVHDuTBwMEmx{txO NH3CTpA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG1PVgyPCd-MkKxOVk5OTR:L3G+
SNU-638 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnlW2I4Omh? M4O5O2ROW09? MX\JR|UxRTJwMkiyxtExNjB3M988US=> MoPtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNUm4NVQoRjJ{MUW5PFE1RC:jPh?=
SNU-16 MlnXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXq3Nog> NELndI1FVVOR MkHrTWM2OD1zLkW3N:KyOC5yMEJOwG0> NVLo[od2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKxOVk5OTRpPkKyNVU6QDF2PD;hQi=>
SNU-484 M2PWU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\pblczcA>? MnfrSG1UVw>? NGnmSW1KSzVyPUGuO|I5yrFyLkC0Oe69VQ>? M3zKSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MUW5PFE1Lz5{MkG1PVgyPDxxYU6=
SNU-620 NWfJRpU6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV23Nog> M3HqPGROW09? NGTZR|JKSzVyPUKuPVM6yrFyLkCwNe69VQ>? NHWyOmo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG1PVgyPCd-MkKxOVk5OTR:L3G+
SNU-719 NFvPPINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{f1S|czcA>? MkfNSG1UVw>? M2TmSWlEPTB;Mz6wN|fDuTBwMEOy{txO NFrEd2I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG1PVgyPCd-MkKxOVk5OTR:L3G+
MM cell lines NXvpcI5OT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTDSZYyOM7:TR?= M37IelI1cA>? M1\sdmROW09? MlHITWM2OCC4YYLp[ZMh[W2xbneg[Iln\mW{ZX70JINmdGxibHnu[ZMhcW5idHnt[UBidmRiZH;z[UBl\XCnbnTlcoNm NFrPWYI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkKwO|Q5PSd-MkKyNFc1QDV:L3G+
ARP-1 NFLNUJFCeG:ydH;zbZMhSXO|YYm= NHGwVoMyOM7:TR?= NIH6VWozPGh? MkLUSG1UVw>? M1X1Volv\HWlZYOgUW0h[2WubDDhdI9xfG:|aYOgeIhzd3WpaDDjZZNx[XOnIHHjeIl3[XSrb36= NHHvWZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkKwO|Q5PSd-MkKyNFc1QDV:L3G+
colon cancer cell lines M3:5UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXuNYtyOC1zMN88US=> NH;NeFY4Omh? M3rLdmROW09? MYfJR|UxRTIQvF2= NHv5SWM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkW0N|g2Pyd-MkK1OFM5PTd:L3G+
gastric cancer cell lines M{HT[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TVdVAuOTEQvF2= MoXwO|Jp NE\YOnJFVVOR NY[wPVV7UUN3ME2yMVXPxE1? MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjV2M{i1O{c,OjJ3NEO4OVc9N2F-
HCT-116/HT-29/MKN-45 NYLDO2hESXCxcITvd4l{KEG|c3H5 MlXDNu69VQ>? M4DTdFQ5cA>? Morrd4hq\nRiaX6gS|IheGijc3W= NFPxN|Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkW0N|g2Pyd-MkK1OFM5PTd:L3G+
HT-29 and HCT-116 NX6y[lZpS2G|cHHz[UBie3OjeR?= MoX4Oe69VQ>? MlPLNlRp M2XoSolv\HWlZYOgZ4F{eGG|ZTDhZ5Rqfmm2eR?= M{D1RlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NUSzPFU4Lz5{MkW0N|g2PzxxYU6=
PIK3CA-mutant MCF7 Mnn2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PmT2dKPTB;MU[wxtE6OW6P78{MUGQ2OD17OEFCtVI4O26P MXi3Nog> MmHoS2k2OD1zNkFCtVkydk4xvJzMSFUxRTl6MNMxNlc{dk1? NUHxU3E2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2OVM6PjdpPkKyOlU{QTZ5PD;hQi=>
PIK3CA-mutant MCF7 MlTpT4lv[XOnIFHzd4F6 NV7jNIpYUUN3ME2xNVTDuTOwTR?= NWjJTZJJPzKq MUTJR|UxRTFzNNMxN45OKGmwIILl[JVkcW6pIFHreEBxcG:|cHjvdplt[XSrb36gcIV3\Wy| M4TNXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkWzPVY4Lz5{Mk[1N|k3PzxxYU6=
MCF7-myr-Akt M3LwUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXWwcVU1T0l3ME2yPVnDuTZ6bl5vwKxNTDVy78{eNVAtODBybl2= MXq3Nog> NGfiOZpIUTVyPUK5PeKyPjiwTf-8kGxFPTExvK6xNEwxODCwTR?= MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ3M{m2O{c,OjJ4NUO5Olc9N2F-
Y1 cell line NY\t[YxST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHoNE4y|ryPL{JOwG0> MXyyOIg> M3TwZWROW09? NILQc4xqdmirYnn0d{A3OO,:hTDj[YxtKH[rYXLpcIl1gSCrbjDNfYMuW2O2cj30doFve2[nY4Tl[EBk\Wyucx?= MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ7MkmwOEc,OjJ4OUK5NFQ9N2F-
human NSCLC M3P4fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWSwMlUuOs7:TR?= MmLDO|Jp NXvUbJdiUUN3ME2x{txO M2P3UlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{N{ixN|k{Lz5{Mke4NVM6OzxxYU6=
human NSCLC M1;2WWtqdmG|ZTDBd5NigQ>? MmGxNe69VQ>? NVfGd4tEOjSq M3HR[IlvcGmkaYTzJJRp\SCDa4SvcXRQWiC|aXfuZYxqdmdicHH0bJdigSCjdDCzbEBi\nSncjD0doVifG2nboS= MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjd6MUO5N{c,OjJ5OEGzPVM9N2F-
JVM2 NHL4[oJEgXSxdH;4bYNqfHliYYPzZZk> M2\rSFAvOi1{MN88US=> MWK3Nog> NIfSc5VFVVOR NX:0R5Z2UUN3ME2wMlnPxE1? NW\tVm82RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyN|g3OzlpPkKzNlM5PjN7PD;hQi=>
EHEB M3LMU2N6fG:2b4jpZ4l1gSCjc4PhfS=> MmL6NE4zNTJyzszN MUS3Nog> NILNVpNFVVOR NGDCOohKSzVyPUCuO:69VQ>? NEnueJM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{KzPFY{QSd-MkOyN|g3Ozl:L3G+
MEC2 M4XqOWN6fG:2b4jpZ4l1gSCjc4PhfS=> M2PwNlAvOi1{MN88US=> M3H6OVczcA>? MVLEUXNQ NYjMN4lQUUN3ME2wMlfPxE1? NEThZpM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{KzPFY{QSd-MkOyN|g3Ozl:L3G+
primary B-CLL lymphocytes NIjUcI1CeG:ydH;zbZMhSXO|YYm= M2fRV2lEPTBiZn;yJIVi[2hicILpcYFzgSClZXzsJIxqdmV? MVKyOIg> MlrPSG1UVw>? MYrJR|Ux97zeM988UUBnd3JiYXzsJJBifGmnboTz M4j5eFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MkO4OlM6Lz5{M{KzPFY{QTxxYU6=
primary B-CLL lymphocytes NXLCfpZuU2mwYYPlJGF{e2G7 Mo\NTWM2OCCob4Kg[YFkcCCycnntZZJ6KGOnbHygcIlv\Q>? MXSyOIg> NYXMVnlRcW6qaXLpeJMheDdyU{\LJEYhPEVvQmCxJIV5eHKnc4Ppc44> NF;qUJo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{KzPFY{QSd-MkOyN|g3Ozl:L3G+
SK-HEP1 M2Pu[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnuPGROOS1{MN88US=> NUPGTXVnPzKq MoewSG1UVw>? M{W1TmlEPTExvKyx{txO NY\aOoV2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0O|kyOzZpPkKzOFc6OTN4PD;hQi=>
786-0 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn71NU0zOM7:TR?= NYX5VXNuPzKq M1mzOmROW09? NHHHXWJKSzVy78{cNe69VQ>? NX7DZ4FMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0O|kyOzZpPkKzOFc6OTN4PD;hQi=>
human HCC cell lines MnjrR4VtdCC4aXHibYxqfHliYYPzZZk> M2rYfFAvODB3LUJOwG0> M1;Q[VQ5cA>? MlH6TWM2OD1zzszN MkTRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2OEm5PVkoRjJ|NEi5PVk6RC:jPh?=
Huh7 MYXLbY5ie2ViQYPzZZk> NWTHeZJ3Oc7:TR?= MWK0PIg> MkPvd4lodmoxrJHjZY51dHlicnXkeYNmeyCyaH;zdIhwenmuYYTpc44hd2ZiQXv0 NFLEb|k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S4PVk6QSd-MkO0PFk6QTl:L3G+
human NSCLC cell lines NHHiO21CeG:ydH;zbZMhSXO|YYm= MVGwMlEzPS12zszN MnvsNlRp NE\GfJlFVVOR NEfWT2JKSzVyczDyZY5o\XNiZoLvcUAxNjRvMt88US=> MmXBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3NkK0O|IoRjJ|NU[yOFczRC:jPh?=
Primary CLL cells NYHOTlRDSXCxcITvd4l{KEG|c3H5 MYmxMVEx|ryP M1PFOVQ5cA>? M2TSdIlv\HWlZYOgZZBweHSxc3nzJIlvKEOOTDDj[YxteyCrbnTldIVv\GWwdDDv[kBxem:pbn;zeIlkKG2jcnvldpM> NGnlOGw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i1NFgxPyd-MkO4OVA5ODd:L3G+
Primary CLL cells MXHLbY5ie2ViQYPzZZk> MlPPNu69VQ>? NGT1NVA{OG2rbh?= MUTk[YNz\WG|ZXSgVGk{UyCjY4Tpeol1gQ>? M3TNO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OEWwPFA4Lz5{M{i1NFgxPzxxYU6=
Primary CLL cells NEfWTGZEgXSxdH;4bYMhSXO|YYm= M4LHbVLPxE1? MWqyOIg> MWTpcoR2[2W|IHPlcIwh[3m2b4TvfIlkcXS7 NUHCT2hrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OVA5ODdpPkKzPFUxQDB5PD;hQi=>
LC-1/SQSF MmfQSpVv[3Srb36gRZN{[Xl? NUD1c5FEO87:TR?= MX6yOIg> MXfEUXNQ NUKycGlP\GWlcnXhd4UhVlKIMjDwdo91\WmwIHzleoVt MoH5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7OECwPVMoRjJ|OUiwNFk{RC:jPh?=
BCR-ABL MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LDfVAvOjVvMUFOwG0> MknCOIQ> NYXwb|hre2mpbnnmbYNidnSueTDpcohq[mm2IHPlcIwheHKxbHnm[ZJifGmxbh?= MmPGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR{NES2NVIoRjJ2MkS0OlEzRC:jPh?=
T-ALL NF7pVXpCeG:ydH;zbZMhSXO|YYm= NGq2TYxj\XS5ZXXuJFEvPCCjbnSgOU4{KG2PIHH0JFI1cCCjbnSgNE46KGGwZDC1MlUhdU1iYYSgOFhpKGmwIHTp[oZmemWwdDDj[YxtKGyrbnW= NHnC[4wzPCCxcjC0PIg> MYfEUXNQ Ml2zZYZn\WO2czD0bIUhWEl|SzDwZZRpf2G7IHnuJHQuSUyOIHPlcIwhdGmwZYO= MmfSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|MUC3N|YoRjJ2M{GwO|M3RC:jPh?=
H1975 M3XNS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jPV|AvOy17LkdOwG0> M1Gz[VczcA>? M1XIS2ROW09? MmXuTWM2OD1zLkO4Oe69VQ>? MlzFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|M{e4OFYoRjJ2M{O3PFQ3RC:jPh?=
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TC32 MXzxTHRUKGG|c3H5 M2KyZ5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCWQ{OyJINmdGy| NHL2T5Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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BT-12 MljSdWhVWyCjc4PhfS=> MkXsdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUGyJINmdGy| MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
MG 63 (6-TG R) NVLVfGZweUiWUzDhd5NigQ>? NHHiWYFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTVegOlMhMDZvVFegVkkh[2WubIO= NYTReYZGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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OHS-50 NG[xPFRyUFSVIHHzd4F6 MWHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhV0iVLUWwJINmdGy| MnfsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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insect MUDGeY5kfGmxbjDhd5NigQ>? M{\LR2lvcGmkaYTpc44hd2ZicnXjc41jcW6jboSgbJVu[W5iSHnzMZRi\2enZDDwPFVidHCqYT;wNVEx[WyyaHGgSVU1PUtibYX0ZY51KGW6cILld5Nm\CCrbjDpcpNm[3RiY3XscJMtKEmFNUCgQUAxNjBzMTFOwG0v NGfQWHc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MECzOFYxPyd-M{CwN|Q3ODd:L3G+
insect NHLBPHhHfW6ldHnvckBie3OjeR?= MoO1TY5pcWKrdHnvckBw\iC{ZXPvcYJqdmGwdDDoeY1idiCKaYOteIFo\2WmIIC4OYFteGijL4CxNVBidHCqYTDFOVQzUyCvdYThcpQh\XiycnXzd4VlKGmwIHnud4VkfCClZXzsd{whUUN3MDC9JFAvODJ7IN88UU4> MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODB|NE[wO{c,OzByM{S2NFc9N2F-
Sf21 NXvkU3JDTnWwY4Tpc44h[XO|YYm= MmjHNUBpeg>? NWrOU2w2UW6qaXLpeIlwdiCxZjDy[YNwdWKrbnHueEBpfW2jbjDmeYxtNWynbnf0bEBPNXSncn3pcoFtKEirc{[teIFo\2WmIICxNVBl\Wy2YT;y[YNwdWKrbnHueEBpfW2jbjDmeYxtKGynbnf0bEBxQDWjbIDoZUBmgHC{ZYPz[YQhcW5iYnHjeYxwfmm{dYOgbY5n\WO2ZXSgV4YzOSCrboPlZ5Qh[2WubIOgeZNqdmdiUFnQNkBieyC|dXLzeJJifGVibXXhd5Vz\WRiYX\0[ZIhOSCqcjDifUBCdGW6YU[zN{BVemGlZYKtZoF{\WRiZnz1c5Jme2OnbnPlJJBwdGG{LDDJR|UxKD1iMD6xNlUh|ryPLh?= MkfkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByM{S2NFcoRjNyMEO0OlA4RC:jPh?=
MCF7 MXfBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NX7HW|FZPzJiaILz M2\kW2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDoZZJjd3KrbnegVGlMO0ODIFW1OFVMKG23dHHueEBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gNE4zODZizszNMi=> NIr4cWQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MECzOFYxPyd-M{CwN|Q3ODd:L3G+
Sf21 Mlq0SpVv[3Srb36gZZN{[Xl? MVixJIhz MnH6TY5pcWKrdHnvckBw\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>? NXy4WpFXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwN|Q3ODdpPkOwNFM1PjB5PD;hQi=>
T47D M4[5WWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 M{DWSlczKGi{cx?= Mn3uRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCWNEfEJINmdGy|IHjhdoJwemmwZzDQTVNMS0FiSEGwOFdTKG23dHHueEBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gNE4zQDZizszNMi=> M4W1SFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMEO0OlA4Lz5|MECzOFYxPzxxYU6=
PC3 NFq0PFRHfW6ldHnvckBie3OjeR?= NGLqeFczKGi{cx?= MX;Jcohq[mm2aX;uJI9nKFCLM1ugbY4hcHWvYX6gVGM{KGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDBT3QheGixc4Doc5J6dGG2aX;uJIF1KFOnckS3N{Bu\WG|dYLl[EBi\nSncjCyJIhzeyCkeTDmcJVwemW|Y3XuZ4Uh[XO|YYmsJGlEPTBiPTCwMlM3PSEQvF2u MoLlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByM{S2NFcoRjNyMEO0OlA4RC:jPh?=
HT-29 MmTOR4VtdCCleXPs[UBie3OjeR?= MkLONE4yOTFidH:gN{B2VQ>? NWrqVpFWOjRiaILz NH:wbVFE\WyuIHP5Z4xmKGG{cnXzeEBqdiCqdX3hckBJXC1{OTDj[YxteyCjc4Pld5Nm\CCjczDhZ4N2dXWuYYTpc44h[XRiR{KvUUBxcGG|ZTDheEAxNjFzMTD0c{A{KHWPIHHmeIVzKDJ2IHjyd{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oKGKjc3XkJIZtd3diY4n0c41mfHK7 NYnNUWpURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwN|Q3ODdpPkOwNFM1PjB5PD;hQi=>
A2058 MnHaSpVv[3Srb36gZZN{[Xl? NGmzSWsyKGi{ M3fhXGlvcGmkaYTpc44hd2ZiVF;SR|IhcW5iaIXtZY4hSTJyNUigZ4VtdHNiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4hWEuEL1HreEBxcG:|cHjvdplt[XSrb36gZZQhW2W{NEezJIFnfGW{IEGgbJIh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nzMEBKSzVyIE2gNE41OTZizszNMi=> Mmf6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB|NUmwNFMoRjNyM{W5NFA{RC:jPh?=
A2058 NWnUZYlETnWwY4Tpc44h[XO|YYm= Ml\1NUBpeg>? M3zLTmlvcGmkaYTpc44hd2ZiVF;SR|EhcW5iaIXtZY4hSTJyNUigZ4VtdHNiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4hWzZicHjvd5Bpd3K7bHH0bY9vKGG2IGPldlI{PS9{M{[gZYZ1\XJiMTDodkBjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYOsJGlEPTBiPTCwMlU2OyEQvF2u NIHuWnM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEO1PVAxOyd-M{CzOVkxODN:L3G+

... 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

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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