Home PI3K/Akt/mTOR PI3K inhibitor - Apoptosis related activator Buparlisib (BKM120)

Buparlisib (BKM120)

Catalog No.S2247 Synonyms: NVP-BKM120

For research use only.

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.

Buparlisib (BKM120) Chemical Structure

CAS No. 944396-07-0

Selleck's Buparlisib (BKM120) has been cited by 230 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)		 Click to View More Targets
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 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfWOnlTPzKq NEnneHlKSzVyPUGtNu69VQ>? MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjB4NUC4NEc,OjJyNkWwPFA9N2F-
U87 NYLPW2FxSXCxcITvd4l{KEG|c3H5 M{L3ZVLPxE1? NXzYdph4PzKq NYe1VmticW6mdXPld{Bk\WyuIHHwc5B1d3OrczDhcoQh[2ynYY\l[EBRSVKSIHHu[EBk[XOyYYPlMVM> M3vmSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{ME[1NFgxLz5{MkC2OVA5ODxxYU6=
SNU-601 M4jhVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYe3Nog> NHK1cotFVVOR MmL0TWM2OD1yLkixOuKyOC5yNkROwG0> NFPsWlU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG1PVgyPCd-MkKxOVk5OTR:L3G+
SNU-1 M1yyfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXkTWZDPzKq NGDBfphFVVOR MlzyTWM2OD1zLkC4NuKyOC5yMklOwG0> NXnkdFdMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKxOVk5OTRpPkKyNVU6QDF2PD;hQi=>
SNU-668 M3jtVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHRO|Jp Mkm4SG1UVw>? MYHJR|UxRTFwNUe5xtExNjB5NN88US=> MmiyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNUm4NVQoRjJ{MUW5PFE1RC:jPh?=
AGS Moi5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDydlM4Omh? NWHC[28{TE2VTx?= Mnn2TWM2OD1zLkexOOKyOC5zMUhOwG0> NIPPV|E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG1PVgyPCd-MkKxOVk5OTR:L3G+
SNU-216 NUfHdYdZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrSVJM4Omh? M2PGOGROW09? NFzYRldKSzVyPUKuOlkzyrFyLkC4Nu69VQ>? NHO3OJo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG1PVgyPCd-MkKxOVk5OTR:L3G+
SNU-5 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHMO|Jp NFXPNJVFVVOR M3rpXmlEPTB;MT6zOVHDuTBwMEmx{txO M4PmWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MUW5PFE1Lz5{MkG1PVgyPDxxYU6=
SNU-638 M1W1R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXFO|Jp MWPEUXNQ M2ftOWlEPTB;Mj6yPFLDuTBwMEWz{txO Ml\rQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNUm4NVQoRjJ{MUW5PFE1RC:jPh?=
SNU-16 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLEO|Jp M{[5bWROW09? NV;BfVVOUUN3ME2xMlU4O8LzMD6wNFHPxE1? MoTRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNUm4NVQoRjJ{MUW5PFE1RC:jPh?=
SNU-484 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jPclczcA>? Moi1SG1UVw>? MXfJR|UxRTFwN{K4xtExNjB2Nd88US=> Ml;OQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNUm4NVQoRjJ{MUW5PFE1RC:jPh?=
SNU-620 NEjkU45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE[3NlE4Omh? NWjlb25DTE2VTx?= M2fqdmlEPTB;Mj65N|nDuTBwMECx{txO NGPxWVQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG1PVgyPCd-MkKxOVk5OTR:L3G+
SNU-719 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLEWGNKPzKq M1e2VWROW09? M1;hW2lEPTB;Mz6wN|fDuTBwMEOy{txO MoS5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNUm4NVQoRjJ{MUW5PFE1RC:jPh?=
MM cell lines M1j4ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWmxNO69VQ>? MUOyOIg> Mny2SG1UVw>? MWLJR|UxKH[jcnnld{BidW:wZzDkbYZn\XKnboSgZ4VtdCCuaX7ld{BqdiC2aX3lJIFv\CCmb4PlJIRmeGWwZHXuZ4U> NI[zUJc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkKwO|Q5PSd-MkKyNFc1QDV:L3G+
ARP-1 NUfoZ3R[SXCxcITvd4l{KEG|c3H5 Mm\LNVDPxE1? MoXYNlRp NHHWXFdFVVOR NVTObJZicW6mdXPld{BOVSClZXzsJIFxd3C2b4Ppd{B1cHKxdXfoJINie3Cjc3WgZYN1cX[jdHnvci=> MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJyN{S4OUc,OjJ{MEe0PFU9N2F-
colon cancer cell lines NGn6cYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnr5NE0yOM7:TR?= NH71eWw4Omh? NVnvWZlUTE2VTx?= MmTtTWM2OD1zzszN MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjV2M{i1O{c,OjJ3NEO4OVc9N2F-
gastric cancer cell lines NEP2coNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3FVlAxNTFyzszN MYi3Nog> MnjhSG1UVw>? NHPQ[XlKSzVyPUKtOe69VQ>? NV\YTItxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK1OFM5PTdpPkKyOVQ{QDV5PD;hQi=>
HCT-116/HT-29/MKN-45 Mln0RZBweHSxc3nzJGF{e2G7 M1PLSFLPxE1? MnrrOFhp M1LBT5NpcW[2IHnuJGczKHCqYYPl M{\HZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NUSzPFU4Lz5{MkW0N|g2PzxxYU6=
HT-29 and HCT-116 NF\1V5NE[XOyYYPlJIF{e2G7 MkO2Oe69VQ>? MmnrNlRp M3[xUYlv\HWlZYOgZ4F{eGG|ZTDhZ5Rqfmm2eR?= MoXmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ3NEO4OVcoRjJ{NUSzPFU4RC:jPh?=
PIK3CA-mutant MCF7 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLpS2k2OD1zNkFCtVkydk4xvJzMSFUxRTl6MNMxNlc{dk1? M4LmRVczcA>? MUTHTVUxRTF4MNMxPVFvVe,:jFzEOVA:QThywsGyO|NvVQ>? M3npNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkWzPVY4Lz5{Mk[1N|k3PzxxYU6=
PIK3CA-mutant MCF7 MlzMT4lv[XOnIFHzd4F6 NEDDWFlKSzVyPUGxOOKyO26P MoLJO|Jp MmnLTWM2OD1zMUVCtVNvVSCrbjDy[YR2[2mwZzDBb5QheGixc4Doc5J6dGG2aX;uJIxmfmWucx?= Mli3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4NUO5OlcoRjJ{NkWzPVY4RC:jPh?=
MCF7-myr-Akt Mn\QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXrS2k2OD1{OUpCtVY5dk4xvJzMSFUx97zgMUCsNFAxdk1? M{nUelczcA>? M2HXb2dKPTB;Mkm5xtE3QG6P78{MUGQ2OO,:nkGwMFAxOG6P MoDYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4NUO5OlcoRjJ{NkWzPVY4RC:jPh?=
Y1 cell line MorTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX6wMlHPxE1xMd88US=> MWmyOIg> MoTZSG1UVw>? NUnteVRycW6qaXLpeJMhPjExvJWgZ4VtdCC4aXHibYxqfHliaX6gUZlkNVOldIKteJJidnOoZXP0[YQh[2WubIO= NYHnTYNtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2PVI6ODRpPkKyOlkzQTB2PD;hQi=>
human NSCLC M2G5fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYq3UHVGOC53LUNOwG0> NWrTOGtuPzKq MoDRTWM2OD1zzszN MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjd6MUO5N{c,OjJ5OEGzPVM9N2F-
human NSCLC NGDPRZhMcW6jc3WgRZN{[Xl? NVvU[|ZQOc7:TR?= M3u2V|I1cA>? MofhbY5pcWKrdIOgeIhmKEGtdD;tWG9TKHOrZ37hcIlv\yCyYYToe4F6KGG2IEPoJIFnfGW{IITy[YF1dWWwdB?= MmXUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ5OEGzPVMoRjJ{N{ixN|k{RC:jPh?=
JVM2 M{DOd2N6fG:2b4jpZ4l1gSCjc4PhfS=> Ml3GNE4zNTJyzszN M1LWTVczcA>? NYPrTIxNTE2VTx?= MoHUTWM2OD1yLkpOwG0> M{HoVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MkO4OlM6Lz5{M{KzPFY{QTxxYU6=
EHEB NYDLTmt1S3m2b4TvfIlkcXS7IHHzd4F6 M3vjc|AvOi1{MN88US=> M4\VR|czcA>? MmPKSG1UVw>? MXzJR|UxRTBwN988US=> MojIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN{M{i2N|koRjJ|MkO4OlM6RC:jPh?=
MEC2 NH\pWJFEgXSxdH;4bYNqfHliYYPzZZk> NUj6Z25VOC5{LUKw{txO MUG3Nog> NEDPZoRFVVOR NF3zW2FKSzVyPUCuO:69VQ>? MkX1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN{M{i2N|koRjJ|MkO4OlM6RC:jPh?=
primary B-CLL lymphocytes NGW1fXZCeG:ydH;zbZMhSXO|YYm= M3TIZWlEPTBiZn;yJIVi[2hicILpcYFzgSClZXzsJIxqdmV? NFHhb44zPGh? M2nmUWROW09? MXHJR|Ux97zeM988UUBnd3JiYXzsJJBifGmnboTz MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzJ|OE[zPUc,OjN{M{i2N|k9N2F-
primary B-CLL lymphocytes NYrwdHFpU2mwYYPlJGF{e2G7 NYixNYVFUUN3MDDmc5Ih\WGlaDDwdolu[XK7IHPlcIwhdGmwZR?= M3izU|I1cA>? Mo\XbY5pcWKrdIOgdFcxWz[NID[gOGUuSlBzIHX4dJJme3Orb36= NUnvZmJCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyN|g3OzlpPkKzNlM5PjN7PD;hQi=>
SK-HEP1 NU[xUG1GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPRNVIyNTJyzszN MnPYO|Jp MUjEUXNQ MUjJR|Ux97zeMd88US=> MnTFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2N{mxN|YoRjJ|NEe5NVM3RC:jPh?=
786-0 M1SzOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3Fd4RzOS1{MN88US=> NFXRXYc4Omh? NYfJPGF[TE2VTx?= NIm5fohKSzVy78{cNe69VQ>? M3LnWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NEe5NVM3Lz5{M{S3PVE{PjxxYU6=
human HCC cell lines NFnKOWFE\WyuII\pZYJqdGm2eTDhd5NigQ>? MXOwMlAxPS1zzszN NHyxW2I1QGh? NVyzeYh{UUN3ME2x{txO M2G2[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NEi5PVk6Lz5{M{S4PVk6QTxxYU6=
Huh7 MX;LbY5ie2ViQYPzZZk> MmfuNe69VQ>? NHTUXlI1QGh? Mn25d4lodmoxrJHjZY51dHlicnXkeYNmeyCyaH;zdIhwenmuYYTpc44hd2ZiQXv0 MkTDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2OEm5PVkoRjJ|NEi5PVk6RC:jPh?=
human NSCLC cell lines NUHE[WRPSXCxcITvd4l{KEG|c3H5 M3;jbFAvOTJ3LUVOwG0> NH;LfG8zPGh? NILNVW5FVVOR MV\JR|UxeyC{YX7n[ZMh\nKxbTCwMlQuOs7:TR?= M2LLT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NU[yOFczLz5{M{W2NlQ4OjxxYU6=
Primary CLL cells MlnXRZBweHSxc3nzJGF{e2G7 MY[xMVEx|ryP NYHWO3RyPDiq NXTFPWltcW6mdXPld{BieG:ydH;zbZMhcW5iQ1zMJINmdGy|IHnu[IVx\W6mZX70JI9nKHC{b3fuc5N1cWNibXHyb4Vzew>? NVzaWlg{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OVA5ODdpPkKzPFUxQDB5PD;hQi=>
Primary CLL cells MmTKT4lv[XOnIFHzd4F6 Mn7rNu69VQ>? MYSzNI1qdg>? MkDO[IVkemWjc3XkJHBKO0tiYXP0bZZqfHl? NHTzN489[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i1NFgxPyd-MkO4OVA5ODd:L3G+
Primary CLL cells NYLjZpRyS3m2b4TvfIlkKEG|c3H5 NIn0UZAz|ryP Mnr0NlRp MYnpcoR2[2W|IHPlcIwh[3m2b4TvfIlkcXS7 NHrFcpo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i1NFgxPyd-MkO4OVA5ODd:L3G+
LC-1/SQSF MljISpVv[3Srb36gRZN{[Xl? MnnwN:69VQ>? NGHuUG8zPGh? NXzRWIY6TE2VTx?= M33UV4Rm[3KnYYPlJG5TTjJicILveIVqdiCuZY\lcC=> MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl6MEC5N{c,OjN7OECwPVM9N2F-
BCR-ABL M3S0UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vpelAvOjVvMUFOwG0> NXjZeol6PGR? NF;Gd3F{cWewaX\pZ4FvfGy7IHnubIljcXRiY3XscEBxem:uaX\ldoF1cW:w NYf6RYNsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyOFQ3OTJpPkK0NlQ1PjF{PD;hQi=>
T-ALL MoPTRZBweHSxc3nzJGF{e2G7 M4rpWYJmfHenZX6gNU41KGGwZDC1MlMhdU1iYYSgNlRpKGGwZDCwMlkh[W6mIEWuOUBuVSCjdDC0PIghcW5iZHnm[oVz\W62IHPlcIwhdGmwZR?= MVqyOEBweiB2OHi= NEDCVJVFVVOR NWq2SHB5[W[oZXP0d{B1cGViUFmzT{Bx[XSqd3H5JIlvKFRvQVzMJINmdGxibHnu[ZM> Moq4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|MUC3N|YoRjJ2M{GwO|M3RC:jPh?=
H1975 MoTxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjzNE4{NTlwNt88US=> Mn3aO|Jp M4Xic2ROW09? MXvJR|UxRTFwM{i1{txO MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN|N{i0Okc,OjR|M{e4OFY9N2F-
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MDA-MB-231 MXTDfZRwfG:6aXPpeJkh[XO|YYm= NUXGNHRLPzJiaILz Mn7oR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iMT64PEDPxE1w NVzuNWdNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxNFc1OjlpPkK5NVA4PDJ7PD;hQi=>
PC3 NH7PSGhEgXSxdH;4bYNqfHliYYPzZZk> M1HIeFczKGi{cx?= NWLBTHFES3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWEN|IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUA2NjN2IN88UU4> M{LNfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUC3OFI6Lz5{OUGwO|QzQTxxYU6=
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TC32 NVrHOYdKeUiWUzDhd5NigQ>? MXjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhXEN|MjDj[Yxtew>? NV3sdpV{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
A673 NGXLXZByUFSVIHHzd4F6 MVHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>? MkLVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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Saos-2 NX7hRnRbeUiWUzDhd5NigQ>? MU\xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW2Gxcz2yJINmdGy| NVO3fIt4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
BT-37 NEPpfIJyUFSVIHHzd4F6 NHvvNFVyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQmStN|ch[2WubIO= NUjIN4wxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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BT-12 NWnOVnNYeUiWUzDhd5NigQ>? NV;aV5NueUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFLUMVEzKGOnbHzz MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
MG 63 (6-TG R) NGfWPFByUFSVIHHzd4F6 MV3xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN? NE\CXZA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB1643 MYLxTHRUKGG|c3H5 Ml62dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6EMU[0N{Bk\Wyucx?= NUXu[VR6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
OHS-50 M3n6R5FJXFNiYYPzZZk> NEjXV25yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiT1jTMVUxKGOnbHzz NU\IUpVQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-SH M3zwNZFJXFNiYYPzZZk> MlzMdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgV2suVi2VSDDj[Yxtew>? M3zBXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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A673 MU\xTHRUKGG|c3H5 Mle4dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgRVY4OyClZXzsd{k> MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh30 M1OxS5FJXFNiYYPzZZk> NEiwcmtyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUnizNEBk\Wyucx?= M4HldFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
MG 63 (6-TG R) MULxTHRUKGG|c3H5 NXG4fXJ5eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN? NVjCfGZzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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insect MmrWSpVv[3Srb36gZZN{[Xl? M{K4VGlvcGmkaYTpc44hd2ZicnXjc41jcW6jboSgbJVu[W5iSHnzMZRi\2enZDDwPFVidHCqYT;wNVEx[WyyaHGgSVU1PUtibYX0ZY51KGW6cILld5Nm\CCrbjDpcpNm[3RiY3XscJMtKEmFNUCgQUAxNjBzMTFOwG0v NUDhbZpvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwN|Q3ODdpPkOwNFM1PjB5PD;hQi=>
insect MVnGeY5kfGmxbjDhd5NigQ>? M2XoTmlvcGmkaYTpc44hd2ZicnXjc41jcW6jboSgbJVu[W5iSHnzMZRi\2enZDDwPFVidHCqYT;wNVEx[WyyaHGgSVU1OktibYX0ZY51KGW6cILld5Nm\CCrbjDpcpNm[3RiY3XscJMtKEmFNUCgQUAxNjB{OTFOwG0v MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODB|NE[wO{c,OzByM{S2NFc9N2F-
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MCF7 NH3YTZFCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MoDxO|IhcHK| Mn\zRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IHjhdoJwemmwZzDQTWs{S0FiRUW0OWshdXW2YX70JIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTBiPTCwMlIxPiEQvF2u NYjPUIpTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwN|Q3ODdpPkOwNFM1PjB5PD;hQi=>
Sf21 NH\4d2hHfW6ldHnvckBie3OjeR?= NXvyOY5WOSCqch?= NWDLTHk6UW6qaXLpeIlwdiCxZjDy[YNwdWKrbnHueEBpfW2jbjDmeYxtNWynbnf0bEBPNXSncn3pcoFtKEirc{[teIFo\2WmIICxNVBj\XSjL4LlZ49u[mmwYX70JIh2dWGwIH\1cIwhdGWwZ4ToJJA5PWGucHjhJIV5eHKnc4Pl[EBqdiCkYXP1cI93cXK3czDpcoZm[3SnZDDT[lIyKGmwc3XjeEBk\WyuczD1d4lv\yCSSWCyJIF{KHO3YoP0doF1\SCvZXHzeZJm\CCjZoTldkAyKGi{IHL5JGFt\XijNkOzJHRz[WOncj3iZZNm\CCobIXvdoV{[2WwY3WgdI9t[XKrLDDJR|UxKD1iMD6yN|Qh|ryPLh?= MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODB|NE[wO{c,OzByM{S2NFc9N2F-
T47D MkX0RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M16zTVczKGi{cx?= NGS0d5dCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGS0O2Qh[2WubIOgbIFz[m:{aX7nJHBKO0uFQTDINVA1P1JibYX0ZY51KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUAxNjJ6NjFOwG0v NX[2cWRERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwN|Q3ODdpPkOwNFM1PjB5PD;hQi=>
PC3 MoK5SpVv[3Srb36gZZN{[Xl? MVGyJIhzew>? MWXJcohq[mm2aX;uJI9nKFCLM1ugbY4hcHWvYX6gVGM{KGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDBT3QheGixc4Doc5J6dGG2aX;uJIF1KFOnckS3N{Bu\WG|dYLl[EBi\nSncjCyJIhzeyCkeTDmcJVwemW|Y3XuZ4Uh[XO|YYmsJGlEPTBiPTCwMlM3PSEQvF2u NV;5XI1rRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwN|Q3ODdpPkOwNFM1PjB5PD;hQi=>
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A2058 M17CNGZ2dmO2aX;uJIF{e2G7 M3nIflEhcHJ? M4HvUGlvcGmkaYTpc44hd2ZiVF;SR|IhcW5iaIXtZY4hSTJyNUigZ4VtdHNiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4hWEuEL1HreEBxcG:|cHjvdplt[XSrb36gZZQhW2W{NEezJIFnfGW{IEGgbJIh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nzMEBKSzVyIE2gNE41OTZizszNMi=> NG\DOo09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEO1PVAxOyd-M{CzOVkxODN:L3G+
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Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot p-AKT (T308) / p-AKT (S473) / AKT ; p-FOXO3a (S253) / FOXO3a ; Nuclear NF-κB p65 / NF-κB p65 ; p-ERK / ERK / LC3 ; p-STAT3 / STAT3 / p-ERK / ERK / p-S6 ; p-MET / MET 27283525 28036259 26673665 27572309 29928341
Immunofluorescence FOXO3a 28036259
Growth inhibition assay Cell viability 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 (from reference)

Kinase Assay:[1]
  • 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]
  • 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.
Animal Research:[1]
  • Animal Models: U87MG and A2780 xenografts are established in female nu/nu mice.
  • Dosages: ~60 mg/kg.
  • Administration: Dosed orally daily (q.d.).

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 410.39
Formula

C18H21F3N6O2
CAS No. 944396-07-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1COCCN1C2=NC(=NC(=C2)C3=CN=C(C=C3C(F)(F)F)N)N4CCOCC4

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04338399 Recruiting Drug: Buparlisib & Paclitaxel Head and Neck Cancer Adlai Nortye Biopharma Co. Ltd. December 12 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

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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

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