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 218 publications

Purity & Quality Control

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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)
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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 M1L0WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXv3bmk2PzKq NF[1OWVKSzVyPUGtNu69VQ>? M2nVXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{ME[1NFgxLz5{MkC2OVA5ODxxYU6=
U87 Mn7PRZBweHSxc3nzJGF{e2G7 M2rOflLPxE1? MoPqO|Jp NVXZOVNicW6mdXPld{Bk\WyuIHHwc5B1d3OrczDhcoQh[2ynYY\l[EBRSVKSIHHu[EBk[XOyYYPlMVM> M133UlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{ME[1NFgxLz5{MkC2OVA5ODxxYU6=
SNU-601 Ml3XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\qV2N[PzKq MVPEUXNQ NITybndKSzVyPUCuPFE3yrFyLkC2N:69VQ>? M2L3TFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MUW5PFE1Lz5{MkG1PVgyPDxxYU6=
SNU-1 MlfpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXDUpA4Omh? MXPEUXNQ M{e1TWlEPTB;MT6wPFLDuTBwMEK4{txO NXfDfoFwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKxOVk5OTRpPkKyNVU6QDF2PD;hQi=>
SNU-668 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTXOms4Omh? NXjhcoluTE2VTx?= MVPJR|UxRTFwNUe5xtExNjB5NN88US=> NUH5d3lRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKxOVk5OTRpPkKyNVU6QDF2PD;hQi=>
AGS MlWyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV[3Nog> M4XiR2ROW09? MV\JR|UxRTFwN{G0xtExNjFzN988US=> M3zM[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MUW5PFE1Lz5{MkG1PVgyPDxxYU6=
SNU-216 NWrJTlFlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHsO|Jp MUTEUXNQ M2jwWWlEPTB;Mj62PVLDuTBwMEiy{txO NXLXVHlFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKxOVk5OTRpPkKyNVU6QDF2PD;hQi=>
SNU-5 M1fQVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;LTlczcA>? M4XZWmROW09? MX;JR|UxRTFwM{WxxtExNjB7Md88US=> M1HtelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MUW5PFE1Lz5{MkG1PVgyPDxxYU6=
SNU-638 M2DtfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfwZXk4Omh? NUnLbmoyTE2VTx?= NI[xPHNKSzVyPUKuNlgzyrFyLkC1N:69VQ>? Ml3PQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNUm4NVQoRjJ{MUW5PFE1RC:jPh?=
SNU-16 NInzO5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnzUO|Jp NV\aRol5TE2VTx?= M1r2d2lEPTB;MT61O|PDuTBwMECx{txO MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjF3OUixOEc,OjJzNUm4NVQ9N2F-
SNU-484 MmnJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfTO|Jp MXfEUXNQ MU\JR|UxRTFwN{K4xtExNjB2Nd88US=> M3HDZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MUW5PFE1Lz5{MkG1PVgyPDxxYU6=
SNU-620 MmX6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlH5O|Jp MWXEUXNQ M17KUGlEPTB;Mj65N|nDuTBwMECx{txO NEX2UFU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG1PVgyPCd-MkKxOVk5OTR:L3G+
SNU-719 Mo\kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2m2RVczcA>? MnXQSG1UVw>? NH;3dFRKSzVyPUOuNFM4yrFyLkCzNu69VQ>? NHfvZ2I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG1PVgyPCd-MkKxOVk5OTR:L3G+
MM cell lines M2T1[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYSzWoR3OTEQvF2= M{HyZVI1cA>? MlvRSG1UVw>? MlH3TWM2OCC4YYLp[ZMh[W2xbneg[Iln\mW{ZX70JINmdGxibHnu[ZMhcW5idHnt[UBidmRiZH;z[UBl\XCnbnTlcoNm NUnpcpVSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyNFc1QDVpPkKyNlA4PDh3PD;hQi=>
ARP-1 M{n2V2Fxd3C2b4Ppd{BCe3OjeR?= M1HlR|Ex|ryP M2TV[lI1cA>? MoLySG1UVw>? M1v0Oolv\HWlZYOgUW0h[2WubDDhdI9xfG:|aYOgeIhzd3WpaDDjZZNx[XOnIHHjeIl3[XSrb36= M2PMU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MkC3OFg2Lz5{MkKwO|Q5PTxxYU6=
colon cancer cell lines M3jj[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXVNE0yOM7:TR?= NHfXT4U4Omh? MUPEUXNQ NYXFbJpNUUN3ME2x{txO M3LZcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NUSzPFU4Lz5{MkW0N|g2PzxxYU6=
gastric cancer cell lines NEfMV3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX:wMVEx|ryP MnLQO|Jp NFvkVmdFVVOR NITyeWFKSzVyPUKtOe69VQ>? MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjV2M{i1O{c,OjJ3NEO4OVc9N2F-
HCT-116/HT-29/MKN-45 NYrxSphNSXCxcITvd4l{KEG|c3H5 NV75c41DOs7:TR?= MVy0PIg> M4\5bpNpcW[2IHnuJGczKHCqYYPl M2ixfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NUSzPFU4Lz5{MkW0N|g2PzxxYU6=
HT-29 and HCT-116 M1;w[WNie3Cjc3WgZZN{[Xl? MoDnOe69VQ>? MlnvNlRp NU[zU4ZNcW6mdXPld{Bk[XOyYYPlJIFkfGm4aYT5 M{LnWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NUSzPFU4Lz5{MkW0N|g2PzxxYU6=
PIK3CA-mutant MCF7 M4nt[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\3[o1IUTVyPUG2NOKyQTGwTf-8kGxFPTB;OUiwxtEzPzOwTR?= NGruRoI4Omh? MoPuS2k2OD1zNkFCtVkydk4xvJzMSFUxRTl6MNMxNlc{dk1? MoHwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4NUO5OlcoRjJ{NkWzPVY4RC:jPh?=
PIK3CA-mutant MCF7 MYjLbY5ie2ViQYPzZZk> NI\NdJlKSzVyPUGxOOKyO26P NGPEVJE4Omh? NXXteXVKUUN3ME2xNVTDuTOwTTDpckBz\WS3Y3nu[{BCc3RicHjvd5Bpd3K7bHH0bY9vKGyndnXsdy=> MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ3M{m2O{c,OjJ4NUO5Olc9N2F-
MCF7-myr-Akt NYrSPGJyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHJS2k2OD1{OUpCtVY5dk4xvJzMSFUx97zgMUCsNFAxdk1? MV23Nog> NXLQW|F[T0l3ME2yPVnDuTZ6bl5vwKxNTDVy78{eNVAtODBybl2= M2PWWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkWzPVY4Lz5{Mk[1N|k3PzxxYU6=
Y1 cell line MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnKTYFGOC5zzszNM|HPxE1? M2jj[FI1cA>? NX7nbI5lTE2VTx?= NVe5cmZqcW6qaXLpeJMhPjExvJWgZ4VtdCC4aXHibYxqfHliaX6gUZlkNVOldIKteJJidnOoZXP0[YQh[2WubIO= MnjUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4OUK5NFQoRjJ{NkmyPVA1RC:jPh?=
human NSCLC MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXSwMlUuOs7:TR?= MkDsO|Jp Mle1TWM2OD1zzszN NFvFcXM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mke4NVM6Oyd-MkK3PFE{QTN:L3G+
human NSCLC MWLLbY5ie2ViQYPzZZk> MXKx{txO NHHTXokzPGh? NETjbGRqdmirYnn0d{B1cGViQXv0M41VV1Jic3nncoFtcW6pIIDheIh4[XliYYSgN4gh[W[2ZYKgeJJm[XSvZX70 MkLyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ5OEGzPVMoRjJ{N{ixN|k{RC:jPh?=
JVM2 NHjkZXJEgXSxdH;4bYNqfHliYYPzZZk> MWOwMlIuOjEQvF2= M2CydFczcA>? M1HKXWROW09? NIXWOlBKSzVyPUCuPe69VQ>? NEKxNpU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{KzPFY{QSd-MkOyN|g3Ozl:L3G+
EHEB MVPDfZRwfG:6aXPpeJkh[XO|YYm= M{DZclAvOi1{MN88US=> NHHueXU4Omh? MUTEUXNQ MV\JR|UxRTBwN988US=> MormQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN{M{i2N|koRjJ|MkO4OlM6RC:jPh?=
MEC2 Mlu3R5l1d3SxeHnjbZR6KGG|c3H5 NYnGSFVuOC5{LUKw{txO MV[3Nog> NG\aeJpFVVOR NF;DdpNKSzVyPUCuO:69VQ>? NYLLdFNrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyN|g3OzlpPkKzNlM5PjN7PD;hQi=>
primary B-CLL lymphocytes NFvIb2tCeG:ydH;zbZMhSXO|YYm= M2H5VGlEPTBiZn;yJIVi[2hicILpcYFzgSClZXzsJIxqdmV? M37ORlI1cA>? MUfEUXNQ M1yzbGlEPTExvKyz{txOKG[xcjDhcIwheGG2aXXueJM> M4XKN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MkO4OlM6Lz5{M{KzPFY{QTxxYU6=
primary B-CLL lymphocytes NF:wcJFMcW6jc3WgRZN{[Xl? M{nxV2lEPTBiZn;yJIVi[2hicILpcYFzgSClZXzsJIxqdmV? NV\GTWF3OjSq M{TJOolvcGmkaYTzJJA4OFN4SzCmJFRGNUKSMTDlfJBz\XO|aX;u MnvXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN{M{i2N|koRjJ|MkO4OlM6RC:jPh?=
SK-HEP1 NH;HdWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVmxMVIx|ryP NYD5c5JKPzKq Ml2xSG1UVw>? NVrkdndNUUN3MP-8oFHPxE1? MkjyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2N{mxN|YoRjJ|NEe5NVM3RC:jPh?=
786-0 NIjvOI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTrdI5ZOS1{MN88US=> NVHzb|F{PzKq NUnUTYExTE2VTx?= NFO2V5dKSzVy78{cNe69VQ>? MmjUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2N{mxN|YoRjJ|NEe5NVM3RC:jPh?=
human HCC cell lines MnrFR4VtdCC4aXHibYxqfHliYYPzZZk> MV:wMlAxPS1zzszN MYC0PIg> NITlO4NKSzVyPUJOwG0> Mmr5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2OEm5PVkoRjJ|NEi5PVk6RC:jPh?=
Huh7 MmX0T4lv[XOnIFHzd4F6 NVjBVYxVOc7:TR?= NXW1Ro5MPDiq MnzNd4lodmoxrJHjZY51dHlicnXkeYNmeyCyaH;zdIhwenmuYYTpc44hd2ZiQXv0 NX7GTpFSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0PFk6QTlpPkKzOFg6QTl7PD;hQi=>
human NSCLC cell lines NGXzZZpCeG:ydH;zbZMhSXO|YYm= NEjxfogxNjF{NT20{txO NF25cnAzPGh? M4fl[2ROW09? M4LpSGlEPTC|IILhcodmeyCocn;tJFAvPC1{zszN MoLiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3NkK0O|IoRjJ|NU[yOFczRC:jPh?=
Primary CLL cells M{Hz[2Fxd3C2b4Ppd{BCe3OjeR?= NWL6SYRkOS1zMN88US=> M4DtdVQ5cA>? MmX2bY5lfWOnczDhdI9xfG:|aYOgbY4hS0yOIHPlcIx{KGmwZHXw[Y5l\W62IH;mJJBzd2ewb4P0bYMhdWG{a3Xydy=> M4GxWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OEWwPFA4Lz5{M{i1NFgxPzxxYU6=
Primary CLL cells Mmj4T4lv[XOnIFHzd4F6 MlTWNu69VQ>? NHrVV5U{OG2rbh?= M{P2TYRm[3KnYYPl[EBRUTONIHHjeIl3cXS7 MlLWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NUC4NFcoRjJ|OEWwPFA4RC:jPh?=
Primary CLL cells NGPNZ2FEgXSxdH;4bYMhSXO|YYm= MVyy{txO NUDOPYF{OjSq MV;pcoR2[2W|IHPlcIwh[3m2b4TvfIlkcXS7 NHizOmo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i1NFgxPyd-MkO4OVA5ODd:L3G+
LC-1/SQSF NWTi[HVLTnWwY4Tpc44hSXO|YYm= NGftdWc{|ryP NFmzPVYzPGh? MUDEUXNQ NVLtV4VX\GWlcnXhd4UhVlKIMjDwdo91\WmwIHzleoVt MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl6MEC5N{c,OjN7OECwPVM9N2F-
BCR-ABL NHu5[5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLsd2YxNjJ3LUGw{txO MnLrOIQ> NHLNVWt{cWewaX\pZ4FvfGy7IHnubIljcXRiY3XscEBxem:uaX\ldoF1cW:w MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ2NE[xNkc,OjR{NES2NVI9N2F-
T-ALL NUDnTJBmSXCxcITvd4l{KEG|c3H5 NG\JeGRj\XS5ZXXuJFEvPCCjbnSgOU4{KG2PIHH0JFI1cCCjbnSgNE46KGGwZDC1MlUhdU1iYYSgOFhpKGmwIHTp[oZmemWwdDDj[YxtKGyrbnW= M2jodlI1KG:{IES4bC=> MYLEUXNQ MWXh[oZm[3S|IITo[UBRUTONIIDheIh4[XliaX6gWE1CVExiY3XscEBtcW6ncx?= MojHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|MUC3N|YoRjJ2M{GwO|M3RC:jPh?=
H1975 NFTMO3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFi0SpExNjNvOT62{txO NXrSVWduPzKq MX;EUXNQ M4jzOGlEPTB;MT6zPFXPxE1? NF:0T2w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEOzO|g1Pid-MkSzN|c5PDZ:L3G+
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BT-12 MlTpdWhVWyCjc4PhfS=> NWT4WIFZeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFLUMVEzKGOnbHzz NWjvNHBURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
MG 63 (6-TG R) NV36O4VjeUiWUzDhd5NigQ>? Mnr0dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE2JIE[zJEg3NVSJIGKpJINmdGy| NUPYZYlNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB1643 MoLwdWhVWyCjc4PhfS=> MUTxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJzNkSzJINmdGy| MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
OHS-50 NYfWRoxzeUiWUzDhd5NigQ>? M2jkRpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCRSGOtOVAh[2WubIO= NWHOOJpnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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Rh30 M2q4PJFJXFNiYYPzZZk> M2\SVZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCUaEOwJINmdGy| M2f0S|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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insect NHjYRpZHfW6ldHnvckBie3OjeR?= MmTVTY5pcWKrdHnvckBw\iC{ZXPvcYJqdmGwdDDoeY1idiCKaYOteIFo\2WmIIC4OYFteGijL4CxNVBidHCqYTDFOVQ2UyCvdYThcpQh\XiycnXzd4VlKGmwIHnud4VkfCClZXzsd{whUUN3MDC9JFAvODFzIN88UU4> Mo\3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByM{S2NFcoRjNyMEO0OlA4RC:jPh?=
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T47D NYP2R4JGSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NGH2fFg4OiCqcoO= MXnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFR2N1SgZ4VtdHNiaHHyZo9zcW6pIGDJN2tESSCKMUC0O3IhdXW2YX70JIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTBiPTCwMlI5PiEQvF2u NH7qPI89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MECzOFYxPyd-M{CwN|Q3ODd:L3G+
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A2058 MmfkSpVv[3Srb36gZZN{[Xl? MnvVNUBpeg>? NXKzOY9xUW6qaXLpeIlwdiCxZjDUU3JEOiCrbjDoeY1idiCDMkC1PEBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCSS1KvRYt1KHCqb4PwbI9zgWyjdHnvckBifCCVZYK0O|Mh[W[2ZYKgNUBpeiCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZMtKEmFNUCgQUAxNjRzNjFOwG0v M1TaPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{W5NFA{Lz5|MEO1PVAxOzxxYU6=
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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.
  • (Only for Reference)
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.).
  • (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 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 2021-09-06)

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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