Buparlisib (BKM120)

For research use only. Not for use in humans.

目录号:S2247 别名: NVP-BKM120 中文名称:布帕尼西

Buparlisib (BKM120) Chemical Structure

CAS No. 944396-07-0

Buparlisib (BKM120, NVP-BKM120) 是一种选择性 PI3K 抑制剂,在无细胞试验中作用于p110α/β/δ/γIC50分别为 52 nM/166 nM/116 nM/262 nM。对 VPS34,mTOR,DNAPK 的作用效果下降,而对 PI4Kβ几乎没有活性。Buparlisib 可诱导凋亡。Phase 2。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 2227.95 现货
RMB 1400.12 现货
RMB 2607.65 现货
RMB 7928.28 现货
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客户使用Selleck生产的Buparlisib (BKM120)发表文献208篇:

产品安全说明书

PI3K抑制剂选择性比较

生物活性

产品描述 Buparlisib (BKM120, NVP-BKM120) 是一种选择性 PI3K 抑制剂,在无细胞试验中作用于p110α/β/δ/γIC50分别为 52 nM/166 nM/116 nM/262 nM。对 VPS34,mTOR,DNAPK 的作用效果下降,而对 PI4Kβ几乎没有活性。Buparlisib 可诱导凋亡。Phase 2。
特性 BKM120是可用于口服的生物有效的PI3K抑制剂。
靶点
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
体外研究

BKM120作用于解除PI3K调节的细胞系,包括A2780, U87MG, MCF7和DU145时,具有抗增殖活性,GI50为0.1-0.7 nM。[1] BKM120诱导多发性骨髓瘤细胞(ARP1, ARK, MM.1S, MM1.R和U266)凋亡,导致G1期细胞增多,S期细胞减少。BKM120诱导CD138+原代MM 细胞凋亡,且作用于CD138−基质细胞时毒性较低。BKM120可引起BimS的上调和XIAP的下调。[2]BKM120作用于人类胃癌细胞系,降低mTOR下游信号,具有抗增殖活性。BKM120作用于KRAS突变的胃癌细胞系,可以增强p-ERK或 p-STAT3。BKM120 和STAT3阻断剂联用, 作用于含突变KRAS的细胞,诱导凋亡,具有协同效应,但是作用于KRAS野生型细胞没有这种效果。[3]BKM120主要通过Aurora B激酶调节有丝分裂崩坏。[4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
glioma cell lines MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;DdFlWPzKq MlLqTWM2OD1zLUNOwG0> NXHYeYJKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKwOlUxQDBpPkKyNFY2ODhyPD;hQi=>
U87 M3fmcmFxd3C2b4Ppd{BCe3OjeR?= M3LNPVLPxE1? MojVO|Jp MkHTbY5lfWOnczDj[YxtKGGyb4D0c5NqeyCjbnSgZ4xm[X[nZDDQRXJRKGGwZDDjZZNx[XOnLUO= MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjB4NUC4NEc,OjJyNkWwPFA9N2F-
SNU-601 NYTPXJd6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWGxe3ZQPzKq NYHjVFhsTE2VTx?= MnvNTWM2OD1yLkixOuKyOC5yNkROwG0> NH3wPWg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG1PVgyPCd-MkKxOVk5OTR:L3G+
SNU-1 M2DuU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX23Nog> MmXwSG1UVw>? MXTJR|UxRTFwMEiyxtExNjB{ON88US=> NUHxSZJNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKxOVk5OTRpPkKyNVU6QDF2PD;hQi=>
SNU-668 NETQWWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEm2Opg4Omh? NY\4WGFzTE2VTx?= NYfCS4xEUUN3ME2xMlU4QcLzMD6wO|TPxE1? NH64UXU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG1PVgyPCd-MkKxOVk5OTR:L3G+
AGS MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDPeYlIPzKq NEnlR2hFVVOR M3XGXmlEPTB;MT63NVTDuTBwMUG3{txO NVjmNIJyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKxOVk5OTRpPkKyNVU6QDF2PD;hQi=>
SNU-216 MljQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLWO|Jp MYXEUXNQ MlrPTWM2OD1{Lk[5NuKyOC5yOENOwG0> MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjF3OUixOEc,OjJzNUm4NVQ9N2F-
SNU-5 NHHDWnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPqO|Jp NIH1WpdFVVOR NFjqPHpKSzVyPUGuN|UyyrFyLkC5Ne69VQ>? NFjyeVk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG1PVgyPCd-MkKxOVk5OTR:L3G+
SNU-638 NH3qN49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlu3O|Jp NHfRflVFVVOR NVXUXot2UUN3ME2yMlI5OsLzMD6wOVPPxE1? M4fNeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MUW5PFE1Lz5{MkG1PVgyPDxxYU6=
SNU-16 M4rCNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDsO|Jp NFmwT5dFVVOR NGrpTJhKSzVyPUGuOVc{yrFyLkCwNe69VQ>? NHjoTYs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG1PVgyPCd-MkKxOVk5OTR:L3G+
SNU-484 MnLtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHRO|Jp M1v3V2ROW09? MXrJR|UxRTFwN{K4xtExNjB2Nd88US=> MmHXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNUm4NVQoRjJ{MUW5PFE1RC:jPh?=
SNU-620 NWPLeWF2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLXVIJzPzKq NF;SbFRFVVOR Mlu1TWM2OD1{LkmzPeKyOC5yMEJOwG0> MlTyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNUm4NVQoRjJ{MUW5PFE1RC:jPh?=
SNU-719 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\wUFI4Omh? MUTEUXNQ NHewNWNKSzVyPUOuNFM4yrFyLkCzNu69VQ>? NVHhVZhxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKxOVk5OTRpPkKyNVU6QDF2PD;hQi=>
MM cell lines MoHzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfQWG8yOM7:TR?= M1vFSFI1cA>? NU[zO2I4TE2VTx?= M4LXZmlEPTBidnHybYV{KGGvb37nJIRq\m[ncnXueEBk\WyuIHzpcoV{KGmwIITpcYUh[W6mIHTvd4Uh\GWyZX7k[Y5k\Q>? M2\lZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MkC3OFg2Lz5{MkKwO|Q5PTxxYU6=
ARP-1 NGL5ZpRCeG:ydH;zbZMhSXO|YYm= M{m0e|Ex|ryP MljTNlRp NWLkbo5HTE2VTx?= MlWxbY5lfWOnczDNUUBk\WyuIHHwc5B1d3OrczD0bJJwfWeqIHPhd5Bie2ViYXP0bZZifGmxbh?= NYr5TGd3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyNFc1QDVpPkKyNlA4PDh3PD;hQi=>
colon cancer cell lines M37qXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1z2clAuOTEQvF2= NWHLWGV2PzKq MUPEUXNQ NIjyfG1KSzVyPUJOwG0> NVfRXWVuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK1OFM5PTdpPkKyOVQ{QDV5PD;hQi=>
gastric cancer cell lines MoXkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYSwMVEx|ryP MnPUO|Jp M1izRWROW09? MlXkTWM2OD1{LUZOwG0> MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjV2M{i1O{c,OjJ3NEO4OVc9N2F-
HCT-116/HT-29/MKN-45 NVfqTodvSXCxcITvd4l{KEG|c3H5 M4XIeVLPxE1? MU[0PIg> Mn;3d4hq\nRiaX6gS|IheGijc3W= NEHqOoY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkW0N|g2Pyd-MkK1OFM5PTd:L3G+
HT-29 and HCT-116 NHrGTm5E[XOyYYPlJIF{e2G7 M4S3[VXPxE1? MYeyOIg> M1Lab4lv\HWlZYOgZ4F{eGG|ZTDhZ5Rqfmm2eR?= M2DHSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NUSzPFU4Lz5{MkW0N|g2PzxxYU6=
PIK3CA-mutant MCF7 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFv1Vo1IUTVyPUG2NOKyQTGwTf-8kGxFPTB;OUiwxtEzPzOwTR?= MVi3Nog> MoLvS2k2OD1zNkFCtVkydk4xvJzMSFUxRTl6MNMxNlc{dk1? NXrPbGsxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2OVM6PjdpPkKyOlU{QTZ5PD;hQi=>
PIK3CA-mutant MCF7 NVrse2IzU2mwYYPlJGF{e2G7 MWnJR|UxRTFzNNMxN45O M2LzN|czcA>? MUfJR|UxRTFzNNMxN45OKGmwIILl[JVkcW6pIFHreEBxcG:|cHjvdplt[XSrb36gcIV3\Wy| MmK2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4NUO5OlcoRjJ{NkWzPVY4RC:jPh?=
MCF7-myr-Akt M3i2NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHrDR|FIUTVyPUK5PeKyPjiwTf-8kGxFPTExvK6xNEwxODCwTR?= Mk\zO|Jp NGT4OXdIUTVyPUK5PeKyPjiwTf-8kGxFPTExvK6xNEwxODCwTR?= MkDpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4NUO5OlcoRjJ{NkWzPVY4RC:jPh?=
Y1 cell line NH:1NXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFe1TnkxNjIQvF2vNe69VQ>? Mli2NlRp Mo[3SG1UVw>? M4j1bolvcGmkaYTzJFYx97zHIHPlcIwhfmmjYnnsbZR6KGmwIF35Z{1U[3S{LYTyZY5{\mWldHXkJINmdGy| NWHlW41ZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2PVI6ODRpPkKyOlkzQTB2PD;hQi=>
human NSCLC NIPtOYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInKNVAxNjVvMt88US=> M4PBTFczcA>? NUG3RolwUUN3ME2x{txO Mm\YQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ5OEGzPVMoRjJ{N{ixN|k{RC:jPh?=
human NSCLC NXLGSpZSU2mwYYPlJGF{e2G7 NW\MdWlJOc7:TR?= NVXtbZB[OjSq NWjYO|lncW6qaXLpeJMhfGinIFHreE9uXE:UIIPp[45idGmwZzDwZZRpf2G7IHH0JFNpKGGodHXyJJRz\WG2bXXueC=> MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjd6MUO5N{c,OjJ5OEGzPVM9N2F-
JVM2 NXSxXVlGS3m2b4TvfIlkcXS7IHHzd4F6 NHTYPIwxNjJvMkFOwG0> M3e5S|czcA>? NV7Oem95TE2VTx?= MYLJR|UxRTBwOd88US=> M2XrblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MkO4OlM6Lz5{M{KzPFY{QTxxYU6=
EHEB MUDDfZRwfG:6aXPpeJkh[XO|YYm= NFGzTJIxNjJvMkFOwG0> Mo[0O|Jp NVrtPHJWTE2VTx?= MV\JR|UxRTBwN988US=> M{K2bVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MkO4OlM6Lz5{M{KzPFY{QTxxYU6=
MEC2 MWTDfZRwfG:6aXPpeJkh[XO|YYm= M4HVNFAvOi1{MN88US=> MkT1O|Jp M4f0NGROW09? MVjJR|UxRTBwN988US=> NV3WcItHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyN|g3OzlpPkKzNlM5PjN7PD;hQi=>
primary B-CLL lymphocytes NXvYSoRQSXCxcITvd4l{KEG|c3H5 M3nsZWlEPTBiZn;yJIVi[2hicILpcYFzgSClZXzsJIxqdmV? M2fsdlI1cA>? MUjEUXNQ NV7YNnhwUUN3MP-8oFPPxE1iZn;yJIFtdCCyYYTp[Y51ew>? NVXOb4JbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyN|g3OzlpPkKzNlM5PjN7PD;hQi=>
primary B-CLL lymphocytes NXvtUnZFU2mwYYPlJGF{e2G7 M2m0fGlEPTBiZn;yJIVi[2hicILpcYFzgSClZXzsJIxqdmV? MYqyOIg> MV\pcohq[mm2czDwO|BUPktiJjC0SU1DWDFiZYjwdoV{e2mxbh?= M3;Xc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MkO4OlM6Lz5{M{KzPFY{QTxxYU6=
SK-HEP1 MlPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVWxMVIx|ryP MkDGO|Jp NWPzTYhiTE2VTx?= M4W5NmlEPTExvKyx{txO NV7x[3BORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0O|kyOzZpPkKzOFc6OTN4PD;hQi=>
786-0 NYXwc|gyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnHZpoyNTJyzszN NUPmTo83PzKq M17x[2ROW09? NHnrU45KSzVy78{cNe69VQ>? NILGZoE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S3PVE{Pid-MkO0O|kyOzZ:L3G+
human HCC cell lines NXfCWmlSS2WubDD2bYFjcWyrdImgZZN{[Xl? MXKwMlAxPS1zzszN Mmm2OFhp M1TR[GlEPTB;Md88US=> MoXjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2OEm5PVkoRjJ|NEi5PVk6RC:jPh?=
Huh7 MkPrT4lv[XOnIFHzd4F6 M4jmV|HPxE1? M2PUOFQ5cA>? M3;IeZNq\26r77{BZ4FvfGy7IILl[JVk\XNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> M2m5WVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NEi5PVk6Lz5{M{S4PVk6QTxxYU6=
human NSCLC cell lines MmfWRZBweHSxc3nzJGF{e2G7 MVGwMlEzPS12zszN NYLRfnRiOjSq MXrEUXNQ NVXzUGZ5UUN3MIOgdoFv\2W|IH\yc40hOC52LUNOwG0> M{S5SFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NU[yOFczLz5{M{W2NlQ4OjxxYU6=
Primary CLL cells MkfSRZBweHSxc3nzJGF{e2G7 M2DMXFEuOTEQvF2= M1nnTVQ5cA>? NIrlT3VqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCFTFygZ4VtdHNiaX7k[ZBmdmSnboSgc4YheHKxZ37vd5Rq[yCvYYLr[ZJ{ MkLNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NUC4NFcoRjJ|OEWwPFA4RC:jPh?=
Primary CLL cells MWLLbY5ie2ViQYPzZZk> NI\5R5Qz|ryP MYGzNI1qdg>? M2\ocYRm[3KnYYPl[EBRUTONIHHjeIl3cXS7 MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh3MEiwO{c,OjN6NUC4NFc9N2F-
Primary CLL cells MX\DfZRwfG:6aXOgRZN{[Xl? MX6y{txO M2PxeFI1cA>? M1LpXolv\HWlZYOgZ4VtdCCleYTveI95cWOrdIm= NXfUT4ZnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OVA5ODdpPkKzPFUxQDB5PD;hQi=>
LC-1/SQSF NEnPUVdHfW6ldHnvckBCe3OjeR?= MWmz{txO MkjFNlRp NI\2[JpFVVOR M3fOZYRm[3KnYYPlJG5TTjJicILveIVqdiCuZY\lcC=> MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl6MEC5N{c,OjN7OECwPVM9N2F-
BCR-ABL NYP5SGhrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjENE4zPS1zMN88US=> MV[0[C=> MX7zbYdvcW[rY3HueIx6KGmwaHnibZQh[2WubDDwdo9tcW[ncnH0bY9v MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ2NE[xNkc,OjR{NES2NVI9N2F-
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A2058 MVPGeY5kfGmxbjDhd5NigQ>? NXrWNng6OSCqch?= MmGyTY5pcWKrdHnvckBw\iCWT2LDNkBqdiCqdX3hckBCOjB3ODDj[YxteyCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckBRU0JxQXv0JJBpd3OyaH;yfYxifGmxbjDheEBU\XJ2N{OgZYZ1\XJiMTDodkBjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYOsJGlEPTBiPTCwMlQyPiEQvF2u MnK2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB|NUmwNFMoRjNyM{W5NFA{RC:jPh?=
A2058 MVPGeY5kfGmxbjDhd5NigQ>? Mni0NUBpeg>? M4rBV2lvcGmkaYTpc44hd2ZiVF;SR|EhcW5iaIXtZY4hSTJyNUigZ4VtdHNiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4hWzZicHjvd5Bpd3K7bHH0bY9vKGG2IGPldlI{PS9{M{[gZYZ1\XJiMTDodkBjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYOsJGlEPTBiPTCwMlU2OyEQvF2u MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN3OUCwN{c,OzB|NUmwNFM9N2F-

... 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
体内研究 BKM120按30, 60, 或100 mg/kg剂量作用于A2780移植瘤,完全抑制pAKTser473。BKM120按 30和 60 mg/kg剂量作用于U87MG神经胶质瘤模型,显示抗癌活性。[1]BKM120每天按5μM/kg剂量处理具有持久生命力的ARP1 SCID鼠模型,导致肿瘤体积和K链水平明显降低。[2]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[2]
- 合并

PI3K 生化实验(ATP 消耗实验):

BKM120溶于DMSO中,按每孔1.25 µL直接加到黑色384孔板上。开始反应, 25 µL 10nM PI3K和5 µg/mL 1-α-磷酸肌醇(PI)加到实验 buffer (10 mM Tris pH 为7.5, 5 mM MgCl2, 20 mM NaCl, 1 mM DTT,及0.05% CHAPS),然后加到每孔中,随后在实验buffer中加入25 µL 2 µM ATP。反应进行直到50% ATP被消耗,然后加入25 µL KinaseGlo溶液终止反应。终止的反应温育5分钟,然后通过荧光测定残留的ATP。
细胞实验:[1]
- 合并
  • Cell lines: A2780细 胞
  • Concentrations: 0-6.6 μM
  • Incubation Time: 3天
  • Method: A2780细胞培养在含10% FBS,L-谷氨酸,丙酮酸钠和抗生素的DMEM培养基上。细胞按每孔103个细胞的密度接种在相同培养基上,温育3到5小时。稀释溶于20 mM DMSO中的BKM120。2 µL稀释的BKM120溶液加到细胞培养基上, (浓度为0-6.6 µM)。等体积(100 µL)溶液加到96孔板中,在37oC下温育3天。使用Trilux读取荧光值而测定抑制细胞增殖的效果
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: 携带U87MG 和A2780移植瘤的雌性裸鼠
  • Dosages: ~60 mg/kg
  • Administration: 每天口服处理
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 82 mg/mL (199.8 mM)
Ethanol 2 mg/mL (4.87 mM)
Water Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
5% DMSO+30% PEG 300+ddH2O
15mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 410.39
化学式

C18H21F3N6O2

CAS号 944396-07-0
储存条件 粉状
溶于溶剂
别名 NVP-BKM120

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

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
NCT02194049 Completed Drug: BKM120|Drug: cisplatin|Drug: etoposide Extensive Stage Small Cell Lung Cancer|Unspecified Adult Solid Tumor Protocol Specific University of California Davis|Novartis July 2014 Phase 1
NCT02154776 Completed Drug: LEE011|Drug: Buparlisib|Drug: Letrozole Advanced or Metastatic Breast Cancer Novartis Pharmaceuticals|Novartis June 27 2014 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID