Buparlisib (BKM120)

目录号:S2247 别名: NVP-BKM120 中文名称:布帕尼西

仅限科研使用

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。

Buparlisib (BKM120) Chemical Structure

CAS: 944396-07-0

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 7928.28 现货
大包装 有超大折扣

今日订购,明日送达 全国免运费 分装免费 分装成小规格产品(单支最小为1mg)
如1支10mg产品可分装为10支1mg产品

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的Buparlisib (BKM120)发表文献230篇:

产品安全说明书

PI3K抑制剂选择性比较

相关PI3K产品

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)
点击更多
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 NFuzU4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlj4O|Jp NH3lemZKSzVyPUGtNu69VQ>? NXPnO|lsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKwOlUxQDBpPkKyNFY2ODhyPD;hQi=>
U87 MlvkRZBweHSxc3nzJGF{e2G7 NV\IelM2Os7:TR?= MojnO|Jp MVPpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGGwZDDjcIVifmWmIGDBVnAh[W6mIHPhd5Bie2VvMx?= NF\tfXE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkC2OVA5OCd-MkKwOlUxQDB:L3G+
SNU-601 NILXd5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrIWXA4Omh? NVzQd4NWTE2VTx?= NYjvNWZuUUN3ME2wMlgyPsLzMD6wOlPPxE1? NXi4ZmEzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKxOVk5OTRpPkKyNVU6QDF2PD;hQi=>
SNU-1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;tTHU4Omh? NYPzTW1YTE2VTx?= M2PX[GlEPTB;MT6wPFLDuTBwMEK4{txO MnrJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNUm4NVQoRjJ{MUW5PFE1RC:jPh?=
SNU-668 NXvDVopJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{Xy[|czcA>? Mn;YSG1UVw>? MXfJR|UxRTFwNUe5xtExNjB5NN88US=> M3y5TlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MUW5PFE1Lz5{MkG1PVgyPDxxYU6=
AGS MmS2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\vPXU4Omh? NGPNbmZFVVOR MUnJR|UxRTFwN{G0xtExNjFzN988US=> MojlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNUm4NVQoRjJ{MUW5PFE1RC:jPh?=
SNU-216 NXPWe2FVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWrSfpBSPzKq MkS0SG1UVw>? NWX0SXdLUUN3ME2yMlY6OsLzMD6wPFLPxE1? NGP0XVA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG1PVgyPCd-MkKxOVk5OTR:L3G+
SNU-5 M2myPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLxO|Jp Mle0SG1UVw>? M1ruWWlEPTB;MT6zOVHDuTBwMEmx{txO M{HoTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MUW5PFE1Lz5{MkG1PVgyPDxxYU6=
SNU-638 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4Oz[FczcA>? M4izfWROW09? MlnZTWM2OD1{LkK4NuKyOC5yNUROwG0> MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjF3OUixOEc,OjJzNUm4NVQ9N2F-
SNU-16 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXq3Nog> MWnEUXNQ NHO5PFNKSzVyPUGuOVc{yrFyLkCwNe69VQ>? NUTTTIxERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKxOVk5OTRpPkKyNVU6QDF2PD;hQi=>
SNU-484 M4L3cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jvWlczcA>? MVfEUXNQ Ml\aTWM2OD1zLkeyPOKyOC5yNEZOwG0> MmHGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNUm4NVQoRjJ{MUW5PFE1RC:jPh?=
SNU-620 M3XtRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;sV3c4Omh? MoPqSG1UVw>? M3zpU2lEPTB;Mj65N|nDuTBwMECx{txO MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjF3OUixOEc,OjJzNUm4NVQ9N2F-
SNU-719 M3LHPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDNeFc4Omh? MV;EUXNQ MnLWTWM2OD1|LkCzO:KyOC5yM{NOwG0> NW\odYdjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKxOVk5OTRpPkKyNVU6QDF2PD;hQi=>
MM cell lines M122PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLRbGwyOM7:TR?= NInLdlgzPGh? MWTEUXNQ M4HTfmlEPTBidnHybYV{KGGvb37nJIRq\m[ncnXueEBk\WyuIHzpcoV{KGmwIITpcYUh[W6mIHTvd4Uh\GWyZX7k[Y5k\Q>? MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJyN{S4OUc,OjJ{MEe0PFU9N2F-
ARP-1 NEG0fHRCeG:ydH;zbZMhSXO|YYm= MnTENVDPxE1? Mly5NlRp NVz2Ood1TE2VTx?= MWnpcoR2[2W|IF3NJINmdGxiYYDvdJRwe2m|IITodo92\2hiY3HzdIF{\SCjY4TpeoF1cW:w NYH0V4R6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyNFc1QDVpPkKyNlA4PDh3PD;hQi=>
colon cancer cell lines NEHHbmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XNRlAuOTEQvF2= MmrRO|Jp NXzC[ZZLTE2VTx?= NUL3WWVQUUN3ME2x{txO NUTlbXp2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK1OFM5PTdpPkKyOVQ{QDV5PD;hQi=>
gastric cancer cell lines M2TaNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYCwMVEx|ryP NF:4elc4Omh? Mn3ISG1UVw>? MnLqTWM2OD1{LUZOwG0> MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjV2M{i1O{c,OjJ3NEO4OVc9N2F-
HCT-116/HT-29/MKN-45 MnvIRZBweHSxc3nzJGF{e2G7 M1rPSVLPxE1? MlXxOFhp NXj5dFdZe2irZoSgbY4hTzJicHjhd4U> M3e2O|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NUSzPFU4Lz5{MkW0N|g2PzxxYU6=
HT-29 and HCT-116 NFfh[pFE[XOyYYPlJIF{e2G7 NF;xS2w2|ryP NFK4OmozPGh? NFXGTlJqdmS3Y3XzJINie3Cjc3WgZYN1cX[rdIm= MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjV2M{i1O{c,OjJ3NEO4OVc9N2F-
PIK3CA-mutant MCF7 NXvs[GVrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXrJN2pNT0l3ME2xOlDDuTlzbl5vwKxNTDVyPUm4NOKyOjd|bl2= M4LSOVczcA>? Mo\TS2k2OD1zNkFCtVkydk4xvJzMSFUxRTl6MNMxNlc{dk1? MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ3M{m2O{c,OjJ4NUO5Olc9N2F-
PIK3CA-mutant MCF7 NVPkXHd[U2mwYYPlJGF{e2G7 M3;iO2lEPTB;MUG0xtE{dk1? NWnZfXo5PzKq MmniTWM2OD1zMUVCtVNvVSCrbjDy[YR2[2mwZzDBb5QheGixc4Doc5J6dGG2aX;uJIxmfmWucx?= M{jnTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkWzPVY4Lz5{Mk[1N|k3PzxxYU6=
MCF7-myr-Akt MoezS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUf1RZVuT0l3ME2yPVnDuTZ6bl5vwKxNTDVy78{eNVAtODBybl2= MWe3Nog> M1PKVGdKPTB;Mkm5xtE3QG6P78{MUGQ2OO,:nkGwMFAxOG6P NWHRXmQ{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2OVM6PjdpPkKyOlU{QTZ5PD;hQi=>
Y1 cell line MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWCze2FWOC5zzszNM|HPxE1? MVGyOIg> MoXtSG1UVw>? M4qySIlvcGmkaYTzJFYx97zHIHPlcIwhfmmjYnnsbZR6KGmwIF35Z{1U[3S{LYTyZY5{\mWldHXkJINmdGy| M2nVTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkmyPVA1Lz5{Mk[5NlkxPDxxYU6=
human NSCLC NGm3enhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnWzNE42NTMQvF2= NVS1dVlzPzKq NETuTpVKSzVyPUJOwG0> NHHodVA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mke4NVM6Oyd-MkK3PFE{QTN:L3G+
human NSCLC NFnnfW1McW6jc3WgRZN{[Xl? MWmx{txO NUn4eVFJOjSq M{G2cIlvcGmkaYTzJJRp\SCDa4SvcXRQWiC|aXfuZYxqdmdicHH0bJdigSCjdDCzbEBi\nSncjD0doVifG2nboS= NWf4NXAzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK3PFE{QTNpPkKyO|gyOzl|PD;hQi=>
JVM2 MVfDfZRwfG:6aXPpeJkh[XO|YYm= Mnm0NE4zNTJyzszN NVi5dnZkPzKq MXLEUXNQ NYfFXohVUUN3ME2wMlnPxE1? MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzJ|OE[zPUc,OjN{M{i2N|k9N2F-
EHEB MV3DfZRwfG:6aXPpeJkh[XO|YYm= NUKwT3J1OC5{LUKw{txO NV:3VWFYPzKq M4XTN2ROW09? NFPrUIJKSzVyPUCuO:69VQ>? NU\STWU5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyN|g3OzlpPkKzNlM5PjN7PD;hQi=>
MEC2 MYnDfZRwfG:6aXPpeJkh[XO|YYm= MX[wMlIuOjEQvF2= NXnmSXlqPzKq MVjEUXNQ NUHG[G4yUUN3ME2wMlfPxE1? NXK1V4RERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyN|g3OzlpPkKzNlM5PjN7PD;hQi=>
primary B-CLL lymphocytes M3HnZWFxd3C2b4Ppd{BCe3OjeR?= NXL1PIw1UUN3MDDmc5Ih\WGlaDDwdolu[XK7IHPlcIwhdGmwZR?= MUKyOIg> M4q5ZmROW09? NXPwOHNYUUN3MP-8oFPPxE1iZn;yJIFtdCCyYYTp[Y51ew>? MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzJ|OE[zPUc,OjN{M{i2N|k9N2F-
primary B-CLL lymphocytes NWjJ[IQ5U2mwYYPlJGF{e2G7 MnvBTWM2OCCob4Kg[YFkcCCycnntZZJ6KGOnbHygcIlv\Q>? M2fMUVI1cA>? NUfBTZppcW6qaXLpeJMheDdyU{\LJEYhPEVvQmCxJIV5eHKnc4Ppc44> M1XuNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MkO4OlM6Lz5{M{KzPFY{QTxxYU6=
SK-HEP1 NUe2cI5bT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUO2eFVvOS1{MN88US=> NHzYZnk4Omh? NYm4R|NXTE2VTx?= M4LSOGlEPTExvKyx{txO MojOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2N{mxN|YoRjJ|NEe5NVM3RC:jPh?=
786-0 NVXxR5VET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLDVWUyNTJyzszN MlzQO|Jp MVrEUXNQ M4nBTmlEPTExvKyx{txO MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR5OUGzOkc,OjN2N{mxN|Y9N2F-
human HCC cell lines MX\D[YxtKH[rYXLpcIl1gSCjc4PhfS=> MVWwMlAxPS1zzszN NWPpV5ZrPDiq MoX5TWM2OD1zzszN NIXHSYw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S4PVk6QSd-MkO0PFk6QTl:L3G+
Huh7 MUPLbY5ie2ViQYPzZZk> NVzlTZNSOc7:TR?= MUS0PIg> MlS1d4lodmoxrJHjZY51dHlicnXkeYNmeyCyaH;zdIhwenmuYYTpc44hd2ZiQXv0 M2W5NFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NEi5PVk6Lz5{M{S4PVk6QTxxYU6=
human NSCLC cell lines MoCzRZBweHSxc3nzJGF{e2G7 MlT0NE4yOjVvNN88US=> MoXZNlRp NULBU5ZLTE2VTx?= MX7JR|UxeyC{YX7n[ZMh\nKxbTCwMlQuOs7:TR?= NUn5ZlRmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1OlI1PzJpPkKzOVYzPDd{PD;hQi=>
Primary CLL cells MVLBdI9xfG:|aYOgRZN{[Xl? NH;udnYyNTFyzszN Mlz1OFhp NXT5bGI1cW6mdXPld{BieG:ydH;zbZMhcW5iQ1zMJINmdGy|IHnu[IVx\W6mZX70JI9nKHC{b3fuc5N1cWNibXHyb4Vzew>? MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh3MEiwO{c,OjN6NUC4NFc9N2F-
Primary CLL cells NGHHcXVMcW6jc3WgRZN{[Xl? M4CxXFLPxE1? MWmzNI1qdg>? Mm\3[IVkemWjc3XkJHBKO0tiYXP0bZZqfHl? MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh3MEiwO{c,OjN6NUC4NFc9N2F-
Primary CLL cells NIX3c5FEgXSxdH;4bYMhSXO|YYm= MUOy{txO NVvwXVJ{OjSq M{jDVolv\HWlZYOgZ4VtdCCleYTveI95cWOrdIm= MkDYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NUC4NFcoRjJ|OEWwPFA4RC:jPh?=
LC-1/SQSF NWrhcYFGTnWwY4Tpc44hSXO|YYm= NHHyWIo{|ryP NEH2bGMzPGh? MoqySG1UVw>? MV3k[YNz\WG|ZTDOVmYzKHC{b4TlbY4hdGW4ZXy= M2\LeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUiwNFk{Lz5{M{m4NFA6OzxxYU6=
BCR-ABL NXnDVlFoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfhNE4zPS1zMN88US=> NYfWfGhlPGR? NX\UXoNQe2mpbnnmbYNidnSueTDpcohq[mm2IHPlcIwheHKxbHnm[ZJifGmxbh?= MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ2NE[xNkc,OjR{NES2NVI9N2F-
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BT-12 M{HJOpFJXFNiYYPzZZk> MkT1dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUGyJINmdGy| M4ruflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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SK-N-SH NH3hOXNyUFSVIHHzd4F6 NX\iWm1LeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhW0tvTj3TTEBk\Wyucx?= M2P2dFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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insect M1zKSWZ2dmO2aX;uJIF{e2G7 MXzJcohq[mm2aX;uJI9nKHKnY3;tZolv[W62IHj1cYFvKEircz30ZYdo\WRicEi1ZYxxcGFxcEGxNIFteGijIFW1OFVMKG23dHHueEBmgHC{ZYPz[YQhcW5iaX7z[YN1KGOnbHzzMEBKSzVyIE2gNE4xOTFizszNMi=> Mn3NQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByM{S2NFcoRjNyMEO0OlA4RC:jPh?=
insect NGXGWZNHfW6ldHnvckBie3OjeR?= M3T1e2lvcGmkaYTpc44hd2ZicnXjc41jcW6jboSgbJVu[W5iSHnzMZRi\2enZDDwPFVidHCqYT;wNVEx[WyyaHGgSVU1OktibYX0ZY51KGW6cILld5Nm\CCrbjDpcpNm[3RiY3XscJMtKEmFNUCgQUAxNjB{OTFOwG0v Mn7zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByM{S2NFcoRjNyMEO0OlA4RC:jPh?=
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MCF7 M1S1dmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MUW3NkBpenN? MXfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkegZ4VtdHNiaHHyZo9zcW6pIGDJT|NESSCHNUS1T{BufXSjboSgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IECuNlA3KM7:TT6= Ml74QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByM{S2NFcoRjNyMEO0OlA4RC:jPh?=
Sf21 MoDFSpVv[3Srb36gZZN{[Xl? MWWxJIhz NXjHbmVHUW6qaXLpeIlwdiCxZjDy[YNwdWKrbnHueEBpfW2jbjDmeYxtNWynbnf0bEBPNXSncn3pcoFtKEirc{[teIFo\2WmIICxNVBj\XSjL4LlZ49u[mmwYX70JIh2dWGwIH\1cIwhdGWwZ4ToJJA5PWGucHjhJIV5eHKnc4Pl[EBqdiCkYXP1cI93cXK3czDpcoZm[3SnZDDT[lIyKGmwc3XjeEBk\WyuczD1d4lv\yCSSWCyJIF{KHO3YoP0doF1\SCvZXHzeZJm\CCjZoTldkAyKGi{IHL5JGFt\XijNkOzJHRz[WOncj3iZZNm\CCobIXvdoV{[2WwY3WgdI9t[XKrLDDJR|UxKD1iMD6yN|Qh|ryPLh?= MnG4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByM{S2NFcoRjNyMEO0OlA4RC:jPh?=
T47D NXy5UpVSSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MVy3NkBpenN? NHrsWm1CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGS0O2Qh[2WubIOgbIFz[m:{aX7nJHBKO0uFQTDINVA1P1JibYX0ZY51KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUAxNjJ6NjFOwG0v MkHKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByM{S2NFcoRjNyMEO0OlA4RC:jPh?=
PC3 NHL3XmNHfW6ldHnvckBie3OjeR?= NYDUfmxSOiCqcoO= NELW[3VKdmirYnn0bY9vKG:oIGDJN2shcW5iaIXtZY4hWEN|IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBCU1RicHjvd5Bpd3K7bHH0bY9vKGG2IGPldlQ4OyCvZXHzeZJm\CCjZoTldkAzKGi{czDifUBndHWxcnXzZ4Vv[2ViYYPzZZktKEmFNUCgQUAxNjN4NTFOwG0v NWjF[WtjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwN|Q3ODdpPkOwNFM1PjB5PD;hQi=>
HT-29 MV7D[YxtKGO7Y3zlJIF{e2G7 MYOwMlEyOSC2bzCzJJVO NUXhbIxxOjRiaILz Mm\WR4VtdCCleXPs[UBienKnc4SgbY4hcHWvYX6gTHQuOjliY3XscJMh[XO|ZYPz[YQh[XNiYXPjeY12dGG2aX;uJIF1KEd{L12gdIhie2ViYYSgNE4yOTFidH:gN{B2VSCjZoTldkAzPCCqcoOgZpkheHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{Bj[XOnZDDmcI94KGO7dH;t[ZRzgQ>? NIT1TYg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MECzOFYxPyd-M{CwN|Q3ODd:L3G+
A2058 MV3GeY5kfGmxbjDhd5NigQ>? M{\pWFEhcHJ? NXLGWJNmUW6qaXLpeIlwdiCxZjDUU3JEOiCrbjDoeY1idiCDMkC1PEBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCSS1KvRYt1KHCqb4PwbI9zgWyjdHnvckBifCCVZYK0O|Mh[W[2ZYKgNUBpeiCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZMtKEmFNUCgQUAxNjRzNjFOwG0v NIH4XIo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEO1PVAxOyd-M{CzOVkxODN:L3G+
A2058 M3j5W2Z2dmO2aX;uJIF{e2G7 NVT4cnJDOSCqch?= NYLnS4lXUW6qaXLpeIlwdiCxZjDUU3JEOSCrbjDoeY1idiCDMkC1PEBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCVNjDwbI9{eGixconsZZRqd25iYYSgV4VzOjN3L{KzOkBi\nSncjCxJIhzKGK7IGfld5Rmem5iYnzveEBidmGueYPpd{whUUN3MDC9JFAvPTV|IN88UU4> MofOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB|NUmwNFMoRjNyM{W5NFA{RC:jPh?=
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
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]
  • 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]
  • 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
动物实验:[1]
  • 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

溶解度(25°C)

体外

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 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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)

mg/kg g μL

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
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

摩尔浓度计算器

质量 浓度 体积 分子量

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
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)

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