Dactolisib (BEZ235)

目录号:S1009 别名: NVP-BEZ235 中文名称:达克利司

仅限科研使用

Dactolisib (BEZ235, NVP-BEZ235) 是一种双重ATP竞争性 PI3KmTOR 抑制剂,在无细胞试验中,抑制 p110α/γ/δ/β 和 mTOR(p70S6K) 的 IC50 分别为 4 nM /5 nM /7 nM /75 nM /6 nM。 在 3T3TopBP1-ER 细胞中抑制 ATR,IC50 为 21 nM,而对 Akt 和 PDK1 的抑制作用很弱。Dactolisib可诱导自噬并抑制HIV-1的复制。Phase 2。

Dactolisib (BEZ235) Chemical Structure

CAS: 915019-65-7

规格 价格 库存 购买数量
RMB 895.88 现货
RMB 2530.71 现货
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客户使用Selleck生产的Dactolisib (BEZ235)发表文献427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 Dactolisib (BEZ235, NVP-BEZ235) 是一种双重ATP竞争性 PI3KmTOR 抑制剂,在无细胞试验中,抑制 p110α/γ/δ/β 和 mTOR(p70S6K) 的 IC50 分别为 4 nM /5 nM /7 nM /75 nM /6 nM。 在 3T3TopBP1-ER 细胞中抑制 ATR,IC50 为 21 nM,而对 Akt 和 PDK1 的抑制作用很弱。Dactolisib可诱导自噬并抑制HIV-1的复制。Phase 2。
靶点
p110α [1]
(Cell-free assay)
p110γ [1]
(Cell-free assay)
mTOR (p70S6K) [1]
(Cell-free assay)
p110δ [1]
(Cell-free assay)
ATR [8]
(3T3TopBP1-ER cells)
点击更多
4 nM 5 nM 6 nM 7 nM 21 nM
体外研究

BEZ235显著降低mTOR活化的激酶p70S6K的磷酸化水平。BEZ235导致S235/S236P-RPS6水平减少,IC50为6.5 nM。BEZ235抗mTOR的活性使用生化mTOR K-LISA试验测定,IC50为20.7 nM。BEZ235对其β旁系同源物的活性稍弱,IC50为75 nM。在人肿瘤细胞中,PI3K/Akt/mTOR通路经常被组成性活化。BEZ235阻断PI3K和mTOR激酶活性,通过结合于这些酶的ATP结合槽发挥作用。用逐渐增加浓度BEZ235处理PTEN-null细胞系PC3M和U87MG时,导致细胞增殖剂量依赖性减少,平均GI50为10-12 nM。[1] BEZ235是一种mTORC1/2催化抑制剂。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Trypanosoma brucei brucei M1LlOmFvfGmvaXPyc4Jq[WxiQYPzZZk> M3LN[|E5KGh? M1;3[mROW09? MkLrRY51cXS{eYDhco9{d22jbDDhZ5Rqfmm2eTD3bZRpKEWFNUCgc4YhOC5yMEK1JO69VQ>? NUOzTVlvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4NFU6PDZpPkK0PFA2QTR4PD;hQi=>
MCF7 MlW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HiTVAvODFvMUCwJO69VQ>? MmroOFghcA>? M4TSO2ROW09? M2KzUmlEPTB;MD63N{DPxE1? NFzJWoQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i3NVkxPCd-MkO4O|E6ODR:L3G+
HCT116 NWTUfplOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULifpZnOC5yMT2xNFAh|ryP NEHtOo41QCCq MVrEUXNQ NIjRWWZKSzVyPUGuNVYh|ryP M2PmZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OEexPVA1Lz5{M{i3NVkxPDxxYU6=
U87MG NGfKTJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfndGRHOC5yMT2xNFAh|ryP NXXMeI9{PDhiaB?= Mn7GSG1UVw>? NEGzPFNKSzVyPUGuN|Ih|ryP NHSyV2I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i3NVkxPCd-MkO4O|E6ODR:L3G+
HBC4 NULqS3JjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjCXYcxNjBzLUGwNEDPxE1? M{jVVlQ5KGh? NHLOdVVNd2diR1m1NF0uQC54MTDN M1nGbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{O2NlQ3Lz5{MkOzOlI1PjxxYU6=
BSY1 NGOzR2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3yZms4OC5yMT2xNFAh|ryP NYfTV5ZbPDhiaB?= MljJUI9oKEeLNUC9MVgvPDhiTR?= M2nDWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{O2NlQ3Lz5{MkOzOlI1PjxxYU6=
HBC5 NYS0RWJuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vqXFAvODFvMUCwJO69VQ>? MkjrOFghcA>? NXm0elk2VG:pIFfJOVA:NTdwOEegUS=> Mk\iQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|M{[yOFYoRjJ{M{O2NlQ3RC:jPh?=
MCF7 NEXXVGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmntNE4xOS1zMECg{txO Mn:wOFghcA>? MoLwUI9oKEeLNUC9MVgvOTZiTR?= NGnjdW09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOzOlI1Pid-MkKzN|YzPDZ:L3G+
MDA-MB-231 M3TOUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUmwMlAyNTFyMDFOwG0> NEXEcZY1QCCq MV;Mc4chT0l3ME2tPE4xQSCP NF65WpQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOzOlI1Pid-MkKzN|YzPDZ:L3G+
U251 NHWwb5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrjNE4xOS1zMECg{txO MmHKOFghcA>? NV7pc4hIVG:pIFfJOVA:NTdwNk[gUS=> NXTpSXJ5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzN|YzPDZpPkKyN|M3OjR4PD;hQi=>
SF268 NXrQcWFST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfYNE4xOS1zMECg{txO NEjzcnI1QCCq NILvSmVNd2diR1m1NF0uPy57MjDN NIfON5I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOzOlI1Pid-MkKzN|YzPDZ:L3G+
SF295 Mnf6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYT0XlBoOC5yMT2xNFAh|ryP M{TZWlQ5KGh? NI\3cVNNd2diR1m1NF0uQC5|MTDN MnmyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|M{[yOFYoRjJ{M{O2NlQ3RC:jPh?=
SF539 M17m[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYqwMlAyNTFyMDFOwG0> NH60dHM1QCCq M{PQ[Wxw\yCJSUWwQU05NjV7IF2= Mn75QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|M{[yOFYoRjJ{M{O2NlQ3RC:jPh?=
SNB75 NUC0dYJbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnOfXFWOC5yMT2xNFAh|ryP MUG0PEBp MYTMc4chT0l3ME2tPE42QCCP NVi4XppZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzN|YzPDZpPkKyN|M3OjR4PD;hQi=>
SNB78 MlvwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\YOlAvODFvMUCwJO69VQ>? NYXiNGpCPDhiaB?= NHXlVG1Nd2diR1m1NF0uQC54NTDN NFi2Nmo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOzOlI1Pid-MkKzN|YzPDZ:L3G+
HCC2998 M1\wNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3Pt[VAvODFvMUCwJO69VQ>? MYK0PEBp M2mwOmxw\yCJSUWwQU05NjB3IF2= NF3MWXM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOzOlI1Pid-MkKzN|YzPDZ:L3G+
KM12 NXnWd5FkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXNWmcxNjBzLUGwNEDPxE1? NGXBcY01QCCq M1jUUGxw\yCJSUWwQU04NjV2IF2= MoDBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|M{[yOFYoRjJ{M{O2NlQ3RC:jPh?=
HT-29 MmnZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYOwMlAyNTFyMDFOwG0> MUK0PEBp M2\qZWxw\yCJSUWwQU04Njd3IF2= NVT2UlVlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzN|YzPDZpPkKyN|M3OjR4PD;hQi=>
HCT15 NF:0cZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrjVVVJOC5yMT2xNFAh|ryP NEPkSnM1QCCq MoDnUI9oKEeLNUC9MVgvODNiTR?= NE\sS289[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOzOlI1Pid-MkKzN|YzPDZ:L3G+
HCT116 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVewMlAyNTFyMDFOwG0> MmnFOFghcA>? M{TkR2xw\yCJSUWwQU04NjZzIF2= MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjN|NkK0Okc,OjJ|M{[yOFY9N2F-
NCI-H23 M3;4Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUiwMlAyNTFyMDFOwG0> Mo\qOFghcA>? NIO4VmhNd2diR1m1NF0uPy54NDDN M1HmTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{O2NlQ3Lz5{MkOzOlI1PjxxYU6=
NCI-H226 NWXuZohiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{P1NFAvODFvMUCwJO69VQ>? NHf4S2s1QCCq MVjMc4chT0l3ME2tPE41PCCP M3HtclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{O2NlQ3Lz5{MkOzOlI1PjxxYU6=
NCI-H522 MoDwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYewMlAyNTFyMDFOwG0> NWD1bm1{PDhiaB?= NH;acllNd2diR1m1NF0uQC52NTDN M3y4T|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{O2NlQ3Lz5{MkOzOlI1PjxxYU6=
NCI-H438 MmjFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFixVJkxNjBzLUGwNEDPxE1? Mn3SOFghcA>? MX;Mc4chT0l3ME2tPE4yOSCP MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjN|NkK0Okc,OjJ|M{[yOFY9N2F-
A549 M{\UZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDyWo8xNjBzLUGwNEDPxE1? M37LSFQ5KGh? NV;TepZ5VG:pIFfJOVA:NThwMEegUS=> NH\5Zos9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOzOlI1Pid-MkKzN|YzPDZ:L3G+
DMS273 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYOyXFhsOC5yMT2xNFAh|ryP M2KxO|Q5KGh? NXf2XZptVG:pIFfJOVA:NTdwOECgUS=> M3;xRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{O2NlQ3Lz5{MkOzOlI1PjxxYU6=
DMS114 M3rWd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXEdWExNjBzLUGwNEDPxE1? NUHT[Yd4PDhiaB?= MnTtUI9oKEeLNUC9MVgvOzliTR?= MnXRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|M{[yOFYoRjJ{M{O2NlQ3RC:jPh?=
LOXIMVI NH3heXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nlSVAvODFvMUCwJO69VQ>? NV34WYY4PDhiaB?= MW\Mc4chT0l3ME2tPE43PiCP M3vRdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{O2NlQ3Lz5{MkOzOlI1PjxxYU6=
OVCAR3 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGn5V|ExNjBzLUGwNEDPxE1? NX7kbVNKPDhiaB?= NFjj[3ZNd2diR1m1NF0uQC5zNzDN MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjN|NkK0Okc,OjJ|M{[yOFY9N2F-
OVCAR4 NIr0T5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XielAvODFvMUCwJO69VQ>? NEe1TIU1QCCq NY\CVVFrVG:pIFfJOVA:NThwNUigUS=> M13HN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{O2NlQ3Lz5{MkOzOlI1PjxxYU6=
OVCAR5 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFv0VYIxNjBzLUGwNEDPxE1? NHW3VWM1QCCq NU\l[HdlVG:pIFfJOVA:NTdwNUegUS=> MmH0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|M{[yOFYoRjJ{M{O2NlQ3RC:jPh?=
OVCAR8 NFzoUXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnZNE4xOS1zMECg{txO MmLqOFghcA>? MWHMc4chT0l3ME2tO{45PCCP MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjN|NkK0Okc,OjJ|M{[yOFY9N2F-
SKOV3 NYjTUY9MT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XiclAvODFvMUCwJO69VQ>? MVW0PEBp MVLMc4chT0l3ME2tPE41OSCP NYP4bIYxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzN|YzPDZpPkKyN|M3OjR4PD;hQi=>
RXF631L MnXyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\JNE4xOS1zMECg{txO Ml7POFghcA>? NHPUWlFNd2diR1m1NF0uQC5{MTDN MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjN|NkK0Okc,OjJ|M{[yOFY9N2F-
ACHN NWLLU3hwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2OyXlAvODFvMUCwJO69VQ>? M{LTXFQ5KGh? MXzMc4chT0l3ME2tO{46PSCP M1T6Z|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{O2NlQ3Lz5{MkOzOlI1PjxxYU6=
St-4 NIrtdo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;NboExNjBzLUGwNEDPxE1? NF\EfJA1QCCq MYXMc4chT0l3ME2tO{41PyCP NIXrXHY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOzOlI1Pid-MkKzN|YzPDZ:L3G+
MKN1 NVjhco9HT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHNV4MxNjBzLUGwNEDPxE1? M1vWb|Q5KGh? MWXMc4chT0l3ME2tPE41OSCP NHXBW4k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOzOlI1Pid-MkKzN|YzPDZ:L3G+
MKN7 M3rZdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVmwMlAyNTFyMDFOwG0> MWG0PEBp MonqUI9oKEeLNUC9MVcvPjhiTR?= M{XqNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{O2NlQ3Lz5{MkOzOlI1PjxxYU6=
MKN28 M3vJT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjOR2JHOC5yMT2xNFAh|ryP M1zVPVQ5KGh? MXrMc4chT0l3ME2tO{4xPyCP Ml:1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|M{[yOFYoRjJ{M{O2NlQ3RC:jPh?=
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NCI-H1666 Mn\nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\jS5lKSzVyPUmuO|Ehdk1? NUnGd2tLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh5OUS2N{8oRlODTlfFVlww[T5?
CAMA-1 NH7jXWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TRUmlEPTB;OT64JI5O NU\VVGh[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh5OUS2N{8oRlODTlfFVlww[T5?
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BB65-RCC NGH2TZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;qNo9KSzVyPUGyMlczKG6P MlvCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg4QTR4Mz:nQnNCVkeHUkyvZV4>
NCI-H1793 NH;6e4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XyfWlEPTB;MUKuPFIhdk1? NHHa[5o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDd7NE[zM{c,W0GQR1XSQE9iRg>?
KARPAS-45 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHJT5kyUUN3ME2xN{42OSCwTR?= MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFc6PDZ|Lze+V2FPT0WUPD;hQi=>
GCT MkTDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYewVVlwUUN3ME2xN{43QCCwTR?= NETMflQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDd7NE[zM{c,W0GQR1XSQE9iRg>?
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LB2241-RCC MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2WzcGlEPTB;MUSuNFEhdk1? NHi2[3Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDd7NE[zM{c,W0GQR1XSQE9iRg>?
ES5 NIDPeIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTLNlI6UUN3ME2xOE44PCCwTR?= NHPB[I09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDd7NE[zM{c,W0GQR1XSQE9iRg>?
LOXIMVI NILKSolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2i0fWlEPTB;MUSuPVkhdk1? MnHZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg4QTR4Mz:nQnNCVkeHUkyvZV4>
COR-L105 NUPzWVRnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTF3LkC0JI5O MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFc6PDZ|Lze+V2FPT0WUPD;hQi=>
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CAL-39 NEXxUGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\RTmlEPTB;M{euPUBvVQ>? NYHIXGRORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh5OUS2N{8oRlODTlfFVlww[T5?
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NB5 M1HKS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvGeGxTUUN3ME20NE43PCCwTR?= M3;aWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5Pzl2NkOvK|5USU6JRWK8M4E,
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BHY NFrxVHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TCVmlEPTB;NEKuO|Ihdk1? NUTJemQ5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh5OUS2N{8oRlODTlfFVlww[T5?
NTERA-S-cl-D1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2L5NGlEPTB;NEOgcm0> MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFc6PDZ|Lze+V2FPT0WUPD;hQi=>
T-24 MoniS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;0R2lEPTB;NEOuPFMhdk1? NGP5PIc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDd7NE[zM{c,W0GQR1XSQE9iRg>?
EPLC-272H MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvT[WlKSzVyPUS0MlM6KG6P NGqyWFg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDd7NE[zM{c,W0GQR1XSQE9iRg>?
PSN1 M3Hm[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjmTmFHUUN3ME20OE41KG6P MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFc6PDZ|Lze+V2FPT0WUPD;hQi=>
NCI-H2452 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{ey[2lEPTB;NESuOVghdk1? Ml7GQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg4QTR4Mz:nQnNCVkeHUkyvZV4>
KS-1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILjPWxKSzVyPUS0MlY3KG6P MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFc6PDZ|Lze+V2FPT0WUPD;hQi=>
HD-MY-Z Mne5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF22OlVKSzVyPUS0MlkzKG6P NV\pTGtoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh5OUS2N{8oRlODTlfFVlww[T5?
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NOMO-1 MmS1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2e1dmlEPTB;NEWuPFchdk1? NG\BOpU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDd7NE[zM{c,W0GQR1XSQE9iRg>?
SK-HEP-1 NXTLSmFWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjWem9NUUN3ME20Ok4xPCCwTR?= M3z0RVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5Pzl2NkOvK|5USU6JRWK8M4E,
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KYSE-180 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzLe5NKSzVyPUS2MlE4KG6P M4\KelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5Pzl2NkOvK|5USU6JRWK8M4E,
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NCI-H1355 NH;2bZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFf0e3RKSzVyPUS2MlM1KG6P NF3zZ5c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDd7NE[zM{c,W0GQR1XSQE9iRg>?
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A4-Fuk MkS5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2K0WWlEPTB;NE[uOVIhdk1? MkLFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg4QTR4Mz:nQnNCVkeHUkyvZV4>
PC-14 M1TjNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTR4LkW3JI5O MoDEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg4QTR4Mz:nQnNCVkeHUkyvZV4>
TE-5 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXqyPXJuUUN3ME20Ok45PCCwTR?= MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFc6PDZ|Lze+V2FPT0WUPD;hQi=>
LB996-RCC MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnHTWM2OD12Nz6xPUBvVQ>? MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFc6PDZ|Lze+V2FPT0WUPD;hQi=>
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NCI-H1155 NYPkfZpXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\P[2ZKSzVyPUS4MlMzKG6P MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFc6PDZ|Lze+V2FPT0WUPD;hQi=>
LoVo MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\ufWlEPTB;NEiuOEBvVQ>? MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFc6PDZ|Lze+V2FPT0WUPD;hQi=>
MCF7 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXK3[nRrUUN3ME20PE42QCCwTR?= NF61TYg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDd7NE[zM{c,W0GQR1XSQE9iRg>?
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Assay
Methods Test Index PMID
Western blot Myc / Vinculin / pT58 Myc pAkt / Akt / Skp2 / AR / pS6 / p27 p-S6K / S6K / p-Akt / Akt / p-ABL / BCR-ABL Bcl-2 / Caspase-3 / Cleaved caspase-3 Cyclin D1 / Cyclin D2 mTOR / p-mTOR / p70S6K / p-p70S6K p-EGFR-Tyr1068 / EGFR / p-HER2-Tyr1221 / p-HER2-Tyr1222 / HER2 / p-HER3-Tyr1289 25934076 24347472 28435223 29581778 21278786
Immunofluorescence SP1 p-ErbB2(Y1248) LC3 26336820 24675532 23603977
Growth inhibition assay Cell viability (P3, U87) Cell viability (breast cancer cells) Cell viability (K562, KBM7R) 27542970 28060760 28435223
ELISA VEGF 19671762
体内研究 BEZ235诱导肿瘤(69%)消退,而对体重增加没有统计学上显著的作用。总之,这些初步的体内功效研究结果表明,BEZ235单一口服给药时能够阻断疾病的发展,与其他抗癌药结合使用时能够增强疗效。[1]

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]

  • 体外蛋白激酶,PI3K,和mTOR实验:

    PI3Kα, β, δ蛋白都由与p110全长蛋白相接的p85 N端的iSH2域组成,只是PI3Kα没有最后的20个氨基酸。PI3Kγ由p110全长蛋白去掉前144个氨基酸产生而来。所有PI3K蛋白在羧基末端加组氨酸标签便于纯化,然后克隆到pBlue-Bac4.5 (用于α, β,和δ亚型) 或者pVL1393 (用于γ 亚型) 质粒中。转染BaculoGold WT基因组DNA的不同的载体按说明书推荐的方法生产各自重组体杆状病毒及重组蛋白。使用激酶发光检测试剂盒测定BEZ235 (NVP-BEZ235)作用于PI3K的活力。在384孔板上进行激酶实验。在每个孔中加入50 nl的测试项目(溶在90%DMSO中)和5ul的反应buffer,反应buffer包含10 μg/ml PI基质 (l-α-磷脂酰肌醇; 由Avanti Polar Lipids提供;预备在3%辛基葡萄糖苷中),然后加入PI3K 蛋白(p110α, p110β, p110δ,和p110γ分别为10, 25, 10,和150 nM)。加入预备在反应buffer中的5 ul 1 µM 的ATP反应开始,反应进行60分钟 (测p110α, p110β, p110δ)或者120分钟(测p110γ),随后加入10ul的荧光激酶buffer终止反应。数据用Synergy 2 阅读器阅读用于荧光测试。

细胞实验:

[1]

  • Cell lines: HCT116, DLD-1, SW480
  • Concentrations: 0-1 μM
  • Incubation Time: 48小时
  • Method:

    HCT116 (PIK3CA突变型; 激酶域在H1047R), DLD-1 (PIK3CA突变型;螺旋域在E545K), SW480 (PIK3CA 野生型)人类CRC细胞系,同基因型的DLD-1 PIK3CA突变和野生型细胞培养在含10%FBS和1×青霉素/链霉素的培养基中。细胞按不同的初始密度加入(HCT116: 3000个细胞/每孔, DLD-1: 5500个细胞/每孔, SW480: 4500个细胞/每孔, DLD-1 PIK3CA突变型: 7000个细胞/每孔, DLD-1 PIK3CA野生型: 9000个细胞/每孔),用来计算不同的生长动力学。16个小时后,细胞加入浓度越来越高的BEZ235中进行温育,含有药物的培养基24小时更换一次。根据产品说明书,加入细胞16小时和药物处理48小时,使用单溶液细胞增殖检测试剂盒以比色法检测细胞活力。与没有用药物处理正在生长的细胞相比,药物处理的细胞的活力也逐渐趋于正常化。使用GraphPad Prism 5软件用4个参数的回归曲线计算IC50值。用于western blot 分析,细胞用0 nM 或者最高抑制剂量(500 nM) BEZ235处理 2, 6, 24, 或者48 小时。

动物实验:

[2]

  • Animal Models: 雌性Harlan无胸腺裸鼠
  • Dosages: 45 mg/kg
  • Administration: 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):
NMP+PEG300 (10+90, v+v)

30 mg/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 469.55
化学式

C30H23N5O

CAS号 915019-65-7
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
NCT01856101 Terminated Drug: BEZ235 Carcinoma Transitional Cell Cliniques universitaires Saint-Luc- Université Catholique de Louvain|Novartis February 2013 Phase 2
NCT01717898 Terminated Drug: BEZ235|Drug: Prednisone|Drug: Abiraterone acetate Castrate-resistant Prostate Cancer Charles Ryan|Novartis Pharmaceuticals|University of California San Francisco January 31 2013 Phase 1|Phase 2
NCT01756118 Unknown status Drug: BEZ235 Acute Lymphoblastic Leukemia|Leukemia Myelocytic Acute|Chronic Myelogenous Leukemia With Crisis of Blast Cells Johann Wolfgang Goethe University Hospital June 2012 Phase 1
NCT01290406 Withdrawn Drug: BEZ235 Endometrial Cancer Novartis Pharmaceuticals|Novartis March 2012 Phase 2
NCT01288092 Withdrawn Drug: BEZ235 Metastatic Breast Cancer Novartis Pharmaceuticals|Novartis March 2012 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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常见问题及建议解决方法

问题 1:
With difficulties in dissolving BEZ235, How can I improve its solubility?

回答:
For in vivo study, we suggest the vehicle solution NMP/polyethylene glycol 300 (10/90, v/v). Please dissolve BEZ235 in NMP as more as possible. You can sonicate and warm it in water bath for a while. Then dilute with PEG 300.