Dactolisib (BEZ235)

For research use only. Not for use in humans.

目录号:S1009 别名: NVP-BEZ235

Dactolisib (BEZ235) Chemical Structure

Molecular Weight(MW): 469.55

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。Phase 2。

规格 价格 库存 购买数量  
RMB 895.88 现货
RMB 1414.41 现货
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客户使用Selleck生产的Dactolisib (BEZ235)发表文献258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 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。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)
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 MUDBcpRqdWmlcn;ibYFtKEG|c3H5 MUixPEBp NIHWNVNFVVOR MnXMRY51cXS{eYDhco9{d22jbDDhZ5Rqfmm2eTD3bZRpKEWFNUCgc4YhOC5yMEK1JO69VQ>? NYXaXGpsOjR6MEW5OFY>
MCF7 NWXRWGdHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXv4ZZV[OC5yMT2xNFAh|ryP MmjROFghcA>? MkKzSG1UVw>? NXviVZlyUUN3ME2wMlc{KM7:TR?= MkL5NlM5PzF7MES=
HCT116 NF\1U4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\tNVAvODFvMUCwJO69VQ>? MlrhOFghcA>? NF:3[VNFVVOR NXr6dVRjUUN3ME2xMlE3KM7:TR?= NYnzSWR6OjN6N{G5NFQ>
U87MG NYDVdoNPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYmwMlAyNTFyMDFOwG0> MVK0PEBp NE\KOYVFVVOR NHrMRVBKSzVyPUGuN|Ih|ryP NFrUPIUzOzh5MUmwOC=>
HBC4 NVPyNXJtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LxOFAvODFvMUCwJO69VQ>? M2Dx[FQ5KGh? NF3NeG5Nd2diR1m1NF0uQC54MTDN MofkNlI{OzZ{NE[=
BSY1 NFvtPVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjkNE4xOS1zMECg{txO M{\3VFQ5KGh? NUDNNIt1VG:pIFfJOVA:NThwNEigUS=> M4\aclIzOzN4MkS2
HBC5 M2DBWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXuwMlAyNTFyMDFOwG0> NIDS[G81QCCq NGr4bHZNd2diR1m1NF0uPy56NzDN MkHtNlI{OzZ{NE[=
MCF7 NU\BVZlkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXhcnFyOC5yMT2xNFAh|ryP MX[0PEBp MkDOUI9oKEeLNUC9MVgvOTZiTR?= MWiyNlM{PjJ2Nh?=
MDA-MB-231 NF;rN5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4S4dFAvODFvMUCwJO69VQ>? MX60PEBp MofVUI9oKEeLNUC9MVgvODliTR?= MXqyNlM{PjJ2Nh?=
U251 NEi0dXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjYPJNNOC5yMT2xNFAh|ryP MXy0PEBp M4C1OWxw\yCJSUWwQU04NjZ4IF2= MkjZNlI{OzZ{NE[=
SF268 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkewNE4xOS1zMECg{txO M{LRUVQ5KGh? NXuzcWYxVG:pIFfJOVA:NTdwOUKgUS=> M2DyWlIzOzN4MkS2
SF295 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPmNE4xOS1zMECg{txO MknJOFghcA>? MUTMc4chT0l3ME2tPE4{OSCP M3fzOVIzOzN4MkS2
SF539 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;XNE4xOS1zMECg{txO MU[0PEBp NYXyT5g2VG:pIFfJOVA:NThwNUmgUS=> NFfX[lczOjN|NkK0Oi=>
SNB75 NIC4VI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmriNE4xOS1zMECg{txO MVe0PEBp MnS1UI9oKEeLNUC9MVgvPThiTR?= MkjtNlI{OzZ{NE[=
SNB78 NFPmeoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV6wMlAyNTFyMDFOwG0> NIHlOnI1QCCq M2TUTWxw\yCJSUWwQU05NjZ3IF2= MoPINlI{OzZ{NE[=
HCC2998 M4\QcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEj5boExNjBzLUGwNEDPxE1? NF\pflQ1QCCq NYK3TIFIVG:pIFfJOVA:NThwMEWgUS=> M2TTOlIzOzN4MkS2
KM12 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzENE4xOS1zMECg{txO MWO0PEBp Moq4UI9oKEeLNUC9MVcvPTRiTR?= NHH3UogzOjN|NkK0Oi=>
HT-29 NIjCTZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVj1OoJxOC5yMT2xNFAh|ryP M1u3U|Q5KGh? NW\6dYM1VG:pIFfJOVA:NTdwN{WgUS=> NGrZZnMzOjN|NkK0Oi=>
HCT15 NUHxd412T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XxPFAvODFvMUCwJO69VQ>? MnfUOFghcA>? MVLMc4chT0l3ME2tPE4xOyCP MUKyNlM{PjJ2Nh?=
HCT116 M2XXWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX[wMlAyNTFyMDFOwG0> M1jDNlQ5KGh? Ml7GUI9oKEeLNUC9MVcvPjFiTR?= NXLPNmQ{OjJ|M{[yOFY>
NCI-H23 NHjOVXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXOwMlAyNTFyMDFOwG0> NXfL[WNvPDhiaB?= MYHMc4chT0l3ME2tO{43PCCP NXjBUnljOjJ|M{[yOFY>
NCI-H226 NHvJZ3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M123flAvODFvMUCwJO69VQ>? Mnv1OFghcA>? MYDMc4chT0l3ME2tPE41PCCP NV\heotoOjJ|M{[yOFY>
NCI-H522 NWHDbm4xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LrflAvODFvMUCwJO69VQ>? NF3RZ5I1QCCq NGPDUGZNd2diR1m1NF0uQC52NTDN NW\3N2RoOjJ|M{[yOFY>
NCI-H438 NITMRnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkKzNE4xOS1zMECg{txO NGrJXW01QCCq Mn;FUI9oKEeLNUC9MVgvOTFiTR?= MUCyNlM{PjJ2Nh?=
A549 Mmq0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3xRWd3OC5yMT2xNFAh|ryP M3TUdFQ5KGh? MYPMc4chT0l3ME2tPE4xPyCP Mn3XNlI{OzZ{NE[=
DMS273 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn[xNE4xOS1zMECg{txO NU\LcFd2PDhiaB?= NVr6eYpjVG:pIFfJOVA:NTdwOECgUS=> NIDUcVYzOjN|NkK0Oi=>
DMS114 Mm\WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTmNE4xOS1zMECg{txO MYS0PEBp M{KwRWxw\yCJSUWwQU05NjN7IF2= MV6yNlM{PjJ2Nh?=
LOXIMVI MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlntNE4xOS1zMECg{txO NXLpRod{PDhiaB?= M3vxZWxw\yCJSUWwQU05NjZ4IF2= MUOyNlM{PjJ2Nh?=
OVCAR3 NIDHOWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7HXWpLOC5yMT2xNFAh|ryP MknJOFghcA>? NV\RNpZZVG:pIFfJOVA:NThwMUegUS=> M4GzWVIzOzN4MkS2
OVCAR4 NVHWfWhMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlW2NE4xOS1zMECg{txO M2DxNVQ5KGh? NIPnb4tNd2diR1m1NF0uQC53ODDN MYqyNlM{PjJ2Nh?=
OVCAR5 MonKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHINE4xOS1zMECg{txO MYG0PEBp NVnOcJVlVG:pIFfJOVA:NTdwNUegUS=> MXSyNlM{PjJ2Nh?=
OVCAR8 NHrUPYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWOwMlAyNTFyMDFOwG0> MWq0PEBp NXLHVZI6VG:pIFfJOVA:NTdwOESgUS=> NVj6PIlLOjJ|M{[yOFY>
SKOV3 M1vqd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPDUYwxNjBzLUGwNEDPxE1? MYe0PEBp NX;hSnlOVG:pIFfJOVA:NThwNEGgUS=> NYLLPGdGOjJ|M{[yOFY>
RXF631L NYLCSIJVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;UbGQxNjBzLUGwNEDPxE1? M{TSXlQ5KGh? NEPNWJRNd2diR1m1NF0uQC5{MTDN NGDUPZQzOjN|NkK0Oi=>
ACHN MlPiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIG4TWQxNjBzLUGwNEDPxE1? NFvmbmw1QCCq NFL4PWJNd2diR1m1NF0uPy57NTDN M2TwblIzOzN4MkS2
St-4 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3y0UlAvODFvMUCwJO69VQ>? MmPZOFghcA>? MmnrUI9oKEeLNUC9MVcvPDdiTR?= NUHyO4tyOjJ|M{[yOFY>
MKN1 MoTtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEW4Sm4xNjBzLUGwNEDPxE1? M3HmdVQ5KGh? NFTPXFBNd2diR1m1NF0uQC52MTDN MVWyNlM{PjJ2Nh?=
MKN7 NHn0N5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUK5NWIyOC5yMT2xNFAh|ryP MVi0PEBp NG\zUnZNd2diR1m1NF0uPy54ODDN MX2yNlM{PjJ2Nh?=
MKN28 M1fMb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWewMlAyNTFyMDFOwG0> M1XsNlQ5KGh? NIXXO3FNd2diR1m1NF0uPy5yNzDN M{jLW|IzOzN4MkS2
MKN45 NVjnc5pvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPJNE4xOS1zMECg{txO NHj2XnA1QCCq NHHyZZFNd2diR1m1NF0uQC5|NDDN NXrZbm1iOjJ|M{[yOFY>
MKN74 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\yNE4xOS1zMECg{txO MnT4OFghcA>? NEPWfm5Nd2diR1m1NF0uPy52MjDN MoLLNlI{OzZ{NE[=
DU145 Mm\VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jPe|AvODFvMUCwJO69VQ>? MVu0PEBp Mkn2UI9oKEeLNUC9MVgvOTZiTR?= NHTRPWczOjN|NkK0Oi=>
PC3 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13iUVAvODFvMUCwJO69VQ>? MkLNOFghcA>? MX;Mc4chT0l3ME2tPE43PiCP MWGyNlM{PjJ2Nh?=
Trypanosoma brucei brucei NVX2NnlkTnWwY4Tpc44hSXO|YYm= NV7DOnhLOjByIH7N MUixNkBp MoDXSG1UVw>? NV:zbYdFTGWlcnXhd4UhcW5icHjvd5Bpd3SrZInsJIlvd3OrdH;sJJBpd3OyaHH0[UBt\X[nbB?= NGL6TmgzPDhyNUm0Oi=>
Trypanosoma brucei brucei MlfFSpVv[3Srb36gRZN{[Xl? NXi1W3V4OThiaB?= NGrUXW9FVVOR NUTKZYJTUW6qaXLpeIlwdiCxZjDy[YNmeHSxcj3t[YRq[XSnZDDlcoRw[3m2b4Ppd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjD0doFve2[ncoLpckB2eHSja3W= M2q4[VI1QDB3OUS2
Trypanosoma brucei brucei NXrUZ|ZVTnWwY4Tpc44hSXO|YYm= M4rkd|IxOCCwTR?= M1\pVFEzKGh? MX7EUXNQ NETxNppG\m[nY4Sgc44he3CqaX7nc416dGWrbjDs[ZZmdA>? Mm\JNlQ5ODV7NE[=
Trypanosoma brucei brucei MWjGeY5kfGmxbjDBd5NigQ>? NYHYV2VkOjByIH7N MYOxNkBp NHrsPJZFVVOR MVHF[oZm[3Rib36gdIhwe3CqYYTp[Jlt[2ixbHnu[UBt\X[nbB?= NHHkdZQzPDhyNUm0Oi=>
UM-UC-3 M1LIeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\pbmJzUUN3ME2zNVUheE1? M1zpenNCVkeHUh?=
SBC-1 NYLnZY4xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTd2MjDwUS=> NF7WV5pUSU6JRWK=
MKN1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHsTWM2OD1{Lkigcm0> NYjYUpdoW0GQR1XS
NCI-H720 NXrPXWV{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3HOnhKSzVyPUOuOVchdk1? M1\JUXNCVkeHUh?=
BFTC-909 NYPNR2RiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\DTWM2OD1|LkexJI5O MlvUV2FPT0WU
BPH-1 NYm3[WxqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfLb|NVUUN3ME20Mlc3KG6P NVn5R4M3W0GQR1XS
PC-3 MoHyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLqTWM2OD13LkC5JI5O NYLLblVbW0GQR1XS
AN3-CA MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTVwNU[gcm0> MkTKV2FPT0WU
HN NEDZZmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mor2TWM2OD13Lkm2JI5O NWDDdI9JW0GQR1XS
HCC2218 MnjMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG[yNoZKSzVyPU[uOlEhdk1? NYTDd5BRW0GQR1XS
KP-4 Mn\qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3[z[2lEPTB;NzDuUS=> MkDRV2FPT0WU
LU-139 MnnZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjWTWM2OD15Lke3JI5O MmTlV2FPT0WU
ETK-1 NIjZR2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLNTWM2OD15Lki4JI5O NV7yT5JmW0GQR1XS
Ramos-2G6-4C10 MkDqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDUSHJKSzVyPUiuOFkhdk1? MljZV2FPT0WU
MHH-PREB-1 NV\yUlFWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTlwMUKgcm0> MXnTRW5ITVJ?
DU-4475 MkjqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPhT5pKSzVyPUmuOFQhdk1? MlXjV2FPT0WU
NCI-H1666 M1LRcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELTW49KSzVyPUmuO|Ehdk1? MnnYV2FPT0WU
CAMA-1 NEjlRZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTlwODDuUS=> NVywbWkzW0GQR1XS
TYK-nu M3\hcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTlwOUSgcm0> MVHTRW5ITVJ?
MFE-280 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoqwTWM2OD17Lkm5JI5O NVLwSlNWW0GQR1XS
A549 M3PUUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVf6WVNTUUN3ME2xNE4yPCCwTR?= M4LVWHNCVkeHUh?=
769-P Mn3mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nxWGlEPTB;MUCuOFQhdk1? MkD5V2FPT0WU
L-363 NEfHb5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnqyTWM2OD1zMD62PUBvVQ>? NGHG[VJUSU6JRWK=
ES8 M4\ldWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvHZXU1UUN3ME2xNE46KG6P M{HOWHNCVkeHUh?=
PA-1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rLUWlEPTB;MUGuPFIhdk1? MkXsV2FPT0WU
Mewo NULFdXVQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPRZo5KSzVyPUGxMlk6KG6P MmnnV2FPT0WU
HSC-3 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVT0SIRFUUN3ME2xNk4zOSCwTR?= NF7sZmdUSU6JRWK=
H4 NGnHRmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTF{Lk[3JI5O NV3WW2h4W0GQR1XS
BB65-RCC M3vnXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfWXYxKSzVyPUGyMlczKG6P NHj1RpNUSU6JRWK=
NCI-H1793 MmfFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfPTHlKSzVyPUGyMlgzKG6P NYfCb5BpW0GQR1XS
KARPAS-45 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLib4ZKSzVyPUGzMlUyKG6P NUjGd21xW0GQR1XS
GCT M2rYS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{ezNGlEPTB;MUOuOlghdk1? NYL6coxIW0GQR1XS
EoL-1 NIfoeoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTF|LkmzJI5O NUj5UVU1W0GQR1XS
LB2241-RCC NWDv[29PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTF2LkCxJI5O MnLWV2FPT0WU
ES5 NWrCWW55T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTF2Lke0JI5O M3nIeXNCVkeHUh?=
LOXIMVI NV\EfpVET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTF2Lkm5JI5O M3PpfHNCVkeHUh?=
COR-L105 MofNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjodJJDUUN3ME2xOU4xPCCwTR?= MUnTRW5ITVJ?
P12-ICHIKAWA M{LFNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTF3LkGgcm0> M1fZ[3NCVkeHUh?=
CHL-1 MnTJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnoTWM2OD1zNT60OUBvVQ>? NInpXWpUSU6JRWK=
VMRC-RCZ MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1i3U2lEPTB;MUWuOlMhdk1? NXzEOWlyW0GQR1XS
HH MlqzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\VPFA{UUN3ME2xOU44KG6P NF;COFZUSU6JRWK=
NUGC-3 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzG[|lKSzVyPUG2MlM1KG6P MV7TRW5ITVJ?
EGI-1 NV;2OpZIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYexO3BuUUN3ME2xOk41OyCwTR?= NUDZXlhlW0GQR1XS
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JVM-3 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlv0TWM2OD1|MD64N{BvVQ>? MWHTRW5ITVJ?
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HD-MY-Z MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTR2LkmyJI5O M4rPbXNCVkeHUh?=
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KP-N-YN NGjCOpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGD3WFZKSzVyPUG0MlUyODNizszN MkfSV2FPT0WU
CCRF-CEM M2LneWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTF2Lke4NFkh|ryP M1Pq[nNCVkeHUh?=
ZR-75-30 NH7lR4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;TS2lEPTB;MU[uN|MxOyEQvF2= M1Hne3NCVkeHUh?=
A673 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFrvOIJKSzVyPUKwMlU2ODdizszN M4\mUHNCVkeHUh?=
K-562 NHHjem5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTzTWM2OD1{OD60NVg{KM7:TR?= M4LHV3NCVkeHUh?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Myc / Vinculin / pT58 Myc; 

PubMed: 25934076     


Immunoblots documenting MYC and pT58 MYC stability. SW480 cells were treated with 200nM BEZ235 or solvent control for 24h and cycloheximide (50µg/ml) and harvested at the indicated time points. Vinculin was used as loading control. Exposures of MYC and pT58 MYC blots were adjusted to equalize exposure at 0 min (n=3; unless otherwise indicated, n indicates the number of independent biological repeat experiments in the following legends).

pAkt / Akt / Skp2 / AR / pS6 / p27; 

PubMed: 24347472     


BEZ235 decreases Skp2 and increases AR protein expression inC4-2B cells. Cells were treated with BEZ235 at various doses. Cell lysates were subjected to Westernblot analysis with indicated antibodies. 

p-S6K / S6K / p-Akt / Akt / p-ABL / BCR-ABL; 

PubMed: 28435223     


Dose-dependent inhibition effect of BEZ235 on the phosphorylation levels of S6K, Akt (Ser473), and BCR–ABL in CML cells. Results of Western blot.

Bcl-2 / Caspase-3 / Cleaved caspase-3 ; 

PubMed: 28435223     


K562 (A1) and KBM7R (A2) cells were treated with BEZ235 for 24 h; total protein lysates were immunoblotted with antibodies for Bcl-2, caspase-3, and cleaved caspase-3. 

Cyclin D1 / Cyclin D2 ; 

PubMed: 28435223     


Dose-dependent inhibition effect of BEZ235 on the expression levels of cyclin D1 and cyclin D2 in K562 and KBM7R cells. Western blot results of K562 (A1) and KBM7R (A2) cells.

mTOR / p-mTOR / p70S6K / p-p70S6K ; 

PubMed: 29581778     


Eca-109 cells was treated with increasing concentration of BEZ235 (0, 100, 200 and 500 nM) for 48 hours. Western blot showed the inhibition effect of PI3K/mTOR pathway was dose dependent. 

p-EGFR-Tyr1068 / EGFR / p-HER2-Tyr1221 / p-HER2-Tyr1222 / HER2 / p-HER3-Tyr1289; 

PubMed: 21278786     


Immunoblots of protein lysates from BT474 and MCF7-HER2 cells treated with either BEZ235 alone (0–500 n) or the combination of BEZ235 (0–500 n) and the tyrosine kinase inhibitor lapatinib (LAP, 500 n) for 24 h. 

25934076 24347472 28435223 29581778 21278786
Immunofluorescence
SP1; 

PubMed: 26336820     


Immunofluorescence assessment of SP1 after BEZ235 treatment for 24 hrs in A673, SKNMC cells and in HFF.

p-ErbB2(Y1248); 

PubMed: 24675532     


Immunofluorescence staining of BT474.LapR cells grown in 3-D culture under different treatment conditions for a week. Scale bar indicates 50 μm.

LC3; 

PubMed: 23603977     


(A) SU-2 cells were treated with NVP-BEZ235 (10 nmol/L) for 12 h and then harvested 24 h after treatment with IR (8 Gy), and analyzed for LC3 expression (top) or the formation of autophagolysosomes by using MDC (middle) and LTR (bottom) by immunofluorescence analysis (600×magnification).

26336820 24675532 23603977
Growth inhibition assay
Cell viability (P3, U87); 

PubMed: 27542970     


IC50 doses of dactolisib for P3 (left) and U87 (right) glioma cells, generated from MTS assay. 

Cell viability (breast cancer cells); 

PubMed: 28060760     


Cell viability of breast cancer cells treated by either BEZ235 or TSA for 48h was measured by MTT assay. Each cell line was analyzed in triplicate, and a representative experiment is shown. 

Cell viability (K562, KBM7R); 

PubMed: 28435223     


(A) K562 cells were treated with increasing concentrations of BEZ235 for 24, 48, or 72 h and subjected to MTS assay. (B) KBM7R cells were treated with increasing concentrations of BEZ235 for 24, 48, or 72 h and subjected to MTS assay. (C) K562 cells were treated with imatinib (0–10 μM) alone or imatinib and BEZ235 (0.2 μM) for 48 h and subjected to MTS assay. (D) KBM7R cells were treated with imatinib (0–10 μM) alone or imatinib and BEZ235 (0.2 μM) for 48 h and subjected to MTS assay. Mean ± SD. n=3. *P<0.05, compared to the control group. #P<0.05, compared to the group of IM alone.

27542970 28060760 28435223
ELISA
VEGF; 

PubMed: 19671762     


NVP-BEZ235 attenuated VEGF secretion by at least 40% in U87 cells. The VEGF level in the serum-free medium was measured in triplicate and the experiment repeated at least twice to confirm results.

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]

- 合并

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]

- 合并
  • 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。


    (Only for Reference)
动物实验:

[2]

- 合并
  • Animal Models: 雌性Harlan无胸腺裸鼠
  • Formulation: NMP/聚乙二醇300(10/90,v/v)
  • Dosages: 45 mg/kg
  • Administration: 口服处理
    (Only for Reference)

溶解度 (25°C)

体外 DMF 18 mg/mL warmed (38.33 mM)
DMSO 0.01 mg/mL (0.02 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):
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 粉状
溶于溶剂
别名 NVP-BEZ235

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
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