Dactolisib (BEZ235, NVP-BEZ235)

目录号:S1009

Dactolisib (BEZ235, NVP-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该产品发表文献180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 MoHsRY51cW2rY4LvZolidCCDc4PhfS=> M2jHVVE5KGh? MUDEUXNQ MoflRY51cXS{eYDhco9{d22jbDDhZ5Rqfmm2eTD3bZRpKEWFNUCgc4YhOC5yMEK1JO69VQ>? M1rMTVI1QDB3OUS2
MCF7 NF:xe4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIP0d3YxNjBzLUGwNEDPxE1? MWG0PEBp NU[3NpZmTE2VTx?= Mle2TWM2OD1yLkezJO69VQ>? NUfoU3dGOjN6N{G5NFQ>
HCT116 NHrJWllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\XNE4xOS1zMECg{txO NV;xUnJvPDhiaB?= M{fwPWROW09? NY\1OWhPUUN3ME2xMlE3KM7:TR?= Ml;CNlM5PzF7MES=
U87MG NGjEVHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVywMlAyNTFyMDFOwG0> MXy0PEBp MYLEUXNQ NWCwPJViUUN3ME2xMlMzKM7:TR?= MVSyN|g4OTlyNB?=
HBC4 M1XhSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{P6WVAvODFvMUCwJO69VQ>? NWmwVmEyPDhiaB?= NWXwenR4VG:pIFfJOVA:NThwNkGgUS=> NF3nR2gzOjN|NkK0Oi=>
BSY1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXewMlAyNTFyMDFOwG0> NIjrclI1QCCq NHzjNW1Nd2diR1m1NF0uQC52ODDN M1zhNlIzOzN4MkS2
HBC5 Ml60S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLhfYIxNjBzLUGwNEDPxE1? NWHnOlZRPDhiaB?= NYXUbYt7VG:pIFfJOVA:NTdwOEegUS=> M2fkR|IzOzN4MkS2
MCF7 NHXZfI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPsfmRvOC5yMT2xNFAh|ryP NFHBd5Q1QCCq NVzLO|FqVG:pIFfJOVA:NThwMU[gUS=> NXTw[nQ4OjJ|M{[yOFY>
MDA-MB-231 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXywMlAyNTFyMDFOwG0> MnzNOFghcA>? NVzDflR[VG:pIFfJOVA:NThwMEmgUS=> MUWyNlM{PjJ2Nh?=
U251 NF:zfpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjMfYoxNjBzLUGwNEDPxE1? M3LiVlQ5KGh? NHLRRYRNd2diR1m1NF0uPy54NjDN MVGyNlM{PjJ2Nh?=
SF268 Mo\6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTlNE4xOS1zMECg{txO M332WFQ5KGh? NHPpN3FNd2diR1m1NF0uPy57MjDN M3;aXFIzOzN4MkS2
SF295 NFmySZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVSwMlAyNTFyMDFOwG0> NHj1fpc1QCCq NFPOOnJNd2diR1m1NF0uQC5|MTDN NVPoRm9ZOjJ|M{[yOFY>
SF539 NInyT2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\3RVAvODFvMUCwJO69VQ>? M1HPblQ5KGh? MknEUI9oKEeLNUC9MVgvPTliTR?= M3jiVFIzOzN4MkS2
SNB75 NXTzR3pST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX2zN3AyOC5yMT2xNFAh|ryP NV;6SmpoPDhiaB?= M1;pbWxw\yCJSUWwQU05NjV6IF2= Mnq1NlI{OzZ{NE[=
SNB78 M3PpRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPQXpoxOC5yMT2xNFAh|ryP MmLJOFghcA>? MXfMc4chT0l3ME2tPE43PSCP NUjhNINLOjJ|M{[yOFY>
HCC2998 M2LOZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;0VYVJOC5yMT2xNFAh|ryP M{DDd|Q5KGh? MlqzUI9oKEeLNUC9MVgvODViTR?= MmfiNlI{OzZ{NE[=
KM12 NHzUelZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLzfHYxNjBzLUGwNEDPxE1? NIHD[mY1QCCq NHHiUGRNd2diR1m1NF0uPy53NDDN M1fGOVIzOzN4MkS2
HT-29 Mmm1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPkPGgxNjBzLUGwNEDPxE1? NXLiPIg5PDhiaB?= M1ftN2xw\yCJSUWwQU04Njd3IF2= MWOyNlM{PjJ2Nh?=
HCT15 MoXTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUSwMlAyNTFyMDFOwG0> NGHKRlQ1QCCq NI[4fVBNd2diR1m1NF0uQC5yMzDN MkHrNlI{OzZ{NE[=
HCT116 Mm\HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLiTGgxNjBzLUGwNEDPxE1? Mo\vOFghcA>? MV;Mc4chT0l3ME2tO{43OSCP M{W4ZlIzOzN4MkS2
NCI-H23 NXLrXmI5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TVOVAvODFvMUCwJO69VQ>? NWjJeZNPPDhiaB?= MXLMc4chT0l3ME2tO{43PCCP NEXiWmUzOjN|NkK0Oi=>
NCI-H226 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonpNE4xOS1zMECg{txO M2XKd|Q5KGh? MXHMc4chT0l3ME2tPE41PCCP NEPYRlgzOjN|NkK0Oi=>
NCI-H522 MoDQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYGwMlAyNTFyMDFOwG0> NXHoe21JPDhiaB?= NIe0VIRNd2diR1m1NF0uQC52NTDN NHP3UZYzOjN|NkK0Oi=>
NCI-H438 M3LLXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHJ[ocxNjBzLUGwNEDPxE1? MWe0PEBp NXnIU2lyVG:pIFfJOVA:NThwMUGgUS=> NFHqdJMzOjN|NkK0Oi=>
A549 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrRSWoxNjBzLUGwNEDPxE1? MYW0PEBp NYLh[FZqVG:pIFfJOVA:NThwMEegUS=> NHfvc4IzOjN|NkK0Oi=>
DMS273 NVXXWotwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrGeGExNjBzLUGwNEDPxE1? MXi0PEBp M1O3S2xw\yCJSUWwQU04NjhyIF2= Mn;lNlI{OzZ{NE[=
DMS114 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEP1bWcxNjBzLUGwNEDPxE1? MXm0PEBp NY\RTVRGVG:pIFfJOVA:NThwM{mgUS=> M2XxSFIzOzN4MkS2
LOXIMVI MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLLNE4xOS1zMECg{txO Mor0OFghcA>? M2P5XWxw\yCJSUWwQU05NjZ4IF2= MlXMNlI{OzZ{NE[=
OVCAR3 M4LoZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPoSJFSOC5yMT2xNFAh|ryP NG\5b|c1QCCq NVe1RmNWVG:pIFfJOVA:NThwMUegUS=> M3uxNlIzOzN4MkS2
OVCAR4 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1:5RVAvODFvMUCwJO69VQ>? MWm0PEBp M4XobWxw\yCJSUWwQU05NjV6IF2= MYGyNlM{PjJ2Nh?=
OVCAR5 M3\jOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1f1bFAvODFvMUCwJO69VQ>? MUC0PEBp MorXUI9oKEeLNUC9MVcvPTdiTR?= MUKyNlM{PjJ2Nh?=
OVCAR8 NX7SOmZIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV2wMlAyNTFyMDFOwG0> NEPQUIM1QCCq NXzrU5ZCVG:pIFfJOVA:NTdwOESgUS=> NXHsSmtCOjJ|M{[yOFY>
SKOV3 NUXCcmFMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjYSGpCOC5yMT2xNFAh|ryP M{DJTVQ5KGh? M3r6SWxw\yCJSUWwQU05NjRzIF2= NWPVT5FHOjJ|M{[yOFY>
RXF631L M4HBN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXGNE4xOS1zMECg{txO M2WxVFQ5KGh? M2\qW2xw\yCJSUWwQU05NjJzIF2= MnfwNlI{OzZ{NE[=
ACHN M{j2d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzQNE4xOS1zMECg{txO NXHySVJzPDhiaB?= MnqyUI9oKEeLNUC9MVcvQTViTR?= MlSyNlI{OzZ{NE[=
St-4 NFjq[25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\QfIIxNjBzLUGwNEDPxE1? NH;6WHk1QCCq M1vJRWxw\yCJSUWwQU04NjR5IF2= Ml;jNlI{OzZ{NE[=
MKN1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXywMlAyNTFyMDFOwG0> NFrINHY1QCCq M2n0d2xw\yCJSUWwQU05NjRzIF2= NX\He|I4OjJ|M{[yOFY>
MKN7 NYixc2JLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn[zNE4xOS1zMECg{txO MoG5OFghcA>? MonCUI9oKEeLNUC9MVcvPjhiTR?= M{TFWVIzOzN4MkS2
MKN28 Mon2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mon6NE4xOS1zMECg{txO NX7DZZNNPDhiaB?= NF7qe3pNd2diR1m1NF0uPy5yNzDN NI\1RYQzOjN|NkK0Oi=>
MKN45 M{XBcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\tdXVGOC5yMT2xNFAh|ryP Mn;mOFghcA>? Ml;1UI9oKEeLNUC9MVgvOzRiTR?= MUSyNlM{PjJ2Nh?=
MKN74 NFnWWmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fNPVAvODFvMUCwJO69VQ>? NEnETpM1QCCq M2DJb2xw\yCJSUWwQU04NjR{IF2= NFexOlgzOjN|NkK0Oi=>
DU145 NXrVT3hJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLhemJJOC5yMT2xNFAh|ryP M3TBc|Q5KGh? M1T4VGxw\yCJSUWwQU05NjF4IF2= NHrkXJMzOjN|NkK0Oi=>
PC3 NXPYVW5PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzJZo4zOC5yMT2xNFAh|ryP M1[zZlQ5KGh? NWXTPItPVG:pIFfJOVA:NThwNk[gUS=> M1\JZ|IzOzN4MkS2
Trypanosoma brucei brucei NXvvOmRlTnWwY4Tpc44hSXO|YYm= MV[yNFAhdk1? NGns[lgyOiCq MYrEUXNQ NXHCfW5LTGWlcnXhd4UhcW5icHjvd5Bpd3SrZInsJIlvd3OrdH;sJJBpd3OyaHH0[UBt\X[nbB?= NU\3bnFYOjR6MEW5OFY>
Trypanosoma brucei brucei M1z6PGZ2dmO2aX;uJGF{e2G7 NEXNSnIyQCCq M{O1ZmROW09? Mlm0TY5pcWKrdHnvckBw\iC{ZXPldJRwei2vZXTpZZRm\CCnbnTvZ5l1d3OrczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiC2cnHud4ZmenKrbjD1dJRic2V? NFL1[5UzPDhyNUm0Oi=>
Trypanosoma brucei brucei MofoSpVv[3Srb36gRZN{[Xl? M2XRc|IxOCCwTR?= MoPBNVIhcA>? M4T1[WROW09? M3LlZWVn\mWldDDvckB{eGirbnfvcZlt\WmwIHzleoVt NGnFclEzPDhyNUm0Oi=>
Trypanosoma brucei brucei Ml;USpVv[3Srb36gRZN{[Xl? NIHqNIkzODBibl2= NHzidooyOiCq MUDEUXNQ MX7F[oZm[3Rib36gdIhwe3CqYYTp[Jlt[2ixbHnu[UBt\X[nbB?= MoDjNlQ5ODV7NE[=
UM-UC-3 NILoe5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoOzTWM2OD1|MUWgdG0> NIj5VXBUSU6JRWK=
SBC-1 MlHrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWezbJBjUUN3ME23OFIheE1? NG\pV|hUSU6JRWK=
MKN1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHwTWM2OD1{Lkigcm0> MXfTRW5ITVJ?
NCI-H720 NGKycJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrYTWM2OD1|LkW3JI5O M2\UOHNCVkeHUh?=
BFTC-909 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7yenlHUUN3ME2zMlcyKG6P MnrNV2FPT0WU
BPH-1 M1nyOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjyPG82UUN3ME20Mlc3KG6P M1fGS3NCVkeHUh?=
PC-3 NXnO[GZ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml60TWM2OD13LkC5JI5O MmjwV2FPT0WU
AN3-CA MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\OOmlEPTB;NT61OkBvVQ>? NGf6S2pUSU6JRWK=
HN NYrybVlRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LYTWlEPTB;NT65OkBvVQ>? MlrUV2FPT0WU
HCC2218 NInaUVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\qbZlKSzVyPU[uOlEhdk1? NFP5dnNUSU6JRWK=
KP-4 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M364[GlEPTB;NzDuUS=> M1S2SHNCVkeHUh?=
LU-139 NVvQRod7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjQTWM2OD15Lke3JI5O NFvGV3ZUSU6JRWK=
ETK-1 M3jQRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7ZOFdNUUN3ME23Mlg5KG6P MkjhV2FPT0WU
Ramos-2G6-4C10 NIf0c2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2n5TWlEPTB;OD60PUBvVQ>? MUPTRW5ITVJ?
MHH-PREB-1 M2[2fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfKTWM2OD17LkGyJI5O M{nDcXNCVkeHUh?=
DU-4475 NWWzPIx7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXibG1KSzVyPUmuOFQhdk1? NHLBUHFUSU6JRWK=
NCI-H1666 NV7JOndET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYD1dIg6UUN3ME25MlcyKG6P M3fyU3NCVkeHUh?=
CAMA-1 M2rCc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3nTRmlEPTB;OT64JI5O MoTaV2FPT0WU
TYK-nu NGfrdJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrMTWM2OD17Lkm0JI5O NWjvdXg3W0GQR1XS
MFE-280 M4rTUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTlwOUmgcm0> NEPGbWdUSU6JRWK=
A549 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHi2SldKSzVyPUGwMlE1KG6P Ml[3V2FPT0WU
769-P NWHGcHh5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfJNYtKSzVyPUGwMlQ1KG6P NHrlXVNUSU6JRWK=
L-363 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnu5TWM2OD1zMD62PUBvVQ>? Mof6V2FPT0WU
ES8 M17OUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLwTWM2OD1zMD65JI5O M3;vT3NCVkeHUh?=
PA-1 NFG4NnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfJTWM2OD1zMT64NkBvVQ>? NEW2eotUSU6JRWK=
Mewo NFzPeY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3Xe|VKSzVyPUGxMlk6KG6P MWPTRW5ITVJ?
HSC-3 M3nOcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTF{LkKxJI5O NGDJRZdUSU6JRWK=
H4 M2\xNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTF{Lk[3JI5O MVPTRW5ITVJ?
BB65-RCC NXXkWlZnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTF{LkeyJI5O M2qwTHNCVkeHUh?=
NCI-H1793 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLDOHhKSzVyPUGyMlgzKG6P NUm3c2F7W0GQR1XS
KARPAS-45 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jaVGlEPTB;MUOuOVEhdk1? NWn3d3h6W0GQR1XS
GCT M3S1bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjLTnpKSzVyPUGzMlY5KG6P Mn3DV2FPT0WU
EoL-1 M{DkZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3M[VIzUUN3ME2xN{46OyCwTR?= NWnIS4xMW0GQR1XS
LB2241-RCC Mn3QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPkTWM2OD1zND6wNUBvVQ>? MmLVV2FPT0WU
ES5 MojnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnWWIJKSzVyPUG0Mlc1KG6P M3nsfXNCVkeHUh?=
LOXIMVI M1K4d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\tTWM2OD1zND65PUBvVQ>? Mk\IV2FPT0WU
COR-L105 Mnm3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLGOHFKSzVyPUG1MlA1KG6P M2jIXHNCVkeHUh?=
P12-ICHIKAWA NUL0UJRbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX75PZR{UUN3ME2xOU4yKG6P M1TzbHNCVkeHUh?=
CHL-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTF3LkS1JI5O MWjTRW5ITVJ?
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CCRF-CEM MljTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnLTWM2OD1zND63PFA6KM7:TR?= NF;t[4hUSU6JRWK=
ZR-75-30 MlnqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFrONldKSzVyPUG2MlM{ODNizszN M13JN3NCVkeHUh?=
A673 NYfzcFZIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXtNFN1UUN3ME2yNE42PTB5IN88US=> NGL0XIdUSU6JRWK=
K-562 Mn;xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWK5[ll{UUN3ME2yPE41OTh|IN88US=> M3z3TXNCVkeHUh?=

... 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]

+ 展开

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]

+ 展开
  • 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]

+ 展开
  • 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+polyethylene glycol 300 (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 powder
in solvent
别名 N/A

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 (g) = 浓度 (mol/L) x 体积 (L) 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 Conditions Sponsor/Collaborators Start Date Phases
NCT03373903 Active not recruiting Respiratory Tract Infections Restorbio Inc. November 15 2017 Phase 2
NCT03373903 Active not recruiting Respiratory Tract Infections Restorbio Inc. November 15 2017 Phase 2
NCT01856101 Terminated Carcinoma Transitional Cell Cliniques universitaires Saint-Luc- Université Catholique de Louvain|Novartis February 2013 Phase 2
NCT01856101 Terminated Carcinoma Transitional Cell Cliniques universitaires Saint-Luc- Université Catholique de Louvain|Novartis February 2013 Phase 2
NCT01717898 Terminated Castrate-resistant Prostate Cancer Charles Ryan|Novartis Pharmaceuticals|University of California San Francisco January 31 2013 Phase 1|Phase 2
NCT01717898 Terminated Castrate-resistant Prostate Cancer Charles Ryan|Novartis Pharmaceuticals|University of California San Francisco January 31 2013 Phase 1|Phase 2

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

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.

PI3K Signaling Pathway Map

PI3K Inhibitors with Unique Features

相关PI3K产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID