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。Dactolisib可诱导自噬并抑制HIV-1的复制。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286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。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)
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 MkjBRY51cW2rY4LvZolidCCDc4PhfS=> MV[xPEBp MX3EUXNQ M4X4NmFvfGm2conwZY5we2:vYXygZYN1cX[rdImge4l1cCCHQ{WwJI9nKDBwMECyOUDPxE1? NHTkN|kzPDhyNUm0Oi=>
MCF7 NVOxbXBIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvBNE4xOS1zMECg{txO NVGxSnJsPDhiaB?= MWnEUXNQ NFHIR|dKSzVyPUCuO|Mh|ryP NFjDNGMzOzh5MUmwOC=>
HCT116 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjNNm4xOC5yMT2xNFAh|ryP Mlf5OFghcA>? MkXBSG1UVw>? MX7JR|UxRTFwMU[g{txO M2XUe|I{QDdzOUC0
U87MG MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLUNoNZOC5yMT2xNFAh|ryP MYW0PEBp NXzo[4ZWTE2VTx?= M2LGVGlEPTB;MT6zNkDPxE1? MVKyN|g4OTlyNB?=
HBC4 M2C2eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWCwMlAyNTFyMDFOwG0> NYLCeGNJPDhiaB?= M4LSOWxw\yCJSUWwQU05NjZzIF2= NFjMdnozOjN|NkK0Oi=>
BSY1 MmXPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEO3U3UxNjBzLUGwNEDPxE1? MofVOFghcA>? MX\Mc4chT0l3ME2tPE41QCCP Ml3UNlI{OzZ{NE[=
HBC5 M1TDN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXOwMlAyNTFyMDFOwG0> MVu0PEBp MlPXUI9oKEeLNUC9MVcvQDdiTR?= M4DRSVIzOzN4MkS2
MCF7 NYe0NVZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWSwMlAyNTFyMDFOwG0> MVS0PEBp MkfKUI9oKEeLNUC9MVgvOTZiTR?= NYL0ZnI{OjJ|M{[yOFY>
MDA-MB-231 MmfkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\IelAvODFvMUCwJO69VQ>? NF71[pI1QCCq NGS2NJNNd2diR1m1NF0uQC5yOTDN NInydoEzOjN|NkK0Oi=>
U251 Mnf1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnDepZmOC5yMT2xNFAh|ryP M{C5SVQ5KGh? NEHFPGFNd2diR1m1NF0uPy54NjDN MXWyNlM{PjJ2Nh?=
SF268 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYmwMlAyNTFyMDFOwG0> NV7DTXdLPDhiaB?= M2K3VWxw\yCJSUWwQU04Njl{IF2= NUW0NVJ5OjJ|M{[yOFY>
SF295 NEXHXWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DwblAvODFvMUCwJO69VQ>? M4nhOFQ5KGh? NHvQUI9Nd2diR1m1NF0uQC5|MTDN M1vvZ|IzOzN4MkS2
SF539 NXq4NYQ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PVflAvODFvMUCwJO69VQ>? M1\DNFQ5KGh? MXXMc4chT0l3ME2tPE42QSCP NV76c4JzOjJ|M{[yOFY>
SNB75 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrxRVJCOC5yMT2xNFAh|ryP NF[4ZlM1QCCq NX22V4dwVG:pIFfJOVA:NThwNUigUS=> MXSyNlM{PjJ2Nh?=
SNB78 NGHzNZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY[wMlAyNTFyMDFOwG0> MnvqOFghcA>? NGPuS3dNd2diR1m1NF0uQC54NTDN NXnlVIR2OjJ|M{[yOFY>
HCC2998 M3zDXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWGwMlAyNTFyMDFOwG0> MlXvOFghcA>? MUnMc4chT0l3ME2tPE4xPSCP M4nZWlIzOzN4MkS2
KM12 MkHTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzBNE4xOS1zMECg{txO NFH5VIo1QCCq NW\GU5I3VG:pIFfJOVA:NTdwNUSgUS=> M1f2WlIzOzN4MkS2
HT-29 NUHHW5BoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPYSZVsOC5yMT2xNFAh|ryP M1fneVQ5KGh? NIXMWGpNd2diR1m1NF0uPy55NTDN MX6yNlM{PjJ2Nh?=
HCT15 M{fUfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\ONE4xOS1zMECg{txO MYG0PEBp MlnUUI9oKEeLNUC9MVgvODNiTR?= M{O5blIzOzN4MkS2
HCT116 NV:1WFFsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fXRVAvODFvMUCwJO69VQ>? MkLVOFghcA>? Mmi0UI9oKEeLNUC9MVcvPjFiTR?= M2DrO|IzOzN4MkS2
NCI-H23 M{O3Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rVRlAvODFvMUCwJO69VQ>? MnLJOFghcA>? MkD2UI9oKEeLNUC9MVcvPjRiTR?= MorhNlI{OzZ{NE[=
NCI-H226 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY[xTVQ3OC5yMT2xNFAh|ryP NX62eZc5PDhiaB?= MlrKUI9oKEeLNUC9MVgvPDRiTR?= NEHnUIszOjN|NkK0Oi=>
NCI-H522 NIL6eIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjyVGsxNjBzLUGwNEDPxE1? MWi0PEBp NVntflhHVG:pIFfJOVA:NThwNEWgUS=> M2r2TFIzOzN4MkS2
NCI-H438 NFf5OFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XkVlAvODFvMUCwJO69VQ>? NXTzVHdTPDhiaB?= MmXQUI9oKEeLNUC9MVgvOTFiTR?= M4HkOlIzOzN4MkS2
A549 NYO3doFkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknjNE4xOS1zMECg{txO M4X3TFQ5KGh? NHfh[nFNd2diR1m1NF0uQC5yNzDN M3vETFIzOzN4MkS2
DMS273 M3rlUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjFZZAxNjBzLUGwNEDPxE1? MVS0PEBp M{\sWGxw\yCJSUWwQU04NjhyIF2= MY[yNlM{PjJ2Nh?=
DMS114 M1n3e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrEUmIxNjBzLUGwNEDPxE1? MXq0PEBp M1jDRmxw\yCJSUWwQU05NjN7IF2= MmPXNlI{OzZ{NE[=
LOXIMVI M{G2cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF32boExNjBzLUGwNEDPxE1? NEDje3Q1QCCq MnG1UI9oKEeLNUC9MVgvPjZiTR?= NIXIb5IzOjN|NkK0Oi=>
OVCAR3 NHfBRmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfjNE4xOS1zMECg{txO MkG4OFghcA>? M4HGOWxw\yCJSUWwQU05NjF5IF2= M1L1XlIzOzN4MkS2
OVCAR4 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPYSXM3OC5yMT2xNFAh|ryP NGPL[Zc1QCCq NVnPcIVMVG:pIFfJOVA:NThwNUigUS=> NX21OJBIOjJ|M{[yOFY>
OVCAR5 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYmwMlAyNTFyMDFOwG0> Mlm3OFghcA>? M4f6ZWxw\yCJSUWwQU04NjV5IF2= M2jOeVIzOzN4MkS2
OVCAR8 Mkf3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXuwMlAyNTFyMDFOwG0> MmTyOFghcA>? M{nmU2xw\yCJSUWwQU04Njh2IF2= MVOyNlM{PjJ2Nh?=
SKOV3 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLNdlUxNjBzLUGwNEDPxE1? NUCxNY5jPDhiaB?= MV\Mc4chT0l3ME2tPE41OSCP MV:yNlM{PjJ2Nh?=
RXF631L M1OyZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHuxNJYxNjBzLUGwNEDPxE1? NF[5c4g1QCCq M3\Kfmxw\yCJSUWwQU05NjJzIF2= NH3TfWszOjN|NkK0Oi=>
ACHN Mn3aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXe0UZJ[OC5yMT2xNFAh|ryP MV[0PEBp NVPwXoV2VG:pIFfJOVA:NTdwOUWgUS=> M3rrdlIzOzN4MkS2
St-4 NXn4WlUyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIm3[2kxNjBzLUGwNEDPxE1? MV[0PEBp MofuUI9oKEeLNUC9MVcvPDdiTR?= M1;JfVIzOzN4MkS2
MKN1 M1jwb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2n4W|AvODFvMUCwJO69VQ>? M{C4VlQ5KGh? MXnMc4chT0l3ME2tPE41OSCP M1vRNFIzOzN4MkS2
MKN7 NGq4NllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofsNE4xOS1zMECg{txO NUHOdGUyPDhiaB?= M3Hx[2xw\yCJSUWwQU04NjZ6IF2= MXGyNlM{PjJ2Nh?=
MKN28 NYPOb3hDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmS3NE4xOS1zMECg{txO MVm0PEBp MWTMc4chT0l3ME2tO{4xPyCP MnWxNlI{OzZ{NE[=
MKN45 M175[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\OSYMxNjBzLUGwNEDPxE1? MnPNOFghcA>? MWHMc4chT0l3ME2tPE4{PCCP MV:yNlM{PjJ2Nh?=
MKN74 MnP6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITpUokxNjBzLUGwNEDPxE1? NWH1[lJbPDhiaB?= M{WweGxw\yCJSUWwQU04NjR{IF2= Ml7zNlI{OzZ{NE[=
DU145 MknOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M121XVAvODFvMUCwJO69VQ>? NWHTN|R3PDhiaB?= NH7sUGpNd2diR1m1NF0uQC5zNjDN MWSyNlM{PjJ2Nh?=
PC3 MoPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFixUFgxNjBzLUGwNEDPxE1? NVXhXGpNPDhiaB?= M37WbGxw\yCJSUWwQU05NjZ4IF2= Ml7FNlI{OzZ{NE[=
Trypanosoma brucei brucei MkjVSpVv[3Srb36gRZN{[Xl? NF;1c5YzODBibl2= MoHCNVIhcA>? MnjISG1UVw>? M1T2XmRm[3KnYYPlJIlvKHCqb4PwbI91cWS7bDDpco9{cXSxbDDwbI9{eGijdHWgcIV3\Wx? NWi3WHJbOjR6MEW5OFY>
Trypanosoma brucei brucei MXXGeY5kfGmxbjDBd5NigQ>? M3XHUVE5KGh? M2DFVmROW09? NXnIcodTUW6qaXLpeIlwdiCxZjDy[YNmeHSxcj3t[YRq[XSnZDDlcoRw[3m2b4Ppd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjD0doFve2[ncoLpckB2eHSja3W= MWCyOFgxPTl2Nh?=
Trypanosoma brucei brucei MnuwSpVv[3Srb36gRZN{[Xl? MkDaNlAxKG6P NFnkflMyOiCq MXTEUXNQ NHTleYZG\m[nY4Sgc44he3CqaX7nc416dGWrbjDs[ZZmdA>? NW\HRXpiOjR6MEW5OFY>
Trypanosoma brucei brucei MWnGeY5kfGmxbjDBd5NigQ>? M{fHO|IxOCCwTR?= M1P0TVEzKGh? NHrTWYRFVVOR NH7ZbZlG\m[nY4Sgc44heGixc4DoZZRq\HmuY3jvcIlv\SCuZY\lcC=> MmrQNlQ5ODV7NE[=
UM-UC-3 NWOwZoc6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfuOGdSUUN3ME2zNVUheE1? MUXTRW5ITVJ?
SBC-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULSVIN[UUN3ME23OFIheE1? MkPTV2FPT0WU
MKN1 NFPTZnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTJwODDuUS=> NV\HcmF2W0GQR1XS
NCI-H720 M1vrfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDydYpJUUN3ME2zMlU4KG6P NF\sc5ZUSU6JRWK=
BFTC-909 NEfZdlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33WPGlEPTB;Mz63NUBvVQ>? NYLWXoRqW0GQR1XS
BPH-1 M{TpVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHYTWM2OD12Lke2JI5O M3HX[3NCVkeHUh?=
PC-3 M3jWWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{P5OWlEPTB;NT6wPUBvVQ>? NWPTN4NEW0GQR1XS
AN3-CA NX3EUlFbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTVwNU[gcm0> MUnTRW5ITVJ?
HN Mmf1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTVwOU[gcm0> NFLPdHhUSU6JRWK=
HCC2218 MkXnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTZwNkGgcm0> MkHZV2FPT0WU
KP-4 NXK0TGRKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3kWFNwUUN3ME23JI5O M1LVR3NCVkeHUh?=
LU-139 M4KzbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjWTWM2OD15Lke3JI5O MXfTRW5ITVJ?
ETK-1 NIfiVYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYrpbJhKUUN3ME23Mlg5KG6P M1HlVXNCVkeHUh?=
Ramos-2G6-4C10 NVrJ[Hk6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRThwNEmgcm0> MlLYV2FPT0WU
MHH-PREB-1 MoHhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFyx[FJKSzVyPUmuNVIhdk1? M{jCWnNCVkeHUh?=
DU-4475 NG[zdopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFG4bXRKSzVyPUmuOFQhdk1? NUPxRmlrW0GQR1XS
NCI-H1666 MoLlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHGb2w5UUN3ME25MlcyKG6P NFzvRoJUSU6JRWK=
CAMA-1 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TrUmlEPTB;OT64JI5O MmDWV2FPT0WU
TYK-nu M4faXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nj[WlEPTB;OT65OEBvVQ>? NITNdXJUSU6JRWK=
MFE-280 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TRcmlEPTB;OT65PUBvVQ>? MkXnV2FPT0WU
A549 NWDtSHpWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF64dGhKSzVyPUGwMlE1KG6P M1nDW3NCVkeHUh?=
769-P MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTFyLkS0JI5O M2HBfnNCVkeHUh?=
L-363 M2HIPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGG2XWJKSzVyPUGwMlY6KG6P MWTTRW5ITVJ?
ES8 NGr4XolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\0bpJKSzVyPUGwMlkhdk1? NVHnOHlmW0GQR1XS
PA-1 NV24c5hST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVXxOYdqUUN3ME2xNU45OiCwTR?= MmnaV2FPT0WU
Mewo NXPieVhRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33Rc2lEPTB;MUGuPVkhdk1? M1ewbHNCVkeHUh?=
HSC-3 M1zncWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vtdWlEPTB;MUKuNlEhdk1? NY\lU4w2W0GQR1XS
H4 MlnYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3QfJREUUN3ME2xNk43PyCwTR?= MXfTRW5ITVJ?
BB65-RCC M123bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGC4XZBKSzVyPUGyMlczKG6P MWTTRW5ITVJ?
NCI-H1793 M4rXWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TiRmlEPTB;MUKuPFIhdk1? MV\TRW5ITVJ?
KARPAS-45 NVTOVmo4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jlWWlEPTB;MUOuOVEhdk1? MlO0V2FPT0WU
GCT NFHCTWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn30TWM2OD1zMz62PEBvVQ>? M{CzTHNCVkeHUh?=
EoL-1 MnWzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPWSYduUUN3ME2xN{46OyCwTR?= NGrwXW1USU6JRWK=
LB2241-RCC NEHtcoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTF2LkCxJI5O MWDTRW5ITVJ?
ES5 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fiSWlEPTB;MUSuO|Qhdk1? NH\5UJFUSU6JRWK=
LOXIMVI NEXPR4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;5dZVKSzVyPUG0Mlk6KG6P MWXTRW5ITVJ?
COR-L105 NH:5WJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3zfphKSzVyPUG1MlA1KG6P Mn;kV2FPT0WU
P12-ICHIKAWA MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTF3LkGgcm0> MWrTRW5ITVJ?
CHL-1 MmLvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTF3LkS1JI5O MVnTRW5ITVJ?
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SK-MEL-1 M4nVeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nsdGlEPTB;MUGuOlI5QSEQvF2= NETMTHlUSU6JRWK=
DU-145 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV75PVNqUUN3ME2xOE42ODV{IN88US=> MlK2V2FPT0WU
KP-N-YN MofkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPLTWM2OD1zND61NVA{KM7:TR?= NFXCd5NUSU6JRWK=
CCRF-CEM M{\ycmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;mVnJKSzVyPUG0Mlc5ODlizszN Ml24V2FPT0WU
ZR-75-30 M33NVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonxTWM2OD1zNj6zN|A{KM7:TR?= MXHTRW5ITVJ?
A673 MkLpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTJyLkW1NFch|ryP M1y1d3NCVkeHUh?=
K-562 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PiWmlEPTB;MkiuOFE5OyEQvF2= NH7EUGZUSU6JRWK=

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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