Dactolisib (BEZ235, NVP-BEZ235)

Catalog No.S1009

Dactolisib (BEZ235, NVP-BEZ235) Chemical Structure

Molecular Weight(MW): 469.55

Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell.

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Cited by 258 Publications

Purity & Quality Control

Choose Selective PI3K Inhibitors

Biological Activity

Description Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell.
Targets
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
In vitro

BEZ235 significantly reduces the phosphorylation levels of the mTOR activated kinase p70S6K. BEZ235 results in a reduction of S235/S236P-RPS6 levels with IC50 of 6.5 nM. The activity of BEZ235 against mTOR is determined using a biochemical mTOR K-LISA assay with IC50 of 20.7 nM. BEZ235 shows slightly lower activity against its β paralogue with IC50 of 75 nM. The PI3K/Akt/mTOR pathway is often constitutively activated in human tumor cells. BEZ235 blocks PI3K and mTOR kinase activity by binding to the ATP-binding cleft of these enzymes. Both PTEN-null cell lines PC3M and U87MG show a dose-dependent reduction in cell proliferation when treated with increasing concentrations of BEZ235 with an average GI50 of 10-12 nM. [1] BEZ235 is an mTORC1/2 catalytic inhibitor. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Trypanosoma brucei brucei NXfiTYNLSW62aX3pZ5Jw[mmjbDDBd5NigQ>? NWLSZZpJOThiaB?= M13UVmROW09? M4rVfGFvfGm2conwZY5we2:vYXygZYN1cX[rdImge4l1cCCHQ{WwJI9nKDBwMECyOUDPxE1? NITzU3IzPDhyNUm0Oi=>
MCF7 MnrKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHpNE4xOS1zMECg{txO M3TMZ|Q5KGh? NVXoSo5RTE2VTx?= MUjJR|UxRTBwN{Og{txO M{D6SFI{QDdzOUC0
HCT116 MmjhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnpZWQzOC5yMT2xNFAh|ryP NFT0WHI1QCCq NH3mfZdFVVOR Mm\YTWM2OD1zLkG2JO69VQ>? Ml3XNlM5PzF7MES=
U87MG M1jlbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXm2Z3c3OC5yMT2xNFAh|ryP NFjiOXQ1QCCq NIX4dVlFVVOR MUfJR|UxRTFwM{Kg{txO M{H0T|I{QDdzOUC0
HBC4 Mn:1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;IPXoxNjBzLUGwNEDPxE1? NYjLdFJZPDhiaB?= NU\5PIJXVG:pIFfJOVA:NThwNkGgUS=> NFTM[2YzOjN|NkK0Oi=>
BSY1 MnPuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;xNE4xOS1zMECg{txO NVjPT5Z7PDhiaB?= NEjBOlJNd2diR1m1NF0uQC52ODDN NE\2foUzOjN|NkK0Oi=>
HBC5 NHX4ZVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3YN4ExNjBzLUGwNEDPxE1? MXi0PEBp MUDMc4chT0l3ME2tO{45PyCP MWeyNlM{PjJ2Nh?=
MCF7 NXfR[Ik2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvVRZExNjBzLUGwNEDPxE1? NVS2bHhkPDhiaB?= M{j5eGxw\yCJSUWwQU05NjF4IF2= Mn\aNlI{OzZ{NE[=
MDA-MB-231 M{T2SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;ENE4xOS1zMECg{txO NGTRV2g1QCCq MX\Mc4chT0l3ME2tPE4xQSCP MUmyNlM{PjJ2Nh?=
U251 NXmxWIlZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLoNE4xOS1zMECg{txO NF\MbpE1QCCq M2C0T2xw\yCJSUWwQU04NjZ4IF2= M{P6PFIzOzN4MkS2
SF268 NHv4UI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXye3cxNjBzLUGwNEDPxE1? NVuzR|l4PDhiaB?= Mm\rUI9oKEeLNUC9MVcvQTJiTR?= M3\q[VIzOzN4MkS2
SF295 MkjlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWiwMlAyNTFyMDFOwG0> NYfhWXNGPDhiaB?= NHTXOWVNd2diR1m1NF0uQC5|MTDN MXSyNlM{PjJ2Nh?=
SF539 NUfMS4lVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\MNnZNOC5yMT2xNFAh|ryP MXe0PEBp Mn[2UI9oKEeLNUC9MVgvPTliTR?= MWCyNlM{PjJ2Nh?=
SNB75 Mn3FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\4VGFZOC5yMT2xNFAh|ryP NVrxR5FRPDhiaB?= NULnN2J2VG:pIFfJOVA:NThwNUigUS=> MUiyNlM{PjJ2Nh?=
SNB78 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVGwMlAyNTFyMDFOwG0> NFT0R2o1QCCq M2ntTGxw\yCJSUWwQU05NjZ3IF2= M3TiU|IzOzN4MkS2
HCC2998 M3fjXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fp[FAvODFvMUCwJO69VQ>? NE\TdmU1QCCq M3X2[mxw\yCJSUWwQU05NjB3IF2= NHzGWZIzOjN|NkK0Oi=>
KM12 MoLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUiwMlAyNTFyMDFOwG0> MmL6OFghcA>? MmHQUI9oKEeLNUC9MVcvPTRiTR?= MXiyNlM{PjJ2Nh?=
HT-29 Mmf0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonsNE4xOS1zMECg{txO Mo\HOFghcA>? MX\Mc4chT0l3ME2tO{44PSCP MYGyNlM{PjJ2Nh?=
HCT15 MoTuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\UNE4xOS1zMECg{txO NILr[5c1QCCq MkjTUI9oKEeLNUC9MVgvODNiTR?= NH34TGUzOjN|NkK0Oi=>
HCT116 NI\1XlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3GyW|AvODFvMUCwJO69VQ>? NYXlRopHPDhiaB?= MkPZUI9oKEeLNUC9MVcvPjFiTR?= MlLLNlI{OzZ{NE[=
NCI-H23 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvKXmZPOC5yMT2xNFAh|ryP MlvoOFghcA>? MmX2UI9oKEeLNUC9MVcvPjRiTR?= NF3EfpczOjN|NkK0Oi=>
NCI-H226 M3y3R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkThNE4xOS1zMECg{txO MYK0PEBp MVnMc4chT0l3ME2tPE41PCCP MX[yNlM{PjJ2Nh?=
NCI-H522 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInrXpgxNjBzLUGwNEDPxE1? MWC0PEBp MmW2UI9oKEeLNUC9MVgvPDViTR?= M1TzclIzOzN4MkS2
NCI-H438 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;XfJl7OC5yMT2xNFAh|ryP NXv6elVCPDhiaB?= NIDs[oRNd2diR1m1NF0uQC5zMTDN MV2yNlM{PjJ2Nh?=
A549 NUHWN2x3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTNUpZjOC5yMT2xNFAh|ryP MX:0PEBp MWrMc4chT0l3ME2tPE4xPyCP MVyyNlM{PjJ2Nh?=
DMS273 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2[2clAvODFvMUCwJO69VQ>? MmnvOFghcA>? MXvMc4chT0l3ME2tO{45OCCP NXq4WYxOOjJ|M{[yOFY>
DMS114 MlrzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XC[|AvODFvMUCwJO69VQ>? Mmf6OFghcA>? MULMc4chT0l3ME2tPE4{QSCP MnLCNlI{OzZ{NE[=
LOXIMVI MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHEcZh[OC5yMT2xNFAh|ryP MUe0PEBp MmnqUI9oKEeLNUC9MVgvPjZiTR?= M17SVFIzOzN4MkS2
OVCAR3 NUX1T|U{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjvNE4xOS1zMECg{txO NHvz[441QCCq NEjrRYJNd2diR1m1NF0uQC5zNzDN M1P1d|IzOzN4MkS2
OVCAR4 MnriS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XHeFAvODFvMUCwJO69VQ>? NW\JS5JEPDhiaB?= NHfIenFNd2diR1m1NF0uQC53ODDN NUnFOnhVOjJ|M{[yOFY>
OVCAR5 NHPVcodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlL4NE4xOS1zMECg{txO MYe0PEBp NFnvOIFNd2diR1m1NF0uPy53NzDN NFrvOmczOjN|NkK0Oi=>
OVCAR8 NGDwOnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\iNE4xOS1zMECg{txO M3fHdVQ5KGh? MYLMc4chT0l3ME2tO{45PCCP NYG4TVhKOjJ|M{[yOFY>
SKOV3 NXTndHZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jKSlAvODFvMUCwJO69VQ>? MnnQOFghcA>? MYPMc4chT0l3ME2tPE41OSCP NVX6d|dqOjJ|M{[yOFY>
RXF631L MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{Xxb|AvODFvMUCwJO69VQ>? MlnrOFghcA>? MVvMc4chT0l3ME2tPE4zOSCP NV7sbJN{OjJ|M{[yOFY>
ACHN NI\GT5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;QNE4xOS1zMECg{txO MoTNOFghcA>? MXvMc4chT0l3ME2tO{46PSCP MUWyNlM{PjJ2Nh?=
St-4 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HQW|AvODFvMUCwJO69VQ>? M1fiNlQ5KGh? NF\uV4JNd2diR1m1NF0uPy52NzDN NUjZOHBCOjJ|M{[yOFY>
MKN1 NFzhVI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYOwMlAyNTFyMDFOwG0> NFPheGI1QCCq MYXMc4chT0l3ME2tPE41OSCP NHv5S24zOjN|NkK0Oi=>
MKN7 NET2VYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFK1NWcxNjBzLUGwNEDPxE1? MkD4OFghcA>? MWHMc4chT0l3ME2tO{43QCCP MXyyNlM{PjJ2Nh?=
MKN28 MlnPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITQRmkxNjBzLUGwNEDPxE1? NYrFTplIPDhiaB?= M2D1SWxw\yCJSUWwQU04NjB5IF2= MXOyNlM{PjJ2Nh?=
MKN45 NY\t[YlDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHofndEOC5yMT2xNFAh|ryP M33wO|Q5KGh? Mn\zUI9oKEeLNUC9MVgvOzRiTR?= MoPoNlI{OzZ{NE[=
MKN74 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVewMlAyNTFyMDFOwG0> NWiyNoZQPDhiaB?= M{f6[mxw\yCJSUWwQU04NjR{IF2= M2DpVlIzOzN4MkS2
DU145 Ml\RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLOcYtDOC5yMT2xNFAh|ryP NHHWbGI1QCCq NEPORZFNd2diR1m1NF0uQC5zNjDN NXPNRXJkOjJ|M{[yOFY>
PC3 M3Lr[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlq3NE4xOS1zMECg{txO NUj4eGpEPDhiaB?= M4X0e2xw\yCJSUWwQU05NjZ4IF2= Ml;aNlI{OzZ{NE[=
Trypanosoma brucei brucei MV3GeY5kfGmxbjDBd5NigQ>? NUe2bIxOOjByIH7N NUH6V2xQOTJiaB?= NX7v[HNZTE2VTx?= M2nBSGRm[3KnYYPlJIlvKHCqb4PwbI91cWS7bDDpco9{cXSxbDDwbI9{eGijdHWgcIV3\Wx? NWfOOnVXOjR6MEW5OFY>
Trypanosoma brucei brucei NVTNdI1bTnWwY4Tpc44hSXO|YYm= NUnuNIt5OThiaB?= NVLmU|FOTE2VTx?= MmPzTY5pcWKrdHnvckBw\iC{ZXPldJRwei2vZXTpZZRm\CCnbnTvZ5l1d3OrczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiC2cnHud4ZmenKrbjD1dJRic2V? NFXXSYozPDhyNUm0Oi=>
Trypanosoma brucei brucei NHG3R4NHfW6ldHnvckBCe3OjeR?= M3[5TlIxOCCwTR?= M{PG[VEzKGh? NUW2OnJ6TE2VTx?= NYHWPGF{TW[oZXP0JI9vKHOyaHnu[49ugWynaX6gcIV3\Wx? M3\h[VI1QDB3OUS2
Trypanosoma brucei brucei NFSzOoRHfW6ldHnvckBCe3OjeR?= MUKyNFAhdk1? NXr1fXFmOTJiaB?= NEXyXnZFVVOR NV7oPGlqTW[oZXP0JI9vKHCqb4PwbIF1cWS7bHPoc4xqdmVibHX2[Yw> MmXaNlQ5ODV7NE[=
UM-UC-3 NI\BeWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2q3UmlEPTB;M{G1JJBO MX;TRW5ITVJ?
SBC-1 NYTwRY5FT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rmcWlEPTB;N{SyJJBO NXvGSlFCW0GQR1XS
MKN1 NUnoTJBUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPZflc2UUN3ME2yMlghdk1? NV7xeGxGW0GQR1XS
NCI-H720 MoP3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlu4TWM2OD1|LkW3JI5O MlHuV2FPT0WU
BFTC-909 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTNwN{Ggcm0> NGPwV2tUSU6JRWK=
BPH-1 MlXUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33pOmlEPTB;ND63OkBvVQ>? MUHTRW5ITVJ?
PC-3 NHfwZ3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTVwMEmgcm0> M2PIUnNCVkeHUh?=
AN3-CA NYHvO2xET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUWxdFUzUUN3ME21MlU3KG6P MW\TRW5ITVJ?
HN Mn[2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrIVVN[UUN3ME21Mlk3KG6P NHPERmRUSU6JRWK=
HCC2218 MmfoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUG4b|B{UUN3ME22MlYyKG6P M{W1WnNCVkeHUh?=
KP-4 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXvTWM2OD15IH7N MYrTRW5ITVJ?
LU-139 NELHbGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjXTWM2OD15Lke3JI5O NUHLd2F3W0GQR1XS
ETK-1 NVfw[XNoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDhR29KSzVyPUeuPFghdk1? Mn63V2FPT0WU
Ramos-2G6-4C10 NHHTO49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4S4emlEPTB;OD60PUBvVQ>? NFr6fVVUSU6JRWK=
MHH-PREB-1 Mn34S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4O3bmlEPTB;OT6xNkBvVQ>? NIPSe|dUSU6JRWK=
DU-4475 Mni0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPKeYtKSzVyPUmuOFQhdk1? MWjTRW5ITVJ?
NCI-H1666 M1jhTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfJPHp2UUN3ME25MlcyKG6P MVnTRW5ITVJ?
CAMA-1 M3PrcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3v4VWlEPTB;OT64JI5O NX\IU3d3W0GQR1XS
TYK-nu NVrxfGk1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2[wZ2lEPTB;OT65OEBvVQ>? NH3ONHZUSU6JRWK=
MFE-280 M{\mfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LoO2lEPTB;OT65PUBvVQ>? MW\TRW5ITVJ?
A549 NVTTN2hbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTFyLkG0JI5O NFnYPWtUSU6JRWK=
769-P NY\IbmExT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXTU|BlUUN3ME2xNE41PCCwTR?= M3m5[XNCVkeHUh?=
L-363 NEH0PHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDWVpdKSzVyPUGwMlY6KG6P M1PCU3NCVkeHUh?=
ES8 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnuzTWM2OD1zMD65JI5O Mnq3V2FPT0WU
PA-1 NFTNNnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGGwc4ZKSzVyPUGxMlgzKG6P MVzTRW5ITVJ?
Mewo NHPmXGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;JXWJKSzVyPUGxMlk6KG6P M2rWO3NCVkeHUh?=
HSC-3 NGXBOJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfD[3NKSzVyPUGyMlIyKG6P NF;KbI5USU6JRWK=
H4 M4Hic2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfTNYZKSzVyPUGyMlY4KG6P NWryU3YxW0GQR1XS
BB65-RCC M1TBeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2[xTGlEPTB;MUKuO|Ihdk1? M1rqTHNCVkeHUh?=
NCI-H1793 M2Ly[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTF{LkiyJI5O MoHJV2FPT0WU
KARPAS-45 M2m5emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLHW25KSzVyPUGzMlUyKG6P MWPTRW5ITVJ?
GCT M3PHUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnVV|dPUUN3ME2xN{43QCCwTR?= NInQU4hUSU6JRWK=
EoL-1 M2XSd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTF|LkmzJI5O MoPxV2FPT0WU
LB2241-RCC NHTFcJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jzT2lEPTB;MUSuNFEhdk1? Mmf5V2FPT0WU
ES5 MlTpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{C2WmlEPTB;MUSuO|Qhdk1? NX;RSFl{W0GQR1XS
LOXIMVI MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYXpZ2U6UUN3ME2xOE46QSCwTR?= MXHTRW5ITVJ?
COR-L105 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWWwfZo6UUN3ME2xOU4xPCCwTR?= MnroV2FPT0WU
P12-ICHIKAWA MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTF3LkGgcm0> MoHNV2FPT0WU
CHL-1 NWPyOnJUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vld2lEPTB;MUWuOFUhdk1? MmTnV2FPT0WU
VMRC-RCZ Mn3ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTF3Lk[zJI5O MVPTRW5ITVJ?
HH NUnQXVZrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrDRXFKSzVyPUG1Mlchdk1? M4myenNCVkeHUh?=
NUGC-3 NITwVWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTF4LkO0JI5O NGHHVWFUSU6JRWK=
EGI-1 NGD5V49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TDZ2lEPTB;MU[uOFMhdk1? NGjVSVBUSU6JRWK=
OS-RC-2 NGHoUHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFz3TZdKSzVyPUG2MlQ4KG6P M{jHTXNCVkeHUh?=
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KM12 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTJ|NT63JI5O MmDXV2FPT0WU
BT-474 MmHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTJ|NT63N{BvVQ>? MonkV2FPT0WU
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HT-1197 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nzUWlEPTB;MkO4MlA6KG6P MnfXV2FPT0WU
CAL-54 NXLhTpdtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXWS5FTUUN3ME2yN|gvPDlibl2= M{GwbnNCVkeHUh?=
NB10 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTJ2MD6wOkBvVQ>? M4LRSXNCVkeHUh?=
PANC-10-05 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXMclRmUUN3ME2yOFUvPTZibl2= NGrI[m5USU6JRWK=
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HCE-4 MnLhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTJ4Mj61JI5O NYTTdYdKW0GQR1XS
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HCC38 NXr5TnFUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlf2TWM2OD1{Nk[uOFghdk1? M2Hnd3NCVkeHUh?=
FADU MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjjO4RKSzVyPUK2Ok43OyCwTR?= MlrzV2FPT0WU
CW-2 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmWzTWM2OD1{NkmuPVYhdk1? NHPGPG1USU6JRWK=
L-428 Mlu3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2O0SmlEPTB;Mke1MlE2KG6P NGTaWWJUSU6JRWK=
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NCI-H810 M4PiU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvVTWM2OD1{N{iuN|Ehdk1? NGXuS4hUSU6JRWK=
LB771-HNC MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37Wb2lEPTB;Mki1Mlg1KG6P M2jBZnNCVkeHUh?=
LCLC-103H MkDKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUKyd4Z[UUN3ME2yPFUvQTlibl2= M1HPN3NCVkeHUh?=
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CAL-72 NGnvS3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DXeGlEPTB;MkmzMlE6KG6P NVrrW4d{W0GQR1XS
SCC-9 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLkTWM2OD1{OUOuNlIhdk1? NU[zeo5jW0GQR1XS
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MZ7-mel NYj4Rmh4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrVcZhKSzVyPUOyN{44PiCwTR?= MV\TRW5ITVJ?
NCI-H1770 M32zVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIG0[mFKSzVyPUOyOk44PCCwTR?= NVfBN2pIW0GQR1XS
ChaGo-K-1 Mnz2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXGNWdKSzVyPUOyPE4yKG6P NIj1ZXlUSU6JRWK=
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NCI-SNU-5 MoXKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1riOWlEPTB;M{O2Mlc4KG6P MoDYV2FPT0WU
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OE19 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTN2MD61N{BvVQ>? M2XMS3NCVkeHUh?=
NCI-H1651 Mme0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrSNVVjUUN3ME2zOFQvOThibl2= MWXTRW5ITVJ?
COLO-792 NFv5UZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHX2S|RKSzVyPUO1OE41OiCwTR?= NWDBd4FZW0GQR1XS
ACHN MlP3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWW3NWdvUUN3ME2zOVYvPzFibl2= NFTwV4VUSU6JRWK=
TH-3 M2LrUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7meFNKSzVyPUO3PU46PSCwTR?= NI\uZWhUSU6JRWK=
HT-1376 NFjCUlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnifoZZUUN3ME2zPFQvQDhibl2= MWjTRW5ITVJ?
RH-18 NWq2[2ZFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVXWcZIzUUN3ME2zPVQvPzRibl2= NH7iZmZUSU6JRWK=
NB6 Moq4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXITWM2OD1|OU[uOlYhdk1? M3HwfXNCVkeHUh?=
COLO-320-HSR NH22UlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHez[3RKSzVyPUSwN{4{PyCwTR?= M2LBOXNCVkeHUh?=
UACC-893 MnTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljTTWM2OD12ME[uOFchdk1? MYnTRW5ITVJ?
DSH1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TL[mlEPTB;NEC2MlkyKG6P NXjTXGpoW0GQR1XS
TE-10 NH:0V29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\PTWM2OD12MEeuNFEhdk1? MUTTRW5ITVJ?
HCC70 NXnmR5JOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\jcGlEPTB;NEC5MlIyKG6P NWnvWXMyW0GQR1XS
TGBC11TKB M3rwSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPreWtKSzVyPUSxNE4{OyCwTR?= MV;TRW5ITVJ?
NCI-H727 NEXke41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LVOWlEPTB;NEGyMlEyKG6P NVPjW3JbW0GQR1XS
ALL-PO MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1X6bWlEPTB;NEG1MlY6KG6P NYGzRZBDW0GQR1XS
ABC-1 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlv5TWM2OD12MkCuOFUhdk1? MkDNV2FPT0WU
NCI-H69 MoCwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\CS3dKSzVyPUSyOk44PiCwTR?= M3ToPHNCVkeHUh?=
GP5d NFnHboZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTR|ND60NUBvVQ>? NInoeoRUSU6JRWK=
UMC-11 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPmTWM2OD12NUiuN|Yhdk1? NFjZPZZUSU6JRWK=
RMG-I NI[3O5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjlRo9wUUN3ME20OlcvPTZibl2= M1\HRnNCVkeHUh?=
YAPC M3\5TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzHTWM2OD12OUCuOkBvVQ>? MlPoV2FPT0WU
LS-1034 NUjjfZNtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXGOpZTUUN3ME20PVEvODZibl2= MkPyV2FPT0WU
RCM-1 NUXBdmg{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzuNHZKSzVyPUS5Ok43QCCwTR?= MlLDV2FPT0WU
HCC1954 MoHOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTVzMj61JI5O MX\TRW5ITVJ?
SK-MEL-24 NG\oSHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnzNTWM2OD13MU[uOVEhdk1? NGTGbXhUSU6JRWK=
NB12 NFfJWnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVLZ[IdHUUN3ME21NlgvPDJibl2= MmTVV2FPT0WU
SW756 M2fr[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3m4OmlEPTB;NUW0Mlk3KG6P NYfMRZRTW0GQR1XS
HCC1187 MlnjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTV5NT64N{BvVQ>? MUPTRW5ITVJ?
NCI-H2342 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXaSWhKSzVyPUW5NE4{QSCwTR?= NVjkVmZ2W0GQR1XS
NCI-H2291 Mn3BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfMR2NKSzVyPUW5PE4{OSCwTR?= M3\KZnNCVkeHUh?=
OVCAR-3 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIH0bG9KSzVyPUW5PE46PiCwTR?= NIPZ[FJUSU6JRWK=
MHH-NB-11 NWfiNZBqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fl[mlEPTB;NkK5MlAyKG6P NGjzOopUSU6JRWK=
SAS NF7QWpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\YTWM2OD14NUKuOlchdk1? NV7jXYFiW0GQR1XS
COLO-824 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHxW5p[UUN3ME22PFkvOzdibl2= NWC2PYNqW0GQR1XS
HCC1395 NIKySIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHTRmtLUUN3ME22PVgvPSCwTR?= NVHYXFhlW0GQR1XS
COLO-668 NVH3bWZ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHK5[GVKSzVyPUewOk4yKG6P NETQfIJUSU6JRWK=
NCI-H226 M17YUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2i1S2lEPTB;N{C3Mlghdk1? NWC3bHhVW0GQR1XS
NB17 MkDFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYK2bVNFUUN3ME23NlEvPzVibl2= MnTKV2FPT0WU
SW1463 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\VTWM2OD15M{muNVkhdk1? NHn1THlUSU6JRWK=
TGW NIXLXmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTd4MD6xOUBvVQ>? MoLvV2FPT0WU
NCI-H526 M1z5U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4j1SWlEPTB;OEKzMlU{KG6P MkTtV2FPT0WU
COR-L88 NFv6WHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXvUFRHUUN3ME24OFgvOTJibl2= MVvTRW5ITVJ?
NCI-H441 M1zJdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVK5TJdTUUN3ME24PVUvOjJibl2= MWfTRW5ITVJ?
NCI-H630 NWDLVoJUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1eyR2lEPTB;OUGyMlk3KG6P MXXTRW5ITVJ?
Mo-T MlTPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnlTWM2OD17NEeuPFghdk1? NWDWPGdOW0GQR1XS
JAR MkjVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2W1bmlEPTB;OUW2MlI1KG6P NIKweY1USU6JRWK=
NCI-H1838 M2jreGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULuPI9FUUN3ME2xMlAzOzh6IN88US=> NVjMWZB3W0GQR1XS
DoTc2-4510 NVK3SZdXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3S5b2lEPTB;MT6wO|M4PiEQvF2= NYnsPWUyW0GQR1XS
MKN28 NV3uc5JzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrablY2UUN3ME2xMlA6ODJ2IN88US=> MWLTRW5ITVJ?
HuP-T3 Mmm4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37x[mlEPTB;MT6xNVkxPSEQvF2= NHTPWoxUSU6JRWK=
TE-9 NIfTe4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPWSZVzUUN3ME2xMlEzQTd|IN88US=> M{nFT3NCVkeHUh?=
NY NGfwd|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHsZ2hYUUN3ME2xMlE3Pzl{IN88US=> M2HHWnNCVkeHUh?=
HT55 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXGWpVKSzVyPUGuN|E{PDRizszN M1LDOnNCVkeHUh?=
SW837 M1;Wemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\u[WZzUUN3ME2xMlMzQTd6IN88US=> M3OxUnNCVkeHUh?=
NCI-H2029 MojkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\VTWM2OD1zLkSxO|kyKM7:TR?= NXzJcHh{W0GQR1XS
IST-SL1 NX7TdGxUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTFwNESyOEDPxE1? NUTQbJE2W0GQR1XS
COLO-741 MlLDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fwXWlEPTB;MT60PVc4OSEQvF2= MlHEV2FPT0WU
LU-65 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjuTWM2OD1zLk[yNlQ6KM7:TR?= NWP4N4hXW0GQR1XS
NCI-H1304 MmG5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfiWZRKSzVyPUGuOlU1QThizszN NEPhO2ZUSU6JRWK=
KARPAS-299 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnDZmdpUUN3ME2xMlc6PDd7IN88US=> MWTTRW5ITVJ?
NCI-H358 M{n2Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmq4TWM2OD1zLkm1OVA{KM7:TR?= MkfqV2FPT0WU
OAW-28 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3voSGlEPTB;Mj6wOlkyQSEQvF2= Mli3V2FPT0WU
C8166 NGf4cXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HKPWlEPTB;Mj62N|M6OiEQvF2= NWDyTlJ5W0GQR1XS
COLO-678 NWjuOWZzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{GzZ2lEPTB;Mj64N|c3QCEQvF2= NFXPcY9USU6JRWK=
SK-N-DZ MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HEZ2lEPTB;Mj64OlM5OSEQvF2= NX7X[HpKW0GQR1XS
NCI-H82 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHUTI1KSzVyPUKuPVA{PjlizszN MXPTRW5ITVJ?
JVM-2 NYDDOm1uT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIH3O|RKSzVyPUOuNFMyQDhizszN Mo\SV2FPT0WU
SW1116 M331NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTNwMEW0NVEh|ryP NWj4W2JOW0GQR1XS
MDA-MB-453 NX3jNnZ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TSNmlEPTB;Mz6xNFQ{QSEQvF2= M12wNnNCVkeHUh?=
Calu-6 MnO5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Moq4TWM2OD1|LkG5PVch|ryP MnnNV2FPT0WU
SHP-77 M1XuNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHNepNGUUN3ME2zMlUzQCEQvF2= NXnD[Y9RW0GQR1XS
Capan-2 MkizS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTRwM{K1PFEh|ryP M3\XbHNCVkeHUh?=
SW948 NVrOU|RiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU[wXYFjUUN3ME20Mlc1Pzd7IN88US=> NV;NNXVHW0GQR1XS
HDLM-2 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHq4b2NKSzVyPUWuNFc4OjVizszN NH62S5JUSU6JRWK=
LAN-6 NHLhdY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{ftU2lEPTB;Nj6yNVQ6PSEQvF2= NFHOSWVUSU6JRWK=
LU-135 M2H2Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;aTWM2OD14LkSzNFc4KM7:TR?= MVTTRW5ITVJ?
T84 NWLaS|FUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTZwOUi2OEDPxE1? M1\tfnNCVkeHUh?=
CAPAN-1 NWmxemZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrJVpQxUUN3ME23MlYzOjN|IN88US=> MlrUV2FPT0WU
SW1417 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHrTWM2OD15LkmxO|MyKM7:TR?= MXnTRW5ITVJ?
BALL-1 MkXsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHieXFKSzVyPUiuOVA1ODlizszN MWHTRW5ITVJ?
HT-29 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULsVYF4UUN3ME25MlA4PTl7IN88US=> MW\TRW5ITVJ?
C3A NEHVXIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH61cFJKSzVyPUmuPFg{QTRizszN M2DmbXNCVkeHUh?=
NCI-H1993 M4DJfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETMNVhKSzVyPUGwMlUxQDFizszN NH3JXGNUSU6JRWK=
SK-MEL-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTFzLk[yPFkh|ryP MmfhV2FPT0WU
DU-145 NYXmVIhOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfsTWM2OD1zND61NFUzKM7:TR?= NI\5[2ZUSU6JRWK=
KP-N-YN NVLoUZVtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDXRXVjUUN3ME2xOE42OTB|IN88US=> M{XVPXNCVkeHUh?=
CCRF-CEM M4jHcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTSTWM2OD1zND63PFA6KM7:TR?= NGHFWYhUSU6JRWK=
ZR-75-30 M1\Qb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn32TWM2OD1zNj6zN|A{KM7:TR?= NIrsfJFUSU6JRWK=
A673 NXHzR3AyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPwTWM2OD1{MD61OVA4KM7:TR?= NWexOoptW0GQR1XS
K-562 NXyzS4NiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3NTWM2OD1{OD60NVg{KM7:TR?= NFm5VnRUSU6JRWK=

... 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
In vivo BEZ235 induces regression of the tumors (69%) without statistically significant effect on body weight gain. Altogether, these preliminary in vivo efficacy results show that BEZ235 causes disease stasis when administered orally as a single agent and can enhance the efficacy of other anticancer agents when used in combination studies. [1]

Protocol

Kinase Assay:

[1]

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In vitro Protein Kinase, PI3K, and mTOR Assays:

PI3Kα, β, and δ proteins are composed of the iSH2 domain of p85 NH2-terminally fused to the full-length protein p110 protein, with the exception of α that also does not contain the last 20 amino acids. PI3Kγ is produced as full-length protein deleted for its first 144 amino acids. All constructs are fused to a COOH-terminal His tag for convenient purification and then cloned into the pBlue-Bac4.5 (for α, β, and δ isoforms) or pVL1393 (for γ isoform) plasmids. The different vectors are then cotransfected with BaculoGold WT genomic DNA using methods recommended by the vendor for production of the respective recombinant baculoviruses and proteins. BEZ235 are tested for their activity against PI3K using a Kinase-Glo assay. The kinase reaction is done in 384-well black plate. Each well is loaded with 50 μL of test items (in 90% DMSO) and 5 μL reaction buffer containing 10 μg/mL PI substrate (l-α-phosphatidylinositol; Avanti Polar Lipids; prepared in 3% octyl-glucoside) and the PI3K proteins (10, 25, 10, and 150 nM of p110α, p110β, p110δ, and p110γ, respectively) are then added to it. The reaction is started by the addition of 5 μL of 1 μM ATP prepared in the reaction buffer and is incubated for either 60 (for p110α, p110β, and p110δ) or 120 min (for p110γ). It is terminated by the addition of 10 μL Kinase-Glo buffer. The plates are then read in a Synergy 2 reader for luminescence detection.
Cell Research:

[2]

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

    The human CRC cell lines, HCT116 (PIK3CA mutant; kinase domain at H1047R), DLD-1 (PIK3CA mutant; helical domain at E545K), and SW480 (PIK3CA wild-type) and isogenic DLD-1 PIK3CA mutant as well as wild-type cells are maintained in DMEM with 10% FBS and 1 × Penicillin/Streptomycin. Cells are plated at different initial densities (HCT116: 3 × 103 cells/well, DLD-1: 5.5 × 103 cells/well, SW480: 4.5 × 103 cells/well, DLD-1 PIK3CA mutant: 7 × 103 cells/well, and DLD-1 PIK3CA wild-type: 9 × 103 cells/well) to account for differential growth kinetics. After 16 hours, cells are incubated with increasing concentrations of BEZ235, and the drug-containing growth medium is changed every 24 hours. Cell viability is assessed 16 hours after the initial plating and 48 hours after initiation of drug treatment using the colorimetric MTS assay CellTiter 96® AQueous One Solution Cell Proliferation Assay, as per the manufacturer's instructions. Cell viability after drug treatment is normalized to that of untreated cells also grown for 48 hours. For western blot analysis, cells are plated with zero or maximum inhibitory dose (500 nM) BEZ235 for 2, 6, 24, or 48 hours.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: Female Harlan athymic nude mice
  • Formulation: NMP/polyethylene glycol 300 (10/90, v/v)
  • Dosages: 45 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMF 18 mg/mL warmed (38.33 mM)
DMSO 0.01 mg/mL (0.02 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
NMP+PEG300 (10+90, v+v)
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 469.55
Formula

C30H23N5O

CAS No. 915019-65-7
Storage powder
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • 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):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

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
NCT01482156 Completed Drug: RAD001 + BEZ235 Advanced Solid Tumors|Metastatic Breast Cancer|Metastatic Renal Cell Carcinoma Novartis Pharmaceuticals|Novartis January 2012 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 1:

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

  • Answer:

    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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID