Dactolisib (BEZ235)

For research use only.

Catalog No.S1009 Synonyms: NVP-BEZ235

286 publications

Dactolisib (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. Dactolisib induces autophagy and suppresses HIV-1 replication. Phase 2.

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Selleck's Dactolisib (BEZ235) has been cited by 286 publications

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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. Dactolisib induces autophagy and suppresses HIV-1 replication. Phase 2.
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 NHz3fWhCdnSrbXnjdo9jcWGuIFHzd4F6 M2TucFE5KGh? NH;pZ2VFVVOR M4TkeWFvfGm2conwZY5we2:vYXygZYN1cX[rdImge4l1cCCHQ{WwJI9nKDBwMECyOUDPxE1? MlH4NlQ5ODV7NE[=
MCF7 M4HWdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX[wMlAyNTFyMDFOwG0> NXz1V4RCPDhiaB?= M{Tw[mROW09? NFG2WZVKSzVyPUCuO|Mh|ryP MWiyN|g4OTlyNB?=
HCT116 NHPu[WNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfWNE4xOS1zMECg{txO NITISHA1QCCq M{Tte2ROW09? M{HMXmlEPTB;MT6xOkDPxE1? MmXQNlM5PzF7MES=
U87MG M4PSfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2OweFAvODFvMUCwJO69VQ>? NFuyRY01QCCq MlzmSG1UVw>? M13hb2lEPTB;MT6zNkDPxE1? MV2yN|g4OTlyNB?=
HBC4 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnveWh6OC5yMT2xNFAh|ryP MVe0PEBp MorkUI9oKEeLNUC9MVgvPjFiTR?= MoS1NlI{OzZ{NE[=
BSY1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;ENVAvODFvMUCwJO69VQ>? M3TNXlQ5KGh? NWKyc4tHVG:pIFfJOVA:NThwNEigUS=> NX\JfG9JOjJ|M{[yOFY>
HBC5 NYOxTVZuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXqNE4xOS1zMECg{txO NHLoPWQ1QCCq M2nTVmxw\yCJSUWwQU04Njh5IF2= NYj1WHhlOjJ|M{[yOFY>
MCF7 NVXaW2FYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPoNE4xOS1zMECg{txO M1j5eFQ5KGh? MkmwUI9oKEeLNUC9MVgvOTZiTR?= NVnqTpRSOjJ|M{[yOFY>
MDA-MB-231 MorzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV:wMlAyNTFyMDFOwG0> M4rxelQ5KGh? M3vBdmxw\yCJSUWwQU05NjB7IF2= Mn3sNlI{OzZ{NE[=
U251 M121W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HTWVAvODFvMUCwJO69VQ>? NYP0d3E6PDhiaB?= MXLMc4chT0l3ME2tO{43PiCP MYeyNlM{PjJ2Nh?=
SF268 NF\WOGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17IRlAvODFvMUCwJO69VQ>? MYW0PEBp NEPrZ29Nd2diR1m1NF0uPy57MjDN NUDHeFlIOjJ|M{[yOFY>
SF295 NHTEVmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4ju[|AvODFvMUCwJO69VQ>? M3P4elQ5KGh? MnjPUI9oKEeLNUC9MVgvOzFiTR?= Ml;CNlI{OzZ{NE[=
SF539 NEn1UHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jEV|AvODFvMUCwJO69VQ>? NHTqdpE1QCCq M{e0VGxw\yCJSUWwQU05NjV7IF2= MYKyNlM{PjJ2Nh?=
SNB75 NHuzVZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1P1XlAvODFvMUCwJO69VQ>? MoP5OFghcA>? MYrMc4chT0l3ME2tPE42QCCP Mly2NlI{OzZ{NE[=
SNB78 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MViwMlAyNTFyMDFOwG0> NFG1T4o1QCCq NFrGbJpNd2diR1m1NF0uQC54NTDN NYX2dXdYOjJ|M{[yOFY>
HCC2998 M3i1dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX6ybZVKOC5yMT2xNFAh|ryP NIfGR2E1QCCq M3PTdGxw\yCJSUWwQU05NjB3IF2= Mm\BNlI{OzZ{NE[=
KM12 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYGwMlAyNTFyMDFOwG0> NXPWPFlFPDhiaB?= MkP0UI9oKEeLNUC9MVcvPTRiTR?= NVzrNGZFOjJ|M{[yOFY>
HT-29 MoDKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYKwMlAyNTFyMDFOwG0> M1W0XFQ5KGh? NW[zU29xVG:pIFfJOVA:NTdwN{WgUS=> NHzsOFczOjN|NkK0Oi=>
HCT15 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHJN2wxNjBzLUGwNEDPxE1? M2DrNlQ5KGh? M1LHSmxw\yCJSUWwQU05NjB|IF2= MWGyNlM{PjJ2Nh?=
HCT116 M13VcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHXeJQxNjBzLUGwNEDPxE1? M2fRSVQ5KGh? NFjmdXlNd2diR1m1NF0uPy54MTDN NF32N2wzOjN|NkK0Oi=>
NCI-H23 M3LoV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfDNE4xOS1zMECg{txO NUHYbWQ3PDhiaB?= M1LiWGxw\yCJSUWwQU04NjZ2IF2= MWWyNlM{PjJ2Nh?=
NCI-H226 MnPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXOwMlAyNTFyMDFOwG0> NYfiTo9KPDhiaB?= M1Tvd2xw\yCJSUWwQU05NjR2IF2= MYeyNlM{PjJ2Nh?=
NCI-H522 M1rK[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWqwMlAyNTFyMDFOwG0> MlTpOFghcA>? MXvMc4chT0l3ME2tPE41PSCP MkHpNlI{OzZ{NE[=
NCI-H438 NIPDcopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\nNE4xOS1zMECg{txO NXPzXHM6PDhiaB?= M4\scmxw\yCJSUWwQU05NjFzIF2= NVjIXZM3OjJ|M{[yOFY>
A549 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPjVGFCOC5yMT2xNFAh|ryP NYHNN5ZmPDhiaB?= M13DfWxw\yCJSUWwQU05NjB5IF2= M4DJVVIzOzN4MkS2
DMS273 NFfUdoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XZ[FAvODFvMUCwJO69VQ>? NVz6dXd{PDhiaB?= NYG3XoRRVG:pIFfJOVA:NTdwOECgUS=> MYOyNlM{PjJ2Nh?=
DMS114 MljHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjUNE4xOS1zMECg{txO NHv3dow1QCCq MmPLUI9oKEeLNUC9MVgvOzliTR?= M2rKNlIzOzN4MkS2
LOXIMVI MkDzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUS0TYkxOC5yMT2xNFAh|ryP M13mbVQ5KGh? NUT5blRUVG:pIFfJOVA:NThwNk[gUS=> NV\E[JB{OjJ|M{[yOFY>
OVCAR3 NGW4eFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\E[Gs2OC5yMT2xNFAh|ryP M2fWXVQ5KGh? M2\jUmxw\yCJSUWwQU05NjF5IF2= MoXiNlI{OzZ{NE[=
OVCAR4 NFW5XYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3e2bVAvODFvMUCwJO69VQ>? NUm4PXFbPDhiaB?= NYqzbWZUVG:pIFfJOVA:NThwNUigUS=> NUnqfHBYOjJ|M{[yOFY>
OVCAR5 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF:5Z2kxNjBzLUGwNEDPxE1? Mo\ZOFghcA>? NGHEZZZNd2diR1m1NF0uPy53NzDN MnfGNlI{OzZ{NE[=
OVCAR8 NWTySHhYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13nclAvODFvMUCwJO69VQ>? M4nwfVQ5KGh? NVLRZ|Y2VG:pIFfJOVA:NTdwOESgUS=> M2DL[FIzOzN4MkS2
SKOV3 MnuwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fkSVAvODFvMUCwJO69VQ>? NX7VcIxKPDhiaB?= Moj1UI9oKEeLNUC9MVgvPDFiTR?= MX6yNlM{PjJ2Nh?=
RXF631L MnPOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInkbXUxNjBzLUGwNEDPxE1? NWXOeopsPDhiaB?= NHfvXFJNd2diR1m1NF0uQC5{MTDN NVLlfopoOjJ|M{[yOFY>
ACHN M1;YV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPCZ2FDOC5yMT2xNFAh|ryP NX3odpdsPDhiaB?= NYPlXW9kVG:pIFfJOVA:NTdwOUWgUS=> MVSyNlM{PjJ2Nh?=
St-4 M1O5XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjkNE4xOS1zMECg{txO MUC0PEBp NEThSGRNd2diR1m1NF0uPy52NzDN NFjRXYszOjN|NkK0Oi=>
MKN1 NXnscVJET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTGTY4xNjBzLUGwNEDPxE1? MkjhOFghcA>? NV3EVJNSVG:pIFfJOVA:NThwNEGgUS=> MnPzNlI{OzZ{NE[=
MKN7 M{\lOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jG[FAvODFvMUCwJO69VQ>? MkPROFghcA>? NIXzUI1Nd2diR1m1NF0uPy54ODDN NV7lSZhnOjJ|M{[yOFY>
MKN28 NIe0dmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmD0NE4xOS1zMECg{txO NVP2SZFtPDhiaB?= MV\Mc4chT0l3ME2tO{4xPyCP NEnQUmIzOjN|NkK0Oi=>
MKN45 NV3STmwzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LBd|AvODFvMUCwJO69VQ>? NHrQV481QCCq NWi2TWhPVG:pIFfJOVA:NThwM{SgUS=> MYWyNlM{PjJ2Nh?=
MKN74 NFXzeFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY[wMlAyNTFyMDFOwG0> MVW0PEBp Mn[zUI9oKEeLNUC9MVcvPDJiTR?= NH7NXoQzOjN|NkK0Oi=>
DU145 NGfMdZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGKxZ5MxNjBzLUGwNEDPxE1? M2HFN|Q5KGh? NUntd5lsVG:pIFfJOVA:NThwMU[gUS=> M{j2VFIzOzN4MkS2
PC3 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUSwMlAyNTFyMDFOwG0> NYC3ZVJ5PDhiaB?= M4rvbWxw\yCJSUWwQU05NjZ4IF2= NInUT5czOjN|NkK0Oi=>
Trypanosoma brucei brucei MoTXSpVv[3Srb36gRZN{[Xl? NUXTRVNjOjByIH7N MYqxNkBp M2S2UmROW09? MW\E[YNz\WG|ZTDpckBxcG:|cHjveIllgWxiaX7vd4l1d2xicHjvd5Bp[XSnIHzleoVt NHXROm0zPDhyNUm0Oi=>
Trypanosoma brucei brucei NFnISmpHfW6ldHnvckBCe3OjeR?= MYSxPEBp MonLSG1UVw>? Mn\DTY5pcWKrdHnvckBw\iC{ZXPldJRwei2vZXTpZZRm\CCnbnTvZ5l1d3OrczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiC2cnHud4ZmenKrbjD1dJRic2V? NX7EfoRROjR6MEW5OFY>
Trypanosoma brucei brucei MmXPSpVv[3Srb36gRZN{[Xl? NV\VbHV5OjByIH7N M2O1N|EzKGh? Mmf2SG1UVw>? M1y5SWVn\mWldDDvckB{eGirbnfvcZlt\WmwIHzleoVt M{L0VlI1QDB3OUS2
Trypanosoma brucei brucei M{HQVWZ2dmO2aX;uJGF{e2G7 MlvqNlAxKG6P NWnH[4QyOTJiaB?= MnTJSG1UVw>? M4rlOGVn\mWldDDvckBxcG:|cHjheIllgWylaH;sbY5mKGyndnXs NF;w[pIzPDhyNUm0Oi=>
UM-UC-3 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofETWM2OD1|MUWgdG0> MWPTRW5ITVJ?
SBC-1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MorqTWM2OD15NEKgdG0> NHv0OGhUSU6JRWK=
MKN1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjVOI1KSzVyPUKuPEBvVQ>? MY\TRW5ITVJ?
NCI-H720 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPmWYlkUUN3ME2zMlU4KG6P NXT5Vm9XW0GQR1XS
BFTC-909 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17jVGlEPTB;Mz63NUBvVQ>? MUPTRW5ITVJ?
BPH-1 M2flWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTRwN{[gcm0> MVTTRW5ITVJ?
PC-3 NF\4ZVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTVwMEmgcm0> MlX2V2FPT0WU
AN3-CA NGGxfXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWn5fHZHUUN3ME21MlU3KG6P M1nkT3NCVkeHUh?=
HN MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DHV2lEPTB;NT65OkBvVQ>? MVrTRW5ITVJ?
HCC2218 M4Th[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTuTWM2OD14Lk[xJI5O NGmzOJVUSU6JRWK=
KP-4 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\kNoN6UUN3ME23JI5O MXrTRW5ITVJ?
LU-139 NH\FS|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjuTWM2OD15Lke3JI5O NFfoNIlUSU6JRWK=
ETK-1 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTvZ5ZKSzVyPUeuPFghdk1? MVLTRW5ITVJ?
Ramos-2G6-4C10 NIPuVY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRThwNEmgcm0> NXz6VZk3W0GQR1XS
MHH-PREB-1 NIPYNXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LmfmlEPTB;OT6xNkBvVQ>? NUiwfGs3W0GQR1XS
DU-4475 M2naNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnQSpFJUUN3ME25MlQ1KG6P Mk[zV2FPT0WU
NCI-H1666 M4LVPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\tR5J1UUN3ME25MlcyKG6P MkDqV2FPT0WU
CAMA-1 NIfafIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTlwODDuUS=> Ml:4V2FPT0WU
TYK-nu M1zkTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfuTZNKSzVyPUmuPVQhdk1? NFjtW5pUSU6JRWK=
MFE-280 MlzLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTlwOUmgcm0> MmqzV2FPT0WU
A549 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3NPXlbUUN3ME2xNE4yPCCwTR?= Mn2zV2FPT0WU
769-P NF;Ld3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1f1[2lEPTB;MUCuOFQhdk1? Mn;XV2FPT0WU
L-363 MmHBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvIXGlHUUN3ME2xNE43QSCwTR?= NEDnVppUSU6JRWK=
ES8 NH;ncXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfiTWM2OD1zMD65JI5O Mlq5V2FPT0WU
PA-1 NVfQd2ZbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfBTWM2OD1zMT64NkBvVQ>? NXfnVoJ1W0GQR1XS
Mewo M2fuUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXL3dllFUUN3ME2xNU46QSCwTR?= M4\4b3NCVkeHUh?=
HSC-3 NXfuPXk3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTF{LkKxJI5O NWXBS4h3W0GQR1XS
H4 NInITm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnETWM2OD1zMj62O{BvVQ>? NIH2OXNUSU6JRWK=
BB65-RCC MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HkOGlEPTB;MUKuO|Ihdk1? M3jFd3NCVkeHUh?=
NCI-H1793 NFfDeXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3m1SGlEPTB;MUKuPFIhdk1? MYfTRW5ITVJ?
KARPAS-45 NI\vV2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvWNI9zUUN3ME2xN{42OSCwTR?= NHTmRWNUSU6JRWK=
GCT MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjrU|Z{UUN3ME2xN{43QCCwTR?= NHXpTXhUSU6JRWK=
EoL-1 Mkf6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfkTWM2OD1zMz65N{BvVQ>? M3jLO3NCVkeHUh?=
LB2241-RCC MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkT0TWM2OD1zND6wNUBvVQ>? NEDZbW9USU6JRWK=
ES5 NIflU4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmD6TWM2OD1zND63OEBvVQ>? Mn3LV2FPT0WU
LOXIMVI Mm[yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTRTWM2OD1zND65PUBvVQ>? MmXOV2FPT0WU
COR-L105 NGCz[4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;ETWM2OD1zNT6wOEBvVQ>? NFvFS5RUSU6JRWK=
P12-ICHIKAWA MnzHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnIV2FKSzVyPUG1MlEhdk1? NXTyd5A{W0GQR1XS
CHL-1 NWHNdZNNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFT1dY1KSzVyPUG1MlQ2KG6P Ml\JV2FPT0WU
VMRC-RCZ NWfHcZkzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTF3Lk[zJI5O MlnTV2FPT0WU
HH NGflfYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTF3Lkegcm0> MV;TRW5ITVJ?
NUGC-3 M2T2SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTNTWM2OD1zNj6zOEBvVQ>? Ml7DV2FPT0WU
EGI-1 NXrpTGx6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTF4LkSzJI5O MWTTRW5ITVJ?
OS-RC-2 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTF4LkS3JI5O M1W1eXNCVkeHUh?=
MOLT-16 NHf6O4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LsW2lEPTB;MUeuNVUhdk1? M4nFUHNCVkeHUh?=
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ZR-75-30 MlL1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rqR2lEPTB;MU[uN|MxOyEQvF2= M3vPUXNCVkeHUh?=
A673 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4e5U2lEPTB;MkCuOVUxPyEQvF2= MoXLV2FPT0WU
K-562 NUW1R|VET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTJ6LkSxPFMh|ryP NVzpRVkzW0GQR1XS

... 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
  • 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 NVP-BEZ235

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% DMSO % % Tween 80 % ddH2O
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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
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*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

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