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 221 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 MWTBcpRqdWmlcn;ibYFtKEG|c3H5 MVSxPEBp M3HaN2ROW09? M4LaTWFvfGm2conwZY5we2:vYXygZYN1cX[rdImge4l1cCCHQ{WwJI9nKDBwMECyOUDPxE1? NIPsWogzPDhyNUm0Oi=>
MCF7 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXuwMlAyNTFyMDFOwG0> MWK0PEBp NUnm[IV6TE2VTx?= MVPJR|UxRTBwN{Og{txO M4jWeFI{QDdzOUC0
HCT116 NHTVNpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTxVpBjOC5yMT2xNFAh|ryP MWO0PEBp MnG2SG1UVw>? M{n2ZmlEPTB;MT6xOkDPxE1? MkX4NlM5PzF7MES=
U87MG MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\vRVAvODFvMUCwJO69VQ>? Mn\uOFghcA>? NITnbplFVVOR NVq5SpZbUUN3ME2xMlMzKM7:TR?= MnTCNlM5PzF7MES=
HBC4 NFjqTHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYmwMlAyNTFyMDFOwG0> NH[2RnM1QCCq NYfvdIduVG:pIFfJOVA:NThwNkGgUS=> MVSyNlM{PjJ2Nh?=
BSY1 NYXDOpFOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTrNE4xOS1zMECg{txO NV\USGdzPDhiaB?= NIC2b4tNd2diR1m1NF0uQC52ODDN M3L3e|IzOzN4MkS2
HBC5 NIiyNXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4f0NlAvODFvMUCwJO69VQ>? Mkf5OFghcA>? M4HOOWxw\yCJSUWwQU04Njh5IF2= MWmyNlM{PjJ2Nh?=
MCF7 MnLGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\QNE4xOS1zMECg{txO Mke0OFghcA>? NUfDSotkVG:pIFfJOVA:NThwMU[gUS=> Mlq5NlI{OzZ{NE[=
MDA-MB-231 M3H3b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYCwMlAyNTFyMDFOwG0> M{CxO|Q5KGh? MYfMc4chT0l3ME2tPE4xQSCP MXSyNlM{PjJ2Nh?=
U251 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXewMlAyNTFyMDFOwG0> NUTQ[4hmPDhiaB?= MYTMc4chT0l3ME2tO{43PiCP NFfUVYEzOjN|NkK0Oi=>
SF268 MoTES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTZNE4xOS1zMECg{txO MXO0PEBp NYrFT4Z4VG:pIFfJOVA:NTdwOUKgUS=> NVH0RWZnOjJ|M{[yOFY>
SF295 NWruXINKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrpdoN[OC5yMT2xNFAh|ryP MmrTOFghcA>? NHy4eXJNd2diR1m1NF0uQC5|MTDN NVTnVG9GOjJ|M{[yOFY>
SF539 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLTSlRuOC5yMT2xNFAh|ryP NV\vfZIzPDhiaB?= MW\Mc4chT0l3ME2tPE42QSCP MYWyNlM{PjJ2Nh?=
SNB75 M4G1fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlniNE4xOS1zMECg{txO M13xW|Q5KGh? M1HMSmxw\yCJSUWwQU05NjV6IF2= NYL3Rpg{OjJ|M{[yOFY>
SNB78 NE\4Zm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrtNE4xOS1zMECg{txO Ml\2OFghcA>? NXXRd5JoVG:pIFfJOVA:NThwNkWgUS=> MnTpNlI{OzZ{NE[=
HCC2998 MmT4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvtNHdCOC5yMT2xNFAh|ryP Mn\iOFghcA>? M{W2Tmxw\yCJSUWwQU05NjB3IF2= M3z2NlIzOzN4MkS2
KM12 M3PwSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnrc29[OC5yMT2xNFAh|ryP NHX0T4c1QCCq NEK5[pNNd2diR1m1NF0uPy53NDDN MXGyNlM{PjJ2Nh?=
HT-29 Mn21S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYL6OmZvOC5yMT2xNFAh|ryP MYG0PEBp MXfMc4chT0l3ME2tO{44PSCP MYeyNlM{PjJ2Nh?=
HCT15 M4PONWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\uWY5FOC5yMT2xNFAh|ryP Mn3IOFghcA>? NVntSJBIVG:pIFfJOVA:NThwMEOgUS=> Mm\ZNlI{OzZ{NE[=
HCT116 NH;t[5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnENE4xOS1zMECg{txO MkC0OFghcA>? MYrMc4chT0l3ME2tO{43OSCP MX[yNlM{PjJ2Nh?=
NCI-H23 NUnufJc5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjBNE4xOS1zMECg{txO MmPyOFghcA>? NYrJRVkzVG:pIFfJOVA:NTdwNkSgUS=> MV:yNlM{PjJ2Nh?=
NCI-H226 MlnES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XhfFAvODFvMUCwJO69VQ>? M2nPdVQ5KGh? MmWwUI9oKEeLNUC9MVgvPDRiTR?= NEDXRmQzOjN|NkK0Oi=>
NCI-H522 NUXJ[IhST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPuR3U6OC5yMT2xNFAh|ryP MXi0PEBp NV65VVhZVG:pIFfJOVA:NThwNEWgUS=> MXuyNlM{PjJ2Nh?=
NCI-H438 NVHNW3Q5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonvNE4xOS1zMECg{txO NWfWPG9pPDhiaB?= MUXMc4chT0l3ME2tPE4yOSCP MmPRNlI{OzZ{NE[=
A549 NFXmeWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3S2WlAvODFvMUCwJO69VQ>? MoK1OFghcA>? MY\Mc4chT0l3ME2tPE4xPyCP NIH1dZkzOjN|NkK0Oi=>
DMS273 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{C5blAvODFvMUCwJO69VQ>? M4TBbFQ5KGh? Mn7UUI9oKEeLNUC9MVcvQDBiTR?= MlPLNlI{OzZ{NE[=
DMS114 M3rUSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnP2NE4xOS1zMECg{txO M4C3XVQ5KGh? NHz2Xo1Nd2diR1m1NF0uQC5|OTDN MXWyNlM{PjJ2Nh?=
LOXIMVI MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVmwMlAyNTFyMDFOwG0> NXXZdpRyPDhiaB?= NFnrc3BNd2diR1m1NF0uQC54NjDN MX:yNlM{PjJ2Nh?=
OVCAR3 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnKdYQzOC5yMT2xNFAh|ryP MlvSOFghcA>? MlH2UI9oKEeLNUC9MVgvOTdiTR?= Mn3DNlI{OzZ{NE[=
OVCAR4 NUXTWY9QT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjQTHBJOC5yMT2xNFAh|ryP MYq0PEBp MVHMc4chT0l3ME2tPE42QCCP NIO3cY4zOjN|NkK0Oi=>
OVCAR5 M33wRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvodJAxNjBzLUGwNEDPxE1? NFPMOpE1QCCq NV6ySW1OVG:pIFfJOVA:NTdwNUegUS=> NYSwNGVJOjJ|M{[yOFY>
OVCAR8 M4LUUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;yNE4xOS1zMECg{txO MXm0PEBp MUfMc4chT0l3ME2tO{45PCCP NGHTcHUzOjN|NkK0Oi=>
SKOV3 NV;scZBjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LEVlAvODFvMUCwJO69VQ>? NUDmcXk1PDhiaB?= NUDTPWdMVG:pIFfJOVA:NThwNEGgUS=> NYL2c|RYOjJ|M{[yOFY>
RXF631L MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELhc20xNjBzLUGwNEDPxE1? MkjZOFghcA>? Mn\MUI9oKEeLNUC9MVgvOjFiTR?= M{nZRlIzOzN4MkS2
ACHN MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnhXm0xNjBzLUGwNEDPxE1? NInHenU1QCCq M2rlSmxw\yCJSUWwQU04Njl3IF2= MUmyNlM{PjJ2Nh?=
St-4 MmHUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fDRlAvODFvMUCwJO69VQ>? MneyOFghcA>? MV\Mc4chT0l3ME2tO{41PyCP NVO0UIJlOjJ|M{[yOFY>
MKN1 NFHvW5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TaUVAvODFvMUCwJO69VQ>? NFj0bIQ1QCCq Mn7JUI9oKEeLNUC9MVgvPDFiTR?= MmjrNlI{OzZ{NE[=
MKN7 NFXCN25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;4TZMxNjBzLUGwNEDPxE1? MV[0PEBp Ml:4UI9oKEeLNUC9MVcvPjhiTR?= MX2yNlM{PjJ2Nh?=
MKN28 M1PRfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnhNE4xOS1zMECg{txO MlTIOFghcA>? NWDMOGRRVG:pIFfJOVA:NTdwMEegUS=> MX2yNlM{PjJ2Nh?=
MKN45 M4\0N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHafoQxNjBzLUGwNEDPxE1? MUW0PEBp M1T4NGxw\yCJSUWwQU05NjN2IF2= MlnwNlI{OzZ{NE[=
MKN74 M1[3WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3ezVVAvODFvMUCwJO69VQ>? MmjaOFghcA>? NWLUcY5WVG:pIFfJOVA:NTdwNEKgUS=> MWSyNlM{PjJ2Nh?=
DU145 NXfWZ2ZTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG[1O4wxNjBzLUGwNEDPxE1? MYS0PEBp NF;EXI5Nd2diR1m1NF0uQC5zNjDN M4Oz[|IzOzN4MkS2
PC3 NXnqO2VHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFWyXnUxNjBzLUGwNEDPxE1? NGLlSIY1QCCq MXzMc4chT0l3ME2tPE43PiCP NIPtdGYzOjN|NkK0Oi=>
Trypanosoma brucei brucei NIXZfVFHfW6ldHnvckBCe3OjeR?= M{LkNFIxOCCwTR?= MUexNkBp MoH3SG1UVw>? M{X4dWRm[3KnYYPlJIlvKHCqb4PwbI91cWS7bDDpco9{cXSxbDDwbI9{eGijdHWgcIV3\Wx? NF75XZEzPDhyNUm0Oi=>
Trypanosoma brucei brucei NGXHR4hHfW6ldHnvckBCe3OjeR?= M1nwbFE5KGh? NFv1bXRFVVOR MXHJcohq[mm2aX;uJI9nKHKnY3XweI9zNW2nZHnheIVlKGWwZH;jfZRwe2m|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKHS{YX7z[oVzemmwIIXweIFs\Q>? MkXBNlQ5ODV7NE[=
Trypanosoma brucei brucei M3rTOmZ2dmO2aX;uJGF{e2G7 MYqyNFAhdk1? MoC5NVIhcA>? M1jSVmROW09? Mor6SYZn\WO2IH;uJJNxcGmwZ3;tfYxmcW5ibHX2[Yw> M{\RdVI1QDB3OUS2
Trypanosoma brucei brucei MWDGeY5kfGmxbjDBd5NigQ>? MVWyNFAhdk1? MXexNkBp NILUVVJFVVOR M3LIN2Vn\mWldDDvckBxcG:|cHjheIllgWylaH;sbY5mKGyndnXs NFXXS2ozPDhyNUm0Oi=>
UM-UC-3 NFuwNXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXJTWM2OD1|MUWgdG0> M2jHVHNCVkeHUh?=
SBC-1 NFn0ZmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XyTmlEPTB;N{SyJJBO NUjl[IRsW0GQR1XS
MKN1 NYXpOlhLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUS3N|hQUUN3ME2yMlghdk1? M{jhTHNCVkeHUh?=
NCI-H720 MkXRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXFNmc5UUN3ME2zMlU4KG6P M1;jVHNCVkeHUh?=
BFTC-909 NUmxZ4E6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHjTWM2OD1|LkexJI5O Mm\DV2FPT0WU
BPH-1 NXfHNpE5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PWbmlEPTB;ND63OkBvVQ>? NH2wNYNUSU6JRWK=
PC-3 MornS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTVwMEmgcm0> MkD4V2FPT0WU
AN3-CA MkTmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HkZmlEPTB;NT61OkBvVQ>? NVLIWVNsW0GQR1XS
HN NFewOXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTVwOU[gcm0> MlzwV2FPT0WU
HCC2218 Ml22S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnP2TWM2OD14Lk[xJI5O NWnCNYVpW0GQR1XS
KP-4 MlXGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vNUGlEPTB;NzDuUS=> NH7kdVVUSU6JRWK=
LU-139 NULqXFd5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\LOVBKUUN3ME23Mlc4KG6P NWnjc|M3W0GQR1XS
ETK-1 NVrHeJR3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTdwOEigcm0> NUW4TItoW0GQR1XS
Ramos-2G6-4C10 MlTyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDtTWM2OD16LkS5JI5O NYWyO4pRW0GQR1XS
MHH-PREB-1 NUXhdnFyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4f0WmlEPTB;OT6xNkBvVQ>? Mmq2V2FPT0WU
DU-4475 MkPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HzbWlEPTB;OT60OEBvVQ>? MXvTRW5ITVJ?
NCI-H1666 NVrzcnp3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjoUVFKSzVyPUmuO|Ehdk1? NITzR3NUSU6JRWK=
CAMA-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1[zUmlEPTB;OT64JI5O Mn\pV2FPT0WU
TYK-nu M2nm[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTlwOUSgcm0> NYPhOVBKW0GQR1XS
MFE-280 M2rm[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LDVGlEPTB;OT65PUBvVQ>? NHXq[FhUSU6JRWK=
A549 MkL4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPWTWM2OD1zMD6xOEBvVQ>? NEnvV|lUSU6JRWK=
769-P NELHcodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jDOGlEPTB;MUCuOFQhdk1? NVTjb3lkW0GQR1XS
L-363 MlruS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jDc2lEPTB;MUCuOlkhdk1? Mm\PV2FPT0WU
ES8 M2qzVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTFyLkmgcm0> MWfTRW5ITVJ?
PA-1 NV7ZemJ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDvUXJuUUN3ME2xNU45OiCwTR?= NVfnZ2JsW0GQR1XS
Mewo Mnj6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjpfIRSUUN3ME2xNU46QSCwTR?= M17rbnNCVkeHUh?=
HSC-3 M1PaTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljWTWM2OD1zMj6yNUBvVQ>? M{XnXXNCVkeHUh?=
H4 NWT5NJh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTF{Lk[3JI5O NEXhVGNUSU6JRWK=
BB65-RCC NXzJdW1ZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoKwTWM2OD1zMj63NkBvVQ>? NEnCNm9USU6JRWK=
NCI-H1793 MmHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTF{LkiyJI5O MmW3V2FPT0WU
KARPAS-45 M{fGcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTF|LkWxJI5O MoX6V2FPT0WU
GCT NWLTZ3V4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTF|Lk[4JI5O MorEV2FPT0WU
EoL-1 M{PGTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NED4XVlKSzVyPUGzMlk{KG6P MnPnV2FPT0WU
LB2241-RCC MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmj5TWM2OD1zND6wNUBvVQ>? MkfpV2FPT0WU
ES5 MkjsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XXfWlEPTB;MUSuO|Qhdk1? MmXlV2FPT0WU
LOXIMVI NGXOeFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYrBW|VKUUN3ME2xOE46QSCwTR?= NHu3c5FUSU6JRWK=
COR-L105 MmnES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTF3LkC0JI5O MkDyV2FPT0WU
P12-ICHIKAWA MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\ZTFhqUUN3ME2xOU4yKG6P MUPTRW5ITVJ?
CHL-1 M{i4SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTF3LkS1JI5O NFj0ZotUSU6JRWK=
VMRC-RCZ NXjvVIM5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPncGFkUUN3ME2xOU43OyCwTR?= NIHWcVFUSU6JRWK=
HH MoX0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jB[2lEPTB;MUWuO{BvVQ>? NF:zZlFUSU6JRWK=
NUGC-3 NHXrOGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrmO4FKSzVyPUG2MlM1KG6P Ml\yV2FPT0WU
EGI-1 NIT1S3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLITWM2OD1zNj60N{BvVQ>? M4DmfnNCVkeHUh?=
OS-RC-2 M1;Uemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;qUHBKSzVyPUG2MlQ4KG6P MmHyV2FPT0WU
MOLT-16 MnLNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4C4fGlEPTB;MUeuNVUhdk1? NGj5c2hUSU6JRWK=
NCI-H209 M1;GW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYL5U3VMUUN3ME2xO{4zQSCwTR?= M3PkWHNCVkeHUh?=
697 M3y0SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFr3SGVKSzVyPUG3MlQ{KG6P NUKyfJNlW0GQR1XS
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A673 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{n2RmlEPTB;MkCuOVUxPyEQvF2= Mm\iV2FPT0WU
K-562 M33ZWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnq0TWM2OD1{OD60NVg{KM7:TR?= NXvGT3BuW0GQR1XS

... 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
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    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
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    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