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 203 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 MmPURY51cW2rY4LvZolidCCDc4PhfS=> NEf5cZIyQCCq MkT5SG1UVw>? NYfwengxSW62aYTyfZBidm:|b33hcEBi[3Srdnn0fUB4cXSqIFXDOVAhd2ZiMD6wNFI2KM7:TR?= NVf0XYdpOjR6MEW5OFY>
MCF7 NUTZRWNTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDzRox3OC5yMT2xNFAh|ryP NYnQVYtjPDhiaB?= MVjEUXNQ NUDpSZZWUUN3ME2wMlc{KM7:TR?= NVL2eVlTOjN6N{G5NFQ>
HCT116 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWewMlAyNTFyMDFOwG0> M4n2NlQ5KGh? MUjEUXNQ MVvJR|UxRTFwMU[g{txO NV3TWoExOjN6N{G5NFQ>
U87MG NXLwO|AzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fP[FAvODFvMUCwJO69VQ>? NYCxc3NOPDhiaB?= MnLrSG1UVw>? MUXJR|UxRTFwM{Kg{txO NILYdIczOzh5MUmwOC=>
HBC4 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLQSVVWOC5yMT2xNFAh|ryP Mk[zOFghcA>? MnrPUI9oKEeLNUC9MVgvPjFiTR?= NYLLRWVUOjJ|M{[yOFY>
BSY1 NIfGdFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2K5OlAvODFvMUCwJO69VQ>? M173U|Q5KGh? MoHxUI9oKEeLNUC9MVgvPDhiTR?= MonNNlI{OzZ{NE[=
HBC5 M4HmRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVT3cmd5OC5yMT2xNFAh|ryP NF7Dc2k1QCCq MlnCUI9oKEeLNUC9MVcvQDdiTR?= M4TLelIzOzN4MkS2
MCF7 MmHTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fUcFAvODFvMUCwJO69VQ>? MXu0PEBp M4TZfWxw\yCJSUWwQU05NjF4IF2= Mn7xNlI{OzZ{NE[=
MDA-MB-231 MlnES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\QXGlKOC5yMT2xNFAh|ryP NGDvSWE1QCCq NEXFd5hNd2diR1m1NF0uQC5yOTDN NELk[VAzOjN|NkK0Oi=>
U251 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnzNE4xOS1zMECg{txO MU[0PEBp NWDTR2U3VG:pIFfJOVA:NTdwNk[gUS=> M1LHV|IzOzN4MkS2
SF268 MkPPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofkNE4xOS1zMECg{txO Moe2OFghcA>? MYHMc4chT0l3ME2tO{46OiCP M33VXVIzOzN4MkS2
SF295 NGP2OnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofRNE4xOS1zMECg{txO MXe0PEBp M4TUSmxw\yCJSUWwQU05NjNzIF2= M1rFUVIzOzN4MkS2
SF539 NYnaXFlJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzHfIoxNjBzLUGwNEDPxE1? NF;BV3M1QCCq M{f5e2xw\yCJSUWwQU05NjV7IF2= NVXSeJNtOjJ|M{[yOFY>
SNB75 M4HWbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTNNE4xOS1zMECg{txO M2rme|Q5KGh? MoDBUI9oKEeLNUC9MVgvPThiTR?= M4S3blIzOzN4MkS2
SNB78 MlTCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUWwMlAyNTFyMDFOwG0> M1fxOlQ5KGh? NWfTcoVZVG:pIFfJOVA:NThwNkWgUS=> NFHvcVczOjN|NkK0Oi=>
HCC2998 NX2yZm1rT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXQPIMxNjBzLUGwNEDPxE1? MV:0PEBp NYHzXZk2VG:pIFfJOVA:NThwMEWgUS=> M2WxRVIzOzN4MkS2
KM12 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVyxdnBvOC5yMT2xNFAh|ryP M3rE[|Q5KGh? MV3Mc4chT0l3ME2tO{42PCCP MVqyNlM{PjJ2Nh?=
HT-29 NX6zWopsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXpNE4xOS1zMECg{txO MmDaOFghcA>? MV7Mc4chT0l3ME2tO{44PSCP NHr5d4UzOjN|NkK0Oi=>
HCT15 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLPVWcxNjBzLUGwNEDPxE1? NXf6SY1CPDhiaB?= NUi3XHJDVG:pIFfJOVA:NThwMEOgUS=> M4Lr[|IzOzN4MkS2
HCT116 M2DhZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\TZlkxNjBzLUGwNEDPxE1? MVK0PEBp NWjxT3lZVG:pIFfJOVA:NTdwNkGgUS=> M1jsUlIzOzN4MkS2
NCI-H23 NVXzPGdpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDJNE4xOS1zMECg{txO M{DWblQ5KGh? NHT5d3dNd2diR1m1NF0uPy54NDDN NUTyTVl7OjJ|M{[yOFY>
NCI-H226 NH3oW|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTNO3hWOC5yMT2xNFAh|ryP M1S4d|Q5KGh? NFvWcYhNd2diR1m1NF0uQC52NDDN NXTZbWZQOjJ|M{[yOFY>
NCI-H522 NXnmV2tJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjw[IYxNjBzLUGwNEDPxE1? Ml;COFghcA>? MnLsUI9oKEeLNUC9MVgvPDViTR?= NVjjTZNWOjJ|M{[yOFY>
NCI-H438 NH\rXFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHzNE4xOS1zMECg{txO MmXlOFghcA>? NWnxRYZKVG:pIFfJOVA:NThwMUGgUS=> NGHVTVIzOjN|NkK0Oi=>
A549 M1nvXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXqNE4xOS1zMECg{txO NV\EdpZIPDhiaB?= NX72WHNjVG:pIFfJOVA:NThwMEegUS=> M1nWdlIzOzN4MkS2
DMS273 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vRPFAvODFvMUCwJO69VQ>? MoPnOFghcA>? MVHMc4chT0l3ME2tO{45OCCP NEjrZ|IzOjN|NkK0Oi=>
DMS114 NFnkWG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWGwMlAyNTFyMDFOwG0> NFHpcVk1QCCq M{jBbWxw\yCJSUWwQU05NjN7IF2= Ml;uNlI{OzZ{NE[=
LOXIMVI M4H5R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjhNE4xOS1zMECg{txO NFLQ[Yk1QCCq M17vcGxw\yCJSUWwQU05NjZ4IF2= NWHldnZzOjJ|M{[yOFY>
OVCAR3 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXywMlAyNTFyMDFOwG0> M{HJSVQ5KGh? NYLpPXgzVG:pIFfJOVA:NThwMUegUS=> NXrpVIZkOjJ|M{[yOFY>
OVCAR4 M1zjRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTTNE4xOS1zMECg{txO NHLmeo81QCCq NIfp[IlNd2diR1m1NF0uQC53ODDN NHvGRWMzOjN|NkK0Oi=>
OVCAR5 NV7qPY1wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXve40xNjBzLUGwNEDPxE1? NVmy[WppPDhiaB?= NUn2VZlvVG:pIFfJOVA:NTdwNUegUS=> MVSyNlM{PjJ2Nh?=
OVCAR8 NH3rVmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXuwMlAyNTFyMDFOwG0> NWWxU3p5PDhiaB?= NYGxV|BwVG:pIFfJOVA:NTdwOESgUS=> NFuxdJIzOjN|NkK0Oi=>
SKOV3 MnzIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXWwMlAyNTFyMDFOwG0> MYq0PEBp MWXMc4chT0l3ME2tPE41OSCP MYqyNlM{PjJ2Nh?=
RXF631L NX;6dpFLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWCwMlAyNTFyMDFOwG0> NVz3UY5XPDhiaB?= NUmwc5BjVG:pIFfJOVA:NThwMkGgUS=> M1zkdVIzOzN4MkS2
ACHN M3LVVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonDNE4xOS1zMECg{txO NUT0e2ZWPDhiaB?= NUnhcZc3VG:pIFfJOVA:NTdwOUWgUS=> NXrxVXhTOjJ|M{[yOFY>
St-4 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLIO5M6OC5yMT2xNFAh|ryP MX20PEBp MVjMc4chT0l3ME2tO{41PyCP Mnn5NlI{OzZ{NE[=
MKN1 NFG2eIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUf5XlNjOC5yMT2xNFAh|ryP NW[2TXNbPDhiaB?= NGnxbolNd2diR1m1NF0uQC52MTDN NUjnS5Q2OjJ|M{[yOFY>
MKN7 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXK4V3h[OC5yMT2xNFAh|ryP M2\INVQ5KGh? NH3Zb4hNd2diR1m1NF0uPy54ODDN MVyyNlM{PjJ2Nh?=
MKN28 M1Pjdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUiwMlAyNTFyMDFOwG0> NYPiXnJ6PDhiaB?= Mo\TUI9oKEeLNUC9MVcvODdiTR?= M4jMS|IzOzN4MkS2
MKN45 MkTwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjQNE4xOS1zMECg{txO MlTROFghcA>? NEPpR3VNd2diR1m1NF0uQC5|NDDN MYiyNlM{PjJ2Nh?=
MKN74 NI\MeXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;JNE4xOS1zMECg{txO NHz2PG81QCCq MlfiUI9oKEeLNUC9MVcvPDJiTR?= Mn3ONlI{OzZ{NE[=
DU145 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWKwMlAyNTFyMDFOwG0> NFG3Opk1QCCq NXHDW5BWVG:pIFfJOVA:NThwMU[gUS=> MUKyNlM{PjJ2Nh?=
PC3 NWfNd2JuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXZNE4xOS1zMECg{txO MVW0PEBp NIruWmhNd2diR1m1NF0uQC54NjDN NEnNPFIzOjN|NkK0Oi=>
Trypanosoma brucei brucei NES1[25HfW6ldHnvckBCe3OjeR?= MVyyNFAhdk1? NWPES4VVOTJiaB?= NIWwRppFVVOR MX7E[YNz\WG|ZTDpckBxcG:|cHjveIllgWxiaX7vd4l1d2xicHjvd5Bp[XSnIHzleoVt Mm\5NlQ5ODV7NE[=
Trypanosoma brucei brucei M1zsPWZ2dmO2aX;uJGF{e2G7 NXThW4lMOThiaB?= NInqWHVFVVOR MnzLTY5pcWKrdHnvckBw\iC{ZXPldJRwei2vZXTpZZRm\CCnbnTvZ5l1d3OrczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiC2cnHud4ZmenKrbjD1dJRic2V? Mm\lNlQ5ODV7NE[=
Trypanosoma brucei brucei NF\nb2JHfW6ldHnvckBCe3OjeR?= M1jnPFIxOCCwTR?= M4PQR|EzKGh? M2PMVmROW09? MWnF[oZm[3Rib36gd5BpcW6pb335cIVqdiCuZY\lcC=> NIfDc2MzPDhyNUm0Oi=>
Trypanosoma brucei brucei NVvGVIR[TnWwY4Tpc44hSXO|YYm= MnXQNlAxKG6P MnL1NVIhcA>? M{\DcGROW09? NXrq[G53TW[oZXP0JI9vKHCqb4PwbIF1cWS7bHPoc4xqdmVibHX2[Yw> NXG5WlFoOjR6MEW5OFY>
UM-UC-3 M2DDe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTNzNTDwUS=> MoX5V2FPT0WU
SBC-1 NY\lSYt6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTd2MjDwUS=> NWSzVGlpW0GQR1XS
MKN1 M3XPRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\zTWM2OD1{Lkigcm0> M2C0cnNCVkeHUh?=
NCI-H720 MmDWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTNwNUegcm0> MoTOV2FPT0WU
BFTC-909 NFLobXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTNwN{Ggcm0> NUfOTXhsW0GQR1XS
BPH-1 M2Pjdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfYZpZKSzVyPUSuO|Yhdk1? M4HlVXNCVkeHUh?=
PC-3 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfqTWM2OD13LkC5JI5O NUO0bIhbW0GQR1XS
AN3-CA MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfNVm5KSzVyPUWuOVYhdk1? MkTWV2FPT0WU
HN NYHDNoZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPsTWM2OD13Lkm2JI5O NHu4W4VUSU6JRWK=
HCC2218 M{DzNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzZN29KSzVyPU[uOlEhdk1? NXS5fnFHW0GQR1XS
KP-4 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYD6dJd2UUN3ME23JI5O M3SzdHNCVkeHUh?=
LU-139 NFL2OolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYn4O4VxUUN3ME23Mlc4KG6P MnTsV2FPT0WU
ETK-1 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zHRWlEPTB;Nz64PEBvVQ>? M4HZR3NCVkeHUh?=
Ramos-2G6-4C10 M2rFOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\GcmlEPTB;OD60PUBvVQ>? MoHYV2FPT0WU
MHH-PREB-1 NUXy[Hc6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTlwMUKgcm0> MkPnV2FPT0WU
DU-4475 NHjUZoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTlwNESgcm0> NWPrUHJuW0GQR1XS
NCI-H1666 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTlwN{Ggcm0> MojmV2FPT0WU
CAMA-1 M3rFeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXGW2lKSzVyPUmuPEBvVQ>? NHTCPYZUSU6JRWK=
TYK-nu M2TpWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;nTm9KSzVyPUmuPVQhdk1? NVPaVWdqW0GQR1XS
MFE-280 NWTnWoZoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTlwOUmgcm0> NX3qWWVTW0GQR1XS
A549 MnHSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPjO|NXUUN3ME2xNE4yPCCwTR?= M{\iTHNCVkeHUh?=
769-P M1KwfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jvcWlEPTB;MUCuOFQhdk1? NFvLXnNUSU6JRWK=
L-363 M3nCe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jaSWlEPTB;MUCuOlkhdk1? NFPONGVUSU6JRWK=
ES8 Mn7vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjxTWM2OD1zMD65JI5O M3fkXXNCVkeHUh?=
PA-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTFzLkiyJI5O NWHJRVV7W0GQR1XS
Mewo M4DEfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInSVFZKSzVyPUGxMlk6KG6P M2TFSXNCVkeHUh?=
HSC-3 MlzuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTF{LkKxJI5O MYjTRW5ITVJ?
H4 M2[4Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHTc5BKSzVyPUGyMlY4KG6P M2G0O3NCVkeHUh?=
BB65-RCC NUO5ToxFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTF{LkeyJI5O MVTTRW5ITVJ?
NCI-H1793 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHr4[ZdKSzVyPUGyMlgzKG6P MYDTRW5ITVJ?
KARPAS-45 NHTPTYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LJSmlEPTB;MUOuOVEhdk1? MUTTRW5ITVJ?
GCT MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfp[WZ3UUN3ME2xN{43QCCwTR?= MUTTRW5ITVJ?
EoL-1 NUjkVmoxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHVV2NKSzVyPUGzMlk{KG6P NHqyNYhUSU6JRWK=
LB2241-RCC NYfBNYhRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTF2LkCxJI5O MnO1V2FPT0WU
ES5 M3L1O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TTSWlEPTB;MUSuO|Qhdk1? NFTTWJhUSU6JRWK=
LOXIMVI M13E[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{jHRWlEPTB;MUSuPVkhdk1? NEGxWYFUSU6JRWK=
COR-L105 NFP0c2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTF3LkC0JI5O NH7XXoVUSU6JRWK=
P12-ICHIKAWA M2XuZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PHbWlEPTB;MUWuNUBvVQ>? MVjTRW5ITVJ?
CHL-1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU[3UWQ4UUN3ME2xOU41PSCwTR?= MX;TRW5ITVJ?
VMRC-RCZ MlqzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnvNHhKSzVyPUG1MlY{KG6P MkK1V2FPT0WU
HH Mnv5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTF3Lkegcm0> NYLWXFRCW0GQR1XS
NUGC-3 M3rKRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFG1TY9KSzVyPUG2MlM1KG6P MlPFV2FPT0WU
EGI-1 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTF4LkSzJI5O M4XtVXNCVkeHUh?=
OS-RC-2 MlXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXHVZNkUUN3ME2xOk41PyCwTR?= MUXTRW5ITVJ?
MOLT-16 M4fsSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHkeWdsUUN3ME2xO{4yPSCwTR?= NULzcIxmW0GQR1XS
NCI-H209 M3:2bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3RdnBKSzVyPUG3MlI6KG6P M2flU3NCVkeHUh?=
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NCI-H1651 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnC[|BKSzVyPUO0OE4yQCCwTR?= M4\2eXNCVkeHUh?=
COLO-792 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTN3ND60NkBvVQ>? NVPzbYdMW0GQR1XS
ACHN MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;wV2lEPTB;M{W2MlcyKG6P MVnTRW5ITVJ?
TH-3 M2fsPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGj5bYxKSzVyPUO3PU46PSCwTR?= M3;0Z3NCVkeHUh?=
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COLO-320-HSR MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTRyMz6zO{BvVQ>? M1fmbnNCVkeHUh?=
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DSH1 M1\acmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfpTWM2OD12ME[uPVEhdk1? M3XQUnNCVkeHUh?=
TE-10 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnH6TWM2OD12MEeuNFEhdk1? NELIV5hUSU6JRWK=
HCC70 NFjpOGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPGc5BKUUN3ME20NFkvOjFibl2= MojFV2FPT0WU
TGBC11TKB M3jUR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljWTWM2OD12MUCuN|Mhdk1? MVPTRW5ITVJ?
NCI-H727 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3ISldKSzVyPUSxNk4yOSCwTR?= MXTTRW5ITVJ?
ALL-PO M13Cfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mln6TWM2OD12MUWuOlkhdk1? NUDS[mZ2W0GQR1XS
ABC-1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nVWWlEPTB;NEKwMlQ2KG6P MmjmV2FPT0WU
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RMG-I M1PKcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXLe|RiUUN3ME20OlcvPTZibl2= Ml;0V2FPT0WU
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HCC1954 MkjmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvs[ZdbUUN3ME21NVIvPSCwTR?= NWK5OGNqW0GQR1XS
SK-MEL-24 MnjKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTVzNj61NUBvVQ>? MV7TRW5ITVJ?
NB12 MnviS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7YTWM2OD13MkiuOFIhdk1? NYXhPGNXW0GQR1XS
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HCC1187 M{jwRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTV5NT64N{BvVQ>? M2PVVXNCVkeHUh?=
NCI-H2342 MnHhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnIcYhzUUN3ME21PVAvOzlibl2= MnHpV2FPT0WU
NCI-H2291 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfLTWM2OD13OUiuN|Ehdk1? MlGxV2FPT0WU
OVCAR-3 NUfTVVB4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTV7OD65OkBvVQ>? MknGV2FPT0WU
MHH-NB-11 M2fOVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHWTWM2OD14MkmuNFEhdk1? NHrOSIpUSU6JRWK=
SAS MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rufmlEPTB;NkWyMlY4KG6P Mn61V2FPT0WU
COLO-824 NYnuSI9NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlz5TWM2OD14OEmuN|chdk1? NIPXZYxUSU6JRWK=
HCC1395 NH\wO2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XrOWlEPTB;Nkm4MlUhdk1? MXHTRW5ITVJ?
COLO-668 NHzoc5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;oWopKSzVyPUewOk4yKG6P NWP2[HFuW0GQR1XS
NCI-H226 NFrkPGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfmZ4lkUUN3ME23NFcvQCCwTR?= MofvV2FPT0WU
NB17 NWP1OVNjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7MTWM2OD15MkGuO|Uhdk1? Mlz2V2FPT0WU
SW1463 NH;4c|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTd|OT6xPUBvVQ>? NE\xOJNUSU6JRWK=
TGW NFT5NFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTd4MD6xOUBvVQ>? MYfTRW5ITVJ?
NCI-H526 Mo\aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTh{Mz61N{BvVQ>? M4jZUnNCVkeHUh?=
COR-L88 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rtUmlEPTB;OES4MlEzKG6P MUDTRW5ITVJ?
NCI-H441 NED2W5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfxWI5wUUN3ME24PVUvOjJibl2= MXzTRW5ITVJ?
NCI-H630 MlXtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHuTWM2OD17MUKuPVYhdk1? M133d3NCVkeHUh?=
Mo-T NU\ye3BQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPOfppKSzVyPUm0O{45QCCwTR?= MVnTRW5ITVJ?
JAR NULMOoFDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHKTIlKSzVyPUm1Ok4zPCCwTR?= M2KwXXNCVkeHUh?=
NCI-H1838 NIfSSZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NET2OW5KSzVyPUGuNFI{QDhizszN NGXMb5FUSU6JRWK=
DoTc2-4510 MlX5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonXTWM2OD1zLkC3N|c3KM7:TR?= MU\TRW5ITVJ?
MKN28 NFnaNoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFr3UVBKSzVyPUGuNFkxOjRizszN M1TCO3NCVkeHUh?=
HuP-T3 M{HKTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjVU4VOUUN3ME2xMlEyQTB3IN88US=> NWWwWWR1W0GQR1XS
TE-9 MlzYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTFwMUK5O|Mh|ryP MkfKV2FPT0WU
NY NED6U2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnntTWM2OD1zLkG2O|kzKM7:TR?= M1SzV3NCVkeHUh?=
HT55 M{\0V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TuN2lEPTB;MT6zNVM1PCEQvF2= M2rZd3NCVkeHUh?=
SW837 NXuwTpY4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV:1NWVwUUN3ME2xMlMzQTd6IN88US=> MXnTRW5ITVJ?
NCI-H2029 Mn3LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjufVFKSzVyPUGuOFE4QTFizszN M2K1U3NCVkeHUh?=
IST-SL1 MoDWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLrTpprUUN3ME2xMlQ1OjRizszN NYfzXVRXW0GQR1XS
COLO-741 NEOwco5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjQSWRKSzVyPUGuOFk4PzFizszN M1jNZnNCVkeHUh?=
LU-65 MmTxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{W4TmlEPTB;MT62NlI1QSEQvF2= MW\TRW5ITVJ?
NCI-H1304 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlH0TWM2OD1zLk[1OFk5KM7:TR?= MoPxV2FPT0WU
KARPAS-299 NITEfYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTFwN{m0O|kh|ryP M36zRXNCVkeHUh?=
NCI-H358 M1:1OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGL1SoFKSzVyPUGuPVU2ODNizszN MV7TRW5ITVJ?
OAW-28 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHIT3VUUUN3ME2yMlA3QTF7IN88US=> M{jzeXNCVkeHUh?=
C8166 M2ft[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTFdFdNUUN3ME2yMlY{Ozl{IN88US=> NHGyS4dUSU6JRWK=
COLO-678 M4H2[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTJwOEO3Olgh|ryP NF\yUZRUSU6JRWK=
SK-N-DZ M363[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fNemlEPTB;Mj64OlM5OSEQvF2= M3\4Z3NCVkeHUh?=
NCI-H82 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVe1NWJYUUN3ME2yMlkxOzZ7IN88US=> M1fEcnNCVkeHUh?=
JVM-2 M3zJWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTNwMEOxPFgh|ryP NG[wUppUSU6JRWK=
SW1116 M1rtNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTNwMEW0NVEh|ryP MXTTRW5ITVJ?
MDA-MB-453 NWqz[pZZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDXTWM2OD1|LkGwOFM6KM7:TR?= M2\2UXNCVkeHUh?=
Calu-6 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;tTWM2OD1|LkG5PVch|ryP MlTWV2FPT0WU
SHP-77 NWDHfVF3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTNwNUK4JO69VQ>? MV3TRW5ITVJ?
Capan-2 M4rW[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVznfZJEUUN3ME20MlMzPThzIN88US=> M1jzWHNCVkeHUh?=
SW948 M1XyTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXOd5VKSzVyPUSuO|Q4PzlizszN NY\STIFrW0GQR1XS
HDLM-2 M3XSRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nkVWlEPTB;NT6wO|czPSEQvF2= MnfKV2FPT0WU
LAN-6 MoPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTJZlFoUUN3ME22MlIyPDl3IN88US=> MlKwV2FPT0WU
LU-135 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\XenJKSzVyPU[uOFMxPzdizszN M4\4d3NCVkeHUh?=
T84 NIq4[VhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnO2TWM2OD14Lkm4OlQh|ryP MYXTRW5ITVJ?
CAPAN-1 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrhU3R5UUN3ME23MlYzOjN|IN88US=> M4TmSnNCVkeHUh?=
SW1417 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjQTWM2OD15LkmxO|MyKM7:TR?= NYCyNJo6W0GQR1XS
BALL-1 NF:zNItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjMfFJLUUN3ME24MlUxPDB7IN88US=> MnjlV2FPT0WU
HT-29 NXXicmEyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fnWmlEPTB;OT6wO|U6QSEQvF2= MV\TRW5ITVJ?
C3A NXrid2djT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXrNoFKSzVyPUmuPFg{QTRizszN MWfTRW5ITVJ?
NCI-H1993 M4T4V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnUZ|NpUUN3ME2xNE42ODhzIN88US=> NWe1cHZtW0GQR1XS
SK-MEL-1 MlTyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVL0fFc{UUN3ME2xNU43Ojh7IN88US=> NFm4c4xUSU6JRWK=
DU-145 M2fmUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;ITWM2OD1zND61NFUzKM7:TR?= NVvnPZJYW0GQR1XS
KP-N-YN NHr6OVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETtV5ZKSzVyPUG0MlUyODNizszN NY\SWpVPW0GQR1XS
CCRF-CEM M37VXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHvTpRKSzVyPUG0Mlc5ODlizszN M2jibHNCVkeHUh?=
ZR-75-30 NUHLZ5pKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfsTWM2OD1zNj6zN|A{KM7:TR?= M1r5UXNCVkeHUh?=
A673 MoXGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnS4TWM2OD1{MD61OVA4KM7:TR?= M1:1WHNCVkeHUh?=
K-562 MlrwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHx[YI5UUN3ME2yPE41OTh|IN88US=> NFLHZWpUSU6JRWK=

... 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]

+ Expand

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]

+ Expand
  • 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]

+ Expand
  • 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)

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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 )

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

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Molarity Calculator

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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