Dactolisib (BEZ235)

For research use only.

Catalog No.S1009 Synonyms: NVP-BEZ235

388 publications

Dactolisib (BEZ235) Chemical Structure

CAS No. 915019-65-7

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 388 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 NVewbJAzSW62aX3pZ5Jw[mmjbDDBd5NigQ>? M1T0NFE5KGh? MVrEUXNQ NWTOfVRMSW62aYTyfZBidm:|b33hcEBi[3Srdnn0fUB4cXSqIFXDOVAhd2ZiMD6wNFI2KM7:TR?= M4jTUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEC1PVQ3Lz5{NEiwOVk1PjxxYU6=
MCF7 NVfpUHZnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2f5elAvODFvMUCwJO69VQ>? MUe0PEBp MYPEUXNQ M1rDNmlEPTB;MD63N{DPxE1? NU\WWJFjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4O|E6ODRpPkKzPFcyQTB2PD;hQi=>
HCT116 M4D6Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3T0WlAvODFvMUCwJO69VQ>? M3;Je|Q5KGh? M3G2U2ROW09? NYDlWYVjUUN3ME2xMlE3KM7:TR?= MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh5MUmwOEc,OjN6N{G5NFQ9N2F-
U87MG M{LMb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHNTpIxNjBzLUGwNEDPxE1? MWe0PEBp NFv1[5hFVVOR NULvSm5RUUN3ME2xMlMzKM7:TR?= MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh5MUmwOEc,OjN6N{G5NFQ9N2F-
HBC4 MlnHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjObYliOC5yMT2xNFAh|ryP NHj0O2Y1QCCq M2XUSGxw\yCJSUWwQU05NjZzIF2= MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjN|NkK0Okc,OjJ|M{[yOFY9N2F-
BSY1 NEHGZY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;Od5FSOC5yMT2xNFAh|ryP M1fLZVQ5KGh? NHrhV4FNd2diR1m1NF0uQC52ODDN MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjN|NkK0Okc,OjJ|M{[yOFY9N2F-
HBC5 NInKdplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWmwMlAyNTFyMDFOwG0> NUnXV3djPDhiaB?= NVq0NnNUVG:pIFfJOVA:NTdwOEegUS=> NG\m[489[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOzOlI1Pid-MkKzN|YzPDZ:L3G+
MCF7 NYDWOWJTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTLTZhXOC5yMT2xNFAh|ryP NXfWOnF7PDhiaB?= M3T0WWxw\yCJSUWwQU05NjF4IF2= M3nwc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{O2NlQ3Lz5{MkOzOlI1PjxxYU6=
MDA-MB-231 NIPDVXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zoVlAvODFvMUCwJO69VQ>? M{L2S|Q5KGh? NX7yfXY2VG:pIFfJOVA:NThwMEmgUS=> NHnTVpA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOzOlI1Pid-MkKzN|YzPDZ:L3G+
U251 NFX5SZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3Tr[lAvODFvMUCwJO69VQ>? MXq0PEBp MYrMc4chT0l3ME2tO{43PiCP M2PhS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{O2NlQ3Lz5{MkOzOlI1PjxxYU6=
SF268 NUXydFhDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPmfFh5OC5yMT2xNFAh|ryP NH;wcHA1QCCq NWrDUmJ1VG:pIFfJOVA:NTdwOUKgUS=> MnK1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|M{[yOFYoRjJ{M{O2NlQ3RC:jPh?=
SF295 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUSzc445OC5yMT2xNFAh|ryP MnzkOFghcA>? MnG0UI9oKEeLNUC9MVgvOzFiTR?= MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjN|NkK0Okc,OjJ|M{[yOFY9N2F-
SF539 MkLoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LHNFAvODFvMUCwJO69VQ>? NXz3W3dpPDhiaB?= NHuyblBNd2diR1m1NF0uQC53OTDN M3PqPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{O2NlQ3Lz5{MkOzOlI1PjxxYU6=
SNB75 MmjGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrWUm13OC5yMT2xNFAh|ryP NH\QVlE1QCCq MXTMc4chT0l3ME2tPE42QCCP MlnvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|M{[yOFYoRjJ{M{O2NlQ3RC:jPh?=
SNB78 M4T6PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3K1VlAvODFvMUCwJO69VQ>? MnnYOFghcA>? NH3PdZZNd2diR1m1NF0uQC54NTDN NHzZNoI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOzOlI1Pid-MkKzN|YzPDZ:L3G+
HCC2998 NGrqd4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjLbocxNjBzLUGwNEDPxE1? NWDJPXl[PDhiaB?= NUXQVmd{VG:pIFfJOVA:NThwMEWgUS=> NF7rS4Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOzOlI1Pid-MkKzN|YzPDZ:L3G+
KM12 NGH3RphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mne4NE4xOS1zMECg{txO M1P4TlQ5KGh? M4Gz[Wxw\yCJSUWwQU04NjV2IF2= MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjN|NkK0Okc,OjJ|M{[yOFY9N2F-
HT-29 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWmwMlAyNTFyMDFOwG0> M4H6[|Q5KGh? M37TWWxw\yCJSUWwQU04Njd3IF2= M2LaSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{O2NlQ3Lz5{MkOzOlI1PjxxYU6=
HCT15 NVfwXXI{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX2wMlAyNTFyMDFOwG0> NIPaVpQ1QCCq NW[3cYRiVG:pIFfJOVA:NThwMEOgUS=> NF7FeHk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOzOlI1Pid-MkKzN|YzPDZ:L3G+
HCT116 MmruS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWG3UmVzOC5yMT2xNFAh|ryP M{m0UFQ5KGh? NVPnPW55VG:pIFfJOVA:NTdwNkGgUS=> MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjN|NkK0Okc,OjJ|M{[yOFY9N2F-
NCI-H23 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWGwMlAyNTFyMDFOwG0> MVi0PEBp M3zyfWxw\yCJSUWwQU04NjZ2IF2= M4X3bVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{O2NlQ3Lz5{MkOzOlI1PjxxYU6=
NCI-H226 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX[wMlAyNTFyMDFOwG0> M3;Ie|Q5KGh? MmjUUI9oKEeLNUC9MVgvPDRiTR?= Mk\lQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|M{[yOFYoRjJ{M{O2NlQ3RC:jPh?=
NCI-H522 M{\4WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TneFAvODFvMUCwJO69VQ>? NGLlclE1QCCq MoLhUI9oKEeLNUC9MVgvPDViTR?= MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjN|NkK0Okc,OjJ|M{[yOFY9N2F-
NCI-H438 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1Lnd|AvODFvMUCwJO69VQ>? MX[0PEBp MoP2UI9oKEeLNUC9MVgvOTFiTR?= MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjN|NkK0Okc,OjJ|M{[yOFY9N2F-
A549 M3HGbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDGNE4xOS1zMECg{txO NHnWbG41QCCq NWnFZWY2VG:pIFfJOVA:NThwMEegUS=> MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjN|NkK0Okc,OjJ|M{[yOFY9N2F-
DMS273 M2\J[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV[wMlAyNTFyMDFOwG0> MVK0PEBp NUe2WWJpVG:pIFfJOVA:NTdwOECgUS=> MmDvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|M{[yOFYoRjJ{M{O2NlQ3RC:jPh?=
DMS114 NXjvWGd2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWGwMlAyNTFyMDFOwG0> M{XIOVQ5KGh? M2XxW2xw\yCJSUWwQU05NjN7IF2= NWTyRW1rRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzN|YzPDZpPkKyN|M3OjR4PD;hQi=>
LOXIMVI MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfKNE4xOS1zMECg{txO M2PzR|Q5KGh? M1TBU2xw\yCJSUWwQU05NjZ4IF2= NInjSos9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOzOlI1Pid-MkKzN|YzPDZ:L3G+
OVCAR3 M2LtXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLCNE4xOS1zMECg{txO NFO4PXg1QCCq M{X2fWxw\yCJSUWwQU05NjF5IF2= NFTHU409[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOzOlI1Pid-MkKzN|YzPDZ:L3G+
OVCAR4 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVWwMlAyNTFyMDFOwG0> NF7EXFE1QCCq MmP5UI9oKEeLNUC9MVgvPThiTR?= NWXKTY9ZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzN|YzPDZpPkKyN|M3OjR4PD;hQi=>
OVCAR5 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHaNE4xOS1zMECg{txO MWO0PEBp MljXUI9oKEeLNUC9MVcvPTdiTR?= MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjN|NkK0Okc,OjJ|M{[yOFY9N2F-
OVCAR8 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvrXZcxNjBzLUGwNEDPxE1? MkXHOFghcA>? M{\k[Wxw\yCJSUWwQU04Njh2IF2= MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjN|NkK0Okc,OjJ|M{[yOFY9N2F-
SKOV3 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHVSIwxNjBzLUGwNEDPxE1? MUK0PEBp M3jCWGxw\yCJSUWwQU05NjRzIF2= NVHRU|IzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzN|YzPDZpPkKyN|M3OjR4PD;hQi=>
RXF631L MlHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnz4NE4xOS1zMECg{txO NGnuPY81QCCq MU\Mc4chT0l3ME2tPE4zOSCP MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjN|NkK0Okc,OjJ|M{[yOFY9N2F-
ACHN MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjPe5ppOC5yMT2xNFAh|ryP MmjJOFghcA>? NVy1Zo5xVG:pIFfJOVA:NTdwOUWgUS=> NIm2XJU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOzOlI1Pid-MkKzN|YzPDZ:L3G+
St-4 NIPVWXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfUfZdXOC5yMT2xNFAh|ryP NX:0dIxKPDhiaB?= MXfMc4chT0l3ME2tO{41PyCP NE\lbJc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOzOlI1Pid-MkKzN|YzPDZ:L3G+
MKN1 M1zid2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYGwMlAyNTFyMDFOwG0> NIC3VYY1QCCq NILme|NNd2diR1m1NF0uQC52MTDN MoHHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|M{[yOFYoRjJ{M{O2NlQ3RC:jPh?=
MKN7 M3PqXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXewMlAyNTFyMDFOwG0> M2rRTlQ5KGh? NX3BNFlSVG:pIFfJOVA:NTdwNkigUS=> M3fYSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{O2NlQ3Lz5{MkOzOlI1PjxxYU6=
MKN28 Ml61S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnnWIQxNjBzLUGwNEDPxE1? NYO2N256PDhiaB?= MnnwUI9oKEeLNUC9MVcvODdiTR?= MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjN|NkK0Okc,OjJ|M{[yOFY9N2F-
MKN45 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17mU|AvODFvMUCwJO69VQ>? MWe0PEBp NVvJSFEyVG:pIFfJOVA:NThwM{SgUS=> MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjN|NkK0Okc,OjJ|M{[yOFY9N2F-
MKN74 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWiwMlAyNTFyMDFOwG0> M2HyWVQ5KGh? M{Swd2xw\yCJSUWwQU04NjR{IF2= NYjIfHp[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzN|YzPDZpPkKyN|M3OjR4PD;hQi=>
DU145 NGPYbYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4e0e|AvODFvMUCwJO69VQ>? M4n6OVQ5KGh? M4rDUGxw\yCJSUWwQU05NjF4IF2= NH3w[5g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOzOlI1Pid-MkKzN|YzPDZ:L3G+
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BB65-RCC NWjNfYhoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzMUYhKSzVyPUGyMlczKG6P NVu5U3hORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh5OUS2N{8oRlODTlfFVlww[T5?
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GCT M3jYe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrjRZVKSzVyPUGzMlY5KG6P MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFc6PDZ|Lze+V2FPT0WUPD;hQi=>
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LB2241-RCC NFjhTJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTF2LkCxJI5O NFrsNpo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDd7NE[zM{c,W0GQR1XSQE9iRg>?
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COR-L105 NEX6XWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXOTWM2OD1zNT6wOEBvVQ>? MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFc6PDZ|Lze+V2FPT0WUPD;hQi=>
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VMRC-RCZ M3rTRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TJfGlEPTB;MUWuOlMhdk1? MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFc6PDZ|Lze+V2FPT0WUPD;hQi=>
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KARPAS-299 M3e5cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PqT2lEPTB;MT63PVQ4QSEQvF2= M1\jUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5Pzl2NkOvK|5USU6JRWK8M4E,
NCI-H358 Ml7vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnpNY53UUN3ME2xMlk2PTB|IN88US=> MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFc6PDZ|Lze+V2FPT0WUPD;hQi=>
OAW-28 NV\z[pg6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonmTWM2OD1{LkC2PVE6KM7:TR?= NYixfW9NRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh5OUS2N{8oRlODTlfFVlww[T5?
C8166 NHzZXYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTJwNkOzPVIh|ryP NEnJV4Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDd7NE[zM{c,W0GQR1XSQE9iRg>?
COLO-678 M17hW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37JWWlEPTB;Mj64N|c3QCEQvF2= NWLISWoxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh5OUS2N{8oRlODTlfFVlww[T5?
SK-N-DZ MlPTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1ezNmlEPTB;Mj64OlM5OSEQvF2= MoW4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg4QTR4Mz:nQnNCVkeHUkyvZV4>
NCI-H82 NFHjW3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnoTWM2OD1{LkmwN|Y6KM7:TR?= MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFc6PDZ|Lze+V2FPT0WUPD;hQi=>
JVM-2 NILTO|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTNwMEOxPFgh|ryP NUHqPWo1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh5OUS2N{8oRlODTlfFVlww[T5?
SW1116 NXq0WHFkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTaTWM2OD1|LkC1OFEyKM7:TR?= MlLUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg4QTR4Mz:nQnNCVkeHUkyvZV4>
MDA-MB-453 NFHvVJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33kSmlEPTB;Mz6xNFQ{QSEQvF2= NV7sSWNZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh5OUS2N{8oRlODTlfFVlww[T5?
Calu-6 M4PvcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXW[YxKSzVyPUOuNVk6PyEQvF2= M1W0cFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5Pzl2NkOvK|5USU6JRWK8M4E,
SHP-77 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn6xTWM2OD1|LkWyPEDPxE1? M4fkcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5Pzl2NkOvK|5USU6JRWK8M4E,
Capan-2 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTRwM{K1PFEh|ryP M4TlbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5Pzl2NkOvK|5USU6JRWK8M4E,
SW948 MlPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjjSIhQUUN3ME20Mlc1Pzd7IN88US=> MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFc6PDZ|Lze+V2FPT0WUPD;hQi=>
HDLM-2 M2XuPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPvTWM2OD13LkC3O|I2KM7:TR?= NGr0UXQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDd7NE[zM{c,W0GQR1XSQE9iRg>?
LAN-6 NVHQVoNIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTZwMkG0PVUh|ryP NV3rcYxKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh5OUS2N{8oRlODTlfFVlww[T5?
LU-135 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXDVIlQUUN3ME22MlQ{ODd5IN88US=> NWPzXmZRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh5OUS2N{8oRlODTlfFVlww[T5?
T84 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\UTWM2OD14Lkm4OlQh|ryP M{\3S|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5Pzl2NkOvK|5USU6JRWK8M4E,
CAPAN-1 NUfpcY9ET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVm5NFNxUUN3ME23MlYzOjN|IN88US=> M1XuWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5Pzl2NkOvK|5USU6JRWK8M4E,
SW1417 M{PTPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUG3XYVwUUN3ME23MlkyPzNzIN88US=> MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFc6PDZ|Lze+V2FPT0WUPD;hQi=>
BALL-1 M2CzPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnSZ3RZUUN3ME24MlUxPDB7IN88US=> M{f6clxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5Pzl2NkOvK|5USU6JRWK8M4E,
HT-29 NYjMfZNoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRTlwMEe1PVkh|ryP NV25VmdJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh5OUS2N{8oRlODTlfFVlww[T5?
C3A Ml;PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fVd2lEPTB;OT64PFM6PCEQvF2= M2qze|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5Pzl2NkOvK|5USU6JRWK8M4E,
NCI-H1993 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTxXYxKSzVyPUGwMlUxQDFizszN M{HlcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5Pzl2NkOvK|5USU6JRWK8M4E,
SK-MEL-1 NYD2Oo9{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLUUnBjUUN3ME2xNU43Ojh7IN88US=> MljhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg4QTR4Mz:nQnNCVkeHUkyvZV4>
DU-145 Mn;iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljsTWM2OD1zND61NFUzKM7:TR?= NF\QdpE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDd7NE[zM{c,W0GQR1XSQE9iRg>?
KP-N-YN M3rEXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33Dd2lEPTB;MUSuOVExOyEQvF2= NUDXdVJZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh5OUS2N{8oRlODTlfFVlww[T5?
CCRF-CEM M3zqeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTF2Lke4NFkh|ryP NIHsUHE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDd7NE[zM{c,W0GQR1XSQE9iRg>?
ZR-75-30 NHLpSnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfSZWFKSzVyPUG2MlM{ODNizszN NFnoOpc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDd7NE[zM{c,W0GQR1XSQE9iRg>?
A673 NHr1OphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTJyLkW1NFch|ryP M3yzelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5Pzl2NkOvK|5USU6JRWK8M4E,
K-562 NEix[2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDQVJpKSzVyPUK4MlQyQDNizszN MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFc6PDZ|Lze+V2FPT0WUPD;hQi=>

... 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]

- Collapse

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]

- Collapse
  • 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]

- Collapse
  • 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
Smiles CC(C)(C#N)C1=CC=C(C=C1)N2C3=C4C=C(C=CC4=NC=C3N(C2=O)C)C5=CC6=CC=CC=C6N=C5

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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
    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.

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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.

PI3K Signaling Pathway Map

PI3K Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID