Dactolisib (BEZ235)

Catalog No.S1009 Synonyms: NVP-BEZ235

For research use only.

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.

Dactolisib (BEZ235) Chemical Structure

CAS No. 915019-65-7

Selleck's Dactolisib (BEZ235) has been cited by 433 publications

Purity & Quality Control

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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)
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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 NXPme3JVSW62aX3pZ5Jw[mmjbDDBd5NigQ>? NGHCUpQyQCCq MVfEUXNQ Mln0RY51cXS{eYDhco9{d22jbDDhZ5Rqfmm2eTD3bZRpKEWFNUCgc4YhOC5yMEK1JO69VQ>? NIDMcVU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEiwOVk1Pid-MkS4NFU6PDZ:L3G+
MCF7 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXGwMlAyNTFyMDFOwG0> MmG1OFghcA>? MXTEUXNQ NYHtWpVKUUN3ME2wMlc{KM7:TR?= Mlu1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6N{G5NFQoRjJ|OEexPVA1RC:jPh?=
HCT116 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1ezV|AvODFvMUCwJO69VQ>? MY[0PEBp MVHEUXNQ NEn4W5RKSzVyPUGuNVYh|ryP NIqzPWg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i3NVkxPCd-MkO4O|E6ODR:L3G+
U87MG NVHYcII4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2W5c|AvODFvMUCwJO69VQ>? NXf6PHY5PDhiaB?= NFH2VFdFVVOR NVXN[ZVSUUN3ME2xMlMzKM7:TR?= NYf2bXc1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4O|E6ODRpPkKzPFcyQTB2PD;hQi=>
HBC4 Mnz4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3WU|gxNjBzLUGwNEDPxE1? MV60PEBp M1XQeWxw\yCJSUWwQU05NjZzIF2= NFnxdXQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOzOlI1Pid-MkKzN|YzPDZ:L3G+
BSY1 M3\4NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\TV2sxNjBzLUGwNEDPxE1? MVK0PEBp MnS2UI9oKEeLNUC9MVgvPDhiTR?= NWHqVmxvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzN|YzPDZpPkKyN|M3OjR4PD;hQi=>
HBC5 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\zNE4xOS1zMECg{txO NH24SWw1QCCq NH\hW5JNd2diR1m1NF0uPy56NzDN MlX1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|M{[yOFYoRjJ{M{O2NlQ3RC:jPh?=
MCF7 NVywb5Q5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm[2NE4xOS1zMECg{txO MXy0PEBp MmroUI9oKEeLNUC9MVgvOTZiTR?= MnnSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|M{[yOFYoRjJ{M{O2NlQ3RC:jPh?=
MDA-MB-231 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;kNE4xOS1zMECg{txO M{LaWVQ5KGh? MoPKUI9oKEeLNUC9MVgvODliTR?= NFHGb4U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOzOlI1Pid-MkKzN|YzPDZ:L3G+
U251 M1nNe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUSwMlAyNTFyMDFOwG0> MoLxOFghcA>? MXzMc4chT0l3ME2tO{43PiCP Mnu3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|M{[yOFYoRjJ{M{O2NlQ3RC:jPh?=
SF268 MlfzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTNU2R4OC5yMT2xNFAh|ryP MYm0PEBp MoO0UI9oKEeLNUC9MVcvQTJiTR?= NVLZNpRERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzN|YzPDZpPkKyN|M3OjR4PD;hQi=>
SF295 MkD4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHq4fVkxNjBzLUGwNEDPxE1? NVj1PZlqPDhiaB?= MUfMc4chT0l3ME2tPE4{OSCP NW\ESYNnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzN|YzPDZpPkKyN|M3OjR4PD;hQi=>
SF539 MljIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml:xNE4xOS1zMECg{txO NIXYbVA1QCCq M3Ljd2xw\yCJSUWwQU05NjV7IF2= NVzyUpN[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzN|YzPDZpPkKyN|M3OjR4PD;hQi=>
SNB75 NX7tcYE{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nY[lAvODFvMUCwJO69VQ>? MmnqOFghcA>? NFv5O2ZNd2diR1m1NF0uQC53ODDN M1zMPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{O2NlQ3Lz5{MkOzOlI1PjxxYU6=
SNB78 Mlv0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXF[XgxNjBzLUGwNEDPxE1? M2PHelQ5KGh? M{X3Rmxw\yCJSUWwQU05NjZ3IF2= MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjN|NkK0Okc,OjJ|M{[yOFY9N2F-
HCC2998 MmfrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlu3NE4xOS1zMECg{txO MljJOFghcA>? M4e3bGxw\yCJSUWwQU05NjB3IF2= MlHnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|M{[yOFYoRjJ{M{O2NlQ3RC:jPh?=
KM12 M1TTUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\j[3oxNjBzLUGwNEDPxE1? MUW0PEBp NUXES4tCVG:pIFfJOVA:NTdwNUSgUS=> NV3m[pR{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzN|YzPDZpPkKyN|M3OjR4PD;hQi=>
HT-29 NHT4UIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWOwMlAyNTFyMDFOwG0> NFTwOnk1QCCq NIL4[IJNd2diR1m1NF0uPy55NTDN NHeyclQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOzOlI1Pid-MkKzN|YzPDZ:L3G+
HCT15 NIHZOpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTtNE4xOS1zMECg{txO MYi0PEBp MWXMc4chT0l3ME2tPE4xOyCP NXS3cIs6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzN|YzPDZpPkKyN|M3OjR4PD;hQi=>
HCT116 M2H1Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjySGM4OC5yMT2xNFAh|ryP MWm0PEBp NHPSW49Nd2diR1m1NF0uPy54MTDN NXTxdG9bRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzN|YzPDZpPkKyN|M3OjR4PD;hQi=>
NCI-H23 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnL0NE4xOS1zMECg{txO MlnTOFghcA>? M4n3UWxw\yCJSUWwQU04NjZ2IF2= MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjN|NkK0Okc,OjJ|M{[yOFY9N2F-
NCI-H226 MmjNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Moq0NE4xOS1zMECg{txO NWDNZVJCPDhiaB?= MY\Mc4chT0l3ME2tPE41PCCP NIHheIc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOzOlI1Pid-MkKzN|YzPDZ:L3G+
NCI-H522 NF7pblZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rufVAvODFvMUCwJO69VQ>? MUO0PEBp NV;HfHA4VG:pIFfJOVA:NThwNEWgUS=> NF;tR|Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOzOlI1Pid-MkKzN|YzPDZ:L3G+
NCI-H438 MkPTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrI[YMyOC5yMT2xNFAh|ryP M3PhZVQ5KGh? NVf2b4dbVG:pIFfJOVA:NThwMUGgUS=> MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjN|NkK0Okc,OjJ|M{[yOFY9N2F-
A549 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVqwMlAyNTFyMDFOwG0> M4rkOlQ5KGh? MoLjUI9oKEeLNUC9MVgvODdiTR?= NGfMOHc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOzOlI1Pid-MkKzN|YzPDZ:L3G+
DMS273 NFfhcGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWSwMlAyNTFyMDFOwG0> NV;3cHlxPDhiaB?= NILVRVBNd2diR1m1NF0uPy56MDDN NWDHR2tiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzN|YzPDZpPkKyN|M3OjR4PD;hQi=>
DMS114 M1fvUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXKwMlAyNTFyMDFOwG0> Mn\rOFghcA>? NULGcGV3VG:pIFfJOVA:NThwM{mgUS=> M3jjPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{O2NlQ3Lz5{MkOzOlI1PjxxYU6=
LOXIMVI M3faPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF6yOWUxNjBzLUGwNEDPxE1? MkjtOFghcA>? NWj0OpJYVG:pIFfJOVA:NThwNk[gUS=> MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjN|NkK0Okc,OjJ|M{[yOFY9N2F-
OVCAR3 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYWwMlAyNTFyMDFOwG0> NH3YNpM1QCCq Mn30UI9oKEeLNUC9MVgvOTdiTR?= MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjN|NkK0Okc,OjJ|M{[yOFY9N2F-
OVCAR4 MoDmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\2cZgxNjBzLUGwNEDPxE1? M3vR[|Q5KGh? NI\MZ2dNd2diR1m1NF0uQC53ODDN NGrSSYk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOzOlI1Pid-MkKzN|YzPDZ:L3G+
OVCAR5 NHewPJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml24NE4xOS1zMECg{txO MmfsOFghcA>? Mn\LUI9oKEeLNUC9MVcvPTdiTR?= NEXGflA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOzOlI1Pid-MkKzN|YzPDZ:L3G+
OVCAR8 Mm[0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXGwMlAyNTFyMDFOwG0> MoXIOFghcA>? NFrQ[XRNd2diR1m1NF0uPy56NDDN MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjN|NkK0Okc,OjJ|M{[yOFY9N2F-
SKOV3 NHnvOXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYGwMlAyNTFyMDFOwG0> NWTxTnREPDhiaB?= MXfMc4chT0l3ME2tPE41OSCP M3e1bVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{O2NlQ3Lz5{MkOzOlI1PjxxYU6=
RXF631L NXHEbphRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXWwMlAyNTFyMDFOwG0> MlfoOFghcA>? MYPMc4chT0l3ME2tPE4zOSCP MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjN|NkK0Okc,OjJ|M{[yOFY9N2F-
ACHN MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLBNlZzOC5yMT2xNFAh|ryP M{O4OVQ5KGh? M3XRNWxw\yCJSUWwQU04Njl3IF2= MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjN|NkK0Okc,OjJ|M{[yOFY9N2F-
St-4 Mom5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fRSVAvODFvMUCwJO69VQ>? NEjETW41QCCq NHj3fXVNd2diR1m1NF0uPy52NzDN M1zY[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{O2NlQ3Lz5{MkOzOlI1PjxxYU6=
MKN1 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDONE4xOS1zMECg{txO MmXqOFghcA>? MYHMc4chT0l3ME2tPE41OSCP NGm5NGc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOzOlI1Pid-MkKzN|YzPDZ:L3G+
MKN7 NVfLXpN{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVqwMlAyNTFyMDFOwG0> NUTOUVB3PDhiaB?= NU\FWnU{VG:pIFfJOVA:NTdwNkigUS=> NFzxeWM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOzOlI1Pid-MkKzN|YzPDZ:L3G+
MKN28 NHnkeJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXuwMlAyNTFyMDFOwG0> NFX6Umk1QCCq NXjGdVNbVG:pIFfJOVA:NTdwMEegUS=> NYT4c3NYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzN|YzPDZpPkKyN|M3OjR4PD;hQi=>
MKN45 MnvWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfqd5IxNjBzLUGwNEDPxE1? MVG0PEBp NWXzdZRZVG:pIFfJOVA:NThwM{SgUS=> M2HKW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{O2NlQ3Lz5{MkOzOlI1PjxxYU6=
MKN74 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjTNE4xOS1zMECg{txO NH35VZY1QCCq M{P3[2xw\yCJSUWwQU04NjR{IF2= NGrTfnk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOzOlI1Pid-MkKzN|YzPDZ:L3G+
DU145 M3uxVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXKwMlAyNTFyMDFOwG0> NF;jN5I1QCCq MkLDUI9oKEeLNUC9MVgvOTZiTR?= MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjN|NkK0Okc,OjJ|M{[yOFY9N2F-
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Trypanosoma brucei brucei MWfGeY5kfGmxbjDBd5NigQ>? NHe0VlkzODBibl2= MoDWNVIhcA>? MoPwSG1UVw>? NXy0dIhRTGWlcnXhd4UhcW5icHjvd5Bpd3SrZInsJIlvd3OrdH;sJJBpd3OyaHH0[UBt\X[nbB?= MknxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6MEW5OFYoRjJ2OEC1PVQ3RC:jPh?=
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BB65-RCC Ml\jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\EXmlEPTB;MUKuO|Ihdk1? NUDHZph{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh5OUS2N{8oRlODTlfFVlww[T5?
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GCT M1rL[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPxRphCUUN3ME2xN{43QCCwTR?= NX\QXVdORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh5OUS2N{8oRlODTlfFVlww[T5?
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LB2241-RCC NYXrSZhmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnt[WR1UUN3ME2xOE4xOSCwTR?= NVjlPGJVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh5OUS2N{8oRlODTlfFVlww[T5?
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COR-L105 NH3vOVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTF3LkC0JI5O NVjx[nhnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh5OUS2N{8oRlODTlfFVlww[T5?
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VMRC-RCZ NVm5eGw2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vY[WlEPTB;MUWuOlMhdk1? NGj4NHE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDd7NE[zM{c,W0GQR1XSQE9iRg>?
HH MmT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7kdo5KSzVyPUG1Mlchdk1? M1u0WFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5Pzl2NkOvK|5USU6JRWK8M4E,
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LAMA-84 NGf2dHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2X0TWlEPTB;M{WuPFchdk1? MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFc6PDZ|Lze+V2FPT0WUPD;hQi=>
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EPLC-272H NGjuSVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XnVmlEPTB;NESuN|khdk1? NX33VIx5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh5OUS2N{8oRlODTlfFVlww[T5?
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KYSE-180 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTR4LkG3JI5O MlzMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg4QTR4Mz:nQnNCVkeHUkyvZV4>
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PC-14 NHf2c2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHsW|FiUUN3ME20Ok42PyCwTR?= NEDTWms9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDd7NE[zM{c,W0GQR1XSQE9iRg>?
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LB996-RCC NUPiNWpIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTR5LkG5JI5O MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFc6PDZ|Lze+V2FPT0WUPD;hQi=>
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MCF7 NH3EU41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnUTWM2OD12OD61PEBvVQ>? M1[wWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5Pzl2NkOvK|5USU6JRWK8M4E,
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NCI-H82 NETI[WtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmm3TWM2OD1{LkmwN|Y6KM7:TR?= MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFc6PDZ|Lze+V2FPT0WUPD;hQi=>
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SHP-77 NX[0dYc1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2P0ZWlEPTB;Mz61Nlgh|ryP NFHuZ5M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDd7NE[zM{c,W0GQR1XSQE9iRg>?
Capan-2 NEfy[Y5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXFNJFRUUN3ME20MlMzPThzIN88US=> NYr3c41yRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh5OUS2N{8oRlODTlfFVlww[T5?
SW948 NFTxTlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTyRnJKSzVyPUSuO|Q4PzlizszN M1fIZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5Pzl2NkOvK|5USU6JRWK8M4E,
HDLM-2 NYXEcmpkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nJcWlEPTB;NT6wO|czPSEQvF2= NH34WJQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDd7NE[zM{c,W0GQR1XSQE9iRg>?
LAN-6 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInieIZKSzVyPU[uNlE1QTVizszN MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFc6PDZ|Lze+V2FPT0WUPD;hQi=>
LU-135 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17HVWlEPTB;Nj60N|A4PyEQvF2= Mmq4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg4QTR4Mz:nQnNCVkeHUkyvZV4>
T84 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7pTWM2OD14Lkm4OlQh|ryP NGXEO2c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDd7NE[zM{c,W0GQR1XSQE9iRg>?
CAPAN-1 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTdwNkKyN|Mh|ryP NHv2T4I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDd7NE[zM{c,W0GQR1XSQE9iRg>?
SW1417 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVKzN2F1UUN3ME23MlkyPzNzIN88US=> MlTsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg4QTR4Mz:nQnNCVkeHUkyvZV4>
BALL-1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRThwNUC0NFkh|ryP NHeySpI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDd7NE[zM{c,W0GQR1XSQE9iRg>?
HT-29 M3PXfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7hTWM2OD17LkC3OVk6KM7:TR?= M{n3UVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5Pzl2NkOvK|5USU6JRWK8M4E,
C3A NUD0RVhbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrSemtKSzVyPUmuPFg{QTRizszN MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFc6PDZ|Lze+V2FPT0WUPD;hQi=>
NCI-H1993 M1PiZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13ZbmlEPTB;MUCuOVA5OSEQvF2= NF3adW49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDd7NE[zM{c,W0GQR1XSQE9iRg>?
SK-MEL-1 M4DZZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LZSGlEPTB;MUGuOlI5QSEQvF2= Mmm2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg4QTR4Mz:nQnNCVkeHUkyvZV4>
DU-145 NU\BSJNFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zmcGlEPTB;MUSuOVA2OiEQvF2= MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFc6PDZ|Lze+V2FPT0WUPD;hQi=>
KP-N-YN Mn\VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnCTWM2OD1zND61NVA{KM7:TR?= NE\6enk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDd7NE[zM{c,W0GQR1XSQE9iRg>?
CCRF-CEM MnrpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LkSmlEPTB;MUSuO|gxQSEQvF2= MnXCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg4QTR4Mz:nQnNCVkeHUkyvZV4>
ZR-75-30 M1TPVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX6ye4c2UUN3ME2xOk4{OzB|IN88US=> MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFc6PDZ|Lze+V2FPT0WUPD;hQi=>
A673 NXixSog2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHnsZWRKSzVyPUKwMlU2ODdizszN NXjDbYVERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh5OUS2N{8oRlODTlfFVlww[T5?
K-562 MkW2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\STWM2OD1{OD60NVg{KM7:TR?= MoOxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg4QTR4Mz:nQnNCVkeHUkyvZV4>
Assay
Methods Test Index PMID
Western blot Myc / Vinculin / pT58 Myc ; pAkt / Akt / Skp2 / AR / pS6 / p27 ; p-S6K / S6K / p-Akt / Akt / p-ABL / BCR-ABL ; Bcl-2 / Caspase-3 / Cleaved caspase-3 ; Cyclin D1 / Cyclin D2 ; mTOR / p-mTOR / p70S6K / p-p70S6K ; p-EGFR-Tyr1068 / EGFR / p-HER2-Tyr1221 / p-HER2-Tyr1222 / HER2 / p-HER3-Tyr1289 25934076 24347472 28435223 29581778 21278786
Immunofluorescence SP1 ; p-ErbB2(Y1248) ; LC3 26336820 24675532 23603977
Growth inhibition assay Cell viability (P3, U87) ; Cell viability (breast cancer cells) ; Cell viability (K562, KBM7R) 27542970 28060760 28435223
ELISA VEGF 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 (from reference)

Kinase Assay:

[1]

  • 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]

  • 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.

Animal Research:

[1]

  • Animal Models: Female Harlan athymic nude mice
  • Dosages: 45 mg/kg
  • Administration: p.o.

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 469.55
Formula

C30H23N5O

CAS No. 915019-65-7
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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

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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.

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