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 82 Publications

11 Customer Reviews

  • Level of phospho-proteins in RTK and PI3K–Akt–mTOR pathways in treated tumours, detected with western blot.

    Nature, 2017, 728-732. Dactolisib (BEZ235, NVP-BEZ235) purchased from Selleck.

    Relative kinase activities of p110α mutants and the inhibitory effect of PI3K inhibitors against hotspot mutants of p110α. A, recombinant FLAG-tagged PI3K p110α/p85α protein complex produced in 293T cells was immunoprecipitated , and the immunoprecipitates were used for the quantitative PI3K-HTRF assay (32).

    B, effect of three PI3K inhibitors (ZSTK474, LY294002, and NVP-BEZ235) on the enzymatic activity of two hotspot mutants (E545K and H1047R) p110α compared with the wild-type. No striking difference was observed in the IC50 concentrations of these inhibitors between wild-type and mutant p110α.
     

     

    Cancer Res 2010 70, 4982-4994. Dactolisib (BEZ235, NVP-BEZ235) purchased from Selleck.

  • A, ANOVA of IC50 values of the dual PI3K/mTOR inhibitor NVP-BEZ235 in 23 melanoma cell lines showing no significant difference in sensitivity to this compound in B-Raf mutant and Braf wild-type cells. B, decreases in pAkt and pP70S6K in a dose and time-dependent fashion in 2 melanoma cell lines treated with NVP-BEZ235. pP70S6K levels are undetectable at all concentrations and time points studied, whereas levels of pAkt start rising again after 4 hours of drug exposure in a dose-dependent fashion. C, clonogenic assays in 2 melanoma cell lines (YUVON and YUSIK) treated with NVP-BEZ235 at different concentrations. NVPBEZ235 was effective in inhibiting colony formation at low nanomolar concentrations.

    Clin Cancer Res 2010 16, 6029-6039. Dactolisib (BEZ235, NVP-BEZ235) purchased from Selleck.

    Three-dimensional responses of MCF7/IGF-1R cells to TAM (1 μM), E2 and IGF-1. Compared to parental MCF7 cells (a), MCF7/IGF-1R cells (b) in three-dimensional (3D) culture formed bigger acini in response to IGF-1 stimulation and displayed significant TAM resistance when treated with TAM (1 μM) + E2 + IGF-1, which was removable by kinase inhibitors BMS-536924, U0126 and BEZ235 (c). Cells (10,000/well) were seeded in 96-well plates. Acini were formed on 100% Matrigel and cultured for 14 days in starving medium containing 2% Matrigel and 5% charcoal/dextran-stripped fetal bovine serum with the treatments as indicated. Concentrations used: TAM (1 μM), E2 (1 nM) and IGF-1 (100 ng/mL). Confocal image original magnification, × 20. Red, rhodamine phalloidin (actin). Blue, Hoechst blue stain. Results are representative of two individual experiments.

    Breast Cancer Res 2011 13, R52. Dactolisib (BEZ235, NVP-BEZ235) purchased from Selleck.

  • TAM (10 nM) agonistic behavior in MCF7/IGF-1R cells is not inhibited by phosphatidylinositol 3-kinase/Akt inhibitor BEZ235. (a) Inhibitory effects of kinase inhibitors BMS-536924, U0126 and BEZ235 on agonistic effect of TAM (10 nM) in the presence of IGF-1 (100 ng/mL). **P < 0.01. (b) Inhibitory effects of phosphatidylinositol 3-kinase (PI3K)/Akt inhibitor BEZ235 at various dose ranges on IGF-1R signaling. (c) Agonistic behavior of TAM (10 nM) in response to BEZ235 kinase inhibitor. (-), no BEZ235. Results are representative of three independent experiments. Data are expressed as means ± SD.

    Breast Cancer Res 2011 13:R52. Dactolisib (BEZ235, NVP-BEZ235) purchased from Selleck.

    ZSTK474 and GDC-0941 selectively inhibit class I PI3K over mTOR. (A) Inhibition profiles of the selected five PI3K inhibitors for mTOR. Data shown are mean±SD (n = 3), representative of 2 or 3 independent experiments. (B) IC50 values of the PI3K inhibitors for mTOR. (C) Selectivity of each PI3K inhibitor for PI3Ka over mTOR. The selectivity index is expressed as the ratio of the IC50 value for mTOR over that for PI3Ka. The IC50 values of ZSTK474, NVP-BEZ235 and LY294002 for PI3Ka are 0.016, 0.007 and 0.6 μM, respectively, as reported previously by us.

     

     

    Eur J Cancer 2010 46, 1111-1121. Dactolisib (BEZ235, NVP-BEZ235) purchased from Selleck.

  • (B) The effects of AZD2014, BEZ235, lapatinib, LEE011, pazopanib on PI3K/AKT signaling in sarcoma PDC line were determined by immunoblotting analysis. Cells were treated with 1 μM of the indicated drugs for 72 h.

    Transl Oncol, 2016, 9(3):197-202. Dactolisib (BEZ235, NVP-BEZ235) purchased from Selleck.

    The effects of LY294002, rapamycin and NVP-BEZ235 on activation of PI3K-Akt-mTOR pathway in hepatocytes. (a) The mRNA expression (PI3K, Akt, mTOR, raptor) by Real-Time PCR, (b) protein expression (PI3K, Akt, mTOR, S6K) by ELISA kits; (c) protein expression of S6K and P-S6K by western blotting. The different letters indicated significant differences (P <0.05). LY = LY294002; rapa = rapamycin; NVP = NVP-BEZ235.

    Animal, 2016, 10(8):1319-27. Dactolisib (BEZ235, NVP-BEZ235) purchased from Selleck.

  •  After starved in serum-free medium for 24h,breast cancer cells incubated with the indicated concentrations of BEZ235 for 3h,followed by 20-minute  stimulation of 100ng/ml EGF.

     

     

     

    Dr. Zhang of Tianjin Medical University. Dactolisib (BEZ235, NVP-BEZ235) purchased from Selleck.

    After starved in serum-free medium for 24h,breast cancer cells incubated with the indicated concentrations of BEZ235 for 3h,followed by 20-minute  stimulation of 100ng/ml EGF.

     

     

    Dr. Zhang of Tianjin Medical University. Dactolisib (BEZ235, NVP-BEZ235) purchased from Selleck.

  •  

    FIG. 4. Phospholipase A2 group 4A (PLA2G4A) expression was increased after BEZ235 treatment in basal-like xenografts. The bar graph shows the quantification of the immunoblots (mean±SD). PLA2G4A, Ethanolamine kinase 1 and 2 (ETNK1/2), Choline kinase alpha/beta (ChoKA/B), and β-actin protein expression were examined by immunoblotting of tissue samples after MRS experiments [control group (n= 5) and BEZ235-treated group (n=7)]. This demonstrated a higher expression of PLA2G4A protein ( P=0.005), but no changes in ETNK1 and ChoKA/B in samples from basal-like xenografts treated with BEZ235.

    Dactolisib (BEZ235, NVP-BEZ235) purchased from Selleck.

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 MX;BcpRqdWmlcn;ibYFtKEG|c3H5 MkLzNVghcA>? Mk\4SG1UVw>? M1vmW2FvfGm2conwZY5we2:vYXygZYN1cX[rdImge4l1cCCHQ{WwJI9nKDBwMECyOUDPxE1? NXT1cmJ5OjR6MEW5OFY>
MCF7 M2fGWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUmwMlAyNTFyMDFOwG0> NWrBNJhYPDhiaB?= M3\tcWROW09? MU\JR|UxRTBwN{Og{txO NHXFW|UzOzh5MUmwOC=>
HCT116 NHvxcoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjQU5YxNjBzLUGwNEDPxE1? MX[0PEBp MV7EUXNQ MVPJR|UxRTFwMU[g{txO NH\EcXEzOzh5MUmwOC=>
U87MG NVK4Ood2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIT1PWQxNjBzLUGwNEDPxE1? M{PuXFQ5KGh? NYnCfnpWTE2VTx?= NHjkbYFKSzVyPUGuN|Ih|ryP Mn;FNlM5PzF7MES=
HBC4 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVGwMlAyNTFyMDFOwG0> MV[0PEBp Mk[2UI9oKEeLNUC9MVgvPjFiTR?= NHm3ZVMzOjN|NkK0Oi=>
BSY1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{Phd|AvODFvMUCwJO69VQ>? M1\OS|Q5KGh? Mn;qUI9oKEeLNUC9MVgvPDhiTR?= MknGNlI{OzZ{NE[=
HBC5 M3nzNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7KfYwxNjBzLUGwNEDPxE1? NIHBcHk1QCCq MWnMc4chT0l3ME2tO{45PyCP M1qxc|IzOzN4MkS2
MCF7 M1;sXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrl[JZ6OC5yMT2xNFAh|ryP NHzjfng1QCCq MXLMc4chT0l3ME2tPE4yPiCP MkTENlI{OzZ{NE[=
MDA-MB-231 NEfHRo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXmfJkxNjBzLUGwNEDPxE1? NGrVe4s1QCCq NF7Xc3pNd2diR1m1NF0uQC5yOTDN MUiyNlM{PjJ2Nh?=
U251 M3;kWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYKybYRQOC5yMT2xNFAh|ryP NW\Ic5N6PDhiaB?= MmfFUI9oKEeLNUC9MVcvPjZiTR?= MmDXNlI{OzZ{NE[=
SF268 MnrNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjCNE4xOS1zMECg{txO NEPjNYs1QCCq MoTnUI9oKEeLNUC9MVcvQTJiTR?= NHnISpczOjN|NkK0Oi=>
SF295 MlHCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkD2NE4xOS1zMECg{txO NXjpNGs{PDhiaB?= NFHQPVVNd2diR1m1NF0uQC5|MTDN NFjtdYUzOjN|NkK0Oi=>
SF539 MojsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDSO4poOC5yMT2xNFAh|ryP NILJenU1QCCq NY\oXJhzVG:pIFfJOVA:NThwNUmgUS=> NUHXZY9oOjJ|M{[yOFY>
SNB75 MljUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3P6e|AvODFvMUCwJO69VQ>? NXy3NIJSPDhiaB?= NIG0d4NNd2diR1m1NF0uQC53ODDN NV2zO3g2OjJ|M{[yOFY>
SNB78 M3rDRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlqwNE4xOS1zMECg{txO MWq0PEBp NVja[WE{VG:pIFfJOVA:NThwNkWgUS=> M{mwb|IzOzN4MkS2
HCC2998 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUGwMlAyNTFyMDFOwG0> MknMOFghcA>? NF:wSolNd2diR1m1NF0uQC5yNTDN M3XHVFIzOzN4MkS2
KM12 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnZZnpOOC5yMT2xNFAh|ryP MUi0PEBp MoHBUI9oKEeLNUC9MVcvPTRiTR?= NXn6dYhFOjJ|M{[yOFY>
HT-29 M1rDfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUSwMlAyNTFyMDFOwG0> MXy0PEBp M1HIcWxw\yCJSUWwQU04Njd3IF2= MkSxNlI{OzZ{NE[=
HCT15 MoL6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLWNE4xOS1zMECg{txO NYHsO5U4PDhiaB?= NWexXnNFVG:pIFfJOVA:NThwMEOgUS=> NUPi[IlEOjJ|M{[yOFY>
HCT116 MnjYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYH1W5B3OC5yMT2xNFAh|ryP NGDtPVI1QCCq NXG0UVBQVG:pIFfJOVA:NTdwNkGgUS=> MYiyNlM{PjJ2Nh?=
NCI-H23 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TqdFAvODFvMUCwJO69VQ>? NXHORmxVPDhiaB?= MV;Mc4chT0l3ME2tO{43PCCP MV[yNlM{PjJ2Nh?=
NCI-H226 NWex[GV6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYCwMlAyNTFyMDFOwG0> NYTQS3J7PDhiaB?= MnPLUI9oKEeLNUC9MVgvPDRiTR?= MnT6NlI{OzZ{NE[=
NCI-H522 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYn3c|MyOC5yMT2xNFAh|ryP NF:wNmU1QCCq M2m1Wmxw\yCJSUWwQU05NjR3IF2= NHj4b2IzOjN|NkK0Oi=>
NCI-H438 M1rYNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nkWVAvODFvMUCwJO69VQ>? MVK0PEBp NFK1OGNNd2diR1m1NF0uQC5zMTDN M3TSXFIzOzN4MkS2
A549 M{nUXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjHcHQxNjBzLUGwNEDPxE1? NV\3UI5lPDhiaB?= M4\xdmxw\yCJSUWwQU05NjB5IF2= NY\RfIlJOjJ|M{[yOFY>
DMS273 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHpc2J4OC5yMT2xNFAh|ryP NITGSZM1QCCq Moj6UI9oKEeLNUC9MVcvQDBiTR?= MXWyNlM{PjJ2Nh?=
DMS114 MnvkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljzNE4xOS1zMECg{txO NUG2d5MxPDhiaB?= NULDT25JVG:pIFfJOVA:NThwM{mgUS=> NVq4W4R3OjJ|M{[yOFY>
LOXIMVI NIfRPXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPDZmRxOC5yMT2xNFAh|ryP MXK0PEBp M4TDV2xw\yCJSUWwQU05NjZ4IF2= MnryNlI{OzZ{NE[=
OVCAR3 NUSxZmhST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfEPFExNjBzLUGwNEDPxE1? MUC0PEBp MVHMc4chT0l3ME2tPE4yPyCP MkHUNlI{OzZ{NE[=
OVCAR4 MkfiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjINE4xOS1zMECg{txO NUe5eHZCPDhiaB?= Mo[5UI9oKEeLNUC9MVgvPThiTR?= MVOyNlM{PjJ2Nh?=
OVCAR5 MorVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULWRVlpOC5yMT2xNFAh|ryP NV3STFRiPDhiaB?= NIDjd4FNd2diR1m1NF0uPy53NzDN Mly5NlI{OzZ{NE[=
OVCAR8 M4P6cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVuwMlAyNTFyMDFOwG0> MXy0PEBp NHH6dVNNd2diR1m1NF0uPy56NDDN MWmyNlM{PjJ2Nh?=
SKOV3 NYjTPW9IT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TmUFAvODFvMUCwJO69VQ>? NVXZb2xmPDhiaB?= NIfLc5FNd2diR1m1NF0uQC52MTDN MVqyNlM{PjJ2Nh?=
RXF631L MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfFNG8zOC5yMT2xNFAh|ryP M{HnNVQ5KGh? M{DhfGxw\yCJSUWwQU05NjJzIF2= NELVNI4zOjN|NkK0Oi=>
ACHN M{PQPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYGwMlAyNTFyMDFOwG0> MWG0PEBp NFmydopNd2diR1m1NF0uPy57NTDN M3nlSlIzOzN4MkS2
St-4 MoX4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnL1NE4xOS1zMECg{txO MoWxOFghcA>? NVK2[oI6VG:pIFfJOVA:NTdwNEegUS=> NG\Z[4wzOjN|NkK0Oi=>
MKN1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTJNE4xOS1zMECg{txO M3PVN|Q5KGh? NIPsUodNd2diR1m1NF0uQC52MTDN M2Hxc|IzOzN4MkS2
MKN7 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHC[|YxNjBzLUGwNEDPxE1? NHjyNJc1QCCq NFnjUoFNd2diR1m1NF0uPy54ODDN NH70UWozOjN|NkK0Oi=>
MKN28 MmXjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnqOYJsOC5yMT2xNFAh|ryP MV[0PEBp MnixUI9oKEeLNUC9MVcvODdiTR?= MkT4NlI{OzZ{NE[=
MKN45 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jFN|AvODFvMUCwJO69VQ>? M1vTcVQ5KGh? MYjMc4chT0l3ME2tPE4{PCCP NGXCfHQzOjN|NkK0Oi=>
MKN74 NG\vcG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVWwMlAyNTFyMDFOwG0> NEW2NYg1QCCq NVzN[IEzVG:pIFfJOVA:NTdwNEKgUS=> NHTiVoEzOjN|NkK0Oi=>
DU145 MoX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LLXlAvODFvMUCwJO69VQ>? MoTLOFghcA>? MVzMc4chT0l3ME2tPE4yPiCP MnXrNlI{OzZ{NE[=
PC3 NEniTYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfDcmFCOC5yMT2xNFAh|ryP NYLkU5dJPDhiaB?= NI\hcolNd2diR1m1NF0uQC54NjDN NFnLZpYzOjN|NkK0Oi=>
Trypanosoma brucei brucei Mo\RSpVv[3Srb36gRZN{[Xl? MliwNlAxKG6P MXyxNkBp NICyOXFFVVOR MUnE[YNz\WG|ZTDpckBxcG:|cHjveIllgWxiaX7vd4l1d2xicHjvd5Bp[XSnIHzleoVt NHT2c4czPDhyNUm0Oi=>
Trypanosoma brucei brucei NFLJUYZHfW6ldHnvckBCe3OjeR?= MofsNVghcA>? Mly0SG1UVw>? MmDxTY5pcWKrdHnvckBw\iC{ZXPldJRwei2vZXTpZZRm\CCnbnTvZ5l1d3OrczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiC2cnHud4ZmenKrbjD1dJRic2V? MX2yOFgxPTl2Nh?=
Trypanosoma brucei brucei MX7GeY5kfGmxbjDBd5NigQ>? MVmyNFAhdk1? M3j6TFEzKGh? NEe5Z|NFVVOR MU\F[oZm[3Rib36gd5BpcW6pb335cIVqdiCuZY\lcC=> MXOyOFgxPTl2Nh?=
Trypanosoma brucei brucei MXTGeY5kfGmxbjDBd5NigQ>? NIDVZpczODBibl2= MnT4NVIhcA>? M{W4S2ROW09? M3vyTmVn\mWldDDvckBxcG:|cHjheIllgWylaH;sbY5mKGyndnXs MUSyOFgxPTl2Nh?=
UM-UC-3 NWHhZ4hwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIP3dHFKSzVyPUOxOUBxVQ>? NVS2d2VpW0GQR1XS
SBC-1 NIWyfG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHocZpKSzVyPUe0NkBxVQ>? M1S5UXNCVkeHUh?=
MKN1 NYKyZ5VOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXGbmFKSzVyPUKuPEBvVQ>? MXTTRW5ITVJ?
NCI-H720 M4fWS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHaU2dlUUN3ME2zMlU4KG6P MYjTRW5ITVJ?
BFTC-909 MmrYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfWTWM2OD1|LkexJI5O M1HqTXNCVkeHUh?=
BPH-1 NWWyeYxoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrNTWM2OD12Lke2JI5O MlmyV2FPT0WU
PC-3 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoH3TWM2OD13LkC5JI5O NE\VeFhUSU6JRWK=
AN3-CA MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPYZ21wUUN3ME21MlU3KG6P NHLj[WxUSU6JRWK=
HN NEXzfW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnH1TWM2OD13Lkm2JI5O M4\VVnNCVkeHUh?=
HCC2218 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHIe2xoUUN3ME22MlYyKG6P MmPoV2FPT0WU
KP-4 M1qxN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLSTWM2OD15IH7N NVPxWHZ2W0GQR1XS
LU-139 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTdwN{egcm0> NWi3ZnIxW0GQR1XS
ETK-1 M1LubGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEC2VXBKSzVyPUeuPFghdk1? MmDXV2FPT0WU
Ramos-2G6-4C10 Mo[xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3jT|ZKSzVyPUiuOFkhdk1? M3ywPXNCVkeHUh?=
MHH-PREB-1 M1zLT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfZTWM2OD17LkGyJI5O MkLBV2FPT0WU
DU-4475 Mmq5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTzTWM2OD17LkS0JI5O M1nWfXNCVkeHUh?=
NCI-H1666 M3TGPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGq1O29KSzVyPUmuO|Ehdk1? M1XNeXNCVkeHUh?=
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A549 M{jHbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fSS2lEPTB;MUCuNVQhdk1? MVrTRW5ITVJ?
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L-363 M3nLSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\2OGlEPTB;MUCuOlkhdk1? NGrrSllUSU6JRWK=
ES8 MmS1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37mPGlEPTB;MUCuPUBvVQ>? MYfTRW5ITVJ?
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BB65-RCC MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrJTWM2OD1zMj63NkBvVQ>? MXjTRW5ITVJ?
NCI-H1793 Mkn1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jPdmlEPTB;MUKuPFIhdk1? NEDXeIZUSU6JRWK=
KARPAS-45 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGL6XItKSzVyPUGzMlUyKG6P NVvK[mNyW0GQR1XS
GCT MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4e5dWlEPTB;MUOuOlghdk1? NWjlbHRJW0GQR1XS
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LB2241-RCC MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEiycXhKSzVyPUG0MlAyKG6P MV3TRW5ITVJ?
ES5 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1T3cmlEPTB;MUSuO|Qhdk1? NFrxfFFUSU6JRWK=
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COR-L105 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zYWWlEPTB;MUWuNFQhdk1? NXTiS5JSW0GQR1XS
P12-ICHIKAWA MoK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fkfmlEPTB;MUWuNUBvVQ>? MlXUV2FPT0WU
CHL-1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PlWmlEPTB;MUWuOFUhdk1? NVTLUXIxW0GQR1XS
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HH MonTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTF3Lkegcm0> MXfTRW5ITVJ?
NUGC-3 M1mwdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTF4LkO0JI5O MVrTRW5ITVJ?
EGI-1 MnHjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTF4LkSzJI5O NHLS[4RUSU6JRWK=
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MOLT-16 NGLmS3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkG4TWM2OD1zNz6xOUBvVQ>? NYLabGRjW0GQR1XS
NCI-H209 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoewTWM2OD1zNz6yPUBvVQ>? MUTTRW5ITVJ?
697 M{TYPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUfuVogyUUN3ME2xO{41OyCwTR?= NV[wOI1VW0GQR1XS
D-56MG NHTrZmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3MTllKSzVyPUG3MlY6KG6P MUfTRW5ITVJ?
VA-ES-BJ M4XPRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnJTWM2OD1zNz64N{BvVQ>? NUCxdVgyW0GQR1XS
EW-16 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfscJhKSzVyPUG4MlA1KG6P NIX3WYFUSU6JRWK=
HGC-27 NULRfXR2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTF6LkC2JI5O NH\FU5RUSU6JRWK=
ES7 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoG1TWM2OD1zOD6wPUBvVQ>? Ml:wV2FPT0WU
HuH-7 NInofJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjaTWM2OD1zOD60JI5O M3XPfHNCVkeHUh?=
BCPAP NE\qUlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3lTWM2OD1zOD62OUBvVQ>? MXnTRW5ITVJ?
SW1710 M4nsO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mni5TWM2OD1zOD63NkBvVQ>? MXTTRW5ITVJ?
IST-MEL1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU\JR|UxRTF6Lke3JI5O Ml7mV2FPT0WU
SF295 Mnq1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTF6LkmzJI5O MmP4V2FPT0WU
RPMI-7951 M1i2dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTF7LkK4JI5O NEW0UZJUSU6JRWK=
SF126 NIe2XHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPQ[ldyUUN3ME2xPU41OSCwTR?= NIGxTnZUSU6JRWK=
GAMG MnnyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PZOWlEPTB;MUmuOFghdk1? NGTjcoNUSU6JRWK=
KNS-81-FD M1y4Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTF7LkW0JI5O M{ewbnNCVkeHUh?=
RT-112 NH7wR|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXyOpoyUUN3ME2xPU43PiCwTR?= M3vlW3NCVkeHUh?=
DEL NXyz[YNxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHVXFBKSzVyPUKwMlQ6KG6P MojXV2FPT0WU
CGTH-W-1 NHnMTHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3P0RWlEPTB;MkCuOlMhdk1? NV;oWHlsW0GQR1XS
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RXF393 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\TeXRwUUN3ME2yNU41PSCwTR?= M3m2PHNCVkeHUh?=
NCI-H2030 NWq5eGlwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTJzLkWyJI5O M3\GbXNCVkeHUh?=
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HT-1080 MlftS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIr1XHhKSzVyPUKxMlk{KG6P M2\WXXNCVkeHUh?=
NCI-SNU-1 NXTMRXp{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3XrZmlEPTB;MkGuPVUhdk1? MUHTRW5ITVJ?
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ME-180 M13n[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrlTWM2OD1{Mj60N{BvVQ>? MUPTRW5ITVJ?
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TGBC1TKB MnnnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLtSXI1UUN3ME2yN{4xPSCwTR?= M3Xmd3NCVkeHUh?=
SW780 MkD1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTDTWM2OD1{Mz6xN{BvVQ>? MXvTRW5ITVJ?
MG-63 NYLs[Y9CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTJ|LkS1JI5O M{X2XXNCVkeHUh?=
BV-173 M{TSemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\OU|djUUN3ME2yN{45PyCwTR?= NF7oeVlUSU6JRWK=
CAL-51 M{Gwdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX:ye5BEUUN3ME2yN{45QSCwTR?= NV\0N2VFW0GQR1XS
A375 NUK2V5o4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zvTmlEPTB;MkOuPVMhdk1? MnHOV2FPT0WU
MEL-HO NXrufG0yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\WeWlEPTB;MkSuNFQhdk1? MnzZV2FPT0WU
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CTB-1 M4K0dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rOVmlEPTB;MkSuOlchdk1? M{TGUHNCVkeHUh?=
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TI-73 MmjjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M36yTWlEPTB;MkWuNlghdk1? M1j6RnNCVkeHUh?=
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KYSE-150 MnuzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzLTZZKSzVyPUK1Mlg6KG6P MmrzV2FPT0WU
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SK-LU-1 M3:4Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3VR4xqUUN3ME2yOk4yPyCwTR?= MYLTRW5ITVJ?
HOP-92 NYC5[JoxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zXNmlEPTB;Mk[uOFghdk1? NYC3TVZCW0GQR1XS
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SW962 MnHDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnj1TWM2OD1{Nj63OkBvVQ>? MlvhV2FPT0WU
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NCI-H292 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofLTWM2OD1{NzDuUS=> NILDepFUSU6JRWK=
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SW1088 M37oSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHzXFlKSzVyPUK4MlI6KG6P NG[0XWlUSU6JRWK=
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GI-ME-N NGPE[YxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HSTGlEPTB;MkmuPVEhdk1? MWnTRW5ITVJ?
BHT-101 NYrwW4NqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;zb2lEPTB;M{CuNFUhdk1? M4HDPHNCVkeHUh?=
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QIMR-WIL NXPGWmJqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1K0fGlEPTB;M{CuOkBvVQ>? Mnu5V2FPT0WU
JVM-3 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;FTWM2OD1|MD64N{BvVQ>? NInSWGtUSU6JRWK=
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COLO-800 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\GTWM2OD1|Mj65NkBvVQ>? NVnq[GhWW0GQR1XS
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Ca9-22 M{H2O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DzNWlEPTB;M{OuOVUhdk1? M3\TUnNCVkeHUh?=
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RPMI-8226 NIj5TWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDHPWl3UUN3ME2zN{45OiCwTR?= M1LuR3NCVkeHUh?=
SK-NEP-1 M4roOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTN2LkG1JI5O NInITlFUSU6JRWK=
Becker NI\GVHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fCUmlEPTB;M{SuNlEhdk1? MnTQV2FPT0WU
NCI-H28 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTN2LkS0JI5O M2fEWnNCVkeHUh?=
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OVCAR-5 MlexS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HJUmlEPTB;M{WuOFchdk1? NV\0dmd1W0GQR1XS
LAMA-84 Ml32S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzLeGcxUUN3ME2zOU45PyCwTR?= MnTXV2FPT0WU
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Daoy MlTXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYP2OlFTUUN3ME2zOk44KG6P M4X4RXNCVkeHUh?=
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OAW-28 MnLUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTBTWM2OD1{LkC2PVE6KM7:TR?= NGqzemhUSU6JRWK=
C8166 M1jDdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUXDOZVKUUN3ME2yMlY{Ozl{IN88US=> M{Txd3NCVkeHUh?=
COLO-678 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnjZZBKSzVyPUKuPFM4PjhizszN MnPPV2FPT0WU
SK-N-DZ M3PRRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLo[VNGUUN3ME2yMlg3OzhzIN88US=> NY\qe|dbW0GQR1XS
NCI-H82 M1XNZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXMXGdKSzVyPUKuPVA{PjlizszN MnPFV2FPT0WU
JVM-2 MnTkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7jbmpEUUN3ME2zMlA{OTh6IN88US=> M1rib3NCVkeHUh?=
SW1116 MmrRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLKOZpKSzVyPUOuNFU1OTFizszN MUjTRW5ITVJ?
MDA-MB-453 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jnRmlEPTB;Mz6xNFQ{QSEQvF2= NH3Yc|dUSU6JRWK=
Calu-6 NXjPZZU6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnwTWM2OD1|LkG5PVch|ryP MVvTRW5ITVJ?
SHP-77 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvp[4lKSzVyPUOuOVI5KM7:TR?= M3nMUHNCVkeHUh?=
Capan-2 NIrJO|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTRwM{K1PFEh|ryP M4LENHNCVkeHUh?=
SW948 NGHkO4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfETWM2OD12Lke0O|c6KM7:TR?= NEPpN3hUSU6JRWK=
HDLM-2 MoTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTVwMEe3NlUh|ryP NWL2TFd6W0GQR1XS
LAN-6 M1fmOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrSNndPUUN3ME22MlIyPDl3IN88US=> M{nJTnNCVkeHUh?=
LU-135 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLoTWM2OD14LkSzNFc4KM7:TR?= M1nOVHNCVkeHUh?=
T84 NIPKfFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHGTWg2UUN3ME22Mlk5PjRizszN M1;Ee3NCVkeHUh?=
CAPAN-1 NIWwPXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jYeGlEPTB;Nz62NlI{OyEQvF2= M1voUHNCVkeHUh?=
SW1417 NIOwV3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTdwOUG3N|Eh|ryP M1TGRXNCVkeHUh?=
BALL-1 NIDwNWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk[5TWM2OD16LkWwOFA6KM7:TR?= MYLTRW5ITVJ?
HT-29 NYXu[Jl3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fUS2lEPTB;OT6wO|U6QSEQvF2= MmWxV2FPT0WU
C3A M2PqTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUK0elI6UUN3ME25Mlg5Ozl2IN88US=> MoXTV2FPT0WU
NCI-H1993 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTFyLkWwPFEh|ryP M3;VUHNCVkeHUh?=
SK-MEL-1 NWHaUIM1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDaTWM2OD1zMT62Nlg6KM7:TR?= MofGV2FPT0WU
DU-145 NFu2SIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4rPTmlEPTB;MUSuOVA2OiEQvF2= NX;ydFg2W0GQR1XS
KP-N-YN NX2xeYF6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\DVXBVUUN3ME2xOE42OTB|IN88US=> NWDOZ5Z6W0GQR1XS
CCRF-CEM MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULR[Vk5UUN3ME2xOE44QDB7IN88US=> M{nnSnNCVkeHUh?=
ZR-75-30 MlezS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPiSFh5UUN3ME2xOk4{OzB|IN88US=> MYnTRW5ITVJ?
A673 NHi3cnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3CTWM2OD1{MD61OVA4KM7:TR?= MlThV2FPT0WU
K-562 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTJ6LkSxPFMh|ryP MoWzV2FPT0WU

... Click to View More Cell Line Experimental Data

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:
NMP+polyethylene glycol 300 (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
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 (g) = Concentration (mol/L) × Volume (L) × 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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* 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

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Molecular Weight Calculator

Molecular Weight Calculator

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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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00620594 Completed Breast Cancer|Advanced Solid Tumors|Cowden Syndrome Novartis Pharmaceuticals|Novartis December 21, 2006 Phase 1
NCT01856101 Terminated Carcinoma Transitional Cell Cliniques universitaires Saint-Luc- Université Catholique de Louvain|Novartis February 2013 Phase 2
NCT01717898 Terminated Castrate-resistant Prostate Cancer Patients. Charles Ryan|Novartis Pharmaceuticals|University of California, San Francisco January 2013 Phase 1|Phase 2
NCT01658436 Completed Pancreatic Neuroendocrine Tumors (pNET) Novartis Pharmaceuticals|Novartis November 2012 Phase 2
NCT01628913 Terminated Pancreatic Neuroendocrine Tumors (pNET) Novartis Pharmaceuticals|Novartis October 2012 Phase 2
NCT01690871 Withdrawn Malignant PEComa (Perivascular Epithelioid Cell Tumors) Novartis Pharmaceuticals|Novartis September 2012 Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 1:

    With difficulties in dissolving BEZ235, How can I improve its solubility?

  • Answer:

    For in vivo study, we suggest the vehicle solution NMP/polyethylene glycol 300 (10/90, v/v). Please dissolve BEZ235 in NMP as more as possible. You can sonicate and warm it in water bath for a while. Then dilute with PEG 300.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID