1. PI3K/Akt/mTOR
    Autophagy
  2. mTOR
    PI3K
    Autophagy

BEZ235 Tosylate (Synonyms: NVP-BEZ 235 Tosylate)

Cat. No.: HY-15174 Purity: 99.93%
Data Sheet SDS Handling Instructions

NVP-BEZ235 is a dual PI3K and mTOR kinase inhibitor with IC50 values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively.

For research use only. We do not sell to patients.
BEZ235 Tosylate Chemical Structure

BEZ235 Tosylate Chemical Structure

CAS No. : 1028385-32-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $66 In-stock
50 mg $60 In-stock
100 mg $90 In-stock
200 mg $150 In-stock
500 mg $300 In-stock
1 g   Get quote  
5 g   Get quote  

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Other Forms of BEZ235 Tosylate:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

NVP-BEZ235 is a dual PI3K and mTOR kinase inhibitor with IC50 values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively.

IC50 & Target

IC50: 4nM (PI3Kα), 75 nM (PI3Kβ), 7 nM (PI3Kγ), 5 nM (PI3Kδ)[1]

In Vitro

NVP-BEZ235 is an imidazo[4,5-c]quinoline derivative that inhibits PI3K and mTOR kinase activity by binding to the ATP-binding cleft of these enzymes. The IC50s for PI3Kα, β, γ, δ are 4, 75, 7, 5 nM, respectively. It is also found to be as active against the mutant PI3KαE545K or PI3KαH1047R with IC50s of 5.7 and 4.6 nM, respectively. In human tumor cell lines, it is able to effectively and specifically block the dysfunctional activation of the PI3K pathway, inducing G1 arrest. PTEN-null cell lines PC3M and U87MG shows a dose-dependent reduction in cell proliferation when treated with increasing concentrations of NVP-BEZ235, with an average GI50 of 10 to 12 nM[1].

In Vivo

NVP-BEZ235 is well tolerated, displays disease stasis when administered orally, and enhances the efficacy of other anticancer agents. At a dose of 50 mg/kg, NVP-BEZ235 appears rapidly in plasma with a Cmax of 1.68 μM at 0.5 h and a C24h of 0.03 μM[1].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT01856101 Cliniques universitaires Saint-Luc- Université Catholique de Louvain|Novartis Carcinoma Transitional Cell February 2013 Phase 2
NCT01343498 SCRI Development Innovations, LLC|Novartis Malignant Solid Tumour April 2011 Phase 1
NCT01453595 Memorial Sloan Kettering Cancer Center|Novartis Renal Cancer October 2011 Phase 1|Phase 2
NCT01290406 Novartis Pharmaceuticals|Novartis Endometrial Cancer March 2012 Phase 2
NCT01482156 Novartis Pharmaceuticals|Novartis Advanced Solid Tumors|Metastatic Breast Cancer|Metastatic Renal Cell Carcinoma January 2012 Phase 1
NCT01658436 Novartis Pharmaceuticals|Novartis Pancreatic Neuroendocrine Tumors (pNET) November 2012 Phase 2
NCT01690871 Novartis Pharmaceuticals|Novartis Malignant PEComa (Perivascular Epithelioid Cell Tumors) September 2012 Phase 2
NCT00620594 Novartis Pharmaceuticals|Novartis Breast Cancer|Advanced Solid Tumors|Cowden Syndrome December 21, 2006 Phase 1
NCT01495247 Novartis Pharmaceuticals|Novartis Inoperable Locally Advanced Breast Cancer|Metastatic Breast Cancer (MBC) January 2012 Phase 1|Phase 2
NCT01756118 Johann Wolfgang Goethe University Hospital Acute Lymphoblastic Leukemia|Leukemia, Myelocytic, Acute|Chronic Myelogenous Leukemia With Crisis of Blast Cells June 2012 Phase 1
NCT01717898 Charles Ryan|Novartis Pharmaceuticals|University of California, San Francisco Castrate-resistant Prostate Cancer Patients. January 2013 Phase 1|Phase 2
NCT01628913 Novartis Pharmaceuticals|Novartis Pancreatic Neuroendocrine Tumors (pNET) October 2012 Phase 2
NCT01195376 Novartis Pharmaceuticals|Novartis Advanced Solid Tumor October 2010 Phase 1
NCT01288092 Novartis Pharmaceuticals|Novartis Metastatic Breast Cancer March 2012 Phase 2
NCT01337765 Array BioPharma Unspecified Adult Solid Tumor, Protocol Specific|Solid Tumor July 2011 Phase 1
NCT01634061 Novartis Pharmaceuticals|Novartis Castration-resistant Prostate Cancer September 2012 Phase 1
NCT01471847 Novartis Pharmaceuticals|Novartis Locally Advance Breast Cancer (LABC)|Metastatic Breast Cancer (MBC) February 2012 Phase 1
NCT01508104 University of Cincinnati|Novartis Cancer January 2012 Phase 1|Phase 2
NCT01248494 Vanderbilt-Ingram Cancer Center Metastatic Breast Cancer November 2010 Phase 1
NCT01285466 Novartis Pharmaceuticals|Novartis Metastatic or Locally Advanced Solid Tumors January 2011 Phase 1
NCT01856101 Cliniques universitaires Saint-Luc- Université Catholique de Louvain|Novartis Carcinoma Transitional Cell February 2013 Phase 2
NCT01343498 SCRI Development Innovations, LLC|Novartis Malignant Solid Tumour April 2011 Phase 1
NCT01453595 Memorial Sloan Kettering Cancer Center|Novartis Renal Cancer October 2011 Phase 1|Phase 2
NCT01290406 Novartis Pharmaceuticals|Novartis Endometrial Cancer March 2012 Phase 2
NCT01482156 Novartis Pharmaceuticals|Novartis Advanced Solid Tumors|Metastatic Breast Cancer|Metastatic Renal Cell Carcinoma January 2012 Phase 1
NCT01658436 Novartis Pharmaceuticals|Novartis Pancreatic Neuroendocrine Tumors (pNET) November 2012 Phase 2
NCT01690871 Novartis Pharmaceuticals|Novartis Malignant PEComa (Perivascular Epithelioid Cell Tumors) September 2012 Phase 2
NCT00620594 Novartis Pharmaceuticals|Novartis Breast Cancer|Advanced Solid Tumors|Cowden Syndrome December 21, 2006 Phase 1
NCT01495247 Novartis Pharmaceuticals|Novartis Inoperable Locally Advanced Breast Cancer|Metastatic Breast Cancer (MBC) January 2012 Phase 1|Phase 2
NCT01756118 Johann Wolfgang Goethe University Hospital Acute Lymphoblastic Leukemia|Leukemia, Myelocytic, Acute|Chronic Myelogenous Leukemia With Crisis of Blast Cells June 2012 Phase 1
NCT01717898 Charles Ryan|Novartis Pharmaceuticals|University of California, San Francisco Castrate-resistant Prostate Cancer Patients. January 2013 Phase 1|Phase 2
NCT01628913 Novartis Pharmaceuticals|Novartis Pancreatic Neuroendocrine Tumors (pNET) October 2012 Phase 2
NCT01195376 Novartis Pharmaceuticals|Novartis Advanced Solid Tumor October 2010 Phase 1
NCT01288092 Novartis Pharmaceuticals|Novartis Metastatic Breast Cancer March 2012 Phase 2
NCT01337765 Array BioPharma Unspecified Adult Solid Tumor, Protocol Specific|Solid Tumor July 2011 Phase 1
NCT01634061 Novartis Pharmaceuticals|Novartis Castration-resistant Prostate Cancer September 2012 Phase 1
NCT01471847 Novartis Pharmaceuticals|Novartis Locally Advance Breast Cancer (LABC)|Metastatic Breast Cancer (MBC) February 2012 Phase 1
NCT01508104 University of Cincinnati|Novartis Cancer January 2012 Phase 1|Phase 2
NCT01248494 Vanderbilt-Ingram Cancer Center Metastatic Breast Cancer November 2010 Phase 1
NCT01285466 Novartis Pharmaceuticals|Novartis Metastatic or Locally Advanced Solid Tumors January 2011 Phase 1
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 1.5583 mL 7.7913 mL 15.5826 mL
5 mM 0.3117 mL 1.5583 mL 3.1165 mL
10 mM 0.1558 mL 0.7791 mL 1.5583 mL
Kinase Assay
[1]

NVP-BEZ235 is dissolved in DMSO to a stock concentration of 10 mM and diluted with cell media. The kinase reaction is done in 384-well black plate. Each well is loaded with 50 nL of test items (in 90% DMSO) and 5 μL reaction buffer containing 10 μg/mL PI substrate and the PI3K proteins (10, 25, 10, and 150 nM of p110α, p110β, p110γ, and p110δ, respectively) are then added. The reaction is started by the addition of 5 μL of 1 μM ATP prepared in the reaction buffer and ran for either 60 or 120 min and subsequently terminated by the addition of 10 μL Kinase-Glo buffer. The plates are then read in a Synergy 2 reader for luminescence detection[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mouse: The NVP-BEZ235 powder is dissolved in NMP on sonication, and the remaining volume of polyethylene glycol 300 is added to a concentration of 5 mg/mL. The application volume is 10 mL/kg. For analytics, frozen tissues are minced and then homogenized in an equal volume of ice-cold PBS and centrifugation, supernatants are analyzed. Samples are then eluted with a linear gradient of 10% to 90% (v/v) acetonitrile in water containing 0.05% (v/v) trifluoroacetic acid over a period of 20 min at a flow rate of 1 mL/min. The compounds are detected by UV absorbance at 340 nm, and concentrations are determined by the external standard method using peak heights[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

641.74

Formula

C₃₇H₃₁N₅O₄S

CAS No.

1028385-32-1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
BEZ235 Tosylate
Cat. No.:
HY-15174
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