Acetate gossypol

Acetate gossypol Structure
Acetate gossypol structure
Common Name Acetate gossypol
CAS Number 12542-36-8 Molecular Weight 578.606
Density N/A Boiling Point 707.9ºC at 760 mmHg
Molecular Formula C32H34O10 Melting Point 164-168ºC
MSDS Chinese USA Flash Point 395.9ºC
Symbol GHS07 GHS08
GHS07, GHS08
Signal Word Warning

The investigational agent MLN2238 induces apoptosis and is cytotoxic to CLL cells in vitro, as a single agent and in combination with other drugs.

Br. J. Haematol. 165(1) , 78-88, (2014)

Chronic lymphocytic leukaemia (CLL) is the most common haematological malignancy in the U.S. The course of the disease has been shown to be negatively impacted by increased levels of BCL2. Strategies to downregulate BCL2 and shift the balance towards cellular...

Pan-Bcl-2 inhibitor AT-101 enhances tumor cell killing by EGFR targeted T cells.

PLoS ONE 7(11) , e47520, (2012)

Pancreatic cancer is a deadly disease and has the worst prognosis among almost all cancers and is in dire need of new and improved therapeutic strategies. Conditioning of tumor cells with chemotherapeutic drug has been shown to enhance the anti-tumor effects ...

Bcl-2 family of proteins as therapeutic targets in genitourinary neoplasms.

Clin. Genitourin. Cancer 11(1) , 10-9, (2013)

Overexpression of antiapoptotic B-cell lymphoma (Bcl-2) proteins confers the dysregulation of apoptosis and results in drug resistance in a variety of cancers, including those of the genitourinary tract. Inhibitors that target prosurvival Bcl-2 proteins are i...

Combination therapy with gossypol reveals synergism against gemcitabine resistance in cancer cells with high BCL-2 expression.

PLoS ONE 7(12) , e50786, (2012)

Although gemcitabine is highly active in several cancer types, intrinsic and acquired drug resistance remains a major challenge. Overexpression of Bcl-2 has been associated with gemcitabine resistance. The aim of this study is to determine whether gossypol ca...

Radiographic progression by Prostate Cancer Working Group (PCWG)-2 criteria as an intermediate endpoint for drug development in metastatic castration-resistant prostate cancer.

BJU Int. 114(6b) , E25-31, (2014)

To investigate the association of radiographic progression defined by Prostate Cancer Working Group (PCWG)-2 guidelines and overall survival (OS) in men with metastatic castration-resistant prostate cancer (mCRPC).Two trials that used PCWG-2 guidelines to def...

Neutropenia as a potential pharmacodynamic marker for docetaxel-based chemotherapy in men with metastatic castration-resistant prostate cancer.

Clin. Genitourin. Cancer 10(4) , 239-45, (2012)

Docetaxel clearance appears increased in men who are castrated. Neutropenia in cycle 1 may be a pharmacodynamic marker for docetaxel, which may enable tailored dosing in metastatic castration-resistant prostate cancer (mCRPC).The association of cycle 1 neutro...

Proapoptotic protein Smac mediates apoptosis in cisplatin-resistant ovarian cancer cells when treated with the anti-tumor agent AT101.

J. Biol. Chem. 287 , 68-80, (2012)

Chemoresistance of ovarian cancer has been previously attributed to the expression and activation of Bcl-2 family proteins. BH3-mimetic molecules possessing potential anticancer activity are able to inhibit antiapoptotic Bcl-2 family proteins. AT101 (R-(-)-go...

AT-101, a pan-Bcl-2 inhibitor, leads to radiosensitization of non-small cell lung cancer.

J. Thorac. Oncol. 5(5) , 680-7, (2010)

Radiotherapy has a central role in the treatment of lung cancer. However, its effectiveness is often limited, in part, because of the defects in key apoptosis regulators, such as Bcl-2 family members, that contribute to cancer ability to evade apoptosis. In t...

Mechanisms of drug sensitization to TRA-8, an agonistic death receptor 5 antibody, involve modulation of the intrinsic apoptotic pathway in human breast cancer cells.

Mol. Cancer Res. 9(4) , 403-17, (2011)

TRA-8, a monoclonal antibody to death receptor 5 induces apoptosis in various cancer cells; however, the degree of sensitivity varies from highly sensitive to resistant. We have previously shown that resistance to TRA-8 can be reversed by using chemotherapeut...

Metronomic dosing of BH3 mimetic small molecule yields robust antiangiogenic and antitumor effects.

Cancer Res. 72 , 716-725, (2012)

Bcl-2 is an antiapoptotic protein that has also been found to function as a proangiogenic signaling molecule. Improvements in antiangiogenic therapy can be engendered by metronomic dosing. Thus, we hypothesized that BH3-mimetic drugs that antagonize Bcl-2 fam...