Obatoclax mesylate - CAS 803712-79-0
Catalog number: B0084-135253
Category: Inhibitor
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Bcl-2 Family
Obatoclax mesylate is the mesylate salt of obatoclax, a synthetic small-molecule inhibitor of the bcl-2 family of proteins with potential pro-apoptotic and antineoplastic activities. Obatoclax binds to members of the Bcl-2 protein family, preventing the binding of these anti-apoptotic proteins to the pro-apoptotic proteins Bax and Bak and so promoting the activation of the apoptotic pathway in Bcl-2-overexpressing cells. The Bcl-2 family of proteins (bcl-2, bcl-xl, bcl-w, and Mcl-1) are overexpressed in a wide variety of cancers, including those of the lymphatic system, breast, lung, prostate, and colon.
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B0084-135253 500 mg $650 In stock
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light brown to black Solid
(2E)-2-[(5Z)-5-[(3,5-dimethyl-1H-pyrrol-2-yl)methylidene]-4-methoxypyrrol-2-ylidene]indole methanesulfonic acid
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Gemin X.
1.Physiologically-Based Pharmacokinetic Modeling in Pediatric Oncology Drug Development.
Rioux N1, Waters NJ2. Drug Metab Dispos. 2016 Mar 2. pii: dmd.115.068031. [Epub ahead of print]
Childhood cancer represents more than 100 rare and ultra-rare diseases with an estimated 12,400 new cases diagnosed each year in the US, and as such this much smaller patient population has led to pediatric oncology drug development lagging behind that for adult cancers. Developing drugs for pediatric malignancies also brings with it a number of unique trial design considerations including flexible enrolment approaches, age appropriate formulation, acceptable sampling schedules, and balancing the need for age-stratified dosing regimens given the smaller patient populations. The regulatory landscape for pediatric pharmacotherapy has evolved with US FDA legislation such as the FDA Safety and Innovation Act, 2012. In parallel, the regulatory authorities have recommended the application of physiologically-based PK modeling (PBPK) for example, in the recently issued FDA Strategic Plan for Accelerating the Development of Therapies for Pediatric Rare Diseases.
2.Obatoclax as a perpetrator in drug-drug interactions and its efficacy in multidrug resistance cell lines.
Theile D1, Allendorf D1, Köhler BC2, Jassowicz A2, Weiss J1. J Pharm Pharmacol. 2015 Nov;67(11):1575-84. doi: 10.1111/jphp.12455. Epub 2015 Aug 10.
OBJECTIVES: Obatoclax is a pan-Bcl-2 inhibitor with promising efficacy, especially when combined with other antineoplastic agents. Pharmacokinetic drug-drug interactions can occur systemically and at the level of the tumour cell. Thus, this study scrutinised the interaction potential of obatoclax in vitro.
3.Mitochondrial protection impairs BET bromodomain inhibitor-mediated cell death and provides rationale for combination therapeutic strategies.
Lasorsa E1, Smonksey M1, Kirk JS1, Rosario S1,2, Hernandez-Ilizaliturri FJ3, Ellis L1,2. Cell Death Dis. 2015 Dec 10;6:e2014. doi: 10.1038/cddis.2015.352.
Inhibitors of the bromodomain and extraterminal domain family (BETI) have recently entered phase I clinical trials. In patients with advanced leukemia's, potent antileukemia activity was displayed with minimum dose-limiting toxicity. In preclinical models of hematological malignancies, including aggressive B-cell lymphomas, BETI induced cell-cycle arrest and apoptosis. However, the underlying cell death mechanisms are still not well understood. Dissecting the mechanisms required by BETI to mediate cell death would provide strong direction on how to best utilize BETI to treat patients with aggressive hematological malignancies. Herein, we provide understanding of the molecular mechanisms underlying BETI-mediated cell death using I-BET762. Induction of cell death occurred in primary murine and human B-cell lymphomas through apoptosis. Genetic dissection using Eμ-myc B-cell lymphoma compound mutants demonstrated that I-BET762-induced apoptosis does not require the p53 pathway.
4.Pan-Bcl-2 inhibitor Obatoclax is a potent late stage autophagy inhibitor in colorectal cancer cells independent of canonical autophagy signaling.
Koehler BC1, Jassowicz A2, Scherr AL3, Lorenz S4, Radhakrishnan P5, Kautz N6, Elssner C7, Weiss J8, Jaeger D9, Schneider M10, Schulze-Bergkamen H11,12. BMC Cancer. 2015 Nov 19;15:919. doi: 10.1186/s12885-015-1929-y.
BACKGROUND: Colorectal cancer is the third most common malignancy in humans and novel therapeutic approaches are urgently needed. Autophagy is an evolutionarily highly conserved cellular process by which cells collect unnecessary organelles or misfolded proteins and subsequently degrade them in vesicular structures in order to refuel cells with energy. Dysregulation of the complex autophagy signaling network has been shown to contribute to the onset and progression of cancer in various models. The Bcl-2 family of proteins comprises central regulators of apoptosis signaling and has been linked to processes involved in autophagy. The antiapoptotic members of the Bcl-2 family of proteins have been identified as promising anticancer drug targets and small molecules inhibiting those proteins are in clinical trials.
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CAS 803712-79-0 Obatoclax mesylate

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