Navitoclax(ABT-263) Chemical Structure
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A potent, orally bioavailable Bad-like BH3 mimetic (Ki's of <1nmol/l for Bcl-2, Bcl-xL, and Bcl-w).
An orally bioavailable, synthetic small-molecule antagonist of a subset of the B-cell leukemia 2 (Bcl-2) family of proteins with potential antineoplastic activity. BcI-2 family protein inhibitor ABT-263 selectively binds to apoptosis suppressor proteins Bcl-2, Bcl-XL, and Bcl-w and prevents their binding to the apoptotic effectors Bax and Bak proteins, which may trigger apoptosis in tumor cells overexpressing Bcl-2, Bcl-XL, and Bcl-w. Bcl-2, Bcl-XL, and Bcl-w are frequently overexpressed in a wide variety of cancers, including those of the lymphatic system, breast, lung, prostate, and colon, and have been linked to tumor drug resistance.
Chemical Name: 4-[4-[[2-(4-chlorophenyl)-5,5-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-N-[4-[[(2R)-4-morpholin-4-yl-1-phenylsulfanylbutan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonylbenzamide
Optical purity: 100% by chiral HPLC
Chemical Purity: >99% by HPLC
Solubility : Chloroform, DMSO, Methanol
Storage Conditions :Room temperature, or -20ºC for 2 year.
ABT-263 tablets (100mg) orally administered to both intact and TDC dogs exhibited low clearance (0.673 ml/min per kilogram) and low volume of distribution (0.5-0.7 l/kg) with a half-life of 22.2 hours and the bioavailablity of 56.5%, where 13.5% of the total ABT-263 dose in TDC dogs was transported in lymph with the bioavailability of 21.7%. However, in fasted TDC dogs, a 1.8-fold decrease in lymph transport of ABT-263 was observed.
Identification of expression signatures predictive of sensitivity to the Bcl-2 family member inhibitor ABT-263 in small cell lung carcinoma and leukemia/lymphoma cell
SK Tahir, J Wass, MK Joseph, V Devanarayan - Molecular cancer..., 2010 - AACR
Bcl-2 inhibitors: small molecules with a big impact on cancer therapy
M Vogler, D Dinsdale, MJS Dyer... - Cell Death & ..., 2008 - nature.com
Bcl-2 inhibitors: targeting mitochondrial apoptotic pathways in cancer therapy
MH Kang - Clinical Cancer Research, 2009 - AACR
ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor
C Tse, AR Shoemaker, J Adickes, MG Anderson - Cancer research, 2008 - AACR
Phase II study of single-agent navitoclax (ABT-263) and biomarker correlates in patients with relapsed small cell lung cancer
CM Rudin, CL Hann, EB Garon, MR De Oliveira... - Clinical Cancer ..., 2012 - AACR
Purpose: Bcl-2 is a critical regulator of apoptosis that is overexpressed in the majority of
small cell lung cancers (SCLC). Nativoclax (ABT-263) is a potent and selective inhibitor of
Bcl-2 and Bcl-x L. The primary objectives of this phase IIa study included safety at the
Purchase(buy) Bcl-2 inhibitor Navitoclax(ABT-263),Potent Bcl-2 family inhibitor, inhibits Bcl-2, Bcl-xL, and Bcl-w, at Active Biochem and the United State(U.S.), Germany, Japan, France,United Kingdom(UK),Switzerland, Australia distributors.
ABT-263 is an orally sellecitive inhibitor of B-cell leukemia 2 (Bcl-2) family of proteins with potential antineoplastic activity. ABT-263 is a small molecular with the formula of C47H55ClF3N5O6S3 and Molecular Weight of 974. As a Bad-like Bh3 minetic, ABT-263 binds to Bcl-2 family proteins Bcl-2, Bcl-xl and Bcl-w, disrupts the interaction between Bcl-2/Bcl-xl /Bcl-w and pro-apoptotic proteins such as Bim, Bad and Bak, which trigger the caspases-initiated cell death pathway to induce apoptosis.