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product name ABT-263 (Navitoclax)


Description: ABT-263 (Navitoclax) is an highly potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with Ki of ~ 0.5 nM, ~1 nM and ~1 nM in cell-free assays, Phase 2 study. 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.

References:  Cancer Res. 2008, 68(9), 3421-428.; Clin Cancer Res, 2008, 14(11), 3268-77.



Molecular Weight (MW)

974.61
Formula

C47H55ClF3N5O6S3
CAS No.

923564-51-6
Storage

-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)

DMSO: 100 mg/mL (102.6 mM)
Water: <1 mg/mL (slightly soluble or insoluble)
Ethanol: <1 mg/mL
Solubility (In vivo)

55% DMSO+Corn oil: 8mg/mL

other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19399889

General When ABT-263 is administered at 100 mg/kg/day in the H345 xenograft model, significant antitumor efficacy is observed with 80% TGI and 20% of treated tumors indicating at least a 50% reduction in tumor volume.
Animal model C.B -17 scid-bg or C.B -17 scid mice
Formulation Formulated in 10% ethanol, 30% polyethylene glycol 400, and 60% Phosal 50 PG
Dosages 100 mg/kg/day
Administration Oral gavage
Reference Cancer Res. 2008, 68(9), 3421-428.; Clin Cancer Res, 2008, 14(11), 3268-77.

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