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Formula: C47H55ClF3N5O6S3 N
H
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Solubility: DMSO N
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Overexpression of the prosurvival Bcl-2 family members (Bcl-2,Bcl-xL,and Mcl-1) is commonly
associated with tumor maintenance, progression, and chemoresistance. Binding affinities were
determined with competitive fluorescence polarization assays and a time-resolved fluorescence
resonance energy transfer assay (Ki's of <1 nmol/L for Bcl-2, Bcl-xL, and Bcl-w). The oral
bioavailability of ABT-263 in preclinical animal models is 20% to 50%, depending on formulation.[1]
A wide range of SCLC cellular activity was observed with ABT-263 having a 50% growth
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inhibition (EC50) of 110 nmol/L against the most sensitive line (H146), whereas its activity in the
least sensitive line (H82) resulted in an EC50 at 22 μmol/L. In all cell lines where the EC50 was
<1 μmol/L, ABT-263 was more potent than its enantiomer by a factor of >20.[2]
[2] Alex R. Shoemaker et al. Clinical Cancer Research. 2008 June 1;14:3268-3277 3 days of delivery of any damage or
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