s1001 abt-263

Product Information

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 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]

Biological Activity

[1] Christin Tse et al. Cancer Res. 2008 May 1;68:3421-3428

[2] Alex R. Shoemaker et al. Clinical Cancer Research. 2008 June 1;14:3268-3277

References

Novel Kinase Inhibitors for cell signaling & oncology research

S1001 ABT-263

Technical Data:M.Wt:Formula:Solubility:Purity:Storage:CAS No.:

974.61C47H55ClF3N5O6S3

DMSO99%at -20℃ 2 years923564-51-6

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℃

Synonyms: Navitoclax

» Bcl-2

Cl

NN

NH

OS

O O

NH

SPh

NOS

F3C OO

s1001 abt-263

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