Antitumor activity against human NCI-H146 cells xenografted in SCID mouse assessed as tumor free incidence at 25 mg/kg, iv measured on day 58 post tumor implantation
Antitumor activity against human NCI-H146 cells xenografted in SCID mouse assessed as tumor regression at 25 mg/kg, iv administered 5 days per week for 2 weeks
Induction of apoptosis in human NCI-H146 cells xenografted in SCID mouse assessed as caspase 3 cleavage at 25 mg/kg, iv after 3 to 24 hrs by Western blot analysis
Induction of apoptosis in human NCI-H146 cells xenografted in SCID mouse assessed as PARP cleavage at 25 mg/kg, iv after 3 to 6 hrs by Western blot analysis
Antitumor activity against human NCI-H146 cells xenografted in SCID mouse assessed as tumor free incidence at 25 mg/kg, iv measured on day 47 post tumor implantation
Binding affinity to N-terminal 8xHis-tagged human Mcl-1 (171 to 327 amino acid) expressed in Escherichia coli BL21 (DE3) at 5 uM after 2 hrs by fluorescence polarization assay
Binding affinity to c-terminally truncated N-terminal 8xHis-tagged human Bcl-xL deletion mutant expressed in Escherichia coli BL21 (DE3) after 2 hrs by fluorescence polarization assay
Inhibition of c-terminally truncated N-terminal 8xHis-tagged human Bcl-xL deletion mutant expressed in Escherichia coli BL21 (DE3) after 2 hrs by fluorescence polarization assay
ASTRAZENECA: Octan-1-ol/water (pH7.4) distribution coefficent measured by a shake flask method described in J. Biomol. Screen. 2011, 16, 348-355. Experimental range -1.5 to 4.5