Antitumor activity against human HCT116 cells xenografted in athymic nude BALB/cAJcL mouse assessed as inhibition of tumor growth at 25 mg/kg, iv administered on days 1,3,5,8,10 and 12 measured on day 15
Inhibition of His-tagged KSP motor domain (1 to 369) (unknown origin) assessed as inhibition of microtubule-stimulated KSP ATPase activity preincuabted for 30 mins followed by ATP addition measured after 15 mins by Kinase-Glo assay
Binding affinity to KSP motor domain (unknown origin) assessed as change in melting temperature at 100 uM by differential scanning fluorimetry in presence of 1 mM ATP
Toxicity in athymic nude BALB/cAJcL mouse xenografted with HCT116 cells assessed as body weight loss at 25 mg/kg, iv administered on days 1,3,5,8,10 and 12 relative to vehicle-treated control