Aclacinomycin A (aclarubicin) is an anthracycline anticancer agent with demonstrated activity against both leukemias and solid tumors. Aclacinomycin A is the first described non-peptidic inhibitor showing discrete selectivity for the chymotrypsin-like activity of the 20 S proteasome. Aclacinomycin A significantly decreases hydrolysis of Z-E(OtBu)AL-pNA by MPC or by chymotrypsin with IC50 of 18 μM and 24 μM, respectively. Aclacinomycin A (1 μM), in combination with doxorubicin, increases cytotoxic activity of doxorubicin against K562 resistant cells. Aclacinomycin A (1 μM) partly blocks the doxorubicin efflux in resistant cell nuclei of K562 tumour cells, resulting in enhanced accumulation of doxorubicin.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 25 mg/mL|
Aclacinomycin A stabilizes topoisomerase I covalent complexes.
Nitiss JL, et al. Cancer Res. 1997 Oct 15;57(20):4564-9. PMID: 9377570.
The antitumor drug aclacinomycin A, which inhibits the degradation of ubiquitinated proteins, shows selectivity for the chymotrypsin-like activity of the bovine pituitary 20 S proteasome.
Figueiredo-Pereira ME, et al. J Biol Chem. 1996 Jul 12;271(28):16455-9. PMID: 8663210.
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