ABT-263 Chemische Eigenschaften,Einsatz,Produktion Methoden
Chemische Eigenschaften
Pale Yellow Solid
Verwenden
A novel inhibitor of antiapoptotic BCL-2 proteins; a new promising anticancer drug candidate.
Mechanism of action
ABT‐263 exerts its senolytic activity in senescent tumor cells by inhibiting BCL‐XL's interaction with BAX. ABT‐263 is a BH3 mimetic that inhibits anti‐apoptotic BCL‐2 family proteins by impeding their ability to bind pro‐apoptotic proteins, such as BAK and BAX. BCL‐2 and BCL‐XL are the primary targets of ABT‐263 in cancer cells.
Pharmakokinetik
The pharmacokinetic profile of ABT-263 is characterized by low plasma clearance values and low volumes of distribution in mice, rats, dogs, and monkeys, with plasma elimination half-lives after i.v. Dose of 4.6 to 8.4 hours. Bioavailability after oral gavage was ～20% in all four species. Due to its low aqueous solubility, ABT-263 displays a prolonged dissolution rate-limited oral absorption. P.o. administration in lipid-based formulations, in which the compound is significantly more soluble, yields enhanced absorption with bioavailability near 50% and an oral elimination half-life of 8.9 hours in dogs[5].
ABT-263 Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
