Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) is a potent, selective, and orally available ALK inhibitor, exhibiting an IC50 of 1.9 nM and a KD value of 2.4 nM (in an ATP-competitive manner). Additionally, it inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib exhibits efficient penetration into the central nervous system (CNS)[2].
体内研究
Alectinib treatment (0.2-20 mg/kg; oral administration; once daily; for 11 days) in SCID or nude mice bearing NCI-H2228 cells leads to dose-dependent inhibition of tumor growth (EC50 of 0.46 mg/kg) and tumor regression. No differences in body weight or gross signs of toxicity are observed at any dose level[1].
体外研究
Alectinib treatment (0-1000 nM; 2 hours; NCI-H2228 cells) prevented autophosphorylation of ALK and led to significant suppression of phosphorylation of STAT3 and AKT[1].
Alectinib treatment (0-1000 nM; 5 days; HCC827, A549, or NCIH522 cells) reduces cell viability in a dose-dependent manner [1].
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