Alectinib (AF802, CH5424802, RO5424802, RG-7853)是一种选择性抑制ALK酪氨酸激酶的口服药物，IC50为1.9 nM。 应用： Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) 是一种有效，选择性和口服的 ALK 抑制剂，其 IC50 为 1.9 nM，Kd 值为 2.4 nM (以 ATP 竞争方式)，并且还抑制 ALK F1174L 和 ALK R1275Q，其 IC50 分别为 1 nM 和 3.5 nM。Alectinib Hydrochloride 还具有有效的中枢神经系统 (CNS) 渗透能力。 Information Alectinib (CH5424802) hydrochloride Alectinib (AF802, CH5424802, RO5424802, RG-7853) is a second generation oral drug that selectively inhibits the activity of anaplastic lymphoma kinase (ALK) tyrosine kinase. Targets ALK (Cell-free) 1.9 nM In vitro Alectinib inhibits ALK with an IC50 value of 1.9 nmol/L and shows higher selectivity for ALK than for a number of other serine/tyrosine kinases. It also inhibits the ALK gatekeeper mutation L1196M with an IC50 of 1.56 nmol/L. Alectinib is effective with crizotinib-resistant ALK mutations L1196M, F1174L, R1275Q and C1156Y. In the KARPAS-299 (lymphoma), NB-1 (neuroblastoma) and NCI-H2228 (lung cancer) ALK-positive cell lines, alectinib inhibits cell proliferation with IC50 values of 3, 4.5 and 53 nmol/L, respectively. In vivo Alectinib dose-dependently inhibits EML4-ALK positive NCI-H2228 xenograft model at doses ranging from 2 to 20 mg/kg p.o., q.d. Significant efficacy is also achieved in the EML4-ALK L1196M-driven tumors. It has antitumor activity against cancers with ALK gene alterations. Cell Research(from reference) Cell lines：KB cells Concentrations：0.01-100 μM Incubation Time：72 h