Alectinib Hydrochloride 是一种有效的、选择性的、口服具有活力的、ATP 竞争性的ALK抑制剂,其IC50=1.9 nM,Kd=2.4 nM,并且还抑制ALK F1174L和ALK R1275Q,其IC50分别为 1 nM 和 3.5 nM。它还有中枢神经系统渗透能力。
产品描述
Alectinib hydrochloride is a selective, and orally available inhibitor of ALK( IC50 : 1.9 nM)
体内活性
Alectinib hydrochloride(CH5424802), a potent, selective, and orally available ALK inhibitor with a unique chemical scaffold, showing preferential antitumor activity against cancers with gene alterations of ALK, such as nonsmall cell lung cancer (NSCLC) cells expressing EML4-ALK fusion and anaplastic large-cell lymphoma (ALCL) cells expressing NPM-ALK fusion in vitro and in vivo
动物实验
Animal Model:SCID or nude mice bearing NCI-H2228 cells. Dosage:0.2 mg/kg, 0.6 mg/kg, 2 mg/kg, 6 mg/kg, 20 mg/kg. Administration:Oral administration; once daily; for 11 days
Cas No.
1256589-74-8
分子式
C30H35ClN4O2
分子量
519.08
别名
AF-802 (Hydrochloride);CH5424802 (Hydrochloride);RO5424802 (Hydrochloride);艾乐替尼盐酸盐
储存和溶解度
DMSO:6 mg/mL (11.56 mM),Need ultrasonic and warming
Powder: -20°C for 3 years
In solvent: -80°C for 2 years