货号	规格	价格	上海	北京	珠海	南京	武汉
S80233-5mg	99.90%	￥232.00 S80233-5mg ￥232.00 现货	8 8	-	-	-	-
S80233-10mg	99.90%	￥400.00 S80233-10mg ￥400.00 现货	7 7	-	-	-	-
S80233-50mg	99.90%	￥960.00 S80233-50mg ￥960.00 现货	9 9	-	-	-	-
S80233-250mg	99.90%	￥3040.00 S80233-250mg ￥3040.00 现货	3 3	-	-	-	-

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产品描述：

Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively. Alectinib demonstrates effective central nervous system (CNS) penetration

靶点：

IC50: 1.9 nM(ALK), 1 nM (ALKF1174L), 3.5 nM (ALKR1275Q) Kd: 2.4 nM (ALK);VEGFR;TyrosineKinases;ALK

体内研究：

Alectinib (0.2-20 mg/kg; oral administration; once daily; for 11 days; SCID or nude mice bearing NCI-H2228 cells) treatment can result in dose-dependent tumor growth inhibition (EC50 of 0.46 mg/kg) and tumor regression. At any dose level, no differences in body weight or gross signs of toxicity are observed[1]

参考文献：

1. Sakamoto H, et al. CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant. Cancer Cell. 2011, 19(5), 679-690. 2. Gadgeel S, et al. Alectinib versus crizotinib in treatment-naive anaplastic lymphoma kinase-positive (ALK+) non-small-cell lung cancer: CNS efficacy results from the ALEX study. Ann Oncol. 2018 Nov 1;29(11):2214-2222.

溶解性：

DMSO : 6.2 mg/mL (12.85 mM; Need warming)

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.072 ml	10.36 ml	20.72 ml
5 mM	0.414 ml	2.072 ml	4.144 ml
10 mM	0.207 ml	1.036 ml	2.072 ml
50 mM	0.041 ml	0.207 ml	0.414 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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