| 產(chǎn)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 |
| 靶點(diǎn)： |
IC50: 1.9 nM(ALK), 1 nM (ALKF1174L), 3.5 nM (ALKR1275Q) Kd: 2.4 nM (ALK);VEGFR;TyrosineKinases;ALK |
| 體內(nèi)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] |
| 參考文獻(xiàn)： |
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) |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
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： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
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危險(xiǎn)品化學(xué)品經(jīng)營許可證（不帶存儲(chǔ)）
營業(yè)執(zhí)照(三證合一)
北京