Alectinib Hydrochloride|1256589-74-8|(艾乐替尼盐酸盐; CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride)-陌孚医药/Medlife

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Alectinib Hydrochloride (Synonyms: 艾乐替尼盐酸盐; CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride)

目录号: PL03102 纯度: ≥99%

CAS No. :1256589-74-8

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中文名称	Alectinib Hydrochloride
中文别名	9-乙基-6,11-二氢-6,6-二甲基-8-[4-(4-吗啉基)-1-哌啶基]-11-氧代-5H-苯并[B]咔唑-3-甲腈盐酸盐;艾乐替尼盐酸盐;盐酸艾乐替尼;乙二醇单乙醚-D4;CH5424802 (Hydrochloride)
英文名称	Alectinib Hydrochloride
英文别名	9-Ethyl-6,6-dimethyl-8-(4-morpholinopiperidin-1-yl)-11-oxo-5a,6,11,11a-tetrahydro-5h-benzo[b]carbazole-3-carbonitrile hydrochloride;Alectinib hydrochloride;9-ethyl-6,6-dimethyl-8-(4-morpholin-4-ylpiperidin-1-yl)-11-oxo-5H-benzo[b]carbazole-3-carbonitrile,hydrochloride;9-ethyl-6,6-dimethyl-8-(4-morpholin-4-yl-piperidin-1-yl)-11-oxo-6,11-dihydro-5H-benzo[b]carbazole-3-carbonitrile monohydrochloride salt;9-ethyl-6,6-dimethyl-8-[4-(morpholin-4-yl)piperidin-1-yl]-11-oxo-6,11-dihydro-5H-benzo[b]carbazole-3-carbonitrile hydrochloride;AF-802 hydrochloride;Alectinib hydrochloride (JAN);CH-5424802 Hydrochloride;RG-7853 Hydrochloride;RO-5424802 Hydrochloride;UNII-P9YY73LO6J;CH5424802 (Hydrochloride);CH 5424802,Alectinib(HCl);alectinib HCl;P9YY73LO6J;Alectinib (Hydrochloride);CH5424802 Hydrochloride;Alecensa (TN);alectini
Cas No.	1256589-74-8
分子式	C₃₀H₃₅ClN₄O₂
分子量	519.08
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

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，K_d 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。

生物活性

Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) is a potent, selective, and orally available ALK inhibitor with an IC 50 of 1.9 nM and a K d value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC 50 s of 1 nM and 3.5 nM, respectively. Alectinib demonstrates effective central nervous system (CNS) penetration.

性状

Solid

IC50 & Target[1][2]

IC50: 1.9 nM (ALK), 1 nM (ALK), 3.5 nM (ALK)
Kd: 2.4 nM (ALK)

体外研究(In Vitro)

Alectinib (0-1000 nM; 2 hours; NCI-H2228 cells) treatment could prevent autophosphorylation of ALK in NCI-H2228 cells expressing EML4-ALK, and it also resulted in substantial suppression of phosphorylation of STAT3 and AKT.
Alectinib (0-1000 nM; 5 days; HCC827, A549, or NCIH522 cells) treatment reduces cell activity in a dose-dependent manner. has not independently confirmed the accuracy of these methods. They are for reference only.Western Blot Analy

体内研究(In Vivo)

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 (EC 50 of 0.46 mg/kg) and tumor regression. At any dose level, no differences in body weight or gross signs of toxicity are observed. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

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.

溶解度数据	In Vitro: DMSO : 4.55 mg/mL (8.77 mM; ultrasonic and heat to 60°C)H₂O : < 0.1 mg/mL (insoluble)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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