生物活性分子抑制剂Alectinib Hydrochloride(Synonyms: 艾乐替尼盐酸盐; CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Alectinib Hydrochloride (Synonyms: 艾乐替尼盐酸盐; CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) 纯度: 99.89%

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。

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

Alectinib Hydrochloride Chemical Structure

CAS No. : 1256589-74-8

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生物活性

Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) 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[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].

IC50 & Target

IC50: 1.9 nM (ALK), 1 nM (ALKF1174L), 3.5 nM (ALKR1275Q)[1]
Kd: 2.4 nM (ALK)[1]
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[1].
Alectinib (0-1000 nM; 5 days; HCC827, A549, or NCIH522 cells) treatment reduces cell activity in a dose-dependent manner[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: NCI-H2228 cells
Concentration: 0 nM,10 nM,100 nM, 1000 nM
Incubation Time: 2 hours
Result: Inhibition of ALK phosphorylation and signal transduction.

Cell Viability Assay[1]

Cell Line: HCC827, A549, or NCIH522 cells
Concentration: 0-1000 nM
Incubation Time: 5 days
Result: Reduced cell activity in a dose-dependent manner.

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 (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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SCID or nude mice bearing NCI-H2228 cells[1]
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
Result: Resulted in dose-dependent tumor growth inhibition (EC50 of 0.46 mg/kg) and tumor regression.

Clinical Trial

分子量

519.08

Formula

C30H35ClN4O2
CAS 号

1256589-74-8
中文名称

艾乐替尼盐酸盐；盐酸阿雷替尼
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

DMSO : 5 mg/mL (9.63 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9265 mL 9.6324 mL 19.2649 mL
5 mM 0.3853 mL 1.9265 mL 3.8530 mL
10 mM — — —

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
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.

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