Alectinib(Synonyms: 艾乐替尼; CH5424802; RO5424802; AF802)

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Alectinib (Synonyms: 艾乐替尼; CH5424802; RO5424802; AF802) 纯度: 99.87%

Alectinib (CH5424802) 是一种有效、选择性、具有口服活性的 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 还具有有效的中枢神经系统 (CNS) 渗透能力。

Alectinib(Synonyms: 艾乐替尼; CH5424802; RO5424802; AF802)

Alectinib Chemical Structure

CAS No. : 1256580-46-7

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10 mM * 1 mL in DMSO ￥902 In-stock
2 mg ￥520 In-stock
5 mg ￥850 In-stock
10 mg ￥1400 In-stock
50 mg ￥4000 In-stock
100 mg ￥6500 In-stock
200 mg ￥12000 In-stock
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生物活性

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[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

482.62

Formula

C30H34N4O2
CAS 号

1256580-46-7
中文名称

艾乐替尼；阿雷替尼
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

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

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0720 mL 10.3601 mL 20.7202 mL
5 mM 0.4144 mL 2.0720 mL 4.1440 mL
10 mM 0.2072 mL 1.0360 mL 2.0720 mL

*

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。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 0.5% CMC-Na/saline water

    Solubility: 20 mg/mL (41.44 mM); Suspended solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 0.38 mg/mL (0.79 mM); Clear solution

    此方案可获得 ≥ 0.38 mg/mL (0.79 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 3.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 0.38 mg/mL (0.79 mM); Clear solution

    此方案可获得 ≥ 0.38 mg/mL (0.79 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 3.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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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