Alectinib (Synonyms:艾乐替尼; CH5424802; RO5424802; AF802)
目录号 : KM10830 CAS No. : 1256580-46-7 纯度 : 98%

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。

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5mg
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50mg
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100mg
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200mg
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500mg 询价 In-stock
1g 询价 In-stock

Other Forms of Rapamycin:

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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. Alectinib demonstrates effective central nervous system (CNS) penetration.

体外研究

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.

Western Blot Analysis

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

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

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.

Animal Model: SCID or nude mice bearing NCI-H2228 cells
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.
分子式
C30H34N4O2
分子量
482.62
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。

  • 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。

临床试验
科研文献
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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