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。
| 生物活性 | Alectinib (CH5424802) is a potent, selective, and orally availableALKinhibitor with anIC50of 1.9 nM and aKdvalue of 2.4 nM (in an ATP-competitive manner), and also inhibitsALK F1174LandALK R1275QwithIC50s 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].
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. |
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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 (EC50of 0.46 mg/kg) and tumor regression. At any dose level, no differences in body weight or gross signs of toxicity are observed[1].
| 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 (EC50of 0.46 mg/kg) and tumor regression. |
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| 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 |
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| 溶解性数据 | In Vitro: DMSO : 6.2 mg/mL(12.85 mM;Need warming) 配制储备液 | 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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。 *以上所有助溶剂都可在本网站选购。
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