CH5424802|1256580-46-7|(艾乐替尼; CH5424802; RO5424802; RG7853)-陌孚医药/Medlife

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CH5424802 (Synonyms: 艾乐替尼; CH5424802; RO5424802; RG7853)

目录号: PC16076 纯度: ≥98%

CAS No. :1256580-46-7

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中文名称

CH5424802

中文别名

9-乙基-6,6-二甲基-8-(4-吗啉哌啶-1-基)-11-氧代-6,11-二氢-5H-苯并[b]咔唑-3-甲腈;艾乐替尼;1-羟基-2-(咪唑-1-基)-亚乙基-1,1-二磷酸一水化物;2-碘-3-甲氧基苯酚;Alectinib (CH5424802) 抑制剂;3-异丙基-(1H)-苯骈-2,1,3-噻二嗪-4-酮-2,2-二氧化物;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;艾乐替尼（alectinib,CH5424802）;灭草松

英文名称

CH5424802

英文别名

CH 5424802;9-ethyl-6,6-dimethyl-8-(4-morpholin-4-ylpiperidin-1-yl)-11-oxo-5H-benzo[b]carbazole-3-carbonitrile;9-ethyl-6,6-dimethyl-8-(4-morpholinopiperidin-1-yl)-11-oxo-6,11-dihydro-5H-benzo[b]carbazole-3-carbonitrile;Alectinib;Alectinib (CH5424802);9-ethyl-6,11-dihydro-6,6-dimethyl-8-(4-(4-morpholinyl)-1-piperidinyl)-11-oxo-5h-benzo(b)carbazole-3-carbonitrile;9-ethyl-6,6-dimethyl-8-(4-morpholin-4-ylpiperidin-1-yl)-11-oxo-6,11-dihydro-5H-benzo[b]carbazole-3-carbonitrile;AF802;AF-802;CH-5424802;UNII-LIJ4CT1Z3Y;9-Ethyl-6,11-dihydro-6,6-dimethyl-8-[4-(4-morpholinyl)-1-piperidinyl]-11-oxo-5H-benzo[b]carbazole-3-carbonitrile;CH 5424802,Alectinib;CH5424802;Alecensa;RO5424802;Alectinib free base;AF 802;LIJ4CT1Z3Y

Cas No.

1256580-46-7

分子式

C₃₀H₃₄N₄O₂

分子量

482.62

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC₅₀ 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 IC₅₀s 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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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(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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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. [Information]

[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. [Information]

溶解度数据

体外研究:

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

配制储备溶液

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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： 0.5% CMC-Na/saline water
Solubility: 20 mg/mL (41.44 mM); Suspended solution; Need ultrasonic
2.

建议依照次序添加每种溶剂： 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 ddH?O 中，得到澄清透明的生理盐水溶液
3.

建议依照次序添加每种溶剂： 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。

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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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