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

目录号: HY-13011 纯度: 99.51%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

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，K_d 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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Alectinib Chemical Structure

CAS No. : 1256580-46-7

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Customer Review

Other Forms of Alectinib:

MCE 顾客使用本产品发表的 32 篇科研文献

: Alectinib purchased from MCE. Usage Cited in: Cell Death Discov. 2018 May 10;4:56. [Abstract]; NB39-nu cells are treated with either 1000 nM Crizotinib (CR) or Alectinib (AL) for the indicated times and subjected to immunoblot analysis. CLTC is the loading control.

: Alectinib purchased from MCE. Usage Cited in: Cancer Lett. 2017 Aug 1;400:61-68. [Abstract]; In contrast to tumors treated with DMSO, tumors treated with Alectinib exhibits significantly decreased levels of p-Akt and p-S6. Furthermore, increased PARP and Caspase 3 cleavages are observed in tumors treated with Alectinib compared to controls.

: Alectinib purchased from MCE. Usage Cited in: Cancer Lett. 2017 Aug 1;400:61-68. [Abstract]; Alectinib inhibits PI3K/Akt/mTOR signaling and induces apoptosis in NB cells. NB-19, Kelly, IMR-32, SH-SY5Y, SK-N-AS and LA-N-6 cells are treated with 10 mM alectinib for various time points as indicated. The anti-b-Actin antibody is used as a loading control for whole cell extracts.

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生物活性
纯度 & 产品资料
参考文献

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^[1]. Alectinib demonstrates effective central nervous system (CNS) penetration^[2].

IC₅₀ & Target

IC50: 1.9 nM(ALK), 1 nM (ALK^F1174L), 3.5 nM (ALK^R1275Q)^[1]
Kd: 2.4 nM (ALK)^[1]

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	> 1000 nM Compound: 1	Cytotoxicity against mouse BA/F3 cells assessed as cell viability after 72 hrs by MTS assay Cytotoxicity against mouse BA/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	169 nM Compound: 1	Inhibition of EML4-ALK L1152R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK L1152R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	2 nM Compound: 1	Inhibition of wild type EML4-ALK (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of wild type EML4-ALK (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	2 nM Compound: 1	Inhibition of EML4-ALK C1156Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK C1156Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	2 nM Compound: 1	Inhibition of EML4-ALK S1206Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK S1206Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	207 nM Compound: 1	Inhibition of EML4-ALK G1202R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK G1202R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	3 nM Compound: 1	Inhibition of EML4-ALK F1174L mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK F1174L mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	72 nM Compound: 1	Inhibition of EML4-ALK 1151Tins mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK 1151Tins mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	9 nM Compound: 1	Inhibition of EML4-ALK G1269A mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK G1269A mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	90 nM Compound: 1	Inhibition of EML4-ALK L1196M mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK L1196M mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
KARPAS-299	IC₅₀	15 nM Compound: 3; CH5424802	Antiproliferative activity against human KARPAS299 cells after 72 hrs by SRB/CCK-8 assay Antiproliferative activity against human KARPAS299 cells after 72 hrs by SRB/CCK-8 assay	[PMID: 27131066]
KARPAS-299	IC₅₀	3 nM Compound: Alectinib	Antiproliferative activity against human KARPAS-299 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human KARPAS-299 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay	[PMID: 34402300]
KARPAS-299	IC₅₀	3 nM Compound: 18a, CH5424802	Antiproliferative activity against human KARPAS299 cells after 96 hrs by cell counting assay Antiproliferative activity against human KARPAS299 cells after 96 hrs by cell counting assay	[PMID: 22225917]
KARPAS-299	IC₅₀	47 nM Compound: 3	Antiproliferative activity against ALK-positive human KARPAS-299 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against ALK-positive human KARPAS-299 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 34176264]
Kelly	EC₅₀	434 nM Compound: 1	Antiproliferative activity against human Kelly cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human Kelly cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
NB1	IC₅₀	4.5 nM Compound: Alectinib	Antiproliferative activity against human NB1 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human NB1 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay	[PMID: 34402300]
NCI-H2228	IC₅₀	53 nM Compound: Alectinib	Antiproliferative activity against human NCI-H2228 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human NCI-H2228 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay	[PMID: 34402300]
NCI-H2228	IC₅₀	6.5 nM Compound: CH5424802	Cytotoxicity in human NCI-H2228 cells harboring EML4-fused ALK variant 3 incubated for 72 hrs by alamar blue reagent based assay Cytotoxicity in human NCI-H2228 cells harboring EML4-fused ALK variant 3 incubated for 72 hrs by alamar blue reagent based assay	[PMID: 31425908]
NCI-H3122	IC₅₀	17.4 nM Compound: 3; CH5424802	Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB/CCK-8 assay Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB/CCK-8 assay	[PMID: 27131066]
NCI-H3122	IC₅₀	19 nM Compound: 5	Antiproliferative activity against ALK-dependent human NCI-H3122 cells after 72 hrs Antiproliferative activity against ALK-dependent human NCI-H3122 cells after 72 hrs	[PMID: 26476749]
NCI-H3122	IC₅₀	45 nM Compound: 3	Antiproliferative activity against ALK-positive human NCI-H3122 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against ALK-positive human NCI-H3122 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 34176264]
NCI-H3122	EC₅₀	9 nM Compound: 1	Antiproliferative activity against human NCI-H3122 cells after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human NCI-H3122 cells after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
NIH3T3	IC₅₀	132 nM Compound: 3; CH5424802	Antiproliferative activity against mouse NIH/3T3 cells expressing EML4-ALK L1196 mutant after 72 hrs by SRB/CCK-8 assay Antiproliferative activity against mouse NIH/3T3 cells expressing EML4-ALK L1196 mutant after 72 hrs by SRB/CCK-8 assay	[PMID: 27131066]
NIH3T3	IC₅₀	32.3 nM Compound: 3; CH5424802	Antiproliferative activity against mouse NIH/3T3 cells expressing wild type EML4-ALK after 72 hrs by SRB/CCK-8 assay Antiproliferative activity against mouse NIH/3T3 cells expressing wild type EML4-ALK after 72 hrs by SRB/CCK-8 assay	[PMID: 27131066]
SH-SY5Y	EC₅₀	1150 nM Compound: 1	Antiproliferative activity against human SH-SY5Y cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human SH-SY5Y cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
SK-N-AS	EC₅₀	2139 nM Compound: 1	Antiproliferative activity against human SK-N-AS cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human SK-N-AS cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
SK-N-FI	EC₅₀	2401 nM Compound: 1	Antiproliferative activity against human SK-N-FI cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human SK-N-FI cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
SK-N-SH	EC₅₀	872 nM Compound: 1	Antiproliferative activity against human SK-N-SH cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human SK-N-SH cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
SU-DHL-1	IC₅₀	20.5 nM Compound: 3; CH5424802	Antiproliferative activity against human SU-DHL1 cells after 72 hrs by SRB/CCK-8 assay Antiproliferative activity against human SU-DHL1 cells after 72 hrs by SRB/CCK-8 assay	[PMID: 27131066]

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].

MCE 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].

MCE 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

性状

固体

颜色

White to off-white

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	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : 4.33 mg/mL (8.97 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

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	---	---	---

查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

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

方案一

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); 澄清溶液

此方案可获得 ≥ 0.38 mg/mL（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；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 0.38 mg/mL (0.79 mM); 澄清溶液

此方案可获得 ≥ 0.38 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
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。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。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。

方案一

请依序添加每种溶剂： 0.5% CMC-Na/saline water
Solubility: 12.5 mg/mL (25.90 mM); 悬浊液; 超声助溶

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.59%

选择批次：

Data Sheet (627 KB) SDS (393 KB)

COA (286 KB) HNMR (264 KB) LCMS (97 KB)

产品使用指南 (1538 KB)

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. [Content Brief]

[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. [Content Brief]

Alectinib 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.0720 mL	10.3601 mL	20.7202 mL	51.8006 mL
DMSO	5 mM	0.4144 mL	2.0720 mL	4.1440 mL	10.3601 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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

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Other Forms of Alectinib:

MCE 顾客使用本产品发表的 32 篇科研文献

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Alectinib 相关分类

完整储备液配制表

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

Customer Review

Other Forms of Alectinib:

Alectinib 相关抗体

MCE 顾客使用本产品发表的 32 篇科研文献

Alectinib 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

生物活性

纯度 & 产品资料

参考文献

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