Brigatinib (Synonyms: 布格替尼; AP-26113)

目录号: HY-12857 纯度: 99.98%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Brigatinib (AP-26113) 是一种有效，选择性的，具有口服活性的 ALK 抑制剂，IC₅₀ 值为 0.6 nM。Brigatinib 可用于非小细胞肺癌 (NSCLC) 的研究。

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Brigatinib Chemical Structure

CAS No. : 1197953-54-0

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规格	价格	是否有货
1 mg	￥272	In-stock
5 mg	￥600	In-stock
10 mg	￥950	In-stock
50 mg	￥2850	In-stock
100 mg	￥4550	In-stock
200 mg		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

Other Forms of Brigatinib:

Brigatinib-¹³C₆ 询价
Brigatinib-d3 询价

MCE 顾客使用本产品发表的 25 篇科研文献

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Brigatinib (AP-26113) is a highly potent, selective and orally active ALK inhibitor, with an IC₅₀ of 0.6 nM. Brigatinib can be used for research of NSCLC^[1].

IC₅₀ & Target

IC50: 0.6 nM (ALK)^[1]

体外研究
(In Vitro)

Brigatinib potently inhibits the in vitro kinase activity of ALK (IC₅₀, 0.6 nM) and all five mutant variants tested, including G1202R (IC₅₀, 0.6-6.6 nM).
Brigatinib demonstrates a high degree of selectivity, only inhibiting 11 additional native or mutant kinases with IC₅₀ <10 nM. These include ROS1, FLT3, and mutant variants of FLT3 (D835Y) and EGFR (L858R; IC₅₀, 1.5-2.1 nM).
Brigatinib exhibits more modest activity against EGFR with a T790M resistance mutation (L858R/T790M), native EGFR, IGF1R, and INSR (IC₅₀, 29-160 nM) and does not inhibit MET (IC₅₀ >1000 nM).
In cellular assays, brigatinib inhibits ALK and ROS1 with IC₅₀s of 14 and 18 nM, respectively.
Brigatinib inhibits FLT3 and IGF-1R with about 11-fold lower potency (IC₅₀, 148-158 nM) and inhibits mutant variants of FLT3 and EGFR with 15- to 35-fold lower potency (IC₅₀, 211-489 nM).
Brigatinib inhibits cell growth with GI₅₀ values ranging from 503 to 2,387 nM in three ALK-negative ALCL and NSCLC cell lines^[1].
Brigatinib inhibits ALK activity and abrogates proliferation of ALK addicted neuroblastoma cell lines, with IC₅₀ of 75.27 ± 8.89 nM.
Brigatinib inhibits both the ALK-I1171N and the ALK-G1269A mutant receptors at 10 and 4 nM levels, respectively^[3].

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

体内研究
(In Vivo)

Brigatinib (10, 25, or 50 mg/kg once daily, p.o.) leads to a dose-dependent inhibition of tumor growth in ALK⁺ Karpas-299 (ALCL) and H2228 (NSCLC) xenograft mouse models. Brigatinib markedly enhances survival of mice bearing ALK⁺ brain tumors compared with PF-02341066^[1].
Brigatinib (10, 25, 50 mg/kg, p.o.) results in dose-dependent antitumor activity, with tumor regressions in a mouse model of NSCLC^[2].

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

Clinical Trial

分子量

584.09

Formula

C₂₉H₃₉ClN₇O₂P

CAS 号

1197953-54-0

性状

固体

颜色

White to light yellow

中文名称

布格替尼

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：

Ethanol 中的溶解度 : 10 mg/mL (17.12 mM; 超声加热助溶)

DMSO 中的溶解度 : 2 mg/mL (3.42 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	1.7121 mL	8.5603 mL	17.1206 mL
5 mM	0.3424 mL	1.7121 mL	3.4241 mL
10 mM	0.1712 mL	0.8560 mL	1.7121 mL

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% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1 mg/mL (1.71 mM); 澄清溶液

此方案可获得 ≥ 1 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 EtOH 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% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (1.71 mM); 澄清溶液

此方案可获得 ≥ 1 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 EtOH 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% EtOH 90% Corn Oil
Solubility: ≥ 1 mg/mL (1.71 mM); 澄清溶液

此方案可获得 ≥ 1 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 10.0 mg/mL 的澄清 EtOH 储备液加到 900 μL 玉米油中，混合均匀。
方案四

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.5 mg/mL (0.86 mM); 澄清溶液

此方案可获得 ≥ 0.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 5.0 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。
方案五

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.5 mg/mL (0.86 mM); 澄清溶液

此方案可获得 ≥ 0.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案六

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 0.5 mg/mL (0.86 mM); 澄清溶液

此方案可获得 ≥ 0.5 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 5.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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: 99.98%

选择批次：

Data Sheet (631 KB) SDS (615 KB)

COA (285 KB) LCMS (107 KB) 元素分析报告 (208 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Zhang S, et al. The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models. Clin Cancer Res. 2016 Nov 15;22(22):5527-5538 [Content Brief]

[2]. Huang WS, et al. Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase. J Med Chem. 2016 May 26;59(10):4948-64. [Content Brief]

[3]. Siaw JT, et al. Brigatinib, an anaplastic lymphoma kinase inhibitor, abrogates activity and growth in ALK-positive neuroblastoma cells, Drosophila and mice. Oncotarget. 2016 May 17;7(20):29011-22 [Content Brief]

Kinase Assay ^[1]	In vitro HotSpot^SM kinase profiling of 289 kinases is performed. The assay is conducted in the presence of 10 μM [³³P]-ATP, using brigatinib concentrations ranging from 0.05 nM to 1 μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[3]	Cells are seeded at 15,000 per well with serial dilutions of the indicated inhibitors. After 72 hours cell viability is assessed by resazurin. IC₅₀ values are calculated with GraphPad Prism 6.0 by fitting data to a log (inhibitor concentration) vs. normalized response (variable slope) equation. Each experiment is performed in duplicate and repeated at least three times. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Mice: (1) Eight- to 10-week-old female SCID/beige mice are injected intravenously with 5×10⁶ H3122 cells per mouse and are randomly selected into treatment groups (n=10) when the average tumor size reaches appr 300 mm³ (day zero). Treatments are administered orally for up to 21 consecutive days at a 10 mL/kg dose volume. Subcutaneous tumors are measured two or three times weekly. Tumor volume (in mm³) is calculated using the formula (L×W²)/2. When a tumor reaches 10% of the body weight of the host, the animal is euthanized via CO₂ asphyxiation. (2) Eight- to 10-week old female SCID/beige mice are injected subcutaneously with 2.5×10⁶ Karpas-299 cells per mouse and are randomly selected into treatment groups (n=10) when the average tumor size reached appr 180 mm³ (day zero). Treatments are administered orally for 14 consecutive days at a 10 mL/kg dose volume. Tumor volume is measured and calculated as described for the H3122 model. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Zhang S, et al. The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models. Clin Cancer Res. 2016 Nov 15;22(22):5527-5538 [Content Brief] [2]. Huang WS, et al. Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase. J Med Chem. 2016 May 26;59(10):4948-64. [Content Brief] [3]. Siaw JT, et al. Brigatinib, an anaplastic lymphoma kinase inhibitor, abrogates activity and growth in ALK-positive neuroblastoma cells, Drosophila and mice. Oncotarget. 2016 May 17;7(20):29011-22 [Content Brief]

Brigatinib 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 / Ethanol	1 mM	1.7121 mL	8.5603 mL	17.1206 mL	42.8016 mL
Ethanol	5 mM	0.3424 mL	1.7121 mL	3.4241 mL	8.5603 mL
	10 mM	0.1712 mL	0.8560 mL	1.7121 mL	4.2802 mL
	15 mM	0.1141 mL	0.5707 mL	1.1414 mL	2.8534 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.

Keywords:

Brigatinib1197953-54-0AP-26113布格替尼AP26113AP 26113Anaplastic lymphoma kinase (ALK)Anaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246NSCLCcancerALK mutationInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

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上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

Brigatinib (Synonyms: 布格替尼; AP-26113)

Customer Review

Other Forms of Brigatinib:

MCE 顾客使用本产品发表的 25 篇科研文献