Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Brigatinib (AP-26113) 是一种有效,选择性的ALK 抑制剂 (IC50:0.6 nM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 219 | 现货 | ||
5 mg | ¥ 483 | 现货 | ||
10 mg | ¥ 788 | 现货 | ||
25 mg | ¥ 1,420 | 现货 | ||
50 mg | ¥ 2,370 | 现货 | ||
100 mg | ¥ 3,770 | 现货 | ||
200 mg | ¥ 4,990 | 现货 | ||
500 mg | ¥ 7,820 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 658 | 现货 |
产品描述 | Brigatinib (AP-26113) is a highly potent and selective ALK inhibitor. |
靶点活性 | FLT3:2.1 nM, ROS1:1.9 nM, ALK:0.37 nM, IGF1R:24.9 nM, EGFR(C797S/del19):39.9 nM |
体外活性 | Beyond ALK, IGF1R, and InsR, brigatinib also potently inhibits FLT3 and ROS1 with IC50 values of 2.1 and 1.9 nM, respectively. It does not show significant activity toward c-Met or Ron up to 1 μM[1]. Brigatinib overcomes the resistance of EGFR-triple-mutant and the activity depends on ATP-competitive manner with less affection to wild-type EGFR[2]. |
体内活性 | Mouse PK parameters for Brigatinib following oral dosing (10 mg/kg): Cmax=448 ng/mL,t1/2=5.8 h. And in CD rats, after dosing at 3 mg/kg i.v, CL=0.46 L/(h·kg), t1/2=4.8 h, Vss=7.8 L/kg; Dosed at 10 mg/kg p.o, Cmax=305 ng/mL, tmax=4 h, t1/2=3.4 h, F%=52. Brigatinib demonstrates dose-dependent antitumor activity[1]. Brigatinib demonstrates growth inhibition activity in PC9 triple-mutant xenograft model and in combination with anti-EGFR antibody to potentiate the efficacy both in vitro and in vivo as shown in first-generation EGFR-TKI-resistant patients[2]. |
激酶实验 | In vitro HotSpotSM 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. |
细胞实验 | All cell lines were used within 20 passages of the initial thaw. Following inhibitor treatment for 72 h, cell growth was assessed to determine the concentration that causes 50% inhibition of cell viability (IC50). (Only for Reference) |
别名 | 布格替尼, AP-26113 |
分子量 | 584.09 |
分子式 | C29H39ClN7O2P |
CAS No. | 1197953-54-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: Insoluble
DMSO: 5.84 mg/mL (10 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.7121 mL | 8.5603 mL | 17.1206 mL | 42.8016 mL |
5 mM | 0.3424 mL | 1.7121 mL | 3.4241 mL | 8.5603 mL | |
10 mM | 0.1712 mL | 0.856 mL | 1.7121 mL | 4.2802 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Brigatinib 1197953-54-0 Angiogenesis Immunology/Inflammation JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR FLT ROS IGF-1R ALK Inhibitor inhibit ALK tyrosine kinase receptor AP26113 CD246 布格替尼 AP 26113 Anaplastic lymphoma kinase (ALK) AP-26113 Cluster of differentiation 246 Anaplastic lymphoma kinase inhibitor