Brigatinib (AP26113)

For research use only. Not for use in humans.

目录号:S8229 中文名称:布格替尼

Brigatinib (AP26113) Chemical Structure

CAS No. 1197953-54-0

Brigatinib (AP26113) 是一种有效的、选择性的ALK抑制剂,IC50=0.6 nM;也是ROS1抑制剂,IC50=0.9 nM。它还能以相对较低的效力抑制IGF-1R、FLT3、FLT3(D835Y)和EGFR。

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客户使用Selleck生产的Brigatinib (AP26113)发表文献13篇:

客户使用该产品的1个实验数据:

  • Immunoblotting analysis of H3122 and H3122-CER cells showing that brigatinib did not inhibit EGFR phosphorylation (p-EGFR). Total EGFR (t-EGFR) is also shown. Actin was used as a loading control. The cells were treated with brigatinib for 2 hours.

    Mol Cancer Res, 2017, 15(1):106-114. Brigatinib (AP26113) purchased from Selleck.

产品安全说明书

ALK抑制剂选择性比较

生物活性

产品描述 Brigatinib (AP26113) 是一种有效的、选择性的ALK抑制剂,IC50=0.6 nM;也是ROS1抑制剂,IC50=0.9 nM。它还能以相对较低的效力抑制IGF-1R、FLT3、FLT3(D835Y)和EGFR。
靶点
ALK [1]
(Cell-free assay)
ROS1 [1]
(Cell-free assay)
FLT3 [1]
(Cell-free assay)
IGF1R [1]
(Cell-free assay)
EGFR(C797S/del19) [2]
(cell-based)
0.37 nM 1.9 nM 2.1 nM 24.9 nM 39.9 nM
体外研究

除了ALK, IGF1R和InsR,brigatinib也能有效地抑制FLT3和ROS1,IC50分别为2.1 nM和1.9 nM。在1 μM时,brigatinib对c-Met或Ron没有显著活性[1]。Brigatinib可克服EGFR三突变体的耐药性,这一活性依赖于ATP竞争性,对野生型EGFR的影响较小[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
KARPAS299 MXvBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NGrDbJE4OiCqcoO= NHjFO5BCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFHMT{1xd3OrdHn2[UBMSVKSQWOyPVkh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KG2nYYP1doVlKGGodHXyJFczKGi{czDifUBE\WyuVHn0[ZIhQTZiYYH1[Y92eyCxbnWgd49tfXSrb36gZ4VtdCCycn;sbYZmemG2aX;uJIF{e2G7LDDHTVUxKD1iMD6wNUDPxE1w NE\sV5I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{G0OFg{OSd-MkexOFQ5OzF:L3G+
KARPAS299 NV71UVJQSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MoT1O|IhcHK| NVza[JJVSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBUGsueG:|aYTpeoUhU0GUUFHTNlk6KGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCvZXHzeZJm\CCjZoTldkA4OiCqcoOgZpkhS2WubGTpeIVzKDl4IHHxeYVwfXNib37lJJNwdHW2aX;uJINmdGxicILvcIln\XKjdHnvckBie3OjeTygTWM2OCB;IECuNFI6KM7:TT6= NHfxNpc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{G0OFg{OSd-MkexOFQ5OzF:L3G+
Ba/F3 MV\GeY5kfGmxbjDhd5NigQ>? MlSwO|IhcHK| MUTJcohq[mm2aX;uJI9nKGi3bXHuJGVITlJiZHXsNVkwXDd7MF2vR|c6P1NibYX0ZY51KGW6cILld5Nm\CCrbjDtc5V{\SCEYT;GN{Bk\WyuczDhd5Nme3OnZDDhd{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJvR3zvJIF{e2G7LDDHTVUxKD1iMD6wOlczKM7:TT6= NGLYOpI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUGzOlQ3PSd-MkmxN|Y1PjV:L3G+
BAF3 M{TIN2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 M2rUeFczKGi{cx?= NX3VenFZSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBud3W|ZTDCRWY{KGOnbHzzJIhiemKxcnnu[{BGT0[UIEG5SE9VPzlyTT;DO|k4WyCvdYThcpQh[W[2ZYKgO|IhcHK|IHL5JJJme2G8dYLpckBlgWViYnHz[YQh[XO|YYmsJGlEPTBiPTCwMlI3KM7:TT6= MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODR{OUm1Okc,OzB2Mkm5OVY9N2F-
BAF3 NH3CNnRCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NHiwUWY4OiCqcoO= NXrzZoo4SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBud3W|ZTDCRWY{KGOnbHzzJIhiemKxcnnu[{BGT0[UIFy4OVhTN1R5OUDNM2M4QTeVIH31eIFvfCCjZoTldkA4OiCqcoOgZpkhemW|YYr1dolvKGS7ZTDiZZNm\CCjc4PhfUwhUUN3MDC9JFAvPDJizszNMi=> M{\wW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNEK5PVU3Lz5|MESyPVk2PjxxYU6=
NCI-H1975 MWTBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? Mn\aO|IhcHK| M2CyOWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWgyQTd3IHPlcIx{KGijcnLvdolv\yCHR1\SJGw5PTiUL2S3PVBOKG23dHHueEBi\nSncjC3NkBpenNiYomgdoV{[Xq3cnnuJIR6\SCkYYPl[EBie3OjeTygTWM2OCB;IEGuNFkh|ryPLh?= MlG0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB2Mkm5OVYoRjNyNEK5PVU3RC:jPh?=
U937 MW\BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NFz0bJM4OiCqcoO= NIezbI5CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFHMT{1v\WejdHn2[UBWQTN5IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBk\WyuII\pZYJqdGm2eTDt[YF{fXKnZDDh[pRmeiB5MjDodpMh[nliQ3XscHRqfGW{IEm2JIFyfWWxdYOgc45mKHOxbIX0bY9vKGOnbHygdJJwdGmoZYLheIlwdiCjc4PhfUwhUUN3MDC9JFMvOTl2IN88UU4> NH\vfGc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{G0OFg{OSd-MkexOFQ5OzF:L3G+
KARPAS299 NXLLelY1SW62aYT1cY9zKGG|c3H5 Moe0OVAhdWdxa3e= NHHKd4MyOyCmYYnz MUnBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNQWLQRXMzQTliY3XscJMh\XiycnXzd4lv\yCQTWCtRWxMKG[3c3nvckBxem:2ZXnuJJhmdm:pcnHmeIVlKGmwIGPDTWQw[mWrZ3WgcY92e2ViYYPz[ZN{\WRiYYOgeJVud3JicnXndoV{e2mxbjDheEA2OCCvZz;r[{wheG9iYXTtbY5qe3SncnXkJI9v[2ViZHHpcJkh\m:{IEGzJIRigXNuIF7VUGwhRSCQVVzMJO69VS5? MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzF2NEizNUc,OjdzNES4N|E9N2F-

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
pEGFR / EGFR / pAkt / Akt / pERK / ERK / pS6 / S6; 

PubMed: 28287083     


Ba/F3 cells expressing T790M/del19 (d) or C797S/T790M/del19 (e) were treated with the indicated concentrations of brigatinib, AP26113 analog, TAE684, ceritinib or ASP3026 for 6 h. Phosphorylation of EGFR and its downstream signals were evaluated by wester䲧疝Ỵ疞㧀疜膉痘 瘿�෋ᾰƌ෋à 

pALK / ALK; 

PubMed: 21502504     


Suppression of ALK signaling by AP26113 in resistant H3122 CR cells. H3122 parental and resistant cells were exposed to increasing concentrations of AP26113 for 6 h. Cell lysates were immunoblotted to detect the indicated proteins.

pROS1 / ROS1 / pSTAT3 / STAT3 ; 

PubMed: 25351743     


Inhibition of phospho-ROS1 by various ALK inhibitors in Ba/F3 models. CD74-ROS1 expressing Ba/F3 cells were exposed to increasing concentrations of crizotinib, ceritinib, AP26113, or ASP3026 for 3 h. Cell lysates were immunoblotted to detect the indicated䲧疝Ỵ疞㧀

28287083 21502504 25351743
Growth inhibition assay
Cell viability ; 

PubMed: 25351743     


(A) Ba/F3 cells expressing CD74-ROS1 (clone #6) were seeded in 96 well-plates and treated with indicated concentration of crizotinib, ceritinib, AP26113, ASP3026, or alectinib for 72 h. Cell viability was analyzed using the CellTiter-Glo assay. (B) IC50 v䲧疝Ỵ疞㧀疜膉痘 瘿뾠ՂᾰƌՂĀ 㺣痖帉痖Ѐ瑖堘𢡄빢᎒ՂĀ鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤瘯Ɖ⟸෕䐺痖暼瘿⟸෕ᾰƌ ⟸෕Ð㺣痖⟸෕€𢡄⟼෕€䀷痗⟼෕౴⟼෕㵶痗⟼෕뺖᎒泌Itemセ᎒Count﫨呂⠬෕猴፲⟼෕፲씢痗猸፲髸莤䥷堙᎒セ᎒�堞ﻮ᎒፲露𢡄堚ў齃礤v�堞ﻮ᎒猢

25351743
体内研究 Brigatinib的口服途径给药在小鼠中的药代动力学:Cmax=448 ng/mL,t1/2=5.8 h。在CD大鼠中,静脉注射3 mg/kg后,CL=0.46 L/(h·kg), t1/2=4.8 h, Vss=7.8 L/kg;而口服10 mg/kg时,Cmax=305 ng/mL, tmax=4 h, t1/2=3.4 h, F%=52。Brigatinib具有浓度依赖性的抗肿瘤活性[1]。在PC9三突变移植瘤模型中,Brigatinib具有生长抑制作用,当其与anti-EGFR抗体一起结合使用时,能在体内外增强功效[2]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:

[1]

- 合并
  • Cell lines: U937细胞, Karpas-299细胞, H3122细胞
  • Concentrations: --
  • Incubation Time: 72 h
  • Method:

    将细胞用抑制剂处理72小时,检测细胞生长情况,确定IC50值。


    (Only for Reference)
动物实验:

[1]

- 合并
  • Animal Models: 雌性CD大鼠
  • Dosages: 10 mg/kg(p.o); 2 mg/kg(i.v)
  • Administration: p.o, i.v
    (Only for Reference)

溶解度 (25°C)

体外 Ethanol 43 mg/mL warmed (73.61 mM)
DMSO 1 mg/mL warmed (1.71 mM)
Water Insoluble

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 584.09
化学式

C29H39ClN7O2P

CAS号 1197953-54-0
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04634110 Not yet recruiting Drug: Brigatinib Brain Metastases|Lung Cancer University of Colorado Denver|National Cancer Institute (NCI) December 2020 Phase 2
NCT04260009 Withdrawn Drug: Brigatinib|Drug: Brigatinib AAF Anaplastic Lymphoma Kinase Positive (ALK +) Anaplastic Large Cell Lymphoma|Inflammatory Myofibroblastic Tumors|Solid Tumors Takeda September 1 2020 Phase 1|Phase 2
NCT04111705 Recruiting Drug: Lorlatinib Non Small Cell Lung Cancer Metastatic Intergroupe Francophone de Cancerologie Thoracique August 5 2020 Phase 2
NCT04005144 Recruiting Drug: Binimetinib|Drug: Brigatinib ALK Gene Rearrangement|Lung Non-Small Cell Carcinoma|Progressive Disease|ROS1 Gene Rearrangement|Stage IIIB Lung Cancer|Stage IIIC Lung Cancer|Stage IV Lung Cancer|Stage IVA Lung Cancer|Stage IVB Lung Cancer University of California San Francisco|Takeda|Array BioPharma February 25 2020 Phase 1
NCT03410108 Active not recruiting Drug: Brigatinib ALK-positive Advanced NSCLC Takeda January 29 2018 Phase 2
NCT02094573 Completed Drug: Brigatinib Carcinoma Non-Small-Cell Lung Ariad Pharmaceuticals|Takeda June 4 2014 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID