基本信息 产品详情 公司简介 推荐产品
  • 首页
  • 个人中心
  • 委托采购
  • 采购清单
网站主页 化工产品目录 生物化工 抑制剂 蛋白酪氨酸激酶 双马来酸盐阿法替尼 双马来酸盐阿法替尼
  • 双马来酸盐阿法替尼|T1773|TargetMol

双马来酸盐阿法替尼|T1773|TargetMol

Afatinib Dimaleate
850140-73-7
￥176 1mg 起订
￥357 5mg 起订
￥576 10mg 起订
上海 更新日期：2024-12-02

TargetMol中国（陶术生物）

VIP12年
联系人：邵小姐
电话：021-021-33632979拨打
手机：15002134094 拨打
邮箱：marketing@targetmol.com

产品详情:

中文名称：
双马来酸盐阿法替尼
英文名称：
Afatinib Dimaleate
CAS号：
850140-73-7
品牌：
TargetMol
产地：
美国
保存条件：
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格：
99.66%
产品类别：
抑制剂
货号：
T1773

Product Introduction

Bioactivity

名称Afatinib Dimaleate
描述Afatinib Dimaleate (BIBW 2992MA2) is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic activity.
细胞实验Cytotoxicity is determined using MTT assay. The IC 50 value is de?ned as the drug concentration resulting in 50% cell death. Both the ?tted sigmoidal dose response curve and IC50 are calculated by Bliss method.(Only for Reference)
激酶实验In vitro kinase activity assay: EGFR kinase: Each 100 μL enzyme reaction contained 10 μL of inhibitor in 50% Me2SO, 20 μL of substrate solution (200 mM HEPES pH 7.4, 50 mM Mg-acetate, 2.5 mg/mL poly (EY), 5 μg/mL bio-pEY) and 20 μL enzyme preparation. The enzymatic reaction is started by addition of 50 μL of a 100 μM ATP solution made in 10 mM MgCl2. Assays are carried out at room temperature for 30 min and terminated by the addition of 50 μL of stop solution (250 mM EDTA in 20 mM HEPES pH 7.4). 100 μL are transferred to a streptavidin coated microtiterplate, after an incubation time of 60 min at room temperature the plate is washed with 200 μL of wash solution (50 mM Tris, 0.05% Tween20). A 100 μL aliquot of a HRPO- labeled anti-PY antibody (PY20H Anti-Ptyr:HRP ) 250 ng/mL are added to the wells. After 60 min of incubation, the plate is washed three times with a 200 μL wash solution. The samples are then developed with a 100μL TMB Peroxidase Solution (A:B= 1:1). The reaction is stopped after 10 min. The plate is transferred to an ELISA reader and extinction is measured at OD450 nM. HER2-IC enzyme: Enzyme activity is assayed in the presence or absence of serial inhibitor dilutions performed in 50 % Me2SO. Each 100 μL reaction contains similar components as described for EGFR kinase assay with addition of 1000 μM Na3VO4. The enzymatic reaction is started by addition of 50μL of 500 μM ATP solution made in 10 mM Mg-acetate. The dilution of the enzyme is set so that incorporation of phosphate into bio-pEY is linear with respect to time and amount of enzyme. The enzyme preparation is diluted in 20 mM HEPES pH 7.4, 130 mM NaCl, 0.05% Triton X-100, 1 mM DTT and 10% glycerol. Assays are carried out at room temperature for 30 min and terminated by the addition of 50 μL of stop solution. Src kinase assays: Each 100 μL reaction contained 10 μL of inhibitor in 50 % Me2SO, 20μL of enzyme preparation, 20 μL of substrate solution supplemented with 1000 μM Na3VO4.The enzymatic reaction is started by addition of 50 μL of a 1000 μM ATP solution made in 10 mM Mg-acetate. BIRK kinase assay: 250 mM Tris pH 7.4, 10 mM DTT, 2.5 mg/mL poly(EY), 5 mg/mL bio-pEY is used as substrate solution and enzymatic reaction is started by addition of 50 μL of a 2 mM ATP solution made in 8 mM MnCl2, 20 mM Mg-acetate. VEGF2 and HGFR kinase assays: Assays are carried out at room temperature for 20 minutes and terminated by the addition of 10 μL of 5 % H3PO4. The precipitate is then trapped onto GF/B filters using a 96 well filter mate universal harvester. After extensive washing the filter plate is dried for 1 h at 50°C, sealed and incorporated radioactivity is determined by scintillation counting using a TopCount? or a Microbeta b counter?.
体外活性在MDA-MB-453移植瘤模型中,口服给药 Afatinib（20 mg/kg）,下调EGFR和AKT磷酸化水平,能够诱导肿瘤衰退.在HER2阳性胃癌NCI-N87移植瘤模型中,口服 Afatinib（25 mg/kg）能够消除肿瘤.在A7、A431、FaDu、UT-SCC-14和UT-SCC-15移植瘤模型中,口服给药 Afatinib（30 mg/kg）能够抑制肿瘤生长.
体内活性在表达野生型(H1666)或L858R/T790M (NCI-H1975) EGFR的肺癌细胞系中,Afatinib能够更有效的抑制细胞生长。在表达HER2 776insV (NCI-H1781) 或EGFR E746_A750del (HCC827)的NSCLC细胞系中,Afatinib能够更抑制细胞生长。
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 50 mg/mL (69.63 mM)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
关键字HKESC-1 | NIH-3T3 cells | Autophagy | ESCC | orally active | BIBW 2992 | EGFR | Apoptosis | inhibit | Epidermal growth factor receptor | SLMT-1 | Afatinib Dimaleate | BIBW-2992 | c-Met/HGFR | PKB | A431 | Akt | NSCLC | anticancer | Protein kinase B | ErbB-1 | p38 MAPK | H3255 | lung cancer | HER2 | Inhibitor | H1666 | NCI-H1975 | HKESC-2 | Afatinib (BIBW2992) | HER1 | EC-1
相关产品Guanidine hydrochloride | Naringin | Valproic Acid | Taurine | Gefitinib | Aceglutamide | Hydroxychloroquine | Curcumin | Stavudine | Salicylic acid | Paeonol | Sodium 4-phenylbutyrate
相关库抑制剂库 | 经典已知活性库 | 抗癌活性化合物库 | 抗癌上市药物库 | 已知活性化合物库 | EMA 上市药物库 | 激酶抑制剂库 | 酪氨酸激酶分子库 | 药物功能重定位化合物库 | 抗癌药物库
双马来酸盐阿法替尼|||马来酸阿法替尼|||BIBW2992|||BIBW 2992MA2|||Afatinib (BIBW2992) Dimaleate|||Afatinib|TargetMol

公司简介

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。 从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。 经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期 (12年)
注册资本 566.2651万人民币
员工人数 100-500人
年营业额 ￥ 1亿以上
经营模式 贸易,试剂,定制,服务
主营行业 化学试剂,生物活性小分子

双马来酸盐阿法替尼相关厂家报价 更多

内容声明
official 进入官方账号
拨打电话 立即询价