上海佰世凯化学科技有限公司

第7年
京师博仁心理咨询室设备快速供货 招投标报价 整体建设方案
  • $p_name$
  • Afatinib(BIBW 2992)/阿法替尼 CAS:439081-18-2

    参考价格: ¥0.00
    品  牌:Chembest
    产品型号:C13260
    适用范围:高教
    所在地区:上海
    上架时间:2017年04月26日
    留言咨询
    与企业取得联系时请告知该信息获取自中国教育装备采购网
    我要分享
    详细说明

    Product Name: Afatinib(BIBW2992)
    Synonym: BIBW-2992;BIBW 2992;BIBW2992;Tovok;Tomtovok;(S,E)-N-(4-(3-chloro-4-fluorophenylamino)-7-((tetrahydrofuran-3- yl)methyl)quinazolin-6-yl)-4-(dimethylamino)but-2-enamide
    Chemical Name: N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-2-butenamide
    CAS No. : 439081-18-2
    Molecular Formula: C24H25ClFN5O3
    Molecular Weight: 485.94
    Purity: >99% HPLC
    Usage: BIBW2992 (Afatinib) is an irreversible EGFR/HER2 inhibitor with an IC50 of 14 nM for in vitro potency against HER2. In cell-free in vitro kinase assays, BIBW2992 shows potent activity against wild-type and mutant forms of EGFR and HER2, similar to gefitinib in potency for L858R EGFR, but about 100-fold more active against the gefitinib resistant L858R-T790M EGFR double mutant, with an IC50 of 10 nM. BIBW2992 was effective in inhibiting survival of lung cancer cell lines harboring wild-type (H1666) or L858R/T790M (NCI-H1975) EGFR, with IC50s below 100 nM for these isoforms resistant to first-generation inhibitors anda subnanomolar IC50 for the gefitinibsensitive L858R expressedby H3255. Assessed in a standard xenograft model of the epidermoid carcinoma cell line A431. Daily oral treatment with BIBW2992 at 20 mg/kg for 25 days resulted in dramatic tumor regression with a cumulative treated/control tumor volume ratio (T/C ratio) of 2%.Like lapatinib and neratinib, afatinib is a next generation tyrosine kinase inhibitor (TKI) that irreversibly inhibits human epidermal growth factor receptor 2 (Her2) and epidermal growth factor receptor (EGFR) kinases. Afatinib is not only active against EGFR mutations targeted by first generation TKIs like erlotinib or gefitinib, but also against those not sensitive to these standard therapies. Because of its additional activity against Her2, it is investigated for breast cancer as well as other EGFR and Her2 driven cancers.