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  • Altiratinib

    • Altiratinib, DCC2701,DCC 2701,DCC-2701
    货号: abs810250
    CAS号: 1345847-93-9
    分子式: C26H21F3N4O4
    分子量: 510.15
    产品说明书
    分享:
    货号-规格 货期 价格 数量
    abs810250-5mg 1-2周 ¥1161.00
    - +
    abs810250-10mg 1-2周 ¥1870.00
    - +
    abs810250-50mg 1-2周 ¥7383.00
    - +
    abs810250-100mg 1-2周 ¥12067.00
    - +
    大包装询价
    产品描述
    描述
    Altiratinib is a MET/TIE2/VEGFR2/TRK (A,B,C) kinase inhibitor in Phase 1 clinical development for the treatment of invasive solid tumors including glioblastoma.
    纯度
    >98%
    储存/保存方法
    Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
    基本信息
    别名
    Altiratinib, DCC2701,DCC 2701,DCC-2701
    外观
    Powder
    可溶性/溶解性
    DMSO: ≥ 33 mg/mL
    生物活性
    靶点
    Trk Receptor
    In vitro(体外研究)
    Altiratinib also inhibits MET isoforms METD1228H, MET D1228N, METY1230C, METY1230D, METY1230H, METM1250T with IC50s of 3.6, 1.3, 1.2, 0.37, 1.5 and 6 nM, respectively. Altiratinib inhibits MET phosphorylation with IC50 values of 0.85 and 2.2 nM, respectively. In the U-87 glioblastoma cell line, MET and HGF are both expressed. Altiratinib blocks autocrine activation of MET phosphorylation in these cells (IC50=6.2 nM). Altiratinib potently inhibits cellular proliferation in MET-amplified EBC-1 and MKN-45 cells, as well as TPM3-TRKA fusion KM-12 cells. Activation of MET is known to increase the motility and invasiveness of cancer cells: Altiratinib inhibits HGF-induced A549 cell migration, with an IC50 of 13 nM. Altiratinib also inhibits FLT3-ITD mutant MV-4-11 cell proliferation with an IC50 of 12 nM.
    In vivo(体内研究)
    A single oral dose of 30 mg/kg Altiratinib leads to >95% inhibition of MET phosphorylation for the entire 24-hour period. A single 10 mg/kg oral dose of Altiratinib exhibits complete inhibition of MET phosphorylation through 12 hours and 73% inhibition at 24 hours postdose. Altiratinib dosed at 10 mg/kg twice a day leads to a significant 90% decrease in BLI signal. Altiratinib exhibits properties amenable to oral administration and exhibits substantial blood–brain barrier penetration, an attribute of significance for eventual treatment of brain cancers and brain metastases.
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    • 实验方法 实验条件
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