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Altiratinib

源叶(MedMol) 98%
  • 英文名:
  • Altiratinib
  • 别名:
  • Altiratinib(DCC2701); DCC 2701; TETRAKIS(TRIPHENYLPHOSPHINE)PALLADIUM(O); altiratinib; N-(4-(2-(cyclopropanecarbonylamino)pyridin-4-yloxy)-2,5-difluorophenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicar
  • CAS号:
  • 1345847-93-9
  • 分子式:
  • C26H21F3N4O4
  • 分子量:
  • 510.4645
  • 核磁/质谱:
品牌货号产品规格价格(RMB) 库存(上海) 北京 武汉 南京 数量计量单位 加入购物车...
源叶(MedMol) S82916-1mg 98% ¥163.20元 9 - - - EA 加入购物车
源叶(MedMol) S82916-2mg 98% ¥272.00元 10 - - - EA 加入购物车
源叶(MedMol) S82916-5mg 98% ¥353.60元 6 - - - EA 加入购物车
源叶(MedMol) S82916-10mg 98% ¥571.20元 3 - - - EA 加入购物车
源叶(MedMol) S82916-25mg 98% ¥1020.00元 4 - - - EA 加入购物车
源叶(MedMol) S82916-50mg 98% ¥1496.00元 预计交期:2-3天 - - - EA 加入购物车
源叶(MedMol) S82916-100mg 98% ¥2720.00元 预计交期:2-3天 - - - EA 加入购物车
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  • 提示:详情请下载说明书。
  • 产品描述: Altiratinib (DCC-2701) is a multi-targeted kinase inhibitor with IC50s of 2.7, 8, 9.2, 9.3, 0.85, 4.6, 0.83 nM for MET, TIE2, VEGFR2, FLT3, Trk1, Trk2, and Trk3 respectively.
  • 靶点: VEGFR2:9.2 nM (IC50);Trk1:0.85 nM (IC50);Trk2:4.6 nM (IC50);Trk3:0.93 nM (IC50);MET:2.7 nM (IC50);TIE2:8 nM (IC50);FLT3:9.3 nM (IC50);VEGFR; Tie-2; FLT; Trkreceptor; c-Met/HGFR
  • 体外研究:
    Altiratinib also inhibits MET isoforms METD1228H, METD1228N, 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
  • 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
  • 参考文献:
    1. Smith BD, et al. Altiratinib Inhibits Tumor Growth, Invasion, Angiogenesis, and Microenvironment-Mediated DrugResistance via Balanced Inhibition of MET, TIE2, and VEGFR2. Mol Cancer Ther. 2015 Sep;14(9):2023-34.
  • 溶解性: Soluble  in  DMSO
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 1.959 ml 9.795 ml 19.59 ml
    5 mM 0.392 ml 1.959 ml 3.918 ml
    10 mM 0.196 ml 0.98 ml 1.959 ml
    50 mM 0.039 ml 0.196 ml 0.392 ml
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