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S81137

PF-00562271 besylate

源叶(MedMol) 98%
  • 英文名:
  • PF-00562271 besylate
  • 别名:
  • PF 562271 苯磺酸盐;N-甲基-N-[3-[[[2-[(2-氧代-2,3-二氢-1H-吲哚-5-基)氨基]-5-三氟甲基嘧啶-4-基]氨基]甲基]吡啶-2-基]甲磺酰胺苯磺酸盐
  • CAS号:
  • 939791-38-5
  • 分子式:
  • C21H20F3N7O3S·C6H6O3S
  • 分子量:
  • 665.66
  • 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) S81137-5mg 98% ¥560.00元 6 - - - EA 加入购物车
源叶(MedMol) S81137-10mg 98% ¥904.00元 7 - - - EA 加入购物车
源叶(MedMol) S81137-25mg 98% ¥1808.00元 6 - - - EA 加入购物车
源叶(MedMol) S81137-100mg 98% ¥5440.00元 预计交期:2-3天 - - - EA 加入购物车
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参考文献

质检证书(COA)

摩尔浓度计算器

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  • 提示:详情请下载说明书。
  • 产品描述: PF-562271 (VS-6062) besylate is a potent ATP-competitive, reversible inhibitor of FAK and Pyk2 kinase, with an IC50 of 1.5 nM and 13 nM, respectively
  • 靶点: IC50: 1.5 nM (FAK), 13 nM (Pyk2), 30 nM (CDK2), 47 nM (CDK3), 58 nM (CDK1), 97 nM (CDK7), 97 nM (Flt3);FAK; PYK2; CDK
  • 体外研究:
    PF-562271 (VS-6062) besylate is a 30- to 120-nM (15.2 to 60.1 ng/mL) inhibitor of cdk2/E, cdk5/p35, cdk1/B, and cdk3/E in recombinant enzyme assays. PF-562,271 blocks bFGF-stimulated blood vessel angiogenesis as performed in chicken chorioallantoic membrane assays. Treatment of cells with PF-562,271 or knock-down of FAK by siRNA is observed to increase cell-cell adhesion strength
  • 体内研究:
    PF-562,271 (33 mg/kg, p.o.) inhibits FAK phosphorylation in tumors in a dose- and time-dependent manner in tumor-bearing mice. FAK phosphorylation inhibition relative to total blood concentration of PF-562,271 results in a calculated EC50 of 93 ng/mL. PF-562,271 (25 mg/kg, p.o.) induces apoptosis 2-fold greater in treated tumors compared with vehicle-treated control tumors on day 3. PF-562,271 (33 mg/kg, p.o.) and dasatinib extensively inhibit the movement of tumor cells in the animals. Inhibition of FAK kinase activity following treatment with PF-562,271 results in altered E-cadherin dynamics in vivo
  • 参考文献:
    1. Roberts WG, et al. Antitumor activity and pharmacology of a selective focal adhesion kinase inhibitor, PF-562,271. Cancer Res, 2008, 68(6), 1935-1944. 2. Lim ST, et al. FERM control of FAK function: implications for cancer therapy. Cell Cycle, 2008, 7(15), 2306-2314. 3. Canel M, et al. Quantitative in vivo imaging of the effects of inhibiting integrin signaling via Src and FAK on cancer cell movement: effects on E-cadherin dynamics. Cancer Res, 2010, 70(22), 9413-9422.
  • 溶解性: soluble  in  DMSO
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 1.502 ml 7.511 ml 15.023 ml
    5 mM 0.3 ml 1.502 ml 3.005 ml
    10 mM 0.15 ml 0.751 ml 1.502 ml
    50 mM 0.03 ml 0.15 ml 0.3 ml
  • 注意:部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。
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