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PD0325901

PD0325901是一种选择性的,ATP非竞争性的MEK抑制剂,IC50为0.33 nM,对ERK1和ERK2磷酸化抑制作用比CI-1040强500倍左右。

目录号
EY1046
EY1046
EY1046
EY1046
纯度
99.07%
99.07%
99.07%
99.07%
规格
5 mg
10 mg
25 mg
50 mg
原价
420
800
1,420.00_
2000
售价
420
800
1,420.00_
2000
库存
现货
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    PD 0325901 is a potent MEK-1 and Mek-2 inhibitor that suppresses phosphorylation of ERK1/2 in murine colon 26 tumors with an IC50 value of 0.33 nM. As a result of this inhibition, PD 0325901 modulates regulators of cell growth and apoptosis at the protein level. Inhibits MEK activity in mouse colon 26 cells (IC50 = 0.33 nM). Inhibits the growth of melanoma cell lines in vitro and in vivo; induces G1-phase cell cycle arrest and apoptosis in a mouse xenograft model. Studies on M14 models indicate that PD 0325901 inhibits the phosphorylation of ERK and its downstream target ribosomal S6 kinase in a dose-dependent manner. Also inhibits production of proangiogenic cytokines such as VEGF.

  • 体外研究

  • 体内研究

    80 Mm citrate buffer solution(pH 7)

  • 激酶实验

  • 细胞实验

    0.1 nM- 1 μM

  • 动物实验

    20-25 mg/kg 口服饲喂

  • 不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 AKm系数


    例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。


  • 参考文献

    [1] Barrett SD, et al. Bioorg Med Chem Lett, 2008, 18(24), 6501-6504.
    [2] Dorsam, R.T. and Gutkind, J.S. 2007. Nat. Rev. Cancer. 7: 79-94.
    [3] Ying, Q.L., et al. 2008. Nature. 453: 519-523.
    [4] Ciuffreda, L., et al. 2009. Neoplasia. 11: 720-731.

    分子式
    C16H14F3IN2O4
    分子量
    482.19
    CAS号
    391210-10-9
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    96 mg/mL
    Water
    Insoluble
    Ethanol
    40 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT02022982 KRAS Mutant Non-Small Cell Lung Cancer|Solid Tumors Drug: Palbociclib|Drug: PD-0325901 Dana-Farber Cancer Institute Phase 1|Phase 2 2014-01-01 2016-12-15
    NCT02096471 Neurofibromatosis Type 1 and Growing or Symptomatic, Inoperable PN Drug: PD-0325901 University of Alabama at Birmingham Phase 2 2014-06-01 2016-12-14
    NCT00174369 Carcinoma, Non-Small-Cell Lung Drug: PD-0325901 Pfizer Phase 2 2005-11-01 2009-03-16
    NCT02297802 Prior Treatment With PD-0325901 With Ongoing Clinical Response Drug: PD-0325901 Sharp HealthCare Phase 1 2013-06-01 2014-11-24
    NCT02039336 Colorectal Cancer Drug: Dacomitinib|Drug: PD-0325901|Drug: Irinotecan|Drug: Docetaxel|Drug: Capecitabine The Netherlands Cancer Institute|Pfizer Phase 1|Phase 2 2014-01-01 2016-11-10
    NCT00147550 Melanoma|Colonic Neoplasms|Breast Neoplasms Drug: PD-0325901 Pfizer Phase 1|Phase 2 2004-02-01 2013-09-11
    NCT02510001 Solid Tumour|Colorectal Cancer Drug: PF-02341066|Drug: PD-0325901|Drug: Binimetinib University of Oxford|Queen's University, Belfast|Oxford University Hospitals NHS Trust|Velindre NHS Trust|University Hospital, Antwerp|Hospital Vall d'Hebron|Hopital St Antoine, Paris|European Georges Pompidou Hospital|Pfizer|University of Turin, Italy|Belfast Health and Social Care Trust|Beaumont Hospital|European Commission|Array BioPharma|Q2 solutions|Covance|QPS Holdings Phase 1 2014-11-01 2016-08-31
    NCT01347866 Advanced Cancer Drug: PF-05212384|Drug: PD-0325901|Drug: PF-05212384|Drug: irinotecan Pfizer Phase 1 2011-10-01 2016-01-13

    注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。

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