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。
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.
80 Mm citrate buffer solution(pH 7)
0.1 nM- 1 μM
20-25 mg/kg 口服饲喂
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km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。
[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
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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