MK-0752

MK0752,MK 0752

MK-0752是一种适度有效的γ-secretase(γ-分泌酶)抑制剂,降低Aβ40产量,IC50为5 nM。

目录号
EY0340
EY0340
EY0340
EY0340
纯度
99.23%
99.23%
99.23%
99.23%
规格
1 mg
5 mg
10 mg
50 mg
原价
950
1600
2500
6800
售价
950
1600
2500
6800
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

    MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM. Phase 1/2.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

    ≤240 mg/kgp.o.

  • 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] Cook JJ, et al. J Neurosci, 2010, 30(19), 6743-6750.
    [2] I Brana,et al. A parallel-arm phase I trial of the humanised anti-IGF-1R antibody dalotuzumab in combination with the AKT inhibitor MK-2206, the mTOR inhibitor ridaforolimus, or the NOTCH inhibitor MK-0752, in patients with advanced solid tumours.Br J Cancer. 2014 Nov 11; 111(10): 1932–1944. Published online 2014 Oct 7. doi: 10.1038/bjc.2014.497.

    分子式
    C21H21ClF2O4S
    分子量
    442.9
    CAS号
    471905-41-6
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    ≥89 mg/mL
    Water
    <1 mg/mL
    Ethanol
    ≥45 mg/mL

    体内溶解度

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

    NCT00756717 Breast Cancer Drug: MK-0752 Loyola University|Merck Sharp & Dohme Corp. 2008-05-01 2015-04-01
    NCT00645333 Metastatic Breast Cancer Drug: MK-0752, Docetaxel, Pegfilgrastim University of Michigan Cancer Center|Baylor College of Medicine|Ohio State University|Dana-Farber Cancer Institute|Weill Medical College of Cornell University|Merck Sharp & Dohme Corp. Phase 1|Phase 2 2008-03-01 2014-02-24
    NCT00572182 Brain and Central Nervous System Tumors Drug: MK-0752 Pediatric Brain Tumor Consortium|National Cancer Institute (NCI) Phase 1 2008-07-01 2012-03-02
    NCT01295632 Advanced Cancer Drug: ridaforolimus|Drug: MK-0752|Drug: MK-2206 Merck Sharp & Dohme Corp. Phase 1 2011-02-01 2015-08-26
    NCT01243762 Neoplasms Malignant Drug: dalotuzumab + MK-2206|Drug: dalotuzumab + MK-0752|Drug: Dalotuzumab + MK-8669 (ridaforolimus) Merck Sharp & Dohme Corp. Phase 1 2010-11-01 2015-01-29
    NCT00803894 Healthy Drug: MK0752|Drug: Comparator: MK0752.|Drug: Comparator: Placebo Merck Sharp & Dohme Corp. Phase 1 2008-12-01 2016-06-16
    NCT01098344 Pancreatic Cancer Drug: Notch signaling pathway inhibitor MK0752|Drug: gemcitabine hydrochloride|Other: imaging biomarker analysis|Other: laboratory biomarker analysis|Other: pharmacological study Cancer Research UK Phase 1 2010-04-01 2015-10-13
    NCT00106145 Advanced Breast Cancer|Other Solid Tumors Drug: Comparator: MK0752, Notch Inhibitor|Drug: Comparator: MK0752, Notch Inhibitor - 450 mg|Drug: Comparator: MK0752, Notch Inhibitor - 3 days on, 4 off|Drug: Comparator: MK0752, Notch Inhibitor - 1 day on, 6 off|Drug: Comparator: MK0752, Notch Inhibitor - 3 days on, 4 off 350 mg Merck Sharp & Dohme Corp. Phase 1 2005-04-01 2015-01-29
    NCT00100152 Leukemia, Lymphoblastic, Acute, T-cell|Myelogenous Leukemia|Chronic Lymphocytic Leukemia|Myelodysplastic Syndromes Drug: MK0752, (Notch Inhibitor) Merck Sharp & Dohme Corp. Phase 1 2005-02-01 2015-05-25

    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。

  • 相关化合物库

  • 使用AMQUAR产品发表文献后请联系我们

相关推荐

X
  • 联系人 :
  • 收件地址 :
  • 电话号码 :
  • 单位名称 :
  • 产品货号 :
  • 产品规格 :
  • 发票抬头以及单位税号 :