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。
MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM. Phase 1/2.
≤240 mg/kgp.o.
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] 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
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。
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