Antibodies
MK-0752
- 貨號 Cat. No.
- S2660
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
MK-0752
Catalog No.S2660
MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM. Phase 1/2.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM. Phase 1/2. | |||||
|---|---|---|---|---|---|---|
| Targets | γ-secretase | |||||
| IC50 | 5 nM [1] | |||||
| In vitro | MK-0752 is identified as a moderately potent γ-secretase inhibitor, which reduces Aβ40 in a dose-dependent manner with an IC50 of 5 nM in human SH-SY5Y cells. [1] In vitro, MK-0752 blocks Notch-intracellular domain (ICD) cleavage and its subsequent nuclear translocation. [2] | |||||
| In vivo | MK-0752 (240 mg/kg) reduces the generation of newly produced Aβ with 90% decrease of AUV in the brain of rhesus monkeys. In addition, MK-0752 treatment increases levels of Aβ 1-14, Aβ 1-15, and Aβ 1-16 , while decreases levels of Aβ 1-17. [1] In guinea-pigs, oral administration of MK-0752 (10 mg/kg -30 mg/kg) results in the dose-dependent reduction of Aβ40 in plasma, brain and cerebrospinal fluid (CSF) with IC50 of 440 nM in brain. [2] | |||||
| Features | A moderately potent γ-secretase inhibitor. | |||||
Protocol(Only for Reference)
Animal Study: [1]
| Animal Models | Cisterna Magna Ported (CMP) Rhesus Monkey Model. |
|---|---|
| Dosages | ≤240 mg/kg |
| Administration | Administered via p.o. |
| Solubility | 30% propylene glycol, 5% Tween 80, 65% D5W, 30 mg/mL |
References
Clinical Trial Information( data from http://clinicaltrials.gov)
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT00572182 | Terminated | Brain and Central Nervous System Tumors | Pediatric Brain Tumor Consortium|National Cancer Institute (NCI) | 2008-07 | Phase 1 |
| NCT00803894 | Completed | Healthy | Merck | 2008-12 | Phase 1 |
| NCT01098344 | Recruiting | Pancreatic Cancer | Cancer Research UK | 2010-04 | Phase 1|Phase 2 |
| NCT01243762 | Terminated | Neoplasms Malignant | Merck | 2010-11 | Phase 1 |
| NCT01295632 | Recruiting | Advanced Cancer | Merck | 2011-02 | Phase 1 |
Chemical Information
| Molecular Weight (MW) | 442.9 |
|---|---|
| Formula | C21H21ClF2O4S |
| CAS No. | 471905-41-6 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 89 mg/mL (200 mM) |
|---|---|---|---|
| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | 45 mg/mL (101 mM) | ||
| In vivo | 30% propylene glycol, 5% Tween 80, 65% D5W, | 30 mg/mL | |
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | 3-((1r,4s)-4-(4-chlorophenylsulfonyl)-4-(2,5-difluorophenyl)cyclohexyl)propanoic acid |
|---|
Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
|---|---|---|---|---|
| Mass(mg) | 0.4429 | 4.429 | 8.858 | 13.287 |
