product name MK-0752
Description: MK0752 is a synthetic small molecule with potential antineoplastic activity. MK-0752 is a moderately potent γ-secretase inhibitor with IC50 of 5 nM. Inhibition of the Notch signaling pathway by MK-0752 may result in induction of growth arrest and apoptosis in tumor cells in which the Notch signaling pathway is overactivated. The Notch signaling pathway plays an important role in cell-fate determination, cell survival, and cell proliferation.
References: J Neurosci. 2010 May 12;30(19):6743-50; Cancer Res. 2010 Jan 15;70(2):709-18.
442.9
Formula
C21H21ClF2O4S
CAS No.
471905-41-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 89 mg/mL (200.9 mM)
Water: <1 mg/mL
Ethanol: 45 mg/mL (101.6 mM)
Solubility (In vivo)
30% propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19401298
| In Vitro |
In vitro activity: 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. In vitro, MK-0752 blocks Notch-intracellular domain (ICD) cleavage and its subsequent nuclear translocation. Kinase Assay: Cell Assay: As a moderately potent γ-secretase inhibitor, MK-0752 inhibited the production of Aβ40 in a dose-dependent manner with an IC50 of 5 nM in human SH-SY5Y cells. |
|---|---|
| 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. 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. |
| Animal model | Cisterna Magna Ported (CMP) Rhesus Monkey Model. |
| Formulation & Dosage | Dissolved in water; ≤240 mg/kg; Oral gavage |
| References | J Neurosci. 2010 May 12;30(19):6743-50; Cancer Res. 2010 Jan 15;70(2):709-18. |
Related Posts
product name MK-0752
Description: MK0752 is a synthetic small molecule with potential antineoplastic activity. MK-0752 is a moderately potent γ-secretase inhibitor with IC50 of 5 nM. Inhibition of the Notch signaling pathway by MK-0752 may result in induction of growth arrest and apoptosis in tumor cells in which the Notch signaling pathway is overactivated. The Notch signaling pathway plays an important role in cell-fate determination, cell survival, and cell proliferation.
References: J Neurosci. 2010 May 12;30(19):6743-50; Cancer Res. 2010 Jan 15;70(2):709-18.
442.9
Formula
C21H21ClF2O4S
CAS No.
471905-41-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 89 mg/mL (200.9 mM)
Water: <1 mg/mL
Ethanol: 45 mg/mL (101.6 mM)
Solubility (In vivo)
30% propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19401298
| In Vitro |
In vitro activity: 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. In vitro, MK-0752 blocks Notch-intracellular domain (ICD) cleavage and its subsequent nuclear translocation. Kinase Assay: Cell Assay: As a moderately potent γ-secretase inhibitor, MK-0752 inhibited the production of Aβ40 in a dose-dependent manner with an IC50 of 5 nM in human SH-SY5Y cells. |
|---|---|
| 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. 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. |
| Animal model | Cisterna Magna Ported (CMP) Rhesus Monkey Model. |
| Formulation & Dosage | Dissolved in water; ≤240 mg/kg; Oral gavage |
| References | J Neurosci. 2010 May 12;30(19):6743-50; Cancer Res. 2010 Jan 15;70(2):709-18. |