MK-0752

ArtNr	S2660-1000
Hersteller	Selleckchem
CAS-Nr.	471905-41-6
Menge	1 g
Quantity options	10 mg 1 g 10 g 10 mM/1 ml 200 mg 5 mg 50 mg 5 g
Kategorie	Oncology Inhibitors & Compound Libraries Small Molecules By Organ Breast Cancer
Typ	Inhibitors
Specific against	other
Smiles	C1CC(CCC1CCC(=O)O)(C2=C(C=CC(=C2)F)F)S(=O)(=O)C3=CC=C(C=C3)Cl
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	gamma-secretase,Gamma-secretase
Similar products	MK-0752
Lieferbar
Storage Conditions	2 years -80 in solvent
Molecular Weight	442, 9
Administration	Administered via p.o.
Animal Models	Cisterna Magna Ported (CMP) Rhesus Monkey Model.
Clinical Trials	MK-0752 study has been completed in Phase I clinical trials in patients with Metastatic or Locally Advanced Breast Cancer and Other Solid Tumors.
Dosages	<=240 mg/kg
Formulation	MK-0752 is dissolved in water.
IC50	5 nM [1], 5 nM [1], 5 nM [1], 5 nM [1], 5 nM [1], 5 nM [1]
In vitro	MK-0752 is identified as a moderately potent gamma-secretase inhibitor, which reduces Abeta40 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 Abeta with 90% decrease of AUV in the brain of rhesus monkeys. In addition, MK-0752 treatment increases levels of Abeta 1â€“14, Abeta 1â€“15, and Abeta 1â€“16 , while decreases levels of Abeta 1â€“17. [1], In guinea-pigs, oral administration of MK-0752 (10 mg/kg -30 mg/kg) results in the dose-dependent reduction of Abeta40 in plasma, brain and cerebrospinal fluid (CSF) with IC50 of 440 nM in brain. [2]
Solubility (25C)	DMSO 89 mg/mL, Water <1 mg/mL, Ethanol 45 mg/mL
Information	MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM. Phase 1/2.
Chemical Name	3-((1r, 4s)-4-(4-chlorophenylsulfonyl)-4-(2, 5-difluorophenyl)cyclohexyl)propanoic acid
Features	MK-0752 is a moderately potent gamma-secretase inhibitor.

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S2660-1000-datasheet.pdf

S2660-1000-safety-datasheet.pdf