« Back
Home /
MK-0752

MK-0752

Item no.	S2660-10000
Manufacturer	Selleckchem
CASRN	471905-41-6
Amount	10 g
Quantity options	10 mg 1 g 10 g 10 mM/1 ml 200 mg 5 mg 50 mg 5 g
Category	Oncology Inhibitors & Compound Libraries Small Molecules By Organ Breast Cancer
Type	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
Available
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.

Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.

All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.

Request Data Sheet

S2660-10000-datasheet.pdf

S2660-10000-safety-datasheet.pdf