MK-0752

Catalog No.S2660 Batch:S266001

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Technical Data

Formula

C21H21ClF2O4S
Molecular Weight 442.9 CAS No. 471905-41-6
Solubility (25°C)* In vitro DMSO 89 mg/mL (200.94 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 40% PEG 300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO Corn oil
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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
Aβ [1]
(in human SH-SY5Y cells)
5 nM
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 (from reference)

Animal Study:[1]
  • Animal Models

    Cisterna Magna Ported (CMP) Rhesus Monkey Model.

  • Dosages

    ≤240 mg/kg

  • Administration

    Administered via p.o.

Customer Product Validation

Data from [Data independently produced by Oncotarget, 2014, 5(2), 363-74]

Data from [Data independently produced by , , Neoplasia, 2018, 21(1):93-105]

Data from [Data independently produced by , , Cancer Biol Ther, 2014, 15(5):633-42]

Data from [Data independently produced by , , Oncol Lett, 2016, 12(4):2900-2905]

Selleck's MK-0752 has been cited by 23 publications

Distinct pathways drive anterior hypoblast specification in the implanting human embryo [ Nat Cell Biol, 2024, 26(3):353-365] PubMed: 38443567
Simultaneous Inhibition of Ceramide Hydrolysis and Glycosylation Synergizes to Corrupt Mitochondrial Respiration and Signal Caspase Driven Cell Death in Drug-Resistant Acute Myeloid Leukemia [ Cancers (Basel), 2023, 15(6)1883] PubMed: 36980769
In vitro antineoplastic effects of MK0752 in HPV-positive head and neck squamous cell carcinoma [ J Cancer Res Clin Oncol, 2023, 149(16):14691-14699] PubMed: 37587308
Prediction of drug candidates for clear cell renal cell carcinoma using a systems biology-based drug repositioning approach [ EBioMedicine, 2022, 78:103963] PubMed: 35339898
Establishment and characterization of immortalized sweat gland myoepithelial cells [ Sci Rep, 2022, 12(1):7] PubMed: 34997030
Delta/Jagged-mediated Notch signaling induces the differentiation of agr2-positive epidermal mucous cells in zebrafish embryos [ PLoS Genet, 2021, 17(12):e1009969] PubMed: 34962934
PLK1 and NOTCH Positively Correlate in Melanoma and their Combined Inhibition Results in Synergistic Modulations of Key Melanoma Pathways [ Mol Cancer Ther, 2020, molcanther.0654.2020] PubMed: 33177155
A novel human colon signet-ring cell carcinoma organoid line: establishment, characterization and application [ Carcinogenesis, 2020, 41(7):993-1004] PubMed: 31740922
DRUGPATH - a novel bioinformatic approach identifies DNA-damage pathway as a regulator of size maintenance in human ESCs and iPSCs [ Sci Rep, 2019, 9(1):1897] PubMed: 30760778
IL6 blockade potentiates the anti-tumor effects of γ-secretase inhibitors in Notch3-expressing breast cancer. [ Cell Death Differ, 2018, 25(2):330-339] PubMed: 29027990

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.