MK-0752
Based on 14 publication(s) in Google Scholar
MK-0752 is a potent, orally active and specific γ-secretase inhibitor, showing dose-dependent reduction of Aβ40 with an IC50 of 5 nM in human SH-SY5Y cells. MK-0752 crosses the blood-brain barrier. MK-0752 reduces newly generated CNS Aβ in vivo.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.02%
- No. CAS: 471905-41-6
- Fòrmula: C21H21ClF2O4S
- Peso molecular:442.90
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) MK-0752
More- Nat Biotechnol. 2024 Nov 25. [Abstract]
- Nat Mater. 2025 Feb 17. [Abstract]
- EMBO Mol Med. 2017 Jul;9(7):950-966. [Abstract]
- Biofactors. 2025 Jan-Feb;51(1):e2091. [Abstract]
- Int J Mol Sci. 2022 May 26;23(11):5980. [Abstract]
- Cancers (Basel). 2024 Jun 10;16(12):2184. [Abstract]
- J Cell Physiol. 2021 Feb;236(2):1237-1251. [Abstract]
- J Biol Chem. 2019 Jul 19;294(29):11276-11285. [Abstract]
- J Cell Sci. 2021 Oct 8;jcs.258432. [Abstract]
- Front Biosci (Landmark Ed). 2025 Apr 23;30(4):37430. [Abstract]
- Mol Biol Rep. 2024 Nov 8;51(1):1134. [Abstract]
- J Recept Signal Transduct Res. 2021 Oct;41(5):457-465. [Abstract]
- Reprod Fertil Dev. 2019 May;31(6):1091-1103. [Abstract]
- Andrologia. 2019 Nov;51(10):e13413. [Abstract]
Customer Validation & Images
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WB
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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WB
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WB
Actividad biológica
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Cell Line
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Type | Value | Description | References |
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| MCF7 | IC50 |
5 nM
Compound: 13; MK-0752
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Inhibition of gamma secretase in human MCF7 cells assessed as reduction in amyloid beta 40 after 3 days by Western blot analysis
Inhibition of gamma secretase in human MCF7 cells assessed as reduction in amyloid beta 40 after 3 days by Western blot analysis
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[PMID: 27045975] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male rhesus monkeys[1]
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Dosage:60-240 mg/kg
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Administration:P.o.
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Result:Generation of new Aβ was partially blocked with administration of 60 mg/kg, and nearly completely blocked at the 240 mg/kg dose as indicated by the dose-dependent decrease in the amount of 13C6-leucine-labeled Aβ.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 471905-41-6
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Appearance Solid
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Peso molecular 442.90
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Fòrmula C21H21ClF2O4S
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Color White to off-white
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SMILES
O=S([C@@]1(C2=C(C=CC(F)=C2)F)CC[C@@H](CCC(O)=O)CC1)(C3=CC=C(Cl)C=C3)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (14)
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Journal Impact Factor
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Most Recent
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Nat Biotechnol
Intravenous administration of blood-brain barrier-crossing conjugates facilitate biomacromolecule transport into central nervous system. [Abstract]2024 Nov 25. PMID: 39587229 -
Nat Mater
Blood-brain-barrier-crossing lipid nanoparticles for mRNA delivery to the central nervous system. [Abstract]2025 Feb 17. PMID: 39962245 -
EMBO Mol Med
γ-Secretase inhibitors in cancer clinical trials are pharmacologically and functionally distinct. [Abstract]2017 Jul;9(7):950-966. PMID: 28539479
MK-0752 purchased from MedChemExpress. Usage Cited in: EMBO Mol Med. 2017 Jul;9(7):950-966. [Abstract]
IC50 curves of MK-0752 (10-4-104 nM) on cNOTCHsub.
MK-0752 purchased from MedChemExpress. Usage Cited in: EMBO Mol Med. 2017 Jul;9(7):950-966. [Abstract]
Dose responses of cAPPC100sub and full-length APP cleavage to MK-0752 (10-4-104 nM).
MK-0752 purchased from MedChemExpress. Usage Cited in: EMBO Mol Med. 2017 Jul;9(7):950-966. [Abstract]
MK-0752 (100 nM-12.5 μM) strongly decreased NICD levels in the breast cancer line MDA-MB-231.
MK-0752 purchased from MedChemExpress. Usage Cited in: EMBO Mol Med. 2017 Jul;9(7):950-966. [Abstract]
MK-0752 (0.5-12.5 μM) inhibited APP-CTF process in MDA-MB-231 cells in a dose-dependent manner.
MK-0752 purchased from MedChemExpress. Usage Cited in: EMBO Mol Med. 2017 Jul;9(7):950-966. [Abstract]
Absolute viable cell counts of mammospheres from MDA-MB-231 and MDA-MB-468 cell lines treated with MK-0752 (10 μM; 7 d).
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Biofactors
2025 Jan-Feb;51(1):e2091. PMID: 38994725 -
Int J Mol Sci
Gamma Secretase Inhibitors as Potential Therapeutic Targets for Notch Signaling in Uterine Leiomyosarcoma. [Abstract]2022 May 26;23(11):5980. PMID: 35682660 -
Cancers (Basel)
Combined Treatment of Uterine Leiomyosarcoma with Gamma Secretase Inhibitor MK-0752 and Chemotherapeutic Agents Decreases Cellular Invasion and Increases Apoptosis. [Abstract]2024 Jun 10;16(12):2184. PMID: 38927890 -
J Cell Physiol
Vitamin C alleviates the senescence of periodontal ligament stem cells through inhibition of Notch3 during long-term culture. [Abstract]2021 Feb;236(2):1237-1251. PMID: 32662081 -
J Biol Chem
Individual and combined presenilin 1 and 2 knockouts reveal that both have highly overlapping functions in HEK293T cells. [Abstract]2019 Jul 19;294(29):11276-11285. PMID: 31167792 -
J Cell Sci
2021 Oct 8;jcs.258432. PMID: 34622921 -
Front Biosci (Landmark Ed)
Macrophage Notch1 Participates in LPS-Induced Acute Lung Injury via Regulating CCR5 Expression in Mice. [Abstract]2025 Apr 23;30(4):37430. PMID: 40302346 -
Mol Biol Rep
2024 Nov 8;51(1):1134. PMID: 39514048 -
J Recept Signal Transduct Res
Function and mechanism exploration of zinc finger protein 64 in lung adenocarcinoma cell growth and metastasis. [Abstract]2021 Oct;41(5):457-465. PMID: 33054540 -
Reprod Fertil Dev
2019 May;31(6):1091-1103. PMID: 30827331 -
Andrologia
2019 Nov;51(10):e13413. PMID: 31523838
MK-0752 purchased from MedChemExpress. Usage Cited in: Andrologia. 2019 Nov;51(10):e13413. [Abstract]
MK-0752 regulated the expression of cell proliferation-related genes at the mRNA and protein levels. The relative protein expression of p27 and p21Waf1/Cip1 in TM3 Leydig cells after treatment with 25 μM MK-0752 respectively. The representative Western blots for p27 and p21Waf1/Cip1 after treatment with MK-0752.
Solvente y solubilidad
DMSO : ≥ 100 mg/mL (225.78 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Ethanol : 10 mg/mL (22.58 mM; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.64 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.64 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Cook JJ, et al. Acute gamma-secretase inhibition of nonhuman primate CNS shifts amyloid precursor protein (APP) metabolism from amyloid-beta production to alternative APP fragments without amyloid-beta rebound. J Neurosci. 2010;30(19):6743-6750. [Content Brief]
[2]. Krop I, et al. Phase I pharmacologic and pharmacodynamic study of the gamma secretase (Notch) inhibitor MK-0752 in adult patients with advanced solid tumors. J Clin Oncol. 2012;30(19):2307-2313. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| Ethanol / DMSO | 1 mM | 2.2578 mL | 11.2892 mL | 22.5785 mL | 56.4462 mL |
| 5 mM | 0.4516 mL | 2.2578 mL | 4.5157 mL | 11.2892 mL | |
| 10 mM | 0.2258 mL | 1.1289 mL | 2.2578 mL | 5.6446 mL | |
| 15 mM | 0.1505 mL | 0.7526 mL | 1.5052 mL | 3.7631 mL | |
| 20 mM | 0.1129 mL | 0.5645 mL | 1.1289 mL | 2.8223 mL | |
| DMSO | 25 mM | 0.0903 mL | 0.4516 mL | 0.9031 mL | 2.2578 mL |
| 30 mM | 0.0753 mL | 0.3763 mL | 0.7526 mL | 1.8815 mL | |
| 40 mM | 0.0564 mL | 0.2822 mL | 0.5645 mL | 1.4112 mL | |
| 50 mM | 0.0452 mL | 0.2258 mL | 0.4516 mL | 1.1289 mL | |
| 60 mM | 0.0376 mL | 0.1882 mL | 0.3763 mL | 0.9408 mL | |
| 80 mM | 0.0282 mL | 0.1411 mL | 0.2822 mL | 0.7056 mL | |
| 100 mM | 0.0226 mL | 0.1129 mL | 0.2258 mL | 0.5645 mL |
MK-0752 Related Classifications
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