2. Neuronal Signaling Stem Cell/Wnt
  3. γ-secretase
  4. MRK-560

MRK-560 is an orally active, brain barrier-penetrating γ-Secretase inhibitor, can potently reduce Aβ peptide in rat brain and cerebrospinal fluid. MRK-560 also decreases mutant NOTCH1 processing by selectively inhibiting PSEN1. MRK-560 can be used in studies of Alzheimer's disease and T-cell acute lymphoblastic leukaemia (T-ALL).

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MRK-560 Chemical Structure

MRK-560 Chemical Structure

CAS No. : 677772-84-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 80 In-stock
Solution
10 mM * 1 mL in DMSO USD 80 In-stock
Solid
1 mg USD 28 In-stock
5 mg USD 70 In-stock
10 mg USD 110 In-stock
25 mg USD 220 In-stock
50 mg USD 360 In-stock
100 mg USD 580 In-stock
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Based on 1 publication(s) in Google Scholar

MRK-560 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

MRK-560 is an orally active, brain barrier-penetrating γ-Secretase inhibitor, can potently reduce Aβ peptide in rat brain and cerebrospinal fluid. MRK-560 also decreases mutant NOTCH1 processing by selectively inhibiting PSEN1. MRK-560 can be used in studies of Alzheimer's disease and T-cell acute lymphoblastic leukaemia (T-ALL)[1][2].

IC50 & Target

γ-secretase, PSEN1[1][2].
In Vitro

MRK-560 (30, 100, 300, 1000 nM; 15days) blocks mutant NOTCH1 receptor signaling in human T-ALL cell lines[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

MRK-560 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: HPB-ALL, DND-41, and Jurkat cells
Concentration: 30, 100, 300, 1000 nM
Incubation Time: 15 days
Result: Reduced NICD1 generation in cells and resulted in a dose-dependent decrease of proliferation in HPB-ALL and DND-41, which depend on NOTCH signaling for their survival.
In Vivo

MRK-560 (15.54 mg/kg; S.C.; single daily for 14 days) shows strong antileukemic effects on T-ALL model[1].
MRK-560 (1, 3, 10, 30, 100 mg/kg; p.o.; single) shows good blood-brain barrier permeability in a dose-dependent manner in rats[2].

MRK-560 (1, 3, 10, 30, 100 mg/kg; p.o.; single) inhibits the production of Aβ levels in brain and cerebrospinal fluid[2].
MRK-560 (1 mg/kg; p.o.; single) shows a good bioavailability of 70 to 90%, and Tmax is 12 h[2].
MRK-560 (1 mg/kg; i.v.; single) is suitable for once-a-day dosing (with a low plasma clearance and a half-life of more than 15 h)[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Tg (HLA-DRB1) 31Dmz/Szj (NSG) mice (T-ALL (T cell acute lymphoblastic leukemia) model)[1].
Dosage: 15.54 mg/kg
Administration: Subcutaneous injection; single daily for 14 days.
Result: Resulted in strong antileukemic effects and improved median survival to 30 days compared to 18 days in vehicle-treated mice.
Animal Model: Male Sprague-Dawley rats (250-300 g)[2].
Dosage: 1, 3, 10, 30, 100 mg/kg
Administration: Oral administration; single (experiment is performed 8 h later)
Result: Increased the plasma and brain concentrations in a dose-dependent manner.
Reduced (dose-dependent) both brain and CSF Aβ levels, with essentially complete inhibition of the production of both peptides being observed at a dose of 100 mg/kg.
Animal Model: Male Sprague-Dawley rats (250-300 g)[2].
Dosage: 1 mg/kg
Administration: Intravenously and orally administration; single.
Result: Showed Tmax after the oral dose was 12 h,and bioavailability was 70 to 90%.
Revealed a low plasma clearance of less than 5 mL/min/kg with a volume of distribution of approximately 6 L/kg, which translated to a long half-life of more than 15 h.
Molecular Weight

517.92

Formula

C19H17ClF5NO4S2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=S([C@]1(C2=C(C=CC(F)=C2)F)CC[C@H](NS(C(F)(F)F)(=O)=O)CC1)(C3=CC=C(Cl)C=C3)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (193.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9308 mL 9.6540 mL 19.3080 mL
5 mM 0.3862 mL 1.9308 mL 3.8616 mL
View the 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.83 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (4.83 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.51%

COA (253 KB) LCMS (88 KB)

Handling Instructions (2659 KB)
References

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9308 mL 9.6540 mL 19.3080 mL 48.2700 mL
5 mM 0.3862 mL 1.9308 mL 3.8616 mL 9.6540 mL
10 mM 0.1931 mL 0.9654 mL 1.9308 mL 4.8270 mL
15 mM 0.1287 mL 0.6436 mL 1.2872 mL 3.2180 mL
20 mM 0.0965 mL 0.4827 mL 0.9654 mL 2.4135 mL
25 mM 0.0772 mL 0.3862 mL 0.7723 mL 1.9308 mL
30 mM 0.0644 mL 0.3218 mL 0.6436 mL 1.6090 mL
40 mM 0.0483 mL 0.2414 mL 0.4827 mL 1.2068 mL
50 mM 0.0386 mL 0.1931 mL 0.3862 mL 0.9654 mL
60 mM 0.0322 mL 0.1609 mL 0.3218 mL 0.8045 mL
80 mM 0.0241 mL 0.1207 mL 0.2414 mL 0.6034 mL
100 mM 0.0193 mL 0.0965 mL 0.1931 mL 0.4827 mL
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MRK-560 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MRK-560677772-84-8MRK560MRK 560γ-secretaseGamma secretaseAβ peptidesAlzheimer’s diseaseT-ALLHPB-ALLDND-41Jurkat cellsInhibitorinhibitorinhibit

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