GW280264X [866924-39-2]

Referência HY-115670-25mg

Tamanho : 25mg

Marca : MedChemExpress

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Description

GW280264X is the mixed ADAM10/TACE (ADAM17) metalloproteinases inhibitor. GW280264X potently blocks TACE (ADAM17) and ADAM10 with IC50s of 8.0 nM and 11.5 nM, respectively[1]. ADAM10 and 17 modulate the immunogenicity of glioblastoma-initiating cells[2].

IC50 & Target[1]

ADAM17

8 nM (IC50)

ADAM10

11.5 nM (IC50)

In Vitro

The proliferation of GS-7 cells was significantly reduced upon treatment with GW280264X or ADAM10/17 co-knockdown[2].

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

Cell Viability Assay[2]

Cell Line: Glioblastoma-initiating cells (GIC) GS-7 cells
Concentration: 0.1, 1, and 3 µM
Incubation Time: 48 hours
Result: Proliferation of GIC is inhibited through inhibition of ADAM10 and ADAM17.
In Vivo

Pharmacological inhibition of ADAM10 and ADAM17 improves functional recovery after spinal cord injury (SCI)[3].

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

Animal Model: C57BL/6 mice[3]
Dosage: 100  µg/kg
Administration: I.p. injected; every day for one week starting 4 h post-surgery
Result: Showed significantly improved functional recovery compared to the control group.
Masse moléculaire

575.72

Formule

C28H41N5O6S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(OCC1=CC=CC=C1)NCCCC[C@H](NC([C@H](CC(C)C)[C@@H](N(C=O)O)CCC)=O)C(NC2=NC=CS2)=O

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvant et solubilité
In Vitro: 

DMSO : 100 mg/mL (173.70 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 1.7370 mL 8.6848 mL 17.3696 mL
5 mM 0.3474 mL 1.7370 mL 3.4739 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.

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    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (3.61 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Pureté et documentation
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