2. Metabolic Enzyme/Protease
  3. MMP
  4. GW280264X

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. ADAM10 and 17 modulate the immunogenicity of glioblastoma-initiating cells.

For research use only. We do not sell to patients.

GW280264X Chemical Structure

GW280264X Chemical Structure

CAS No. : 866924-39-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 545 In-stock
Solution
10 mM * 1 mL in DMSO USD 545 In-stock
Solid
1 mg USD 204 In-stock
5 mg USD 430 In-stock
10 mg USD 750 In-stock
25 mg USD 1580 In-stock
50 mg   Get quote  
100 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 3 publication(s) in Google Scholar

GW280264X Related Antibodies

Top Publications Citing Use of Products

View All MMP Isoform Specific Products:

View All Isoforms
MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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.

GW280264X Related Antibodies

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.
Molecular Weight

575.72

Formula

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
Shipping

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

DMSO : 125 mg/mL (217.12 mM; ultrasonic and warming and heat to 60°C; 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
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    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.

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: 98.28%

COA (248 KB) HNMR (311 KB) LCMS (95 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 1.7370 mL 8.6848 mL 17.3696 mL 43.4239 mL
5 mM 0.3474 mL 1.7370 mL 3.4739 mL 8.6848 mL
10 mM 0.1737 mL 0.8685 mL 1.7370 mL 4.3424 mL
15 mM 0.1158 mL 0.5790 mL 1.1580 mL 2.8949 mL
20 mM 0.0868 mL 0.4342 mL 0.8685 mL 2.1712 mL
25 mM 0.0695 mL 0.3474 mL 0.6948 mL 1.7370 mL
30 mM 0.0579 mL 0.2895 mL 0.5790 mL 1.4475 mL
40 mM 0.0434 mL 0.2171 mL 0.4342 mL 1.0856 mL
50 mM 0.0347 mL 0.1737 mL 0.3474 mL 0.8685 mL
60 mM 0.0289 mL 0.1447 mL 0.2895 mL 0.7237 mL
80 mM 0.0217 mL 0.1086 mL 0.2171 mL 0.5428 mL
100 mM 0.0174 mL 0.0868 mL 0.1737 mL 0.4342 mL
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GW280264X 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:

GW280264X866924-39-2MMPMatrix metalloproteinasesMixedADAM10TACEADAM17metalloproteinasesimmunogenicityglioblastomaimmunotherapystemNKGICInhibitorinhibitorinhibit

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