NSC 405020 MMP inhibitor

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Quality Control

Batch: S807201 DMSO]125 mg/mL]false]Ethanol]52 mg/mL]false]Water]Insoluble]false Purity: 99.07%

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

99.07

Related Targets	HDAC Caspase Proteasome Secretase HCV Protease Cysteine Protease DPP Tyrosinase HIV Protease Serine Protease
Other MMP Inhibitors	Ilomastat (GM6001) Marimastat (BB-2516) Batimastat (BB-94) SB-3CT T-5224 Nobiletin MMP-9-IN-1 1, 10-Phenanthroline monohydrate JNJ0966 Cordycepin

Chemical Information, Storage & Stability

Molecular Weight	260.16	Formula	C₁₂H₁₅Cl₂NO	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	7497-07-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CCCC(C)NC(=O)C1=CC(=C(C=C1)Cl)Cl

Solubility

In vitro
Batch:

DMSO : 125 mg/mL (480.47 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 52 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	6.250mg/ml (24.02mM)	Taking the 1 mL working solution as an example, add 50 μL of 125 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	MT1-MMP
In vitro	NSC 405020 is a noncatalytic inhibitor of MT1-MMP, directly interacts with PEX domain of MT1-MMP. This compound affects PEX homodimerization but not catalytic activity of MT1-MMP. It (100μM) inhibits migration of cells with high level of MT1-MMP, with a reduction of migration efficiency by about 75%. This chemical does not inhibit migration of cells with low level of MT1-MMP and does not inhibit cell adhesion on collagen.
Kinase Assay	Migration assays
Kinase Assay	Assays are conducted in wells of a 24-well, 8 μm pore size Transwell plate. A 6.5-mm insert membrane is coated with 0.1 mL COL-I (300 μg/mL in MEGM) and then air dried for 16 hours. The collagen coating is rehydrated for 1 hour in 0.2 mL MEGM. The inner chamber contains MEGM-10% FBS as a chemoattractant. This compound (10–100 μmol/L) or DMSO (0.1%–1%) are added to both inner and outer chambers. Before plating in the outer chamber, cells (5×10⁴) are coincubated for 20 minutes with this compound or DMSO in MEGM. Cells are allowed to migrate for 16 to 18 hours. The cells remaining on the top surface of the membrane are removed with a cotton swab. The cells on the bottom surface of the membrane are fixed and stained (0.2% crystal violet). The incorporated dye is extracted with 1% SDS and the A570 is measured.
In vivo	NSC 405020 (0.5 mg/kg, intratumoral injection) significantly represses tumour growth. This compound causes a fibrotic, ΔPEX-like tumour phenotype and increases the level of COL-I.
References	[1] https://pubmed.ncbi.nlm.nih.gov/22406620/

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Chemical Structure

Molecular Weight: 260.16