NSC 405020

Catalog No.S8072

NSC 405020 is a noncatalytic inhibitor of MT1-MMP, directly interacts with PEX domain of MT1-MMP, affects PEX homodimerization but not catalytic activity of MT1-MMP.

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NSC 405020 Chemical Structure

NSC 405020 Chemical Structure
Molecular Weight: 260.16

Validation & Quality Control

Quality Control & MSDS

Product Information

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Product Description

Biological Activity

Description NSC 405020 is a noncatalytic inhibitor of MT1-MMP, directly interacts with PEX domain of MT1-MMP, affects PEX homodimerization but not catalytic activity of MT1-MMP.
Targets MT1-MMP [1]
In vitro NSC 405020 is a noncatalytic inhibitor of MT1-MMP, directly interacts with PEX domain of MT1-MMP. NSC 405020 affects PEX homodimerization but not catalytic activity of MT1-MMP. NSC 405020 (100μM) inhibits migration of cells with high level of MT1-MMP, with a reduction of migration efficiency by about 75%. NSC 405020 does not inhibit migration of cells with low level of MT1-MMP and does not inhibit cell adhesion on collagen.[1]
In vivo NSC 405020 (0.5 mg/kg, intratumoral injection) significantly represses tumor growth. NSC 405020 causes a fibrotic, ΔPEX-like tumor phenotype and increases the level of COL-I. [1]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

Migration assays 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. The compounds (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 the compounds 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.

Cell Assay: [1]

Cell lines 184B5-MT and MCF7-β3/MT
Concentrations ~400 μM
Incubation Time 24 or 30 h
Method Assays are conducted in wells of a 96-well flat bottom, white wall plates. 184B5-MT and MCF7-β3/MT cells (5×104) are grown for 16 hours in MEGM-10% FBS and DMEM-10% FBS, respectively. 184B5-MT cells are replenished with fresh MEGM (0.1 mL per well) and incubated for an additional 24 hours in the presence of the compounds (100 μM) or vehicle (1% DMSO). MCF7-β3/MT cells are replenished with fresh DMEM-10% FBS (0.1 mL per well) and incubated for an additional 6 hours in the presence of the compounds (400 μM) or vehicle (2% DMSO). The viable cells are counted using a luminescent ATP-Lite assay.

Animal Study: [1]

Animal Models BALB/c nu/nu mice injected with MCF7-β3/WT and MCF7-β3/ΔPEX cells
Formulation 2% DMSO
Dosages 0.5 mg/kg, 3 times per week
Administration Intratumoral injection

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Remacle GG, et al. Cancer Res, 2012, 72(9), 2339-49.

Chemical Information

Download NSC 405020 SDF
Molecular Weight (MW) 260.16
Formula

C12H15Cl2NO

CAS No. 7497-07-6
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 52 mg/mL (199.87 mM)
Ethanol 52 mg/mL (199.87 mM)
Water <1 mg/mL (<1 mM)
In vivo 1% DMSO+30% polyethylene glycol+1% Tween 80 5 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 3,4-Dichloro-N-(1-methylbutyl)benza-mide

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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