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NCGC00378430

NCGC00378430 is an inhibitor of the SIX1/EYA2 complex that significantly suppresses breast cancer-associated metastasis in vivo without significantly altering primary tumor growth.

NCGC00378430 Chemical Structure

NCGC00378430 Chemical Structure

CAS No. 920650-00-6

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NCGC00378430 Related Products

Biological Activity

Description NCGC00378430 is an inhibitor of the SIX1/EYA2 complex that significantly suppresses breast cancer-associated metastasis in vivo without significantly altering primary tumor growth.
Targets
SIX1/EYA2 complex [1]
In vitro
In vitro

NCGC00378430 reduces the SIX1/EYA2 interaction. NCGC00378430 partially reverses transcriptional and metabolic profiles mediated by SIX1 overexpression and reverses SIX1-induced TGF-β signaling and EMT.[1]
Cell Research Cell lines breast cancer cell lines
Concentrations 10 μM, 20 μM, 50 μM
Incubation Time 24 h
Method

Cells are transfected with the PGL3 Renilla reporter vector (as a control for transfection efficiency) along with either PGL3 empty vector (EV) or PGL3 MEF3 Firefly reporter for 48 hours in triplicate. After 48h, vehicle (DMSO) or NCGC00378430 treatment at the mentioned doses is administered for 1 day prior to luciferase activity measurement. Renilla and Firefly luciferase activity is measured following protocols provided in the Dual-Luciferase Reporter Assay System, and data is collected using a Modulus II Microplate Multimode Reader. All Firefly/Renilla ratios are normalized to the empty vector with vehicle treatment condition.
In Vivo
In vivo

NCGC00378430 is well tolerated when delivered to mice and significantly suppresses breast cancer-associated metastasis in vivo without significantly altering primary tumor growth.[1]
Animal Research Animal Models 6-8 week old NSG mice
Dosages 25 mg/kg
Administration intra tumor injection

Chemical Information & Solubility

Molecular Weight 441.5 Formula

C22H23N3O5S
CAS No. 920650-00-6 SDF --
Smiles COC1=C(C=C(NC(=O)C2=CC(=CC=C2)[N]3C=CC=C3)C=C1)[S](=O)(=O)N4CCOCC4
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 88 mg/mL ( (199.32 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

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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.

Handling Instructions

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