NCGC00378430

Catalog No.S9677 Batch:S967702

Technical Data

Formula	C₂₂H₂₃N₃O₅S
Molecular Weight	441.5	CAS No.	920650-00-6
Solubility (25°C)*	In vitro	DMSO	88 mg/mL (199.32 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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

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]

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]

Protocol (from reference)

Cell Assay:^{^[1]}	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.
Animal Study:^{^[1]}	Animal Models 6-8 week old NSG mice Dosages 25 mg/kg Administration intra tumor injection

Cell Assay:^{^[1]}

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.

Animal Study:^{^[1]}

Animal Models
6-8 week old NSG mice
Dosages
25 mg/kg
Administration
intra tumor injection

References

[1] Hengbo Zhou, et al. Cancer Res. 2020 Jun 15;80(12):2689-2702.

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