NCGC00378430

SKU: orb1217471

Description

NCGC00378430 is a potent SIX1/EYA2 interaction inhibitor that disrupts the SIX1/EYA2 complex, EMT, and Metastasis.

Key Properties

• CAS Number: 920650-00-6
• MW: 441.5
• Purity: >98% (HPLC)
• Formula: C₂₂H₂₃N₃O₅S
• SMILES: O=C(NC1=CC=C(OC)C(S(=O)(N2CCOCC2)=O)=C1)C3=CC=CC(N4C=CC=C4)=C3
• Target: SIX1-EYA2
• Solubility: DMSO:90 mg/mL (203.85 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  Animal model: 6-8 week old NSG mice with MCF7 tumor cells. Dosage: 25 mg/kg. Administration: Local Injection to the site of tumor; every other day; from day 3 until the day 21. Result: Dramatically decreased distant metastatic burden compared to vehicle treatment. Had no growth inhibitory effect. Animal model: Mice. Dosage: 20 mg/kg (Pharmacokinetic Analysis). Administration: IV. Result: Had a T1/2α of 0.25 hours, a CL of 6.19 L/hr kg, a Vss of 4.08 L/kg, a Cmax of 6703 ng/mL and an AUC of 3234 ng/mL hr.
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• In Vitro:
  Western blot analysis. Cell line: T47D cells. Concentration: 20 μM. Incubation time: 3 days. Result: Blocked TGF-β induced activation of p-Smad3, upregulation of FN1, and downregulation of E-CAD.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

SIX1-EYA2