PND-1186

SKU: orb1227051

Description

PND-1186 (VS-4718) is a reversible and selective FAK inhibitor with IC50 of 1.5 nM. Phase 1.(In Vitro):PND-1186 has an IC50 of ~100 nM in breast carcinoma cells as determined by anti-phospho-specific immunoblotting to FAK Tyr-397.In murine 4T1 breast carcinoma cells, FAK is important in promoting an invasive and metastatic cell phenotype. Increasing concentrations of PND-1186 (0.1 to 1.0 μM) added to 4T1 cells inhibits FAK Tyr-397 phosphorylation (pY397) and results in elevated levels of total FAK protein within 1 h.(In Vivo):PND-1186 (30 mg/kg or 100 mg/kg; subcutaneously; injected subcutaneously in the neck region) inhibits 4T1 subcutaneous tumor growth by induction of apoptosis.

Key Properties

• CAS Number: 1061353-68-1
• MW: 501.5
• Purity: >98% (HPLC)
• Formula: C₂₅H₂₆F₃N₅O₃
• SMILES: O=C(NC)C1=CC=CC=C1NC2=CC(NC3=C(OC)C=C(N4CCOCC4)C=C3)=NC=C2C(F)(F)F
• Target: FAK
• Solubility: DMSO: 24 mg/mL (47.85 mM)

Bioactivity

• In Vivo:
  PND-1186 (30 mg/kg or 100 mg/kg; subcutaneously; injected subcutaneously in the neck region) inhibits 4T1 subcutaneous tumor growth by induction of apoptosis. Animal model: BALB/c mice. Dosage: 30 mg/kg or 100 mg/kg. Administration: Injected (100 μL) subcutaneously in the neck region; every 12 h (twice-daily, b. i. d.) for 5 days. Result: 100 mg/kg treatment significantly reduced final 4T1 tumor weight 2-fold whereas 30 mg/kg treatment slightly reduced final tumor weight but was not significantly different compared to control.
• In Vitro:
  PND-1186 has an IC50 of ~100 nM in breast carcinoma cells as determined by anti-phospho-specific immunoblotting to FAK Tyr-397. In murine 4T1 breast carcinoma cells, FAK is important in promoting an invasive and metastatic cell phenotype. Increasing concentrations of PND-1186 (0.1 to 1.0 μM) added to 4T1 cells inhibits FAK Tyr-397 phosphorylation (pY397) and results in elevated levels of total FAK protein within 1 h. Western blot analysis. Cell line: 4T1 breast carcinoma cells. Concentration: 0.1, 0.2, 0.4, 0.6 and 1.0 μM Incubation time: 1 hour. Result: Inhibited FAK Tyr-397 phosphorylation (pY397) and resulted in elevated levels of total FAK protein.

Storage & Handling

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

Alternative Names

SR 2516 | VS-4718

Quick Database Links

Gene Symbol

FAK