PND-1186

SKU: orb1307003

Description

PND-1186 (VS-4718) is a potent, reversible, and selective focal adhesion kinase (FAK) inhibitor with an IC50 of 1.5 nM. It is a valuable research tool for investigating FAK's role in cancer cell migration, proliferation, and survival in both in vitro and in vivo models.

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1061353-68-1
• MW: 501.5
• Purity: 99.70%
• Formula: C₂₅H₂₆F₃N₅O₃
• SMILES: CNC(=O)c1ccccc1Nc1cc(Nc2ccc(cc2OC)N2CCOCC2)ncc1C(F)(F)F
• Target: FAK,Apoptosis
• Solubility: DMSO:34 mg/mL (67.8 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.99 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  FAK:1.5 nM|RD cells:1.22 μM|FAK Tyr-397 ( breast carcinoma cells ):~100 nM
• In Vivo:
  In vitro, PND-1186 demonstrates an inhibitory effect on the motility of 4T1 breast cancer cells, promotes apoptosis in suspended 4T1 cells, and reduces both the number and size of 4T1 soft agar colonies. Additionally, in HEY and OVCAR8 cells, PND-1186 induces G0-G1 cell cycle arrest, leading to cell death.
• In Vitro:
  In mice implanted with 4T1 tumors, PND-1186 (100 mg/kg, s.c.) induces apoptosis and inhibits the growth of subcutaneous 4T1 tumors. Additionally, in mice carrying ID8 tumors, PND-1186 (0.5 mg/mL, p.o.) suppresses the growth of ovarian cancer tumors.
• Cell Research:
  For soft agar assays, 48-well plates are coated with a 1:4 mix of 2% agar (EM Science) in 0.2 mL growth media (bottom layer). 5×104 cells are plated per well (in triplicate) in a mixture of 0.3% agar in 0.2 mL growth media (top layer). After agar solidification, 0.2 mL growth media is added containing DMSO or PND-1186 (final concentration for 0.6 mL). In separate experiments, PND-1186 is added after 4 days. After 10 days, colonies are imaged in phase contrast, enumerated by counting 9 fields (3 fields per well), and total area determined using Image J. For all analyses, experimental points are performed in triplicate and repeated at least two times. (Only for Reference)

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Apoptosis, cell, growth, Focal adhesion kinase, FAK, Inhibitor, integrin, inhibit, PTK2, PTK2 protein tyrosine kinase 2, SR2516, SR-2516, SR 2516, survival, PND1186, PND-1186, PND 1186, VS 4718, VS4718, VS-4718, tumor

Compound Identifiers

PubChem CID

25073775