GSK3179106

SKU: orb1301746

Description

GSK3179106 is a potent and selective small-molecule inhibitor of the RET kinase, demonstrating an IC50 of 0.4 nM. It is a valuable research tool for investigating RET-driven pathologies, such as certain cancers, in both cellular and animal models.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1627856-64-7
• MW: 467.41
• Purity: 99.80%
• Formula: C₂₂H₂₁F₄N₃O₄
• SMILES: CCOc1cc(=O)[nH]cc1-c1ccc(CC(=O)Nc2cc(on2)C(C)(C)C(F)(F)F)c(F)c1
• Target: c-RET
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (8.56 mM);DMSO:100 mg/mL (213.94 mM);H2O:< 1 mg/mL (insoluble)

Bioactivity

• Target IC50:
  RET:0.4 nM
• In Vivo:
  GSK3179106 (3 or 10 mg/kg; orally; BID for 3.5 days) reduces the visceromotor response (VMR) compared to rats administered an acetic acid enema and treated with a vehicle.
• In Vitro:
  The effect of GSK3179106 on human and rat RET enzymatic activity and motesanib on human RET enzymatic activity was determined in an in vitro biochemical homogeneous time-resolved fluorescence (HTRF) assay.

Storage & Handling

• Storage: 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

cRET, bowel, orally, inhibit, irritable, GSK 3179106, GSK3179106, GSK-3179106, hypersensitivity, IBS, Inhibitor, visceral, RET, syndrome, stress-induced, post-inflammatory

Compound Identifiers

PubChem CID

78427026