AK-1690

SKU: orb2695519

Description

AK-1690 is a potent, selective STAT6-targeting PROTAC degrader with a cellular DC50 of 1 nM. It effectively depletes STAT6 protein in both cellular assays and mouse tissues, making it a valuable chemical probe for oncology research, particularly in studying STAT6-dependent signaling pathways in cancer.

Research Area

Pharmacology & Drug Discovery, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 2984505-88-4
• MW: 1016.05
• Purity: 99.95%
• Formula: C₅₁H₅₆F₂N₅O₁₁PS
• SMILES: C(#CCCCCCO[C@H]1C[C@@H](C(=O)N2C[C@H](OCC2)C3=CC=CC=C3)N(C([C@@H](NC(=O)C4=CC=5C(S4)=CC=C(C(P(=O)(O)O)(F)F)C5)[C@@](C)(C)C)=O)C1)C6=C7C(C(=O)N(C7)C8C(=O)NC(=O)CC8)=CC=C6
• Target: STAT,PROTACs
• Solubility: DMSO:80 mg/mL (78.74 mM);10% DMSO+90% Corn Oil:3.3 mg/mL (3.25 mM)

Bioactivity

• Target IC50:
  IL-4-stimulated HEPG2 cells:0.88 nM
• In Vivo:
  In a CCRF-CEM xenograft mouse model, oral administration of AK-1690 at 1, 3, and 10 mg/kg (once daily for 21 days) led to dose-dependent tumor growth inhibition. At 10 mg/kg, STAT6 degradation was significant, and tumor volume was notably reduced without observable weight loss or toxicity, indicating strong in vivo efficacy and tolerability.
• In Vitro:
  In HEPG2 and CCRF-CEM cells, AK-1690 efficiently degrades endogenous STAT6 (DC₅₀ = 3.2 nM, Dmax > 90%). In IL-4-stimulated HEPG2 cells, AK-1690 significantly suppresses expression of downstream genes (e.g., CCL26, SOCS1) with an IC₅₀ of 0.88 nM.

Storage & Handling

• Storage: keep away from direct sunlight | 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

AK1690

Compound Identifiers

PubChem CID

169067446