SX-682

SKU: orb1298883

Description

SX-682 is an oral small molecule allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2. By blocking myeloid-derived suppressor cell recruitment, it enhances T-cell activity and anti-tumor immunity, showing therapeutic potential in preclinical models of castration-resistant prostate cancer and other solid tumors.

Research Area

Immunology & Inflammation

Key Properties

• CAS Number: 1648843-04-2
• MW: 467.2
• Purity: >98%
• Formula: C₁₉H₁₄BF₄N₃O₄S
• SMILES: C(SC=1N=CC(C(NC2=CC=C(F)C=C2)=O)=CN1)C3=C(B(O)O)C=CC(OC(F)(F)F)=C3
• Target: GPCR
• Solubility: Soluble in DMSO (up to 25 mg/ml)

Bioactivity

• Target IC50:
  CXCR2:20 nM|CXCR1:42 nM
• In Vivo:
  METHODS: SX-682 (500 mg/kg, oral, one week) was used to treat tumor suppressor model mice injected subcutaneously with MOC2 cells, and PMN-MDSC accumulation was evaluated by flow cytometry. RESULTS SX-682 significantly reduced PMN-MDSC trafficking into MOC2 tumors, but SX-682 treatment did not alter the proliferation of tumor PMN-MDSC in tumor-bearing mice. The main mechanism of SX-682 is to inhibit PMN-MDSC trafficking into MOC2 tumors.
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• In Vitro:
  SX-682 significantly inhibits PMN-MDSC trafficking without altering CXCR2 ligand expression; combination with SX-682 enhances tumor growth inhibition or established tumor rejection following programmed death axis (PD-axis) immune checkpoint blockade or adoptive cell transfer of engineered T cells; CXCR1/2 are expressed on tumor cells, but SX-682 appears to have little direct antitumor effect on these cancer cells.
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Storage & Handling

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

Alternative Names

allosteric, antitumor, cells, CXCR1, CXCR2, CXCR, CXC chemokine receptors, immunity, MDSCs, Inhibitor, inhibit, myeloid-derived, tumor, SX682, SX-682, SX 682, suppressor, recruitment

Compound Identifiers

PubChem CID

90467234