MSA-2

SKU: orb1220269

Description

MSA-2, a potent and orally available non-nucleotide STING agonist, has EC50s of 8.3 and 24 μM for human STING isoforms WT and HAQ, respectively. MSA-2 shows antitumor activity and stimulates interferon-β secretion in tumors, induces tumor regression with durable antitumor immunity, and synergizes with anti-PD-1 in syngeneic mouse tumor models.

Key Properties

• CAS Number: 129425-81-6
• MW: 294.32
• Purity: >98% (HPLC)
• Formula: O=C(C₁=CC(C(S₁)=C₂)=CC(OC)=C₂OC)CCC(O)=O
• SMILES: O=C(C1=CC(C(S1)=C2)=CC(OC)=C2OC)CCC(O)=O
• Target: STING
• Solubility: DMSO : 50 mg/mL (169.88 mM; ultrasonic and warming and heat to 80°C)

Bioactivity

• In Vivo:
  MSA-2 dosed via either PO or SC regimens achieved comparable exposure in both tumor and plasma. MSA-2 also exhibits dose-dependent antitumor activity when administered by IT, SC, or PO routes, and dosing regimens were identified that induced complete tumor regressions in 80 to 100% of treated animals. MSA-2 (PO: 60 mg/kg or SC: 50 mg/kg; single dose) that effectively inhibits tumor growth induced substantial elevations of IFN-β, interleukin-6 (IL-6), and TNF-α in tumor. Animal model: MC38 tumor-bearing C57BL6 mice. Dosage: 60 mg/kg. Administration: p.o. ; s. c (50 mg/kg); single dose. Result: PO or SC doses of MSA-2 that effectively inhibited tumor growth induced substantial elevations of IFN-β, interleukin-6 (IL-6), and TNF-α in tumor.

Storage & Handling

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

Quick Database Links

Gene Symbol

STING