Biological Activity
MSA-2 is an orally available non-nucleotide STING agonist, with 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[1].
In Vitro
No in vitro data are provided in the current product source. Contact us for further information.
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[1]. 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[1]. Animal Model: MC38 tumor-bearing C57BL6 mice[1] 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.
References & source
1. Altman, M.D., Cash, B.D., Chang, W., et al. Benzo[B]thiophene compounds as STING agonists. (2018). 2. Pan, B.-S., Perera, S.A., Piesvaux, J.A., et al. An orally available non-nucleotide STING agonist with antitumor activity. Science 369(6506), eaba6098
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.