MSA-2|MSA2|CAS 129425-81-6|STING agonist|DC Chemicals

Cas No.:	129425-81-6
Chemical Name:	5,6-dimethoxy-γ-oxo-benzo[b]thiophene-2-Butanoic Acid
Synonyms:	MSA-2;MSA 2;MSA2
SMILES:	O=C(C1=CC(C(S1)=C2)=CC(OC)=C2OC)CCC(O)=O
Formula:	C₁₄H₁₄O₅S
M.Wt:	294.32
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	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

Description:

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 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.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101
2018-0101
2018-0101
2018-0101

Cat. No.	Product name	Field of application
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