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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DC60034	STING inhibitor-1	STING inhbiitor, which inhibited the activation of the STING signal pathway and to prevent or treat a STING-mediated disease.
DC60033	STING INHIBITOR-2	STING inhbiitor, which inhibited the activation of the STING signal pathway and to prevent or treat a STING-mediated disease.
DC39220	STING agonist compound 17	STING agonist compound 17 is a selective stimulator of interferon genes (STING) receptor agonist.
DC39210	MSA-2 analogue	MSA-2 analogue is an orally available human STING agonist.
DC39031	MSA-2	MSA-2 is an orally available human STING agonist.MSA-2 is bound to STING as a noncovalent dimer. Extensive experimental analysis indicates that MSA-2 predimerization is required for binding. Acidic tumor microenvironments favor permeable, uncharged MSA-2.
DC39030	SR-717	SR-717 is a non-nucleotide, small-molecule STING agonist and functions as a direct cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) mimetic that induces the same "closed" conformation of STING.SR-717 functions as a direct cyclic guanosine mo
DC72041	BSP16	BSP16 is a potent, orally active stimulator of interferon genes (STING) agonist. BSP16 can selectively stimulate the STING pathway. BSP16 can be used for the research of cancer.
DC50039	3'3'-cGAMP (sodium salt)	3’3’-cGAMP Fluorinated (c-[2'FdGMP]-[2'FdAMP]) is a synthetic analog of cyclic guanosine monophosphate- adenosine monophosphate (cyclic GMP-AMP, cGAMP) with a fluorine atom at 2’ position of the nucleosides. 3’3’-cGAMP is a cyclic di-nucleotide produced by bacteria. It is also referred to as "canonical" cGAMP due the presence of the classical 3’-5’ phosphodiester linkages between the guanosine and the adenosine. It has been reported that cGAMP binds STING (stimulator of IFN genes) and subsequently induces TBK1-IRF3-dependent production of IFN-β [1]. The incorporation of fluorine into biologically active molecules is commonly used in medicinal chemistry to improve their metabolic stability or to modulate physicochemical properties such as lipophilicity [2, 3]. Moreover, the introduction of a fluorine atom can change the biological activities of a molecule. Interestingly, when used at low concentrations in various cellular assays, 3’3’-cGAMP Fluorinated induces higher levels of type I IFNs than does cGAMP. STING ligands such as cGAMP induce type I IFNs and activate interferon stimulated genes (ISG) through IRFs. To facilitate their study, InvivoGen has developed stable reporter cells in two well established immune cell models: THP-1 human monocytes and RAW 264.7 murine macrophages. These cells express a reporter gene (SEAP or Lucia luciferase), under control of an IRF-inducible promoter.
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