AdipoGen Life Sciences

MSA-2

CHF 45.00

In stock

AG-CR1-0164-M0011 mgCHF 45.00

AG-CR1-0164-M0055 mgCHF 180.00

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Product Details
Synonyms	4-(5,6-Dimethoxybenzo[b]thiophen-2-yl)-4-oxobutanoic acid
Product Type	Chemical
Properties
Formula	C₁₄H₁₄O₅S
MW	294.3
CAS	129425-81-6
Purity Chemicals	≥98%
Appearance	White to off-white solid.
Solubility	Soluble in DMSO (30mg/ml) or DMF (30mg/ml). Slightly soluble in ethanol (1mg/ml).
Identity	Determined by ¹H-NMR.
InChi Key	APCLRHPWFCQIMG-UHFFFAOYSA-N
Smiles	O=C(CCC(O)=O)C1=CC2=CC(OC)=C(OC)C=C2S1
Shipping and Handling
Shipping	AMBIENT
Short Term Storage	+4°C
Long Term Storage	-20°C
Handling Advice	Keep cool and dry.
Use/Stability	Stable for at least 2 years after receipt when stored at -20°C.
Documents
MSDS	Download PDF
Product Specification Sheet
Datasheet	Download PDF

Product-specific References

Description

MSA-2 is a new orally available (cell permeable) non-nucleotide STING (STimulator of INterferon Genes) agonist, with EC50s of 8.3 and 24μM for human STING isoforms WT and HAQ. Activation of the STING protein by its natural ligand, cyclic guanosine monophosphate-adenosine monophosphate (cGAMP, a cytosolic double-stranded DNA sensor), triggers signaling responses, inducing the release of type I interferons and other proinflammatory cytokines. STING-controlled interferon production is involved in antiviral defense as well as antitumor immunity. Pharmacological activation of STING is considered a promising therapeutic strategy for cancer.
MSA-2 highly induces secretion in vitro of IFN-β from THP-1 cells and mouse macrophages at concentration of 10-50μM. It shows in vivo antitumor activity in a MC38 mouse model of colon carcinoma in a dose-dependent manner, stimulating IFN-β secretion in tumors, inducing tumor regression with durable antitumor immunity when administered intratumorally (450μg), subcutaneously (50mg/kg) or orally (50mg/kg), and synergizes with anti-PD-1 therapy.
MSA-2 is a small molecule monomer that undergoes reversible, noncovalent dimerization in solution to become a pharmacologically active ligand. MSA-2 monomers cannot bind STING, whereas the noncovalent MSA-2 dimers bind STING with nanomolar affinity. MSA-2, a weak acid, exhibits substantially higher cellular potency in an acidified tumor microenvironment (versus normal tissue), owing to increased cellular entry and retention combined with its inherent mode of interaction with STING.

Product References

An orally available non-nucleotide STING agonist with antitumor activity: B.S. Pan, et al.; Science 369, 6506 (2020)

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