All AbMole products are for research use only, cannot be used for human consumption.
MSA-2 is an orally available non-nucleotide STING agonist with antitumor activity. MSA-2 shows EC50s of 8.3 and 24 μM for human STING isoforms WT and HAQ, respectively. MSA-2 induces tumor regression with durable antitumor immunity, and synergizes with anti-PD-1 in syngeneic mouse tumor models. 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. In tumor models that are moderately or poorly responsive to PD-1 blockade, combinations of MSA-2 and anti-PD-1 antibody are superior in inhibiting tumor growth and prolonging survival over monotherapy.
Cancer Lett. 2023 Oct 1;573:216370.
Low-dose metronomic chemotherapy triggers oxidized mtDNA sensing inside tumor cells to potentiate CD8+ T anti-tumor immunity
MSA-2 purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | THP-1 cells, mouse macrophages |
| Preparation method | In the primary screen, THP-1 cells are incubated, in 1536-well plates, with test compounds (20 μM) in a RPMI1640-based assay medium in the presence of 5% carbon dioxide at 37°C for 5 hours. IFN-b levels are determined using an AlphaLISA assay and an EnVision Reader and expressed as percentages of IFN-b induced by cGAMP. STING binding activity of compounds is evaluated with a competitive radioligand binding assay using tritiated cGAMP and membrane embedded full-length recombinant human and mouse STING generated in insect cells. STING pathway activation by MSA-2 is assessed by Western blotting, probing phosphorylation status and total protein levels of STING, TBK-1, and IRF3 by using commercially available antibodies. |
| Concentrations | 20 μM, 0.16 μM-100 μM |
| Incubation time | 5 h |
| Animal Experiment | |
|---|---|
| Animal models | C57BL/6J mice, NSG mice, BALB/c mice, nude NCr mice |
| Formulation | - |
| Dosages | 25 mg/kg, 40 mg/kg, 50 mg/kg, 60 mg/kg, 80 mg/kg, 160 mg/kg |
| Administration | intra tumor injection, SC, PO |
| Molecular Weight | 294.32 |
| Formula | C14H14O5S |
| CAS Number | 129425-81-6 |
| Solubility (25°C) | DMSO ≥ 40 mg/mL |
| Storage | 2-8°C, protect from light, sealed |
| Related STING Products |
|---|
| SN-011
SN-011 is a potent and selective mouse and human STING inhibitor, with an IC50 of 76 nM for STING signaling. |
| IACS-8779
IACS-8779 is a highly potent stimulator of interferon genes (STING) agonist with robust systemic antitumor efficacy. |
| IACS-8803
IACS-8803 is a highly potent cyclic dinucleotide STING agonist with robust systemic antitumor efficacy. |
| STING-IN-6
STING-IN-6 is a potent STING inhibitor with a pIC50 of 8.9. |
| MSA-2 dimer
MSA-2 dimer is a selective, orally active non-nucleotide STING agonist (Kd=145 μM) with long-term antitumor and immunogenic activity. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.
