Chemical Properties | Back Directory | [Boiling point ]
553.5±50.0 °C(predicted) | [density ]
1.147±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: 2mg/mL, clear | [form ]
Solid | [pka]
4.59±0.10(predicted) | [color ]
White to off-white |
Hazard Information | Back Directory | [Uses]
NVS-STG2 is a molecular glue that targets STINGSTING by binding to pockets between adjacent STING dimer transmembrane domains, effectively acting as a molecular glue. NVS-STGI enhances the activity of cGAMP by inducing the formation of more abundant and larger oligomers. NVS-STG2 produces antitumor activity in animal models[1][2]. | [Biological Activity]
Potent STING allosteric agonist th at induces a STING-mediated immune responses in cells.
NVS-STG2 is a potent STING (stimulator of interferon genes) allosteric agonist (AC=5.2 μM) th at induces a STING-mediated immune responses in cells. It elicits potent antitumor activity in animal models. NVS-STG2 acts as molecular glue th at binds the transmembrane domains of the neighboring STING dimers. | [in vivo]
NVS-STG2 (800 μg; intratumoral injection; 3 times; days 11, 14, and 18) can significantly slow tumor growth in the MC38 tumor model of hSTING gene knock-in mice[1]. NVS-STG2 (400 μg, 800 μg; intratumoral injection; 1 time; day 8) can induce significant dose-dependent T cell priming responses in the B16-SIY tumor model of hSTING gene knock-in mice[1].
Animal Model: | Female C57BL/6 wild-type and hSTING knock-in mice (10-12 weeks old, 20-25 g) with MC38 flank tumors and B16-SIY flank tumors[1] | Dosage: | 800 μg, 400 μg (not specified in the article about the solvent)
| Administration: | For the MC38 tumor model, intratumoral injection, 3 times, on days 11, 14, and 18. For the B16-SIY tumor model, intratumoral injection, single dose, on day 8
| Result: | In the MC38 tumor model, slowed tumor growth significantly, and resulted in no significant tumor growth among 4/9 mouse during the 33-day experimental period.
In the B16-SIY tumor model, exhibited a dose-dependent and significant induction of T-cell priming response. Resulted a significant increase in plasma IFNγ level at 6 h after dosing.
|
| [References]
[1] Li J et al. Activation of human STING by a molecular glue-like compound. Nat Chem Biol. 2023 Oct 12. DOI:10.1038/s41589-023-01434-y [2] Sulpizio A, et al. A new road to STING activation. Nat Chem Biol. 2023 Oct 13. DOI:10.1038/s41589-023-01455-7 |
|
Company Name: |
Enzo Biochem Inc
|
Tel: |
Enzo Biochem Inc. 13797054060 |
Website: |
www.enzo.com |
Company Name: |
Merck KGaA
|
Tel: |
21-20338288 |
Website: |
www.sigmaaldrich.cn |
Company Name: |
Biorbyt Ltd.
|
Tel: |
+44 (0)1223 859 353 |
Website: |
http://www.biorbyt.com |
|