Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
产品类别:
抑制剂
货号:
T10252
Product Introduction
Bioactivity
名称
ADU-S100 disodium salt
描述
ADU-S100 (MIW815) disodium salt is an activator of stimulator of interferon genes (STING).
细胞实验
Cryopreserved hPBMCs are thawed and 1×10^6 cells per well are plated in a 96 well plate in RPMI media supplemented with 10% FBS, 1% non-essential amino acids, 1% penicillin/streptomycin, L-glutamine, 10 mM HEPES buffer, 1 mM Sodium Pyruvate, 0.055 mM β-ME at 37°C with 5% CO2. Cells are stimulated with 10 μM ADU-S100 or ML cGAMP for 6 hours and supernatants are harvested. Supernatants are diluted 1:2 and assayed for IFN-α protein using Cytometric Bead Array (CBA) Human Flex Set. Data is collected using a FACSVerse cytometer.
动物实验
WT C57BL/6 mice are inoculated with 5×10^4 B16.F10 cells in the left flank (n=8). When tumor volumes are 100 mm3 mice receive three IT doses of either ML RR-S2 CDG (25 μg), ADU-S100 (50 μg), or HBSS as control. WT C57BL/6 mice are inoculated with 5×10^4 B16.F10 cells in the left flank (n=5). When tumor volumes are 100 mm3 they received three IT doses of ADU-S100 at 5, 25, 50, or 100 μg or HBSS as control. WT C57BL/6 mice are inoculated with 5×104 B16.F10 cells in the left flank (n=8). When tumor volumes are 100 mm3 they receive three IT doses of 100 μg ADU-S100 or HBSS as control. Treatments are administered on days 13, 17, and 20 and tumor measurements are taken twice weekly. Results are shown as percent survival by Log-rank (Mantel-Cox) test (A and C).
体外活性
ADU-S100 shows enhanced type I IFN production over CDA in THP-1 human monocytes. ADU-S100 induces the highest expression of IFN-β and the pro-inflammatory cytokines TNF-α, IL-6, and MCP-1 on a molar equivalent basis, as compared to endogenous ML cGAMP and the TLR3 agonist poly I:C. ADU-S100 is also found to induce aggregation of STING and induce phosphorylation of TBK1 and IRF3 in mouse bone marrow macrophage (BMM). ADU-S100 induces significantly higher levels of IFN-α when compared to ML cGAMP.
体内活性
ADU-S100 shows higher anti-tumor control than the endogenous ML cGAMP. A dose-response of the ADU-S100 compound is performed in B16 tumor-bearing mice, which identifies an optimal antitumor dose level that also elicits maximum tumor antigen-specific CD8+ T cell responses, and improves long-term survival to 50%.
存储条件
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度
H2O : 300 mg/mL (408.44 mM), Sonication is recommended.
关键字
ADU-S 100 | ML RR-S2 CDA | MIW 815 | ADU-S100 | ADUS100 disodium salt | MIW815 | MIW815 disodium | ADU S100 disodium salt | ADU-S100 disodium | ADU-S-100 disodium salt | ML RR-S2 CDA disodium | MIW-815 | ADU-S-100
ML RR-S2 CDA disodium salt|||MIW815 disodium salt|TargetMol