2. Immunology/Inflammation
  3. STING
  4. ZSA-215

ZSA-215 is a potent and orally active STING agonist with an EC50 of 3.3 μM. ZSA-215 inhibits tumor regression and long-term survival of mice in MC38 colon cancer model. ZSA-215 can be used to the study of colon cancerr.

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ZSA-215 Chemical Structure

ZSA-215 Chemical Structure

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ZSA-215 Related Antibodies

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Description

ZSA-215 is a potent and orally active STING agonist with an EC50 of 3.3 μM. ZSA-215 inhibits tumor regression and long-term survival of mice in MC38 colon cancer model. ZSA-215 can be used to the study of colon cancerr[1].
In Vitro

ZSA-215 (2dr) (0-1.5 μM, 24 h) displays an EC50 as low as 3.3 μM in THP1-Blue ISG cells[1].
ZSA-215 (0.5-1.5μM, 24 h) displays best activity for STINGR232 (EC50 = 9.0 μM) and mSTING (EC50 = 9.3 μM) in THP1 cells[1].
ZSA-215 enhances STING signaling through promoting the phosphorylation of STING and interferon regulatory factor 3 (IRF3) and secretion of IFN-β：
(1) ZSA-215 (6-13 μM, 24 h) dramatically induces the expression of IFN-β in THP1 cells[1].
(2) ZSA-215 (13-50μM, 3 h) significantly increases the phosphorylation of STING and IRF3 in THP1-Blue ISG cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

ZSA-215 Related Antibodies

ELISA Assay[1]

Cell Line: THP1 cells
Concentration: 6 μM, 13 μM
Incubation Time: 24 h
Result: Enhanced STING signaling through promoting the secretion of IFN-β.

Western Blot Analysis[1]

Cell Line: THP1-Blue ISG cells
Concentration: 13 μM, 25 μM, 50 μM
Incubation Time: 3 h
Result: Significantly increased the phosphorylation of STING and IRF3.
Parmacokinetics[1]
Species Dose Route Indicator value
Mice 10 mg/kg p.o. T1/2 1.1 hr
Mice 5 mg/kg i.v. Cmax 48366.7 ng/mL
Mice 10 mg/kg p.o. Cmax 20633.3 ng/mL
Mice 5 mg/kg i.v. T1/2 0.6 hr
Mice 10 mg/kg p.o. CL 416.7 mL/h/kg
Mice 5 mg/kg i.v. AUC 20647.7 ng·h/mL
Mice 10 mg/kg p.o. AUC 23835 ng·h/mL
Mice 5 mg/kg i.v. CL 242.2 mL/h/kg
Mice 10 mg/kg p.o. F 58 %
In Vivo

ZSA-215 (dr) (60 mg/kg, PO, every 3 Days, 2 or 6 doses) dramatically suppresses tumor growth and achieves long-term survival in MC38 tumor model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: MC38 tumor model established in BALB/C female mice (6 weeks)[1]
Dosage: 60 mg/kg
Administration: PO, Every 3 Days, 2 or 6 doses
Result: Achieved CR and long-term survival of all mice, which significantly exceeded its parental compound ZSA-52 (CR = 60%) in combination with anti-PD-1.
Reached CR and long-term survival of all mice with monotherapy.
Did not show any tumor recurrence during additional 74 days observation (total 157 days observation).
Achieved a 60% complete response (CR) rate in mice following two-dose administration.
Produced a high concentration of IFN-β, IL-6 and CXCL10 in tumor and serum, which outperformed MSA-2.
Molecular Weight

402.28

Formula

C16H18FNO5Se
SMILES

COC1=C(C=C2C([Se]C(C(NC[C@H](C(O)=O)CC)=O)=C2F)=C1)OC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ZSA-215 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ZSA-215ZSA215ZSA 215STINGStimulator of Interferon GenesTMEM173MITAERISMPYSColon cancerIntramolecular hydrogen bond ring mimicMC38 colon cancer modelInhibitorinhibitorinhibit

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