ZSA-215
ZSA-215 is a potent and orally active STING agonist with an EC50 of 3.3 μM. ZSA-215 enhances STING signaling through promoting the phosphorylation of STING and interferon regulatory factor 3 (IRF3) and secretion of IFN-β. 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.
For research use only. We do not sell to patients.
- Formula: C16H18FNO5Se
- Molecular Weight:402.28
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
ZSA-215 (Compound 2dr) (0-1.5 μM, 24 h) displays an EC50 as low as 3.3 μM in THP1-Blue ISG cells[1].
ZSA-215 (0.5-1.5 μM, 24 h) displays best activity for STINGR232 (EC50 = 9.0 μM) and mSTING (EC50 = 9.3 μM) in THP1 cells[1].
ZSA-215 (6-13 μM, 24 h) dramatically induces the expression of IFN-β in THP1 cells[1].
ZSA-215 (13-50 μM, 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.
-
Cell Line:THP1 cells
-
Concentration:6 μM, 13 μM
-
Incubation Time:24 h
-
Result:Enhanced STING signaling through promoting the secretion of IFN-β.
-
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.
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:Oral administration (p.o.), 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.
Chemical Information
-
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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Powered by Bioz