| Field | Specification |
|---|---|
| Alternative names | TAK-676 free base |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C21H22F2N8O10P2S2 |
| SMILES | |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Dazostinag, also known as TAK-676 free base, is an agonist of the stimulator of interferon genes (STING) protein with antineoplastic activity. It can serve as a payload for the synthesis of antibody-drug conjugates (ADCs)[1][2]. It has a molecular formula of C21H22F2N8O10P2S2 and a molecular weight of 710.52 g/mol.
Physical & Chemical Properties
| CAS Number | 2553413-86-6 |
|---|---|
| Molecular Formula | C21H22F2N8O10P2S2 |
| Molecular Weight | 710.52 g/mol |
| SMILES | FC1=CN([C@H]2[C@H](O[P@@](OC[C@@H]3[C@@H](O4)[C@@H](F)[C@H](N5C6=NC=NC(N)=C6N=C5)O3)(S)=O)[C@H](O)[C@@H](COP4(S)=O)O2)C7=C1C(N=CN7)=O |
| Signaling Pathway | Immunology/Inflammation |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
[1]. Ishii Yumiko, et al. Antibody drug conjugates comprising STING modulators: World Intellectual Property Organization, WO2020229982. 2020-11-19.
[2]. WHO Drug Information-World Health Organization (WHO).
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with your institution's chemical hygiene plan.
In Vitro
In rat liver tritosomes, Dazostinag (ADC-1, linker-payload) (121 μM; 10 min-24 hr) shows a half-life (t1/2) of 2.4 hr[1]. In THPl cells carrying the R232 variant of human STING, Dazostinag (ADC-1, linker-payload) activates human Guanylyl cyclase C (GCC), with an EC50 value of 0.068 nM[1]. Dazostinag (ADC-1) (10 μg/mL; 0-96 hr) is stable in human, primate and mouse plasma[1].
In Vivo
In Balb/C mice bearing CT26-GCC tumors, Dazostinag (ADC-1) (0.1 mg/kg; single dose) has a half-life of 33 h and an AUC (last) value of 51432 h·nM[1]. In Balb/C mice bearing GCC-expressing CT26 colon carcinoma tumors, Dazostinag (ADC-1) at 50 μg/kg and 100 μg/kg (i.v.; single dose; monitored for 2 weeks) markedly inhibits tumor growth[1].
| Animal Model | CT26 colon carcinoma model in female Balb/C mice (6-8 weeks old)[1] |
|---|---|
| Dosage | 50 μg/kg, 100 μg/kg |
| Administration | IP; single dose, monitored for 15 days, measured two times per week |
| Result | Significantly suppressed the volume of tumor in mice. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Intermetallic nanoassemblies potentiate systemic STING activation. Science 2026 May 7;392(6798):eadx1893. PMID: 42096576