| Identification | Back Directory | [Name]
1H-Benzimidazole-5-carboxamide, 1-[(2E)-4-[5-(aminocarbonyl)-2-[[(1-ethyl-3-methyl-1H-pyrazol-5-yl)carbonyl]amino]-7-methoxy-1H-benzimidazol-1-yl]-2-buten-1-yl]-2-[[(1-ethyl-3-methyl-1H-pyrazol-5-yl)carbonyl]amino]-7-[3-(4-morpholinyl)propoxy]- | [CAS]
2138299-33-7 | [Synonyms]
STING agonist compound 1
1H-Benzimidazole-5-carboxamide, 1-[(2E)-4-[5-(aminocarbonyl)-2-[[(1-ethyl-3-methyl-1H-pyrazol-5-yl)carbonyl]amino]-7-methoxy-1H-benzimidazol-1-yl]-2-buten-1-yl]-2-[[(1-ethyl-3-methyl-1H-pyrazol-5-yl)carbonyl]amino]-7-[3-(4-morpholinyl)propoxy]- | [Molecular Formula]
C42H51N13O7 | [MDL Number]
MFCD31746911 | [MOL File]
2138299-33-7.mol | [Molecular Weight]
849.94 |
| Chemical Properties | Back Directory | [density ]
1.44±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
11.87±0.43(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
diABZI STING agonist-1 is a tautomerism of diABZI STING agonist-1 tautomerism (HY-112921). diABZI STING agonist-1 is a selective stimulator of interferon genes (STING) receptor agonist, with EC50s of 130, 186 nM for human and mouse, respectively[1]. | [in vivo]
diABZI STING agonist-1 (subcutaneous injection; 2.5 mg/kg) induces STING-dependent activation of type-I interferon and pro-inflammatory cytokines in vivo[1].
diABZI STING agonist-1 (intravenous injection; 3 mg/kg) exhibits systemic exposure with a half-life of 1.4 h and achieves systemic concentrations greater than the half-maximal effective concentration (EC50) for mouse STING (200 ng/ml)[1].
diABZI STING agonist-1 (intravenous injection; 1.5 mg/kg; days 1, 4 and 8; 43 days) results in significant tumour growth inhibition and significantly improves survival (P < 0.001) with 8 out of 10 mice remaining tumor free at the end of the study on day 43[1]. | Animal Model: | Wild and Sting?/? C57Blk6 mice[1] | | Dosage: | 2.5 mg/kg | | Administration: | Subcutaneous injection; 2.5 mg/kg | | Result: | Activated secretion of IFNβ, IL-6, TNF, and CXCL1 in wild-type but not Sting?/? mice. |
| Animal Model: | Syngeneic mouse model of colorectal tumours (CT-26) in BALB/c mice[1] | | Dosage: | 3 mg/kg | | Administration: | Intravenous injection; 3 mg/kg | | Result: | Exhibited a half-life of 1.4 hours and achieved systemic concentrations greater than EC50 for mouse STING (200 ng/ml). |
| Animal Model: | Syngeneic mouse model of colorectal tumours (CT-26) in BALB/c mice[1] | | Dosage: | 1.5 mg/kg | | Administration: | Intravenous injection; 1.5 mg/kg; 43 days | | Result: | Resulted in significant tumour growth inhibition and improved survival.
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| [References]
[1] Ramanjulu JM, et al. Design of amidobenzimidazole STING receptor agonists with systemic activity. Nature. 2018 Nov 7. DOI:10.1038/s41586-018-0705-y |
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Wuhan Topule
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http://www.topule.com/ |
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