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 No.
- 2138299-33-7
- Chemical 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]-
- 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]-
- CBNumber:
- CB85490110
- Molecular Formula:
- C42H51N13O7
- Molecular Weight:
- 849.94
- MDL Number:
- MFCD31746911
- MOL File:
- 2138299-33-7.mol
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]- Properties
Density | 1.44±0.1 g/cm3(Predicted) |
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storage temp. | Store at -20°C |
solubility | Soluble in DMSO |
form | Solid |
pka | 11.87±0.43(Predicted) |
color | White to off-white |
FDA UNII | L7DUG75C36 |
SAFETY
Risk and Safety Statements
Symbol(GHS) | ![]() GHS07 |
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Signal word | Warning |
Hazard statements | H302-H315-H319-H335 |
Precautionary statements | P261-P280-P301+P312-P302+P352-P305+P351+P338 |
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]- price
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]- Chemical Properties,Uses,Production
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. |
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
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]- Preparation Products And Raw materials
Raw materials
Preparation Products
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]- Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
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ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32239 | 58 |
InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8467 | 58 |
Aladdin Scientific | tp@aladdinsci.com | United States | 52924 | 58 | |
Wuhan Jingkang en Biomedical Technology Co., Ltd | +8613720134139 | orders@jknbiochem.com | China | 5221 | 58 |
ShangHai Caerulum Pharma Discovery Co., Ltd. | 18149758185 18149758185 | sales-cpd@caerulumpharma.com | China | 3466 | 58 |
Shanghai Lollane Biological Technology Co.,Ltd. | 021-52996696,15000506266 15000506266 | China | 4613 | 55 | |
Shanghai Rechem science Co., Ltd. | 21-31433387 15618786686 | sales@rechemscience.com | China | 2991 | 58 |
Shanghai Chaolan Chemical Technology Center | 021-QQ:65489617 15618227136 | Sales@ATKchemical.com | China | 9342 | 58 |
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2025-04-27 | diABZI STING agonist-1
2138299-33-7
|
US $148.00-619.00 / mg | 98.29% | 10g | TargetMol Chemicals Inc. |
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- diABZI STING agonist-1
2138299-33-7
- US $148.00-619.00 / mg
- 98.29%
- TargetMol Chemicals Inc.