diABZI STING agonist-1 trihydrochloride
CAS No. 2138299-34-8
diABZI STING agonist-1 trihydrochloride( —— )
Catalog No. M20172 CAS No. 2138299-34-8
diABZI STING agonist-1 (trihydrochloride) is stimulator of interferon genes (STING) receptor agonist.
Purity : >98% (HPLC)
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Datasheet
HNMR
HPLC
MSDS
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Biological Information
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Product NamediABZI STING agonist-1 trihydrochloride
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NoteResearch use only, not for human use.
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Brief DescriptiondiABZI STING agonist-1 (trihydrochloride) is stimulator of interferon genes (STING) receptor agonist.
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DescriptiondiABZI STING agonist-1 (trihydrochloride) is stimulator of interferon genes (STING) receptor agonist.(In Vitro):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. At a concentration of 1 μM, diABZI STING agonist-1 (compound 3) demonstrates high selectivity against more than 350 kinases tested.(In Vivo):diABZI STING agonist-1 trihydrochloride (subcutaneous injection; 2.5 mg/kg) induces STING-dependent activation of type-I interferon and pro-inflammatory cytokines in vivo.diABZI STING agonist-1 trihydrochloride (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).diABZI STING agonist-1 trihydrochloride (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.
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In VitrodiABZI STING agonist-1 is a selective stimulator of interferon genes (STING) receptor agonist, with EC50s of 130, 186 nM for human and mouse, respectively. At a concentration of 1 μM, diABZI STING agonist-1 (compound 3) demonstrates high selectivity against more than 350 kinases tested.
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In VivodiABZI STING agonist-1 trihydrochloride (subcutaneous injection; 2.5 mg/kg)induces STING-dependent activation of type-I interferon and pro-inflammatory cytokines in vivo.diABZI STING agonist-1 trihydrochloride (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).diABZI STING agonist-1 trihydrochloride (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. Animal Model:Wild and Sting?/? C57Blk6 mice 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 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 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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Synonyms——
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PathwayImmunology/Inflammation
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TargetSTING
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RecptorSTING
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Research Area——
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Indication——
Chemical Information
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CAS Number2138299-34-8
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Formula Weight959.32
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Molecular FormulaC42H54Cl3N13O7
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Purity>98% (HPLC)
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SolubilityDMSO:125 mg/mL?(130.30 mM)
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SMILESCl.Cl.Cl.CCn1nc(C)cc1C(=O)Nc1nc2cc(cc(OC)c2n1C\C=C\Cn1c(NC(=O)c2cc(C)nn2CC)nc2cc(cc(OCCCN3CCOCC3)c12)C(N)=O)C(N)=O
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1.Ramanjulu JM et al. Design of amidobenzimidazole STING receptor agonists with systemic activity. Nature. 2018 Nov 7.
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