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diABZI STING agonist-1 trihydrochloride

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diABZI STING agonist-1 trihydrochloride
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Cat #: V31645 CAS #: 2138299-34-8 Purity ≥ 99%

Description: diABZI STING agonist-1 (trihydrochloride) is a selective stimulator of interferon genes (STING) receptor agonist, with an EC50s of 130 for human PBMCs.

References: Ramanjulu JM, et al. Design of amidobenzimidazole STING receptor agonists with systemic activity. Nature. 2018 Nov 7.

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Molecular Weight (MW)959.32
Molecular FormulaC42H54Cl3N13O7
CAS No.2138299-34-8
SynonymsdiABZI STING agonist-1 trihydrochloride
ProtocolIn 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.
In VivodiABZI 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. 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 (subcutaneous injection; 2.5 mg/kg) induces STING-dependent activation of type-I interferon and pro-inflammatory cytokines in vivo.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM1.0424 mL5.2120 mL10.4241 mL20.8481 mL
5mM0.2085 mL1.0424 mL2.0848 mL4.1696 mL
10mM0.1042 mL0.5212 mL1.0424 mL2.0848 mL
20mM0.0521 mL0.2606 mL0.5212 mL1.0424 mL
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Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

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Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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