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Réf. CatalogueS7904
| Cibles apparentées | PD-1/PD-L1 CXCR AhR Immunology & Inflammation related CD markers Interleukins Anti-infection Antioxidant COX Histamine Receptor |
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| Autre STING Inhibiteurs | H-151 C-176 CCCP STING inhibitor C-178 MSA-2 C-171 SN-011 G10 (STING agonist-1) SN-001 Cridanimod |
| Lignées cellulaires | Type dessai | Concentration | Temps dincubation | Formulation | Description de lactivité | PMID |
|---|---|---|---|---|---|---|
| 293T | Function assay | 30 mins | Activation of recombinant human STING haplotype R71H/G230A/R293Q mutant expressed in 293T cells measured after 30 mins in presence of digitonin A by bright Glo-luciferase reporter gene assay, EC50 = 0.02 μM. | 31715099 | ||
| 293T | Function assay | 30 mins | Activation of recombinant human wild-type STING expressed in 293T cells measured after 30 mins in presence of digitonin A by bright Glo-luciferase reporter gene assay, EC50 = 0.02 μM. | 31715099 | ||
| 293T | Function assay | 30 mins | Activation of recombinant human STING haplotype G230A/R293Q mutant expressed in 293T cells measured after 30 mins in presence of digitonin A by bright Glo-luciferase reporter gene assay, EC50 = 0.04 μM. | 31715099 | ||
| 293T | Function assay | 30 mins | Activation of recombinant human STING haplotype R293Q mutant expressed in 293T cells measured after 30 mins in presence of digitonin A by bright Glo-luciferase reporter gene assay, EC50 = 0.05 μM. | 31715099 | ||
| 293T | Function assay | 30 mins | Activation of recombinant human STING haplotype R232H mutant expressed in 293T cells measured after 30 mins in presence of digitonin A by bright Glo-luciferase reporter gene assay, EC50 = 0.07 μM. | 31715099 | ||
| 293T | Function assay | 7 hrs | Activation of recombinant human wild-type STING expressed in 293T cells incubated for 7 hrs in absence of digitonin A by bright Glo-luciferase reporter gene assay, EC50 = 13.7 μM. | 31715099 | ||
| THP1 | Function assay | 20 hrs | Agonist activity at STING in human THP1 cells assessed as stimulation of IRF3 pathway measured after 20 hrs by luciferase reporter gene assay, EC50 = 38.6 μM. | 31820985 | ||
| PBMC | Function assay | 69.6 uM | 4 hrs | Agonist activity at STING in human PBMC cells assessed as increase in CXCL10 mRNA level at 69.6 uM measured after 4 hrs by qRT-PCR analysis | 31820985 | |
| PBMC | Function assay | 1.39 to 139 uM | 4 hrs | Agonist activity at STING in human PBMC cells assessed as increase in IFNbeta release at 1.39 to 139 uM measured after 4 hrs by ELISA | 31820985 | |
| PBMC | Function assay | 69.6 uM | 4 hrs | Agonist activity at STING in human PBMC cells assessed as increase in IFNbeta mRNA level at 69.6 uM measured after 4 hrs by qRT-PCR analysis | 31820985 | |
| PBMC | Function assay | 69.6 uM | 4 hrs | Agonist activity at STING in human PBMC cells assessed as increase in IL6 mRNA level at 69.6 uM measured after 4 hrs by qRT-PCR analysis | 31820985 | |
| PBMC | Function assay | 139 uM | 4 hrs | Agonist activity at STING in human PBMC cells assessed as increase in IL6 production at 139 uM measured after 4 hrs by ELISA | 31820985 | |
| B16-OVA | Antitumor assay | Antitumor activity against mouse B16-OVA cells implanted in mouse assessed as tumour regression in injected flank at 10 ug administered intratumorally on day 6, 9 and 12 post implantation | 31500996 | |||
| B16-OVA | Antitumor assay | Antitumor activity against mouse B16-OVA cells implanted in mouse assessed as tumour regression in contralateral flank at 10 ug administered intratumorally on day 6, 9 and 12 post implantation | 31500996 | |||
| B16-OVA | Antitumor assay | Antitumor activity against mouse B16-OVA cells implanted in mouse assessed as higher number of mouse cured of tumors at 10 ug administered intratumorally on day 6, 9 and 12 post implantation | 31500996 | |||
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| Poids moléculaire | 718.37 | Formule | C20H22N10Na2O13P2 |
Stockage (À compter de la date de réception) | 3 years -20°C powder |
|---|---|---|---|---|---|
| N° CAS | 2734858-36-5 | -- | Stockage des solutions mères |
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In vitro |
DMSO
: 100 mg/mL
(139.2 mM)
Water : 100 mg/mL Ethanol : Insoluble |
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In vivo |
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Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)
Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny a pas de formulation in vivo dans la section Solubilité.)
Résultats du calcul :
Concentration de travail : mg/ml;
Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter dabord si la concentration dépasse la solubilité du DMSO du lot de médicament. )
Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouterμL PEG300, mélanger et clarifier, puis ajouterμL Tween 80, mélanger et clarifier, puis ajouter μL ddH2O, mélanger et clarifier.
Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouter μL Huile de maïs, mélanger et clarifier.
Note : 1. Veuillez vous assurer que le liquide est clair avant dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue, lors de lajout précédent, est une solution claire avant de procéder à lajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie chaud peuvent être utilisées pour faciliter la dissolution.
| Targets/IC50/Ki |
STING
(Cell-free assay) 3.79 nM(Kd)
|
|---|---|
| In vitro |
Le 2',3'-cGAMP est un second messager endogène produit par les cellules de mammifères. Le 2',3'-cGAMP est un ligand de haute affinité pour STING. Le 2',3'-cGAMP est un puissant inducteur des interférons de type I. La liaison du 2',3'-cGAMP induit des changements conformationnels de STING. |
Références |
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