AZ084
Based on 2 publication(s) in Google Scholar
AZ084 is a potent, selective, allosteric and oral active CCR8 allosteric antagonist, with a Ki of 0.9 nM. Has potential to treat asthma. AZ084 restrains the formation of the immunologically tolerant pre-metastatic niche (PMN) and tumor cells metastasis in lung by downregulating Treg differentiation. AZ084 can be used in studies of asthma and cancer.
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- Pureza: 99.70%
- No. CAS: 929300-19-6
- Fòrmula: C26H34N4O2
- Peso molecular:434.57
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) AZ084
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Actividad biológica
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CCR8 0.9 nM (Ki) |
AZ084 (5 μg/mL; single daily for 4 days) suppresses proportion of Tregs and reduces T cells that expresses CCR8 (co-cultured in vitro with LLC-exo MPF CM)[1].
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AZ084 (0-10 μM) inhibits AML, DC and T cells with IC50s of 1.3, 4.6 and 5.7 nM, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Splenic T cells
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Concentration:5 μg/mL (single daily)
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Incubation Time:4 days
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Result:Reversed the increased proportion of Tregs among the CD4+ T cells co-cultured in vitro with LLC-exo MPF CM.
Reduced T cells that expressed CCR8 (cultured in vitro with by LLC-exo MPF CM).
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Cell Line:AML, DC and T cells
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Concentration:0-10 µM
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Incubation Time:
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Result:Showed high potency with pronounced dose-response dependent inhibition of chemotaxis with an IC50 of 1.3 nM in AML cells.
? AZ084 (434.57-869.14 mg/kg; i.v.; single) shows a bioavailability >70% in rats[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 J mice (subcutaneous LLC tumor model)[1].
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Dosage:5 mg/kg
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Administration:Intraperitoneal injection, every third day for 9 or 21 days.
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Result:Inhibited Treg differentiation and tumor cell colonization of the lungs and reduced the number of CD4+Foxp3+ Tregs in the lungs of LLC-exo pre-injected mice (every third day for 9 days).
Inhibited the LLC-exo-induced LLC cell seeding in lung and also significantly reduced Treg accumulation in LLC-exo stimulated mouse lungs(every third day for 21 days).
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Animal Model:Female Balb/C mice, male Wistar rats and female Beagle dogs[2].
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Dosage:434.57-869.14 mg/kg (in 0.9% NaCl)
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Administration:Intravenous injection, single.
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Result:
1.19 Pharmacokinetic Parameters of AZ084 in Female Balb/C mice, male Wistar rats and female Beagle dogs[2].
IV (434.57-869.14 mg/kg) Dog plasma protein binding (% free) 45.7 Mu plasma protein binding (% free) 55.6 Hu plasma protein binding (% free) 31.0 Rat plasma protein binding (% free) 47.0 Rat HW plasma PK CL (mL/min/kg) 15.0 Rat HW plasma PK Vss (L/kg) 6.0 Rat HW plasma PK T1/2 (h) 5.4 Rat HW plasma PK Cmax (µM) 0.5 Rat HW plasma PK bioavailability (%) 68.0
Chemical Information
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No. CAS 929300-19-6
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Appearance Solid
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Peso molecular 434.57
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Fòrmula C26H34N4O2
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Color Light yellow to yellow
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SMILES
O=C(C1=NC=C(N)C=C1)N2CCC3(CCN(CC4=C5CC(C)(C)OC5=CC=C4)CC3)CC2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Nat Commun
2021 Dec 8;12(1):7122. PMID: 34880260 -
Nat Commun
Midkine activation of CD8+ T cells establishes a neuron-immune-cancer axis responsible for low-grade glioma growth. [Abstract]2020 May 1;11(1):2177. PMID: 32358581
Solvente y solubilidad
DMSO : 250 mg/mL (575.28 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.79 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.79 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Wang M, et al. Tumor-derived exosomes drive pre-metastatic niche formation in lung via modulating CCL1+ fibroblast and CCR8+ Treg cell interactions. Cancer Immunol Immunother. 2022 Apr 15. [Content Brief]
[2]. Connolly S, et al. Orally bioavailable allosteric CCR8 antagonists inhibit dendritic cell, T cell and eosinophil migration. Biochem Pharmacol. 2012 Mar 15;83(6):778-87. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3011 mL | 11.5056 mL | 23.0113 mL | 57.5281 mL |
| 5 mM | 0.4602 mL | 2.3011 mL | 4.6023 mL | 11.5056 mL | |
| 10 mM | 0.2301 mL | 1.1506 mL | 2.3011 mL | 5.7528 mL | |
| 15 mM | 0.1534 mL | 0.7670 mL | 1.5341 mL | 3.8352 mL | |
| 20 mM | 0.1151 mL | 0.5753 mL | 1.1506 mL | 2.8764 mL | |
| 25 mM | 0.0920 mL | 0.4602 mL | 0.9205 mL | 2.3011 mL | |
| 30 mM | 0.0767 mL | 0.3835 mL | 0.7670 mL | 1.9176 mL | |
| 40 mM | 0.0575 mL | 0.2876 mL | 0.5753 mL | 1.4382 mL | |
| 50 mM | 0.0460 mL | 0.2301 mL | 0.4602 mL | 1.1506 mL | |
| 60 mM | 0.0384 mL | 0.1918 mL | 0.3835 mL | 0.9588 mL | |
| 80 mM | 0.0288 mL | 0.1438 mL | 0.2876 mL | 0.7191 mL | |
| 100 mM | 0.0230 mL | 0.1151 mL | 0.2301 mL | 0.5753 mL |
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