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| 5mg |
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| 10mg |
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| 25mg |
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AZ084 (AZ-084) is a novel potent, orally bioactive, allosteric CCR8 antagonist with anticancer and anti-inflammatory effects. It inhibits CCR8 allosterically with a Ki of 0.9 nM. May be used for asthma and cancer.
| ln Vitro |
AZ084 (5 μg/mL; once daily for 4 days of cells) decreases CCR8-expressing T cells (externally co-cultured with LLC-exo MPF CM) and inhibits the fraction of Tregs [1]. AML, DC, and T cells are inhibited by AZ084 (0–10 μM) with IC50 values of 1.3, 4.6, and 5.7 nM, respectively [2].
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| ln Vivo |
Through the reduction of Treg cells, AZ084 (5 mg/kg; intraperitoneal injection; once every three days for 9 or 21 days) inhibits immune-tolerant PMN and tumor cell metastasis in the lungs [1]. /kg; intravenous dose; single) shown a stent bioavailability of greater than 70% [2].
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| Cell Assay |
Cell Viability Assay [1]
Cell Types: Spleen T cells Tested Concentrations: 5 μg/mL (once daily) Incubation Duration: 4 days Experimental Results: Reversal of increased Tregs in CD4+ T cells co-cultured with LLC-exo MPF CM in vitro proportion. Reduction in CCR8-expressing T cells (cultured in vitro by LLC-exo MPF CM). Cell viability assay[2] Cell Types: AML, DC and T Cells Tested Concentrations: 0-10 µM Incubation Duration: Experimental Results: Displayed high potency with clear dose-response dependent chemotaxis inhibition with IC50 in AML cells is 1.3 nM. |
| Animal Protocol |
Animal/Disease Models: C57BL/6 J mouse (subcutaneousLLC tumor model) [1].
Doses: 5 mg/kg Route of Administration: intraperitoneal (ip) injection, once every three days for 9 or 21 days. Experimental Results: LLC-exo pre-injected mice (once every three days for 9 days) inhibited Treg differentiation and tumor cell colonization in the lungs and diminished the number of CD4+Foxp3+ Tregs in the lungs. Inhibited LLC-exo-induced LLC cell seeding in the lungs and Dramatically diminished Treg accumulation in LLC-exo-stimulated mouse lungs (once every three days for 21 days). Animal/Disease Models: female balb/c (Bagg ALBino) mouse, male Wistar rats and female Beagle dogs [2]. Doses: 434.57-869.14 mg/kg (0.9% NaCl) Route of Administration: intravenous (iv) (iv)injection, single dose. Experimental Results: 1.19 pharmacokinetic/PK/PK parameters of AZ084 in female balb/c (Bagg ALBino) mouse, male Wistar rats and female Beagle dogs [2]. IV (434.57-869.14 mg/kg) Dog plasma protein bound (% free) 45.7 Mu Plasma protein bound (% free) 55.6 Hu Plasma protein bound (% free) 31.0 Rat plasma protein bound (% free) 4 |
| References |
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| Molecular Formula |
C26H34N4O2
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|---|---|
| Molecular Weight |
434.573766231537
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| Exact Mass |
434.268
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| CAS # |
929300-19-6
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| PubChem CID |
16065569
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.2
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
32
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| Complexity |
665
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(N1CCC2(CCN(CC3C4=C(OC(C4)(C)C)C=CC=3)CC2)CC1)C1C=CC(N)=CN=1
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| InChi Key |
WIGFMKMFRGRSDE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H34N4O2/c1-25(2)16-21-19(4-3-5-23(21)32-25)18-29-12-8-26(9-13-29)10-14-30(15-11-26)24(31)22-7-6-20(27)17-28-22/h3-7,17H,8-16,18,27H2,1-2H3
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| Chemical Name |
(5-aminopyridin-2-yl)-[9-[(2,2-dimethyl-3H-1-benzofuran-4-yl)methyl]-3,9-diazaspiro[5.5]undecan-3-yl]methanone
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~575.28 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.79 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.79 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.79 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3011 mL | 11.5056 mL | 23.0113 mL | |
| 5 mM | 0.4602 mL | 2.3011 mL | 4.6023 mL | |
| 10 mM | 0.2301 mL | 1.1506 mL | 2.3011 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(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.
(2) Be sure to add the solvent(s) in order.
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