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| 10mg |
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| 25mg |
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| 100mg |
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Purity: ≥98%
AX-024 is a novel, potent and orally bioavailable inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation (IC50 1 nM). A wide range of autoimmune and inflammatory diseases caused by human T cells may be treated by blocking an immediate TCR signal.
| Targets |
IL-6; IL-10; IL-17A
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|---|---|
| ln Vitro |
Compared to AX-000 hit, AX-024 hydrochloride has a potency that is >10,000-fold greater in terms of preventing TCR-triggered T cell proliferation. AX-024 hydrochloride has an inhibitory effect at a concentration of 1 pM or less, but its IC50 in this assay is 1 nM. At a concentration of 10 nM, AX-024 hydrochloride significantly outperforms AX-000 as an inhibitor of cytokine release by human peripheral blood mononuclear cells stimulated with anti-CD3 and significantly reduces the production of interleukin-6 (IL-6), tumor necrosis factor-α (TNFα), interferon-γ (IFN-γ), IL-10, and IL-17A. AX-024 hydrochloride strongly inhibits T cell proliferation in OT1Tg T cells that are WT for the PRS mutation in mice bearing wild-type (WT) CD8+ T cells at a concentration of 0.1 nM. In these cells, coimmunoprecipitation experiments demonstrate that Nck recruitment to the TCR is induced upon stimulation in the absence of drug but is inhibited in the presence of AX-024 hydrochloride in a dose-dependent manner at concentrations beginning at 1 nM[1].
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| ln Vivo |
In comparison to the vehicle group, the AX-024 hydrochloride-treated group has fewer scales and lessened skin thickening. Significantly lessening the thickness of both skin layers, AX-024 hydrochloride works best on the dermis, which resembles the skin of mice treated with a control cream devoid of imiquimod (IMQ). In both assays, AX-024 hydrochloride significantly reduces the quantity of inflammatory cells in the airways. In contrast to mice receiving the vehicle, which experience persistent ataxia and loss of the righting reflex, mice receiving AX-024 hydrochloride experience a rapid recovery from neurological impairment and weight loss, becoming symptom-free by day 30[1].
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| Cell Assay |
Cell Trace Violet is used to mark the spleen B cells from C57BL/6 mice. The cells are then incubated for 72 hours with either anti-IgM (10 mg/mL) or anti-CD40 (5 mg/mL), as well as IL-4 (5 ng/mL) or LPS (2.5 mg/mL), in the presence of various concentrations of AX-024 hydrochloride. According to the total number of cell divisions, proliferation is calculated[1].
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| References |
| Molecular Formula |
C21H23CLFNO2
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|---|---|
| Molecular Weight |
375.8684
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| Exact Mass |
375.1401
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| Elemental Analysis |
C, 67.11; H, 6.17; Cl, 9.43; F, 5.05; N, 3.73; O, 8.51
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| CAS # |
1704801-24-0
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| Related CAS # |
AX-024;1370544-73-2
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| Appearance |
Solid powder
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| SMILES |
COC1=CC2=C(C=C1)OCC(=C2C3=CC=C(C=C3)F)CN4CCCC4.Cl
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| InChi Key |
DGBCIMPGYRVTPD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H22FNO2.ClH/c1-24-18-8-9-20-19(12-18)21(15-4-6-17(22)7-5-15)16(14-25-20)13-23-10-2-3-11-23;/h4-9,12H,2-3,10-11,13-14H2,1H3;1H
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| Chemical Name |
1-[[4-(4-fluorophenyl)-6-methoxy-2H-chromen-3-yl]methyl]pyrrolidine;hydrochloride
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| Synonyms |
AX-024 hydrochloride; AX-024; AX 024; AX024 HCl
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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: ~75 mg/mL (~199.5 mM)
Water: ~4 mg/mL (~10.6 mM) Ethanol: ~18 mg/mL (~47.9 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.65 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 25.0 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: ≥ 2.5 mg/mL (6.65 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 25.0 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: ≥ 2.5 mg/mL (6.65 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 | 2.6605 mL | 13.3025 mL | 26.6049 mL | |
| 5 mM | 0.5321 mL | 2.6605 mL | 5.3210 mL | |
| 10 mM | 0.2660 mL | 1.3302 mL | 2.6605 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02546635 | Completed | Drug: AX-024.HCl | Healthy | Artax Biopharma Inc | August 2015 | Phase 1 |
| NCT02243683 | Completed | Drug: AX-024.HCl Other: Placebo |
Healthy Volunteers | Artax Biopharma Inc | September 2014 | Phase 1 |
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