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AX-024 HCl

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AX-024 HCl
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Cat #: V6003 CAS #: 1704801-24-0 Purity ≥ 98%

Description: 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).

References: Borroto A, et al. First-in-class inhibitor of the T cell receptor for the treatment of autoimmune diseases. Sci Transl Med. 2016 Dec 21;8(370):370ra184.

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Molecular Weight (MW)375.86
Molecular FormulaC21H23ClFNO2
CAS No.1704801-24-0
SMILES CodeCOC1=CC(C(C2=CC=C(F)C=C2)=C(CN3CCCC3)CO4)=C4C=C1.[H]Cl
SynonymsAX-024 hydrochloride; AX-024; AX 024; AX024 HCl;
ProtocolIn VitroAX-024 hydrochloride is >10,000-fold more potent than the AX-000 hit in terms of inhibition of TCR-triggered T cell proliferation. The IC50 of AX-024 hydrochloride in this assay is 1 nM, although it shows inhibitory effects at a concentration of 1 pM or less. AX-024 hydrochloride is also a much more potent inhibitor of cytokine release by human peripheral blood mononuclear cells stimulated with anti-CD3 than AX-000, strongly hindering interleukin-6 (IL-6), tumor necrosis factor-α (TNFα), interferon-γ (IFN-γ), IL-10, and IL-17A production at a concentration of 10 nM. In CD8+ T cells of OT1 TCR transgenic (OT1Tg) mice bearing wild-type (WT) AX-024 hydrochloride strongly inhibits T cell proliferation at a concentration of 0.1 nM when OT1Tg T cells are WT for the PRS mutation. Coimmunoprecipitation experiments in these cells show 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 starting from 1 nM.
In VivoThe AX-024 hydrochloride-treated group presents less scales and reduces skin thickening compare to the vehicle group. AX-024 hydrochloride significantly reduces thickening of both skin layers, but more effectively of the dermis, which rather resembles that of mice treated with a control cream lacking imiquimod (IMQ). AX-024 hydrochloride significantly diminishes the number of airway inflammatory cells in both assays. Mice receiving AX-024 hydrochloride rapidly recovers from neurological impairment and weight loss, becoming symptom-free by day 30, unlike mice that receives the vehicle, in which ataxia and loss of the righting reflex persist.
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
1mM2.6606 mL13.3028 mL26.6057 mL53.2113 mL
5mM0.5321 mL2.6606 mL5.3211 mL10.6423 mL
10mM0.2661 mL1.3303 mL2.6606 mL5.3211 mL
20mM0.1330 mL0.6651 mL1.3303 mL2.6606 mL
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