AX-024 hydrochloride

Name: AX-024 hydrochloride
Brand: MedChemExpress
SKU: HY-107390A
Rating: 5.0 (1 reviews)

Cat. No.: HY-107390A Purity: 99.75%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

AX-024 hydrochloride is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC₅₀ ~1 nM. AX-024 hydrochloride modulates cell signaling by targeting SH3 domains. AX-024 hydrochloride has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.

For research use only. We do not sell to patients.

AX-024 hydrochloride Chemical Structure

CAS No. : 1704801-24-0

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 66	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 66	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 90	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 190	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 350	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 650	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of AX-024 hydrochloride:

AX-024 In-stock

1 Publications Citing Use of MCE AX-024 hydrochloride

•Life Sci. 2020 May 1;248:117456. [Abstract]

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•Related Screening Libraries:

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TNFRSF1A/CD120a TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

View All Interleukin Related Isoform Specific Products:

View All Isoforms

IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

IL-6

IL-10

IL-17A

In Vitro

AX-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 (OT1^Tg) mice bearing wild-type (WT) AX-024 hydrochloride strongly inhibits T cell proliferation at a concentration of 0.1 nM when OT1^Tg 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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

The 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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

375.86

Formula

C₂₁H₂₃ClFNO₂

CAS No.

1704801-24-0

Appearance

Solid

Color

White to off-white

SMILES

COC1=CC=C(OC2)C(C(C3=CC=C(F)C=C3)=C2CN4CCCC4)=C1.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 33 mg/mL (87.80 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 16.67 mg/mL (44.35 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.6606 mL	13.3028 mL	26.6057 mL
5 mM	0.5321 mL	2.6606 mL	5.3211 mL
10 mM	0.2661 mL	1.3303 mL	2.6606 mL

View the 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.65 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.65 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.65 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.75%

Select Batch:

Data Sheet (278 KB) SDS (583 KB)

COA (251 KB) LCMS (265 KB)

Handling Instructions (2659 KB)

References

[1]. 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. [Content Brief]

Cell Assay ^[1]	Spleen B cells from C57BL/6 mice are labeled with Cell Trace Violet and incubated for 72 hours with either anti-IgM (10 mg/mL) or anti-CD40 (5 mg/mL), supplemented with IL-4 (5 ng/mL) or LPS (2.5 mg/mL) in the presence of different concentrations of AX-024 hydrochloride. Proliferation is calculated according to the total number of cell divisions^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Eight-week-old CD-1 mice are injected intraperitoneally with different amounts of the AX-024 hydrochloride dissolved in 0.5 mL of saline. All animals are observed clinically for the appearance of macroscopically visible adverse reactions twice daily over 14 days, as well as immediately after AX-024 hydrochloride administration. A necropsy is carried out on each animal on day 14, and the abdominal, thoracic, and cranial cavities are examined in situ, together with their associated organs^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. 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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	2.6606 mL	13.3028 mL	26.6057 mL	66.5141 mL
	5 mM	0.5321 mL	2.6606 mL	5.3211 mL	13.3028 mL
	10 mM	0.2661 mL	1.3303 mL	2.6606 mL	6.6514 mL
	15 mM	0.1774 mL	0.8869 mL	1.7737 mL	4.4343 mL
	20 mM	0.1330 mL	0.6651 mL	1.3303 mL	3.3257 mL
	25 mM	0.1064 mL	0.5321 mL	1.0642 mL	2.6606 mL
	30 mM	0.0887 mL	0.4434 mL	0.8869 mL	2.2171 mL
	40 mM	0.0665 mL	0.3326 mL	0.6651 mL	1.6629 mL
DMSO	50 mM	0.0532 mL	0.2661 mL	0.5321 mL	1.3303 mL
	60 mM	0.0443 mL	0.2217 mL	0.4434 mL	1.1086 mL
	80 mM	0.0333 mL	0.1663 mL	0.3326 mL	0.8314 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.