AX-024 free base | CAS# 1370544-73-2 | TCR-triggered T cell activation inhibitor

MedKoo Cat#: 574574 | Name: AX-024 free base

Featured

Description:

WARNING: This product is for research use only, not for human or veterinary use.

AX-024 is an inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation. AX-024 modulates cell signaling by targeting SH3 domains and has low-acute toxicity and high potency and selectivity in the inhibition of the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.

Chemical Structure

AX-024 free base

CAS#1370544-73-2 (free base)

Theoretical Analysis

MedKoo Cat#: 574574

Name: AX-024 free base

CAS#: 1370544-73-2 (free base)

Chemical Formula: C21H22FNO2

Exact Mass: 339.1635

Molecular Weight: 339.41

Elemental Analysis: C, 74.31; H, 6.53; F, 5.60; N, 4.13; O, 9.43

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 295.00	2 Weeks
25mg	USD 650.00	2 Weeks

Bulk Inquiry

Buy Now

Add to Cart

Related CAS #

1370544-73-2 (free base) 1704801-24-0 (HCl)

Synonym

AX-024, AX024, AX 024; AX-024 free base

IUPAC/Chemical Name

1-((4-(4-fluorophenyl)-6-methoxy-2H-chromen-3-yl)methyl)pyrrolidine

InChi Key

VMMKGVRPILDZML-UHFFFAOYSA-N

InChi Code

InChI=1S/C21H22FNO2/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

SMILES Code

COC1=CC(C(C2=CC=C(F)C=C2)=C(CN3CCCC3)CO4)=C4C=C1

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

AX-024 is an inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM.

In vitro activity:

AX-024 reduces T cell proliferation upon weak T cell receptor (TCR) stimulation but neither significantly affects phosphorylation of Zap70 (ζ chain of T cell receptor–associated protein kinase 70) nor interacts directly with Nck1-SH3. AX-024 is likely not involved in modulating the Nck/TCR interaction but probably has other targets in T cells. An array of biophysical techniques did not detect a direct interaction between AX-024 and Nck-SH3.1 in vitro. Reference: J Biol Chem. 2020 Jun 5;295(23):7849-7864. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7278359/#B11

In vivo activity:

TBD

	Solvent	mg/mL	mM
Solubility
	DMSO	35.0	103.12
	Ethanol	100.0	294.63

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 339.41 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Richter K, Rufer AC, Muller M, Burger D, Casagrande F, Grossenbacher T, Huber S, Hug MN, Koldewey P, D'Osualdo A, Schlatter D, Stoll T, Rudolph MG. Small molecule AX-024 reduces T cell proliferation independently of CD3ϵ/Nck1 interaction, which is governed by a domain swap in the Nck1-SH3.1 domain. J Biol Chem. 2020 Jun 5;295(23):7849-7864. doi: 10.1074/jbc.RA120.012788. Epub 2020 Apr 21. PMID: 32317279; PMCID: PMC7278359.

In vitro protocol:

In vivo protocol:

TBD

1. Richter K, Rufer AC, Muller M, et al. Small molecule AX-024 reduces T cell proliferation independently of CD3ϵ/Nck1 interaction, which is governed by a domain swap in the Nck1-SH3.1 domain. J Biol Chem. 2020;295(23):7849-7864. doi:10.1074/jbc.RA120.012788 2. Alarcon B, Borroto A. Small molecule AX-024 targets T cell receptor signaling by disrupting CD3ε-Nck interaction. J Biol Chem. 2020;295(29):10076. doi:10.1074/jbc.L120.014338