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AX-024

Cat. No. M13560
AX-024 Structure
Size Price Availability Quantity
5mg USD 130  USD130 In stock
10mg USD 190  USD190 In stock
25mg USD 460  USD460 In stock
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Quality Control & Documentation
Biological Activity

AX-024 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 modulates cell signaling by targeting SH3 domains. AX-024 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.

Chemical Information
Molecular Weight 339.4
CAS Number 1370544-73-2
Solubility (25°C) Ethanol 90 mg/mL
DMSO 35 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Yolanda Ramrez, et al. Sensors (Basel). New Label-Free Biosensing for the Evaluation of the AX-024 Inhibitor: Case Study for the Development of New Drugs in Autoimmune Diseases

[2] Kirsten Richter, et al. J Biol Chem. Reply to Alarcon and Borroto: Small molecule AX-024 reduces T cell proliferation independently of CD3ε-Nck1 interaction at SH3.1

[3] Balbino Alarcon, et al. J Biol Chem. Small molecule AX-024 targets T cell receptor signaling by disrupting CD3ε-Nck interaction

[4] Kirsten Richter, et al. J Biol Chem. 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

[5] Claudia Juraske, et al. Front Immunol. Anti-CD3 Fab Fragments Enhance Tumor Killing by Human γδ T Cells Independent of Nck Recruitment to the γδ T Cell Antigen Receptor

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Keywords: AX-024 supplier, TNF Receptor, inhibitors, activators


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