Apratastat

Apratastat (TMI-005) is an orally active, non-selective and reversible TACE/MMPs inhibitor, can inhibit inhibit the release of TNF-α. Apratastat has the potential to overcome radiotherapy-resistance in non-small cell lung cancer (NSCLC) [1][2]. Apratastat is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Product Specifications

CAS Number

[287405-51-0]

Product Name Alternative

TMI-005

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

MMP; TNF Receptor

Type

Reference compound

Related Pathways

Apoptosis; Metabolic Enzyme/Protease

Applications

Neuroscience-Neurodegeneration

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/apratastat.html

Purity

99.29

Solubility

DMSO : ≥ 100 mg/mL

Smiles

CC1(C)[C@H](C(NO)=O)N(S(=O)(C2=CC=C(OCC#CCO)C=C2)=O)CCS1

Molecular Formula

C17H22N2O6S2

Molecular Weight

414.50

Precautions

H302, H315, H319, H335

References & Citations

[1]Shu C, et al. Pharmacokinetic-pharmacodynamic modeling of apratastat: a population-based approach. J Clin Pharmacol. 2011 Apr;51 (4) :472-81.|[2]Ieguchi K, et al. Savior or not: ADAM17 inhibitors overcome radiotherapy-resistance in non-small cell lung cancer. J Thorac Dis. 2016 Aug;8 (8) :E813-5. |[3]Lartey NL, et al. ADAM17/MMP inhibition prevents neutrophilia and lung injury in a mouse model of COVID-19. J Leukoc Biol. 2022 Jun;111 (6) :1147-1158.|[4]Stalin J, et al. Targeting of the NOX1/ADAM17 Enzymatic Complex Regulates Soluble MCAM-Dependent Pro-Tumorigenic Activity in Colorectal Cancer. Biomedicines. 2023 Nov 30;11 (12) :3185.