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Apratastat

CAT: 0804-HY-119307-01Size: 1 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-119307-01Size:1 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
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.
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 2
Isoform
TNFRSF5/CD40

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