287405-51-0
Chemical Structure
Apratastat
Synonym(s): TMI-005
- CAS No.: 287405-51-0
- Formula:C17H22N2O6S2
- Molecular Weight:414.50
IUPAC Name: (S)-N-hydroxy-4-((4-((4-hydroxybut-2-yn-1-yl)oxy)phenyl)sulfonyl)-2,2-dimethylthiomorpholine-3-carboxamide
InChIKey: MAVDNGWEBZTACC-HNNXBMFYSA-N
SMILES: CC1(C)[C@H](C(NO)=O)N(S(=O)(C2=CC=C(OCC#CCO)C=C2)=O)CCS1
Biological Activity: 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.
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Apratastat | 99.28% | 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). 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. | ||||||||||||||||||||
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Apratastat (Standard) | ≥98% | Apratastat (Standard) is the analytical standard of Apratastat. This product is intended for research and analytical applications. 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). 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. | ||||||||||||||||||||
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References
- [1]. Shu C, et al. Pharmacokinetic-pharmacodynamic modeling of apratastat: a population-based approach. J Clin Pharmacol. 2011 Apr;51(4):472-81. [Content Brief]
- [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. [Content Brief]
