1135237-88-5
Chemical Structure
ADH-1 TFA
Synonym(s): Exherin TFA
- CAS No.: 1135237-88-5
- Formula:C24H35F3N8O8S2
- Molecular Weight:684.71
IUPAC Name: (4R,7S,10S,13S,16R)-13-((1H-imidazol-5-yl)methyl)-16-acetamido-7-isopropyl-10-methyl-6,9,12,15-tetraoxo-1,2-dithia-5,8,11,14-tetraazacycloheptadecane-4-carboxamide 2,2,2-trifluoroacetate
InChIKey: RMLOJFSXNMROLS-BMLUHVGESA-N
SMILES: O=C([C@@H](NC([C@H](C(C)C)NC([C@H](C)NC([C@H](CC1=CN=CN1)N2)=O)=O)=O)CSSC[C@H](NC(C)=O)C2=O)N.O=C(O)C(F)(F)F
Biological Activity: ADH-1 TFA (Exherin TFA) is a cyclic pentapeptide N-cadherin antagonist. ADH-1 TFA binds to N-cadherin EC1-2 as an HAV mimetic, competitively blocks homophilic trans interactions, forms a stable protein-drug complex, and induces conformational rearrangement. ADH-1 TFA targets tumor microvasculature, causing vascular injury and apoptosis. ADH-1 TFA inhibits tumor growth and metastasis in mouse tumor models. ADH-1 TFA can be used in cancer-related research[1][2][3].
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ADH-1 TFA | 99.81% | ADH-1 TFA (Exherin TFA) is a cyclic pentapeptide N-cadherin antagonist. ADH-1 TFA binds to N-cadherin EC1-2 as an HAV mimetic, competitively blocks homophilic trans interactions, forms a stable protein-drug complex, and induces conformational rearrangement. ADH-1 TFA targets tumor microvasculature, causing vascular injury and apoptosis. ADH-1 TFA inhibits tumor growth and metastasis in mouse tumor models. ADH-1 TFA can be used in cancer-related research. | ||||||||||||||||||||
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References
- [1]. Jonker D J, et al. A phase I study of the novel molecularly targeted vascular targeting agent, Exherin (ADH-1), shows activity in some patients with refractory solid tumors stratified according to N-cadherin expression. J Clin Oncol, 2005, 23(16_suppl):3038.
- [2]. Perotti A, et al. Clinical and pharmacological phase I evaluation of ExherinTM (ADH-1), a selective anti-N-cadherin peptide in patients with N-cadherin-expressing solid tumours. Annals of Oncology, 2009, 20(4):741-745.
- [3]. Biswas J, et al. Modulation of N-cadherin-mediated homophilic trans interaction upon direct binding of ADH-1: Exploring the molecular basis of action of ADH-1 as N-cadherin inhibitor. Biochimie. 2026 Oct;249:141-149. [Content Brief]
