Exherin trifluoroacetate

CAS No. 1135237-88-5

Exherin trifluoroacetate( —— )

Catalog No. M17151 CAS No. 1135237-88-5

Exherin (ADH-1) is a cyclic pentapeptide vascular-targeting agent with potential antineoplastic and antiangiogenic activities.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
5MG 88 Get Quote
10MG 144 Get Quote
25MG 268 Get Quote
50MG 381 Get Quote
100MG 564 Get Quote
200MG Get Quote Get Quote
500MG Get Quote Get Quote
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Biological Information

  • Product Name
    Exherin trifluoroacetate
  • Note
    Research use only, not for human use.
  • Brief Description
    Exherin (ADH-1) is a cyclic pentapeptide vascular-targeting agent with potential antineoplastic and antiangiogenic activities.
  • Description
    Exherin (ADH-1) is a cyclic pentapeptide vascular-targeting agent with potential antineoplastic and antiangiogenic activities. ADH-1 selectively and competitively binds to and blocks N-cadherin, which may result in disruption of tumor vasculature, inhibition of tumor cell growth, and the induction of tumor cell and endothelial cell apoptosis.(In Vitro):ADH-1 (0.2 mg/mL) blocks collagen I-mediated changes in pancreatic cancer cells, and is highly effective at preventing cell motility that is induced by expression of N-cadherin. ADH-1 (0, 0.1, 0.2, 0.5 and 1.0 mg/mL) induces apoptosis in a dose-dependent and N-cadherin-dependent manner.(In Vivo):ADH-1 (50 mg/kg) significantly prevents tumor growth and metastasis in a mouse model for pancreatic cancer. ADH-1 prevents tumor cell invasion and metastasis in an orthotopic model for pancreatic cancer using N-cadherin overexpressing BxPC-3 cells. ADH-1, at the dosages evaluated, does not display either antiangiogenic activity in a rat aortic ring assay or antitumor potential in a PC3 subcutaneous xenograft tumor model. ADH-1 (10 mL/kg, i.p.) augmentation of melanoma tumor growth is overcome through its ability to make regionally infused melphalan more effective. ADH-1 mediated augmentation of melanoma tumor growth is not altered by regionally infused temozolomide. In A375, but not DM443 xenografts, ADH-1 treatment increases phosphorylation of AKT at serine 473. ADH-1 slightly diminishes N-cadherin expression in both xenografts.
  • In Vitro
    ADH-1 (0.2 mg/mL) blocks collagen I-mediated changes in pancreatic cancer cells, and is highly effective at preventing cell motility that is induced by expression of N-cadherin. ADH-1 (0, 0.1, 0.2, 0.5 and 1.0 mg/mL) induces apoptosis in a dose-dependent and N-cadherin-dependent manner.
  • In Vivo
    ADH-1 (50 mg/kg) significantly prevents tumor growth and metastasis in a mouse model for pancreatic cancer. ADH-1 prevents tumor cell invasion and metastasis in an orthotopic model for pancreatic cancer using N-cadherin overexpressing BxPC-3 cells. ADH-1, at the dosages evaluated, does not display either antiangiogenic activity in a rat aortic ring assay or antitumor potential in a PC3 subcutaneous xenograft tumor model. ADH-1 (10 mL/kg, i.p.) augmentation of melanoma tumor growth is overcome through its ability to make regionally infused melphalan more effective. ADH-1 mediated augmentation of melanoma tumor growth is not altered by regionally infused temozolomide. In A375, but not DM443 xenografts, ADH-1 treatment increases phosphorylation of AKT at serine 473. ADH-1 slightly diminishes N-cadherin expression in both xenografts.
  • Synonyms
    ——
  • Pathway
    TGF-beta/Smad
  • Target
    TGFBR
  • Recptor
    N-cadherin
  • Research Area
    Cancer
  • Indication
    ——

Chemical Information

  • CAS Number
    1135237-88-5
  • Formula Weight
    684.71
  • Molecular Formula
    C24H35F3N3O3S2
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO : ≥ 43 mg/mL 62.80 mM
  • SMILES
    S1SC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](C1)NC(=O)C)Cc1nc[nH]c1)C)C(C)C)C(=O)N.C(=O)(C(F)(F)F)O
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Perotti A,etal.Ann Oncol. 2009 Apr;20(4):741-5.
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