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MedKoo product information:
Exherin
Description of Exherin: Exherin,
also known as ADH-1, is a small, 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. N-cadherin, a cell- surface
transmembrane glycoprotein of the cadherin superfamily of proteins
involved in calcium-mediated cell-cell adhesion and signaling
mechanisms; may be upregulated in some aggressive tumors and the
endothelial cells and pericytes of some tumor blood vessels. Check for
active clinical trials or
closed clinical trials using this agent. (NCI
Thesaurus).
Current developer:
Adherix Technologies, Inc.
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MedKoo Code#: 201350
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Name: Exherin
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CAS#: 229971-81-7
Synonym:
Code name: NSC729477; ADH-1. Brand name: Exherin.
IUPAC/Chemical 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
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Chemical structure |
Theoretical analysis
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MedKoo Code#: 201350a
Name: Exherin (free base)
CAS#: 229971-81-7
Chemical Formula: C22H34N8O6S2
Exact Mass: 570.20427
Molecular Weight: 570.68
Elemental Analysis: C, 46.30; H, 6.01; N,
19.63; O, 16.82; S, 11.24
MedKoo Code#: 201350b
Name: Exherin-TFA (salt)
Chemical Formula: C22H34N8O6S2-TFA
(C24H35F3N8O8S2)
Molecular Weight: 684.71
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Availability and price:
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201350a || Exherin (free base), >98%
5 mg / $175.00, in stock
10 mg / $255.00, in stock
25 mg / $345.00, in stock
50 mg / $450.00, in stock
100 mg / $850.00, in stock
200 mg / $1,250.00, in stock
Grams available at low prices.
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201350b || Exherin-TFA salt, >98%
5 mg / $155.00, in stock
10 mg / $210.00, in stock
25 mg / $310.00, in stock
50 mg / $435.00, in stock
100 mg / $750.00, in stock
200 mg / $1,050.00, in stock0.00
Grams available at low prices.
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To inquire quotation and lead time or to ask questions, please send email to
sales@medkoo.com to describe your needs. A representative
will respond your email shortly. We offer big discount for orders of bulk quantities.
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Information about this agent
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1: Yarom N, Stewart D, Malik R, Wells J, Avruch L,
Jonker DJ. Phase I Clinical Trial of Exherin (ADH-1) in Patients with
Advanced Solid Tumors. Curr Clin Pharmacol. 2012 Jan 24. [Epub ahead of
print] PubMed PMID: 22280327.
2: Haseba T, Kameyama K, Mashimo K, Ohno Y. Dose-Dependent Change in
Elimination Kinetics of Ethanol due to Shift of Dominant Metabolizing
Enzyme from ADH 1 (Class I) to ADH 3 (Class III) in Mouse. Int J Hepatol.
2012;2012:408190. Epub 2011 Nov 22. PubMed PMID: 22164338; PubMed
Central PMCID: PMC3227458.
3: Yarom N, Stewart D, Avruch L, Malik R, Wells J, Jonker DJ. ADH-1 in
the treatment of metastatic adrenocortical carcinoma--case report.
Anticancer Res. 2011 Nov;31(11):3921-5. PubMed PMID: 22110220.
4: Beasley GM, Riboh JC, Augustine CK, Zager JS, Hochwald SN, Grobmyer
SR, Peterson B, Royal R, Ross MI, Tyler DS. Prospective multicenter
phase II trial of systemic ADH-1 in combination with melphalan via
isolated limb infusion in patients with advanced extremity melanoma. J
Clin Oncol. 2011 Mar 20;29(9):1210-5. Epub 2011 Feb 22. PubMed PMID:
21343562.
5: Beasley GM, McMahon N, Sanders G, Augustine CK, Selim MA, Peterson B,
Norris R, Peters WP, Ross MI, Tyler DS. A phase 1 study of systemic
ADH-1 in combination with melphalan via isolated limb infusion in
patients with locally advanced in-transit malignant melanoma. Cancer.
2009 Oct 15;115(20):4766-74. PubMed PMID: 19637344.
6: Perotti A, Sessa C, Mancuso A, Noberasco C, Cresta S, Locatelli A,
Carcangiu ML, Passera K, Braghetti A, Scaramuzza D, Zanaboni F, Fasolo
A, Capri G, Miani M, Peters WP, Gianni L. Clinical and pharmacological
phase I evaluation of Exherin (ADH-1), a selective anti-N-cadherin
peptide in patients with N-cadherin-expressing solid tumours. Ann Oncol.
2009 Apr;20(4):741-5. Epub 2009 Feb 3. PubMed PMID: 19190075.
7: Shintani Y, Fukumoto Y, Chaika N, Grandgenett PM, Hollingsworth MA,
Wheelock MJ, Johnson KR. ADH-1 suppresses N-cadherin-dependent
pancreatic cancer progression. Int J Cancer. 2008 Jan 1;122(1):71-7.
PubMed PMID: 17721921.
8: Kelland L. Drug evaluation: ADH-1, an N-cadherin antagonist targeting
cancer vascularization. Curr Opin Mol Ther. 2007 Feb;9(1):86-91. PubMed
PMID: 17330406.
9: Gomulski LM, Brogna S, Babaratsas A, Gasperi G, Zacharopoulou A,
Savakis C, Bourtzis K. Molecular basis of the size polymorphism of the
first intron of the Adh-1 gene of the mediterranean fruit fly, Ceratitis
capitata. J Mol Evol. 2004 Jun;58(6):732-42. PubMed PMID: 15461430.
10: Torney F, Partier A, Says-Lesage V, Nadaud I, Barret P, Beckert M.
Heritable transgene expression pattern imposed onto maize ubiquitin
promoter by maize adh-1 matrix attachment regions: tissue and
developmental specificity in maize transgenic plants. Plant Cell Rep.
2004 Jul;22(12):931-8. Epub 2004 May 4. PubMed PMID: 15127223.
11: Zheng YW, Felder MR. Genetic mapping of a possible new alcohol
dehydrogenase sequence to mouse chromosome 3 at the Adh-1/Adh-3 complex.
Biochem Genet. 1997 Apr;35(3-4):105-17. PubMed PMID: 9241435.
12: Xie D, Narasimhan P, Zheng YW, Dewey MJ, Felder MR. Ten kilobases of
5'-flanking region confers proper regulation of the mouse alcohol
dehydrogenase-1 (Adh-1) gene in kidney and adrenal of transgenic mice.
Gene. 1996 Nov 28;181(1-2):173-8. PubMed PMID: 8973327.
13: Yu M, Edenberg HJ. Structure and function of a long alternating
purine-pyrimidine sequence in the mouse alcohol dehydrogenase Adh-1
gene. Arch Biochem Biophys. 1995 Jan 10;316(1):407-12. PubMed PMID:
7840644..
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Contact MedKoo:
Email:
sales@medkoo.com
(Keyword; CAS#; MedKoo code#)
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