ARP 101

ARP 101 (CAS 849773-64-4)

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Application: An inhibitor of metalloproteinase-2 (MMP-2)
CAS Number: 849773-64-4
Molecular Weight: 406.50
Molecular Formula: C20H26N2O5S
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* Refer to Certificate of Analysis for lot specific data (including water content).
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ARP 101 is a selective inhibitor of the MMP-2 (metalloproteinase-2 ) and, to lesser extent, MMP-9 (metalloproteinase-9), both of which have been shown to play a role in certain key functions of tumour cells, facilitating metastatic tumour dispersion and angiogenesis, resistance to apoptosis and actication of EGF receptors. Studies of ARP 101 show in vitro inhibition of HT1080 sarcoma cell growth on matrigel. ARP 101 has shown ~250 fold selectivity of MMP-2 over MMP-1 and ~100 fold of MMP-9 over MMP-1.


References

1. Coussens, L.M., et al. 2002. Science. 295: 2387-2392. PMID: 11923519
2. Rossello, A., et al. 2004. Bioorg. Med. Chem. 12: 2441-2450. PMID: 15080939
3. Tuccinardi, T., et al. 2006. Bioorg. Med. Chem. 14: 4260-4276. PMID: 16483784
4. Page-McCaw, A., et al. 2007. Nat. Rev. Mol. Cell Biol. 8: 221-233. PMID: 17318226

Physical State :
Solid
Solubility :
Soluble in DMSO (100 mM), and ethanol (25 mM). Insoluble in water.
Storage :
Desiccate at 4° C
Melting Point :
264.14° C
Boiling Point :
610.34° C
Density :
1.23 g/cm3
Refractive Index :
n20D 1.57
Optical Activity :
α20/D +94°, c = 0.01 in Chloroform
IC50 :
inhibitor of MMP-2 : IC50 = 0.81 nM; inhibitor of MMP-1: IC50 = 486 nM; Matrix metalloproteinase 8: IC50 = 1.6 nM (human); Matrix metalloproteinase-2: IC50 = 0.09 nM (human); Matrix metalloproteinase 12: IC50 = 0.2 nM (human); Matrix metalloproteinase 13: IC50 = 4.1 nM (human)
pK Values :
pKa: 9.17
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
Transport :
UN 2811, Class 6.1, Packing group III
PubChem CID :
11292680
MDL Number :
MFCD09753277
SMILES :
CC(C)[C@H](C(=O)NO)N(OC(C)C)S(=O)(=O)C1=CC=C(C=C1)C2=CC=CC=C2

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Certificate of Analysis

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ARP 101  Product Citations

See how others have used ARP 101. Click on the entry to view the PubMed entry .

Citations 1 to 1 of 1 total

PMID: # 23900029  Gyenge, M. et al. 2013. Life Sci. 93: 441-7.

Citations 1 to 1 of 1 total
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