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Delanzomib

Chemical Structure : Delanzomib

CAS No.: 847499-27-8

Delanzomib (CEP-18770, CEP18770)

Catalog No.: PC-42597Not For Human Use, Lab Use Only.

Delanzomib (CEP18770) is a potent, orally active proteasome inhibitor with IC50 of 3.8 nM against chymotrypsin-like proteasome activity.

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Biological Activity

Delanzomib (CEP18770) is a potent, orally active proteasome inhibitor with IC50 of 3.8 nM against chymotrypsin-like proteasome activity.
Delanzomib demonstrates marginal inhibition of the tryptic and peptidyl glutamyl activities of the proteosome.
Delanzomib down-modulates the NF-kappaB activity and the expression of several NF-kappaB downstream effectors, induces apoptotic cell death in MM cells.
Delanzomib demonstrates tumor regression in MM xenografts with favorable tumor selectivity profile.

Physicochemical Properties

M.Wt 413.2751
Formula C21H28BN3O5
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Boronic acid, B-[(1R)-1-[[(2S,3R)-3-hydroxy-1-oxo-2-[[(6-phenyl-2-pyridinyl)carbonyl]amino]butyl]amino]-3-methylbutyl]-

References

1. Piva R, et al. Blood. 2008 Mar 1;111(5):2765-75.

2. Sanchez E, et al. Br J Haematol. 2010 Feb;148(4):569-81.

3. Seavey MM, et al. Int Immunopharmacol. 2012 Jan;12(1):257-70.

4. Berkers CR, et al. Mol Pharm. 2012 May 7;9(5):1126-35.

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