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Delanzomib

Chemical Structure : Delanzomib

CAS No.: 847499-27-8

Delanzomib (CEP-18770;CEP18770;CEP 18770)

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

A potent, orally active proteasome inhibitor with IC50 of 3.8 nM against chymotrypsin-like proteasome activity.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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

Blood Cancer

Phase 1 Discontinued

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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