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Description: Delanzomib (formerly known as CEP-18770) is a novel, potent, and orally bioactive inhibitor of the chymotrypsin-like (CL) activity of proteasome with potential antineoplastic activity. It inhibits CL-proteasome with an IC50 of 3.8 nM, and shows little inhibition against the tryptic and peptidylglutamyl activities of the proteosome. It demonstrate significant in vivo antitumor efficacy in human MM RPMI 8226 subcutaneous xenograft model in SCID mice.
References: Blood. 2008 Mar 1; 111(5):2765-75; Br J Haematol. 2010 Feb; 148(4):569-81; Nat Methods. 2005 May; 2(5):357-62.
Chemical Name: [(1R)-1-[[(2S, 3R)-3-Hydroxy-2-[[(6-phenylpyridin-2-yl)carbonyl]amino]-1-oxobutyl]amino]-3-methylbutyl]boronic acid.
InChi Key: SJFBTAPEPRWNKH-CCKFTAQKSA-N
InChi Code: InChI=1S/C21H28BN3O5/c1-13(2)12-18(22(29)30)24-21(28)19(14(3)26)25-20(27)17-11-7-10-16(23-17)15-8-5-4-6-9-15/h4-11, 13-14, 18-19, 26, 29-30H, 12H2, 1-3H3, (H, 24, 28)(H, 25, 27)/t14-, 18+, 19+/m1/s1
SMILES Code: CC(C)C[CH](B(O)O)NC([CH](NC(C1=NC(C2=CC=CC=C2)=CC=C1)=O)[CH](O)C)=O
CEP18770; CEP 18770; CEP-18770; Delanzomib
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