CEP-18770

• CAT Number: I005071
• CAS Number: 847499-27-8
• Molecular Formula: C₂₁H₂₈BN₃O₅
• Molecular Weight: 413.28
• Purity: ≥95%
• Target: Proteasome
• Solubility: DMSO 83 mg/mL; Water <1 mg/mL; Ethanol 83 mg/mL
• Storage: -20°C
• IC50: 3.8 nM
• IUPAC Name: [(1R)-1-[[(2S,3R)-3-hydroxy-2-[(6-phenylpyridine-2-carbonyl)amino]butanoyl]amino]-3-methylbutyl]boronic acid
• InChI: 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
• InChIKey: SJFBTAPEPRWNKH-CCKFTAQKSA-N
• SMILES: B(C(CC(C)C)NC(=O)C(C(C)O)NC(=O)C1=CC=CC(=N1)C2=CC=CC=C2)(O)O

Delanzomib（Cat No.:I005071）, also known as CEP-18770, is a novel orally-active inhibitor of the chymotrypsin-like activity of the proteasome. By targeting the proteasome, delanzomib effectively inhibits the degradation of proteins, leading to the down-modulation of nuclear factor-kappaB (NF-kappaB) activity. NF-kappaB is a transcription factor involved in various cellular processes, including inflammation and immune responses. By suppressing NF-kappaB activity, delanzomib has the potential to modulate these processes and may hold promise as a therapeutic agent for conditions associated with abnormal NF-kappaB signaling, such as cancer and autoimmune disorders.

Reference

1:Phase I/II study of the novel proteasome inhibitor delanzomib (CEP-18770) for relapsed and refractory multiple myeloma. Vogl DT, Martin TG, Vij R, Hari P, Mikhael JR, Siegel D, Wu KL, Delforge M, Gasparetto C.Leuk Lymphoma. 2017 Aug;58(8):1872-1879. doi: 10.1080/10428194.2016.1263842. Epub 2017 Jan 31. PMID: 28140719 2:CEP-18770 (delanzomib) in combination with dexamethasone and lenalidomide inhibits the growth of multiple myeloma. Sanchez E, Li M, Li J, Wang C, Chen H, Jones-Bolin S, Hunter K, Ruggeri B, Berenson JR.Leuk Res. 2012 Nov;36(11):1422-7. doi: 10.1016/j.leukres.2012.07.018. Epub 2012 Aug 17. PMID: 22906694 3:Probing the specificity and activity profiles of the proteasome inhibitors bortezomib and delanzomib. Berkers CR, Leestemaker Y, Schuurman KG, Ruggeri B, Jones-Bolin S, Williams M, Ovaa H.Mol Pharm. 2012 May 7;9(5):1126-35. doi: 10.1021/mp2004143. Epub 2012 Apr 16. PMID: 22432738 4:Novel, orally active, proteasome inhibitor, delanzomib (CEP-18770), ameliorates disease symptoms and glomerulonephritis in two preclinical mouse models of SLE. Seavey MM, Lu LD, Stump KL, Wallace NH, Ruggeri BA.Int Immunopharmacol. 2012 Jan;12(1):257-70. doi: 10.1016/j.intimp.2011.11.019. Epub 2011 Dec 13. PMID: 22178195