CEP-18770 (Delanzomib) , 97% , 847499-27-8

CAS NO.：847499-27-8

Empirical Formula: C21H28BN3O5

Molecular Weight: 413.28

MDL number: MFCD18251439

PRODUCT Properties

• Melting point: 178-190°C (dec.)
• Density: 1.207
• storage temp.: Hygroscopic, -20°C Freezer, Under Inert Atmosphere
• solubility: Acetonitrile (Slightly), Chloroform (Slightly), Methanol (Slightly)
• form: Solid
• pka: 9.67±0.43(Predicted)
• color: White to Off-White
• Stability: Hygroscopic

Description and Uses

Delanzomib is an orally bioavailable inhibitor of chymotrypsin-like proteasome activity (IC₅₀ = 3.8 nM in isolated human erythrocytes) that only marginally inhibits tryptic and peptidyl glutamyl proteasome activity. Delanzomib pre-treatment (20 nM) in vitro inhibits IκBα degradation, NF-κB activation, and the expression of NF-κB-regulated genes, including IκBα, XIAP, TNF-α, IL-1β, ICAM-1, and VEGF. Delanzomib induces apoptosis in multiple myeloma cell lines and inhibits proliferation in a panel of human hematologic and solid tumor cell lines (IC₅₀s = 5.6-34.2 nM). It reduces tumor weight in an RPMI 8226 human multiple myeloma mouse xenograft model when administered intravenously at doses ranging from 1.5-4 mg/kg twice daily and leads to complete tumor regression at a chronic oral dose of 13 mg/kg. Delanzomib reduces the serum level of circulating cytokines, prevents renal tissue damage, and increases lifespan in a mouse model of fatal lupus nephritis.

Delanzomib is an orally active proteasome inhibitor. Delanzomib has been shown to down-modulate NF-κB, induce apoptosis, inhibit angiogenesis and M-CSF-RANKL-induced osteoclastogenesis.

Safety

• Symbol(GHS): GHS07
• Signal word: Warning
• Hazard statements: H315-H319-H335
• Precautionary statements: P264-P280-P302+P352-P321-P332+P313-P362-P305+P351+P338-P337+P313-P261-P271-P304+P340-P312-P403+P233-P405-P501
• HS Code: 29333990