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ProductsBack/Delanzomib [CEP-18770] [847499-27-8]
Chemical Structure
Chemical Structure
Chemical Structure

Delanzomib [CEP-18770] [847499-27-8]

Research Use Only
AG-CR1-3673
AdipoGen Life Sciences
Estimated Purity>98%
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Product group Chemicals
Molecular Weight413.3
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Overview

  • Supplier
    AdipoGen Life Sciences
  • Product Name
    Delanzomib [CEP-18770] [847499-27-8]
  • Delivery Days Customer
    10
  • Certification
    Research Use Only
  • Estimated Purity
    >98%
  • Hazard Information
    Non-hazardous,Warning
  • Molecular Formula
    C21H28BN3O5
  • Molecular Weight
    413.3
  • Scientific Description
    Chemical. CAS: 847499-27-8. Formula: C21H28BN3O5. MW: 413.3. Synthetic. Potent, selective, reversible orally bioavailable proteasome inhibitor. Synthetic P2 threonine boronic acid. Targets the chymotrypsin-like beta5 subunit of the constitutive 20S proteasome (IC50=3.8nM). Cross-reacts and inhibits the caspase-like/peptidyl-glutamyl peptide-hydrolyzing (PGPH) beta1 subunit (IC50=~70nM). Displays similar potency for the chymotrypsin-like activity of the proteasome compared to bortezomib. Exhibits a favorable cytotoxicity profile toward normal human epithelial cells, bone marrow progenitors and bone marrow-derived stromal cells relative to bortezomib. Anticancer compound effective against multiple myeloma in vivo. In vitro, blocks the growth of representative human solid and hematological tumor cell lines (IC50s=5.6-34nM). Shown to down-modulate NF-kappaB, induce apoptosis, inhibit angiogenesis and M-CSF-RANKL-induced osteoclastogenesis. - Potent, selective, reversible orally bioavailable proteasome inhibitor. Synthetic P2 threonine boronic acid. Targets the chymotrypsin-like beta5 subunit of the constitutive 20S proteasome (IC50=3.8nM). Cross-reacts and inhibits the caspase-like/peptidyl-glutamyl peptide-hydrolyzing (PGPH) beta1 subunit (IC50=~70nM). Displays similar potency for the chymotrypsin-like activity of the proteasome compared to bortezomib. Exhibits a favorable cytotoxicity profile toward normal human epithelial cells, bone marrow progenitors and bone marrow-derived stromal cells relative to bortezomib (Prod. No. AG-CR1-3602). Anticancer compound effective against multiple myeloma in vivo. In vitro, blocks the growth of representative human solid and hematological tumor cell lines (IC50s=5.6-34nM). Shown to down-modulate NF-kappaB, induce apoptosis, inhibit angiogenesis and M-CSF-RANKL-induced osteoclastogenesis.
  • SMILES
    CC(C)C[C@@H](B(O)O)NC([C@H]([C@H](O)C)NC(C1=NC(C2=CC=CC=C2)=CC=C1)=O)=O
  • Storage Instruction
    2°C to 8°C,-20°C
  • UNSPSC
    12352200

References

  • Discovery of a Potent, Selective, and Orally Active Proteasome Inhibitor for the Treatment of Cancer: B.D. Dorsey, et al.; J. Med. Chem. 51, 1068 (2008)
  • CEP-18770: A novel, orally active proteasome inhibitor with a tumor-selective pharmacologic profile competitive with bortezomib: R. Piva, et al.; Blood 111, 2765 (2008)
  • The proteasome inhibitor CEP-18770 enhances the anti-myeloma activity of bortezomib and melphalan: E. Sanchez, et al.; Br. J. Haematol. 148, 569 (2010)
  • Novel, orally active, proteasome inhibitor, delanzomib (CEP-18770), ameliorates disease symptoms and glomerulonephritis in two preclinical mouse models of SLE: M.M. Seavey, et al.; Int. Immunopharmacol. 12, 257 (2012)
  • Probing the specificity and activity profiles of the proteasome inhibitors bortezomib and delanzomib: C.R. Berkers, et al.; Mol. Pharm. 9, 1126 (2012)
  • Molecular mechanisms of acquired proteasome inhibitor resistance: A.J. Kale & B.S. Moore; J. Med. Chem. 55, 10317 (2012)
  • A first in human phase I study of the proteasome inhibitor CEP-18770 in patients with advanced solid tumours and multiple myeloma: E. Gallerani, et al.; Eur. J. Cancer 49, 290 (2013)
  • Proteasome inhibitors in the treatment of multiple myeloma: A. McBride & P.Y. Ryan; Expert Rev. Anticancer Ther. 13, 339 (2013) (Review)
  • Phase I/II study of the novel proteasome inhibitor delanzomib (CEP-18770) for relapsed and refractory multiple myeloma: D.T. Vogl, et al.; Leuk. Lymphoma 58, 1872 (2017)