AdipoGen Life Sciences

Delanzomib [CEP-18770]

CHF 35.00

In stock

AG-CR1-3673-M0011 mgCHF 35.00

AG-CR1-3673-M0055 mgCHF 115.00

AG-CR1-3673-M02525 mgCHF 450.00

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Product Details
Synonyms	NPH 007098; CT 47098; CIP 18770; [(1R)-1-[[(2S,3R)-3-Hydroxy-2-[(6-phenylpyridine-2-carbonyl)amino]butanoyl]amino]-3-methylbutyl]boronic acid
Product Type	Chemical
Properties
Formula	C₂₁H₂₈BN₃O₅
MW	413.3
CAS	847499-27-8
Purity Chemicals	≥95% (¹H-NMR)
Appearance	White solid.
Solubility	Soluble in DMSO (20mg/ml) or ethanol (20mg/ml). Slightly soluble in chloroform or methanol. Poorly soluble in water (<1mg/ml).
Other Product Data	Note: Warming and sonication may be required when dissolving the compound in the solvent of choice. Stock solutions are stable for at least 1 month when stored at -20°C.
InChi Key	SJFBTAPEPRWNKH-CCKFTAQKSA-N
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
Shipping and Handling
Shipping	AMBIENT
Short Term Storage	+4°C
Long Term Storage	-20°C
Handling Advice	Keep cool and dry.
Use/Stability	Stable for at least 2 years after receipt when stored at -20°C.
Documents
MSDS	Download PDF
Product Specification Sheet
Datasheet	Download PDF

Description

Potent, selective, reversible orally bioavailable proteasome inhibitor. Synthetic P2 threonine boronic acid.
Targets the chymotrypsin-like β5 subunit of the constitutive 20S proteasome (IC₅₀=3.8nM). Cross-reacts and inhibits the caspase-like/peptidyl-glutamyl peptide-hydrolyzing (PGPH) β1 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-κB, induce apoptosis, inhibit angiogenesis and M-CSF-RANKL-induced osteoclastogenesis.

Product 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)

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