ChemicalBook > CAS DataBase List > CEP-18770

CEP-18770

Product Name: CEP-18770
CAS No.: 847499-27-8
Chemical Name: CEP-18770
Synonyms: CS-252;CT 47098;CEP-18770;CIP 18770;NPH 007098;Delanzomib;Delanzomib, >=98%;Delanzomib, free base;CEP-18770 (DelanzoMib);DelanzoMib (CEP-18770)
CBNumber: CB42570998
Molecular Formula: C21H28BN3O5
Formula Weight: 413.28
MOL File: 847499-27-8.mol

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CEP-18770 Property

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

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Safety

HS Code: 29333990

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P321Specific treatment (see … on this label).

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P362Take off contaminated clothing and wash before reuse.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 23557
Product name: Delanzomib
Purity: ≥95%
Packaging: 1mg
Price: $32
Updated: 2024/03/01

Cayman Chemical

Product number: 23557
Product name: Delanzomib
Purity: ≥95%
Packaging: 5mg
Price: $122
Updated: 2024/03/01

Cayman Chemical

Product number: 23557
Product name: Delanzomib
Purity: ≥95%
Packaging: 10mg
Price: $214
Updated: 2024/03/01

Cayman Chemical

Product number: 23557
Product name: Delanzomib
Purity: ≥95%
Packaging: 50mg
Price: $911
Updated: 2024/03/01

Usbiological

Product number: 007917
Product name: Delanzomib
Packaging: 5mg
Price: $602
Updated: 2021/12/16

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CEP-18770 Chemical Properties,Usage,Production

Description

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.

Uses

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.

Definition

ChEBI: Delanzomib is a C-terminal boronic acid peptide inhibitor which induces apoptosis in multiple myeloma, hematological and solid tumor cell lines. It has a role as a proteasome inhibitor, an apoptosis inducer and an antineoplastic agent. It is a threonine derivative, a phenylpyridine, a C-terminal boronic acid peptide and a secondary alcohol. It is functionally related to a L-threonine.

in vivo

Delanzomib (CEP-18770; 7.8-13 mg/kg; oral administration; twice a week; for 4 weeks) treatment results in a more sustained pharmacodynamic inhibition of proteasome activity in tumors relative to normal tissues, complete tumor regression of multiple myeloma (MM) xenografts and improves overall median survival in a systemic model of human MM^[1].

Animal Model:	SCID mice injected with RPMI 8226 cells^[1]
Dosage:	7.8 mg/kg, 10 mg/kg, 13 mg/kg
Administration:	Oral administration; twice a week; for 4 weeks
Result:	Resulted in a more sustained pharmacodynamic inhibition of proteasome activity in tumors relative to normal tissues.

target

proteasome

References

[1] ROBERTO PIVA. CEP-18770: A novel, orally active proteasome inhibitor with a tumor-selective pharmacologic profile competitive with bortezomib.[J]. Blood, 2008: 2765-2775. DOI: 10.1182/blood-2007-07-100651
[2] MATTHEW M. SEAVEY. Novel, orally active, proteasome inhibitor, delanzomib (CEP-18770), ameliorates disease symptoms and glomerulonephritis in two preclinical mouse models of SLE[J]. International immunopharmacology, 2012, 12 1: Pages 257-270. DOI: 10.1016/j.intimp.2011.11.019

CEP-18770 Preparation Products And Raw materials

Raw materials

Preparation Products

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CEP-18770 Suppliers

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View Lastest Price from CEP-18770 manufacturers

Zhuozhou Wenxi import and Export Co., Ltd

Product: Delanzomib 847499-27-8
Price: US $15.00-10.00/KG
Min. Order: 1KG
Purity: 99%+ HPLC
Supply Ability: Monthly supply of 1 ton
Release date: 2021-07-10

Zhuozhou Wenxi import and Export Co., Ltd

Product: Delanzomib 847499-27-8
Price: US $15.00-10.00/KG
Min. Order: 1KG
Purity: 99%+ HPLC
Supply Ability: Monthly supply of 1 ton
Release date: 2021-07-09

Career Henan Chemical Co

Product: CEP-18770 847499-27-8
Price: US $2.00/KG
Min. Order: 1KG
Purity: 99
Supply Ability: 100kg
Release date: 2020-01-07

847499-27-8, CEP-18770Related Search:

CPI-455 Maritoclax GDC-0623 IMR-1 CHIR 99021 trihydrochloride LJI308 2-((2-Chlorophenyl)(phenyl)aMino)-N-(7-(hydroxyaMino)-7-oxoheptyl)pyriMidine-5-carboxaMide AZ191 HTH-01-015 GDC-0879 4-iodo-3-nitrobenzamide VBY-825 Bortezomib MLN9708 MK-2206 2HCl (R)-1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutylboronic acid Oprozomib Carfilzomib

CEP-18770

[(1R)-1-[[(2S,3R)-3-Hydroxy-2-[[(6-phenylpyridin-2-yl)carbonyl]amino]-1-oxobutyl]amino]-3-methylbutyl]boronic acid

CIP 18770

CT 47098

Delanzomib

NPH 007098

CEP-18770 (DelanzoMib)

DelanzoMib, Free Base, >99%

((R)-1-((2S,3R)-3-Hydroxy-2-(6-phenylpicolinaMido)butanaMido)-3-Methylbutyl)boronic acid

(R)-1-((2S,3R)-3-hydroxy-2-(2-phenylpicolinamido)butanamido)-3-methylbutan-2-ylboronic acid

Delanzomib [(1R)-1-[[(2S,3R)-3-Hydroxy-2-[[(6-phenylpyridin-2-yl)carbonyl]amino]-1-oxobutyl]amino]-3-methylbutyl]boronic acid

Delanzomib, >=98%

DelanzoMib (CEP-18770)

Boronic acid, B-[(1R)-1-[[(2S,3R)-3-hydroxy-1-oxo-2-[[(6-phenyl-2-pyridinyl)carbonyl]aMino]butyl]aMino]-3-Methylbutyl]-

CEP-18770;CEP 18770;CEP18770

CS-252

(1R)-1-[(2S,3R)-3-hydroxy-2-[(6-phenylpyridin-2-yl)formamido]butanamido]-3-methylbutyl]boronic acid

((R)-1-((2S,3R)-3-hydroxy-2-(6-phenylpicolinamido)butanamido)-3-methylbutan-2-yl)boronic acid

Delanzomib, 10 mM in DMSO

Delanzomib, free base

Delanzomib (CEP-18770) ，S1157

847499-27-8

C21H28BN3O5

Inhibitor

Inhibitors