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

Canada 1 China 126 United States 16 Global 143
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
J & K SCIENTIFIC LTD.
Tel
18210857532; 18210857532
Fax
86-10-82849933
Email
jkinfo@jkchemical.com
Country
China
ProdList
96815
Advantage
76
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6003
Advantage
61
Chemsky（shanghai）International Co.,Ltd.
Tel
021-50135380
Email
shchemsky@sina.com
Country
China
ProdList
32321
Advantage
50
Jinan Trio PharmaTech Co., Ltd.
Tel
0531-88811783
Fax
+86 (531) 55696010 QQ 1762738062
Email
sales@trio-pharmatech.com
Country
China
ProdList
1856
Advantage
62
Shanghai Sphchem Co., Ltd.
Tel
021-56491756 13512199871
Fax
021-5649-1756
Email
2819742715@qq.com
Country
China
ProdList
4000
Advantage
55
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
sales@meilune.com
Country
China
ProdList
4747
Advantage
58
NCE Biomedical Co.,Ltd.
Tel
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988
Fax
+86-27-87599188
Country
China
ProdList
1493
Advantage
55
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
Country
China
ProdList
7552
Advantage
61
Shanghai Aladdin Bio-Chem Technology Co.,LTD
Tel
400-6206333 13167063860
Fax
021-50323701
Email
anhua.mao@aladdin-e.com
Country
China
ProdList
25003
Advantage
65
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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