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CEP-18770

CEP-18770 Structure
CEP-18770
  • CAS No.847499-27-8
  • Chemical Name:CEP-18770
  • CBNumber:CB42570998
  • Molecular Formula:C21H28BN3O5
  • Formula Weight:413.28
  • MOL File:847499-27-8.mol
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
  • FDA UNII 6IF28942WO
  • NCI Drug Dictionary delanzomib
Safety
  • HS Code  :29333990
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal word
  • Hazard statements
  • Precautionary statements

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
CEP-18770 Preparation Products And Raw materials
Raw materials
Preparation Products
CEP-18770 Suppliers
Global(126)Suppliers
  • Supplier：
    career henan chemical co
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    SIMAGCHEM CORP
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    Win-Win chemical CO., Limited
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    AFINE CHEMICALS LIMITED
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CEP-18770 Spectrum
847499-27-8, CEP-18770Related Search:
  • Inhibitors
  • Inhibitor
  • 抑制剂
  • 药靶配体
  • 细胞生物学试剂
  • 蛋白酶
  • 小分子抑制剂，天然产物
  • 抗肿瘤类药物及免疫抑制剂
  • 高纯试剂
  • C21H28BN3O5
  • 德兰佐米,10 MM DMSO 溶液
  • CEP-18770 (DELANZOMIB),蛋白酶体抑制剂
  • 蛋白酶体糜蛋白酶样活性抑制剂(DELANZOMIB)
  • 地兰佐米
  • [(1R)-1-[[(2S,3R)-3-羟基-1-氧代-2-[[(6-苯基-2-吡啶基)羰基]氨基]丁基]氨基]-3-甲基丁基]硼酸
  • 德兰佐米
  • 847499-27-8
  • Delanzomib, 10 mM in DMSO
  • ((R)-1-((2S,3R)-3-hydroxy-2-(6-phenylpicolinamido)butanamido)-3-methylbutan-2-yl)boronic acid
  • CEP-18770;CEP 18770;CEP18770
  • CS-252
  • (1R)-1-[(2S,3R)-3-hydroxy-2-[(6-phenylpyridin-2-yl)formamido]butanamido]-3-methylbutyl]boronic acid
  • Boronic acid, B-[(1R)-1-[[(2S,3R)-3-hydroxy-1-oxo-2-[[(6-phenyl-2-pyridinyl)carbonyl]aMino]butyl]aMino]-3-Methylbutyl]-
  • DelanzoMib (CEP-18770)
  • Delanzomib, >=98%
  • Delanzomib [(1R)-1-[[(2S,3R)-3-Hydroxy-2-[[(6-phenylpyridin-2-yl)carbonyl]amino]-1-oxobutyl]amino]-3-methylbutyl]boronic acid
  • (R)-1-((2S,3R)-3-hydroxy-2-(2-phenylpicolinamido)butanamido)-3-methylbutan-2-ylboronic acid
  • ((R)-1-((2S,3R)-3-Hydroxy-2-(6-phenylpicolinaMido)butanaMido)-3-Methylbutyl)boronic acid
  • DelanzoMib, Free Base, >99%
  • CEP-18770 (DelanzoMib)
  • NPH 007098
  • Delanzomib
  • CT 47098
  • CIP 18770
  • [(1R)-1-[[(2S,3R)-3-Hydroxy-2-[[(6-phenylpyridin-2-yl)carbonyl]amino]-1-oxobutyl]amino]-3-methylbutyl]boronic acid
  • CEP-18770

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