Home Categories Biochemical Engineering CEP-18770(Delanzomib)
A7013258

CEP-18770(Delanzomib) , 10mMinDMSO , 847499-27-8

CAS NO.:847499-27-8

Empirical Formula: C21H28BN3O5

Molecular Weight: 413.28

MDL number: MFCD18251439

Pack Size Price Stock Quantity
1ml RMB399.20 In Stock
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Update time: 2022-07-08

PRODUCT Properties

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

Description and Uses

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.

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.

Safety

HS Code  29333990

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