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Chemical Structure| 847499-27-8 Chemical Structure| 847499-27-8

Structure of Delanzomib
CAS No.: 847499-27-8

Chemical Structure| 847499-27-8

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Delanzomib is an orally active inhibitor of the chymotrypsin-like activity of proteasome with IC50 of 3.8 nM, with only marginal inhibition of the tryptic and peptidylglutamyl activities of the proteosome.

Synonyms: CEP-18770

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Product Details of Delanzomib

CAS No. :847499-27-8
Formula : C21H28BN3O5
M.W : 413.28
SMILES Code : CC(C)C[C@@H](B(O)O)NC([C@@H](NC(C1=NC(C2=CC=CC=C2)=CC=C1)=O)[C@H](O)C)=O
Synonyms :
CEP-18770
MDL No. :MFCD18251439
InChI Key :SJFBTAPEPRWNKH-CCKFTAQKSA-N
Pubchem ID :24800541

Safety of Delanzomib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H317-H319
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • 20S proteasome

    Chymotrypsin-like proteasome, IC50:3.8 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
GIST430 0.0001 μM–10 μM 72 hours Induced cell cycle arrest and apoptosis, IC50 of 12 nM PMC7083865
GIST48 0.0001 μM–10 μM 72 hours Induced cell cycle arrest and apoptosis, IC50 of 9 nM PMC7083865
GIST-T1 0.0001 μM–10 μM 72 hours Induced cell cycle arrest and apoptosis, IC50 of 36 nM PMC7083865
GIST882 0.0001 μM–10 μM 72 hours Induced cell cycle arrest and apoptosis, IC50 of 23 nM PMC7083865
HeLa cells 10 µM 16 hours To assess the effect of delanzomib on the plasma membrane expression levels of pathogenic pendrin variants. Results showed that delanzomib significantly increased the plasma membrane protein expression levels of these variants. PMC11913434
293 Phoenix cells 10 µM 16 hours To evaluate the rescuing effect of delanzomib on the ion transport function of pathogenic pendrin variants p.R409H and p.L236P. Results showed that delanzomib significantly increased the protein expression levels and ion transport function of these variants. PMC11913434
HepG2 cells 50 ng/ml 4 or 8 hours To investigate the effect of Delanzomib on FcRn degradation. Results showed that Delanzomib suppressed the degradation of FcRn. PMC8645831
MCF-7 10, 100, 1000, 10000 nM 6 hours To evaluate the inhibitory activity of Delanzomib on the β5 catalytic site of the 20S proteasome. Results showed 55% inhibition at 1000 nM and 100% inhibition at 10000 nM. PMC10825133
HEK293 cells 30 nM 6 hours Stimulated OAT3-mediated transport of estrone sulfate PMC7997269
COS-7 cells 30 nM 6 hours Increased accumulation of ubiquitinated OAT3 PMC7997269
HeLa cells 1 µM 16 hours Delanzomib increase total protein levels of wild‑type pendrin and its variants.
293 Phoenix cells 1-10 µM 16 hours Delanzomib rescues the function of pathogenic pendrin variants.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rats Collagen-induced arthritis (CIA) model Intravenous injection 0.1 mg Once a week for 8 weeks To evaluate the effect of Delanzomib on the severity of arthritis in CIA rats. Results showed that Delanzomib combined with adalimumab significantly ameliorated arthritis symptoms. PMC8645831
Mice UZLX-GIST1 and UZLX-GIST9 xenograft models Oral 8 mg/kg Twice a week for three weeks Showed significant antitumor activity in both IM-sensitive and IM-resistant GIST xenograft models PMC7083865

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00572637 Solid Tumors|Lymphoma, Non-Hod... More >>gkin Less << PHASE1 COMPLETED 2025-03-10 Europen Institute of Oncology,... More >> Milano, 20141, Italy|IOSI - Oncology Institute of Southern Switzerland - Ospedale S. Giovanni, Bellinzona, 6500, Switzerland|Kantonsspital St. Gallen, St. Gallen, 9007, Switzerland Less <<
NCT01348919 Multiple Myeloma Phase 1 Phase 2 Terminated - United States, Georgia ... More >> Teva Investigational Site 1 Augusta, Georgia, United States United States, Kentucky Teva Investigational Site 3 Lexington, Kentucky, United States United States, Texas Teva Investigational Site 2 Houston, Texas, United States New Zealand Teva Investigational Site 201 Auckland, New Zealand Teva Investigational Site 204 Auckland, New Zealand Teva Investigational Site 200 Christchurch, New Zealand Teva Investigational Site 206 Hamilton, New Zealand Teva Investigational Site 205 Newtown, New Zealand Teva Investigational Site 202 Palmerston North, New Zealand Teva Investigational Site 203 Takapuna, New Zealand Less <<
NCT01023880 Multiple Myeloma PHASE1|PHASE2 TERMINATED 2025-01-13 Mayo Clinic- Scottsdale, Scott... More >>sdale, Arizona, United States|University of Arkansas for Medical Sciences, Little Rock, Arkansas, United States|Stanford Heme Group, Palo Alto, California, United States|University of California, San Francisco, San Francisco, California, United States|Washington Cancer Institute, Washington, District of Columbia, United States|Northwestern University Medical School, Chicago, Illinois, United States|Henry Ford Health System Protocol Review Committee, Detroit, Michigan, United States|Sparrow Regional Cancer Center, Lansing, Michigan, United States|Washington University School of Medicine, St. Louis, Missouri, United States|John Theurer Cancer Center, Hackensack, New Jersey, United States|Duke University Medical Center, Durham, North Carolina, United States|University of Pennsylvania, Philadelphia, Pennsylvania, United States|Medical College of Wisconsin, Milwaukee, Wisconsin, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.42mL

0.48mL

0.24mL

12.10mL

2.42mL

1.21mL

24.20mL

4.84mL

2.42mL

References

 

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