1. Metabolic Enzyme/Protease
    NF-κB
    Apoptosis
  2. Proteasome
    NF-κB
    Apoptosis
  3. Delanzomib

Delanzomib (Synonyms: CEP-18770)

Cat. No.: HY-10454 Purity: ≥98.0%
Handling Instructions

Delanzomib (CEP-18770) is a potent and orally active chymotrypsin-like activity of the proteasome inhibitor with an IC50 of 3.8 nM. Delanzomib inhibits NF-κB activity, induces cancer cell apoptotic, and has strong antiangiogenic and anti-cancer activities.

For research use only. We do not sell to patients.

Delanzomib Chemical Structure

Delanzomib Chemical Structure

CAS No. : 847499-27-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 165 In-stock
Estimated Time of Arrival: December 31
5 mg USD 150 In-stock
Estimated Time of Arrival: December 31
10 mg USD 276 In-stock
Estimated Time of Arrival: December 31
50 mg USD 780 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1152 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

Delanzomib (CEP-18770) is a potent and orally active chymotrypsin-like activity of the proteasome inhibitor with an IC50 of 3.8 nM. Delanzomib inhibits NF-κB activity, induces cancer cell apoptotic, and has strong antiangiogenic and anti-cancer activities[1].

IC50 & Target

IC50: 3.8 nM (Chymotrypsin-like activity of the proteasome)[1]

In Vitro

Delanzomib (CEP-18770; 20 nM; 12-24 hours) treatment results in a progressive appearance of cleaved caspases-3, -7, and -9 between 12 and 24 hours’exposure in the human MM cell lines, RPMI-8226, and U266[1].
Delanzomib (CEP-18770; 5-40 nM; 4-24 hours) treatment induces an accumulation of ubiquitinated proteins over 4 to 8 hours[1].
Delanzomib (CEP-18770) inhibits endothelial cell survival, vasculogenesis, and osteoclastogenesis in vitro; and displays a favorable cytotoxicity profile toward normal cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[1]

Cell Line: RPMI-8226, U266, and K562 cells
Concentration: 20 nM
Incubation Time: 12 hours, 24 hours
Result: Resulted in a progressive appearance of cleaved caspases-3, -7, and -9 between 12 and 24 hours’exposure in the human MM cell lines.

Western Blot Analysis[1]

Cell Line: RPMI-8226, U266, and K562 cells
Concentration: 5 nM, 10 nM, 20 nM, 40 nM
Incubation Time: 4 hours, 8 hours, 12 hours, 24 hours
Result: Induced an accumulation of ubiquitinated proteins over 4 to 8 hours.
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Clinical Trial
Molecular Weight

413.28

Formula

C₂₁H₂₈BN₃O₅

CAS No.

847499-27-8

SMILES

CC(C)C[[email protected]@H](B(O)O)NC([[email protected]@H](NC(C1=NC(C2=CC=CC=C2)=CC=C1)=O)[[email protected]](O)C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (241.97 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4197 mL 12.0983 mL 24.1967 mL
5 mM 0.4839 mL 2.4197 mL 4.8393 mL
10 mM 0.2420 mL 1.2098 mL 2.4197 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.17 mg/mL (5.25 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.17 mg/mL (5.25 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.17 mg/mL (5.25 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: ≥98.0%

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Keywords:

DelanzomibCEP-18770CEP18770CEP 18770ProteasomeNF-κBApoptosisNuclear factor-κBNuclear factor-kappaBchymotrypsin-likeproteasomeantiangiogenicanti-cancerInhibitorinhibitorinhibit

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