Delanzomib
Based on 4 publication(s) in Google Scholar
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.
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- Purity: 98.0%
- CAS No.: 847499-27-8
- 화학식: C21H28BN3O5
- 분자량:413.28
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Delanzomib
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Biological Activity
IC50: 3.8 nM (Chymotrypsin-like activity of the proteasome)[1]
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Cell Line
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Type | Value | Description | References |
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| A2780 | IC50 |
13.7 nM
Compound: 20, CEP-18770
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Cytotoxicity against human A2780 cells
Cytotoxicity against human A2780 cells
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[PMID: 18247547] |
| MOLT-4 | EC50 |
13.5 nM
Compound: 20, CEP-18770
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Inhibition of chymotrypsin-like activity of human 20S proteasome in Molt4 cells
Inhibition of chymotrypsin-like activity of human 20S proteasome in Molt4 cells
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[PMID: 18247547] |
| MOLT-4 | EC50 |
13.5 nM
Compound: 8c, CEP-18770
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Inhibition of cathepsin G in human MOLT4 cells
Inhibition of cathepsin G in human MOLT4 cells
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[PMID: 20925433] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RPMI-8226, U266, and K562 cells
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Concentration:20 nM
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Incubation Time:12 hours, 24 hours
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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.
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Cell Line:RPMI-8226, U266, and K562 cells
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Concentration:5 nM, 10 nM, 20 nM, 40 nM
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Incubation Time:4 hours, 8 hours, 12 hours, 24 hours
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Result:Induced an accumulation of ubiquitinated proteins over 4 to 8 hours.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SCID mice injected with RPMI 8226 cells[1]
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Dosage:7.8 mg/kg, 10 mg/kg, 13 mg/kg
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Administration:Oral administration; twice a week; for 4 weeks
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Result:Resulted in a more sustained pharmacodynamic inhibition of proteasome activity in tumors relative to normal tissues.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 847499-27-8
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Appearance Solid
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분자량 413.28
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화학식 C21H28BN3O5
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Color White to yellow
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SMILES
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
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Synonyms
CEP-18770
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Selective depletion of tumor-associated SAMHD1 enhances chemotherapeutic efficacy and antitumor immune responses. [Abstract]2025 Dec 15;10(1):406. PMID: 41392286 -
Nat Prod Bioprospect
Exploring anti-SARS-CoV-2 natural products: dual-viral target inhibition by delphinidin and the anti-coronaviral efficacy of deapio platycodin D. [Abstract]2025 Jun 13;15(1):39. PMID: 40512442 -
Antimicrob Agents Chemother
Inhibitors of the 20S proteasome β5 subunit as potent and selective agents against Trichomonas vaginalis. [Abstract]2025 Dec 10;69(12):e0089325. PMID: 41218108 -
Biol Pharm Bull
Potential Efficacy of Proteasome Inhibitor, Delanzomib, for the Treatment of Renal Fibrosis. [Abstract]2023;46(2):279-285. PMID: 36724955
용액&용해도
DMSO : 100 mg/mL (241.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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
This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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
This protocol yields a suspended solution of 2.17 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4197 mL | 12.0983 mL | 24.1967 mL | 60.4917 mL |
| 5 mM | 0.4839 mL | 2.4197 mL | 4.8393 mL | 12.0983 mL | |
| 10 mM | 0.2420 mL | 1.2098 mL | 2.4197 mL | 6.0492 mL | |
| 15 mM | 0.1613 mL | 0.8066 mL | 1.6131 mL | 4.0328 mL | |
| 20 mM | 0.1210 mL | 0.6049 mL | 1.2098 mL | 3.0246 mL | |
| 25 mM | 0.0968 mL | 0.4839 mL | 0.9679 mL | 2.4197 mL | |
| 30 mM | 0.0807 mL | 0.4033 mL | 0.8066 mL | 2.0164 mL | |
| 40 mM | 0.0605 mL | 0.3025 mL | 0.6049 mL | 1.5123 mL | |
| 50 mM | 0.0484 mL | 0.2420 mL | 0.4839 mL | 1.2098 mL | |
| 60 mM | 0.0403 mL | 0.2016 mL | 0.4033 mL | 1.0082 mL | |
| 80 mM | 0.0302 mL | 0.1512 mL | 0.3025 mL | 0.7561 mL | |
| 100 mM | 0.0242 mL | 0.1210 mL | 0.2420 mL | 0.6049 mL |
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