Aderbasib
Based on 1 publication(s) in Google Scholar
Aderbasib (INCB007839) is a potent, orally active and target specific low nanomolar hydroxamate-based inhibitor of ADAM10 and ADAM17. Aderbasib exhibits robust antineoplastic activity and can be used for cancer research, including diffuse large B-cell non-Hodgkin lymphoma, HER2+ breast cancer, gliomas, et al.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.44%
- No. CAS: 791828-58-5
- Fòrmula: C21H28N4O5
- Peso molecular:416.47
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Aderbasib
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Actividad biológica
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ADAM10 |
ADAM17 |
Aderbasib inhibits the metalloprotease activity through binding to the active site of the metalloproteinase domain. Aderbasib (10-100 μM) inhibits the interaction between ADAM17 and sE2-Fc, as the concentration of the compound increases, binding of sE2-Fc decreased accordingly, with almost no binding detected at 100 μM in trypsinized PK15 cells[2].Aderbasib (100-1000μM; pre-treated for 0.5 h) shows antiviral effect against CSFV pseudovirus at 100 μM and 1 mM in PK15 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NSG mice[1]
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Dosage:50 mg/kg
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Administration:Intraperitoneal injection; 50 mg/kg; 5 days per week beginning four weeks; 2 weeks
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Result:Robustly inhibited growth of pediatric glioblastoma orthotopic xenografts.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 791828-58-5
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Appearance Solid
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Peso molecular 416.47
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Fòrmula C21H28N4O5
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Color White to light yellow
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SMILES
O=C(N(CC1)CCN1C2=CC=CC=C2)[C@H]([C@H](C3)C(NO)=O)N(CC43CC4)C(OC)=O
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Synonyms
INCB007839; INCB7839
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Clin Cancer Res
Ibrutinib and PD-1 blockade potentiate mesothelin-targeting CAR-T cell therapy in preclinical models of pancreatic cancer. [Abstract]2025 Nov 13. PMID: 41231131
Solvente y solubilidad
DMSO : 100 mg/mL (240.11 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 2.5 mg/mL (6.00 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.00 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Lois Witters, et al. Synergistic inhibition with a dual epidermal growth factor receptor/HER-2/neu tyrosine kinase inhibitor and a disintegrin and metalloprotease inhibitor. Cancer Res. 2008 Sep 1;68(17):7083-9. [Content Brief]
[2]. Fei Yuan, et al. ADAM17 is an essential attachment factor for classical swine fever virus. PLoS Pathog. 2021 Mar 8;17(3):e1009393. [Content Brief]
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.4011 mL | 12.0057 mL | 24.0113 mL | 60.0283 mL |
| 5 mM | 0.4802 mL | 2.4011 mL | 4.8023 mL | 12.0057 mL | |
| 10 mM | 0.2401 mL | 1.2006 mL | 2.4011 mL | 6.0028 mL | |
| 15 mM | 0.1601 mL | 0.8004 mL | 1.6008 mL | 4.0019 mL | |
| 20 mM | 0.1201 mL | 0.6003 mL | 1.2006 mL | 3.0014 mL | |
| 25 mM | 0.0960 mL | 0.4802 mL | 0.9605 mL | 2.4011 mL | |
| 30 mM | 0.0800 mL | 0.4002 mL | 0.8004 mL | 2.0009 mL | |
| 40 mM | 0.0600 mL | 0.3001 mL | 0.6003 mL | 1.5007 mL | |
| 50 mM | 0.0480 mL | 0.2401 mL | 0.4802 mL | 1.2006 mL | |
| 60 mM | 0.0400 mL | 0.2001 mL | 0.4002 mL | 1.0005 mL | |
| 80 mM | 0.0300 mL | 0.1501 mL | 0.3001 mL | 0.7504 mL | |
| 100 mM | 0.0240 mL | 0.1201 mL | 0.2401 mL | 0.6003 mL |
Aderbasib Related Classifications
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