Azenosertib
Based on 5 publication(s) in Google Scholar
Azenosertib (ZN-c3) is a selective, orally active inhibitor for Wee1 inhibitor (IC50=3.9 nM). Azenosertib exhibits antitumor activity.
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- Pureza: 99.96%
- No. CAS: 2376146-48-2
- Fòrmula: C29H34N8O2
- Peso molecular:526.63
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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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) Azenosertib
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Actividad biológica
IC50: 3.9 nM (Wee1)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| LoVo | IC50 |
317 nM
Compound: Zn-c3
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Antiproliferative activity against human LoVo cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
Antiproliferative activity against human LoVo cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
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[PMID: 38847373] |
Azenosertib inhibits proliferations of cancer cells H23 and A427 with IC50s 103 and 75 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NCI H23, A427
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Concentration:
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Incubation Time:3 days for A427 cell and 4 days for NCI H23 cell
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Result:Inhibited proliferation of A427 and NCI H23.
Azenosertib (10 mg/kg, p.o.) shows plasma exposure Cmax of 2.1 μM, a half-time T1/2 of 2.3 h, an AUC0-24 h of 9.7 μM·h, and an oralbioavailability of F=142% in beagle dog model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:A427 xenograft NOD/SCID mice model[1]
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Dosage:80 mg/kg
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Administration:p.o. for 28 days
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Result:Inhibited tumor growth.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2376146-48-2
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Appearance Solid
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Peso molecular 526.63
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Fòrmula C29H34N8O2
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Color Light yellow to yellow
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SMILES
O=C1N(CC=C)N(C2=CC=C(CC[C@@]3(CC)O)C3=N2)C4=NC(NC5=CC=C(N6CCN(C)CC6)C=C5)=NC=C41
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Synonyms
ZN-c3
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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 1 year -20°C 6 months
Publications (5)
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Journal Impact Factor
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Most Recent
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Cancer Lett
2026 Apr 1:642:218300. PMID: 41651400 -
NPJ Breast Cancer
CDK2 inhibition enhances CDK4/6 inhibitor antitumor activity in comprehensive breast cancer PDX model screen. [Abstract]2025 Dec 3;11(1):135. PMID: 41339342 -
bioRxiv
AURKA inhibition amplifies DNA replication stress to foster WEE1 kinase dependency and synergistic antitumor effects with WEE1 inhibition in cancers. [Abstract]2025 May 29:2025.05.28.656693. PMID: 40501675 -
Solvente y solubilidad
DMSO : 175 mg/mL (332.30 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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: ≥ 5 mg/mL (9.49 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (9.49 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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 (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
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- 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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Instrucciones de manejo (2659 KB)
Referencias
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.8989 mL | 9.4943 mL | 18.9887 mL | 47.4717 mL |
| 5 mM | 0.3798 mL | 1.8989 mL | 3.7977 mL | 9.4943 mL | |
| 10 mM | 0.1899 mL | 0.9494 mL | 1.8989 mL | 4.7472 mL | |
| 15 mM | 0.1266 mL | 0.6330 mL | 1.2659 mL | 3.1648 mL | |
| 20 mM | 0.0949 mL | 0.4747 mL | 0.9494 mL | 2.3736 mL | |
| 25 mM | 0.0760 mL | 0.3798 mL | 0.7595 mL | 1.8989 mL | |
| 30 mM | 0.0633 mL | 0.3165 mL | 0.6330 mL | 1.5824 mL | |
| 40 mM | 0.0475 mL | 0.2374 mL | 0.4747 mL | 1.1868 mL | |
| 50 mM | 0.0380 mL | 0.1899 mL | 0.3798 mL | 0.9494 mL | |
| 60 mM | 0.0316 mL | 0.1582 mL | 0.3165 mL | 0.7912 mL | |
| 80 mM | 0.0237 mL | 0.1187 mL | 0.2374 mL | 0.5934 mL | |
| 100 mM | 0.0190 mL | 0.0949 mL | 0.1899 mL | 0.4747 mL |
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