AUZ 454
Based on 7 publication(s) in Google Scholar
AUZ 454 (K03861) is a type II CDK2 inhibitor with Kd of 8.2 nM. AUZ 454 (K03861) inhibits CDK2 activity by competing with binding of activating cyclins.
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- Pureté: 99.15%
- CAS No.: 853299-07-7
- Formule: C24H26F3N7O2
- Masse moléculaire:501.50
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) AUZ 454
More
Activité biologique
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CDK2(C118L/A144C) 9.7 nM (Kd) |
CDK2(A144C) 15.4 nM (Kd) |
CDK2(C118L) 18.6 nM (Kd) |
CDK2(WT) 50 nM (Kd) |
CDK2(C118L/A144C-Cyclin B) 134.1 nM (Kd) |
AUZ 454 (K03861) (10-20 μM; 1, 2, 3, and 4 days) has a inhibitory effect on Caki-1 and ACHN cells with WTAP overexpression by CCK8 assays[2]. AUZ 454 (K03861) (10 μM; 24 hours) decreases the colony fold in Caki-1 and ACHN cells through a CDK2-dependent mechanism[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Caki-1 and ACHN cells
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Concentration:10 μM; 20 μM
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Incubation Time:1, 2, 3, and 4 days
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Result:Inhibited cell proliferation in a CDK2-dependent manner.
Chemical Information
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CAS No. 853299-07-7
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Appearance Solid
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Masse moléculaire 501.50
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Formule C24H26F3N7O2
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Color White to off-white
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SMILES
NC1=NC(OC2=CC=C(NC(NC3=CC(C(F)(F)F)=C(CN4CCN(C)CC4)C=C3)=O)C=C2)=CC=N1
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Synonyms
K03861
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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Nat Commun
CDK4 inactivation inhibits apoptosis via mitochondria-ER contact remodeling in triple-negative breast cancer. [Abstract]2025 Jan 9;16(1):541. PMID: 39788939 -
J Exp Clin Cancer Res
Wilms' tumor 1-associating protein promotes renal cell carcinoma proliferation by regulating CDK2 mRNA stability. [Abstract]2018 Feb 27;37(1):40. PMID: 29482572 -
Br J Cancer
In silico enhancer mining reveals SNS-032 and EHMT2 inhibitors as therapeutic candidates in high-grade serous ovarian cancer. [Abstract]2023 Jul;129(1):163-174. PMID: 37120667 -
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Cancers (Basel)
2022 Jul 11;14(14):3361. PMID: 35884422 -
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Solvant et solubilité
DMSO : 250 mg/mL (498.50 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: ≥ 2.08 mg/mL (4.15 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.15 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Pureté et documentation
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Fiche technique (274 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)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Alexander LT et al. Type II Inhibitors Targeting CDK2. ACS Chem Biol. 2015 Sep 18;10(9):2116-25. [Content Brief]
[2]. Tang J,et al. Wilms' tumor 1-associating protein promotes renal cell carcinoma proliferation by regulating CDK2 mRNA stability.J Exp Clin Cancer Res. 2018 Feb 27;37(1):40. [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, 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 | 1.9940 mL | 9.9701 mL | 19.9402 mL | 49.8504 mL |
| 5 mM | 0.3988 mL | 1.9940 mL | 3.9880 mL | 9.9701 mL | |
| 10 mM | 0.1994 mL | 0.9970 mL | 1.9940 mL | 4.9850 mL | |
| 15 mM | 0.1329 mL | 0.6647 mL | 1.3293 mL | 3.3234 mL | |
| 20 mM | 0.0997 mL | 0.4985 mL | 0.9970 mL | 2.4925 mL | |
| 25 mM | 0.0798 mL | 0.3988 mL | 0.7976 mL | 1.9940 mL | |
| 30 mM | 0.0665 mL | 0.3323 mL | 0.6647 mL | 1.6617 mL | |
| 40 mM | 0.0499 mL | 0.2493 mL | 0.4985 mL | 1.2463 mL | |
| 50 mM | 0.0399 mL | 0.1994 mL | 0.3988 mL | 0.9970 mL | |
| 60 mM | 0.0332 mL | 0.1662 mL | 0.3323 mL | 0.8308 mL | |
| 80 mM | 0.0249 mL | 0.1246 mL | 0.2493 mL | 0.6231 mL | |
| 100 mM | 0.0199 mL | 0.0997 mL | 0.1994 mL | 0.4985 mL |
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