AZ5576
Based on 2 publication(s) in Google Scholar
AZ5576 is a potent and highly selective CDK9 inhibitor (IC50: <5 nM). AZ5576 inhibits the phosphorylation of RNA polymerase II at Ser2, thereby inhibiting transcriptional elongation. AZ5576 can be used for hematological Malignancy research.
For research use only. We do not sell to patients.
- Purity : 99.86%
- CAS No.: 2751721-40-9
- Formula: C21H24FN3O3
- Molecular Weight:385.43
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) AZ5576
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Biological Activity
Description
IC50 & Target
[1]|
CDK9 <5 nM () |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Sf9 | IC50 |
94 nM
Compound: 57
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Inhibition of recombinant human CDK1/cyclin B expressed in baculovirus infected Sf9 insect cells after 80 mins in presence of [33P]ATP by microbeta scintillation counting analysis
Inhibition of recombinant human CDK1/cyclin B expressed in baculovirus infected Sf9 insect cells after 80 mins in presence of [33P]ATP by microbeta scintillation counting analysis
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[PMID: 27171036] |
| Sf9 | IC50 |
94 nM
Compound: 57
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Inhibition of recombinant human CDK3/cyclin E expressed in baculovirus infected Sf9 insect cells after 80 mins in presence of [33P]ATP by microbeta scintillation counting analysis
Inhibition of recombinant human CDK3/cyclin E expressed in baculovirus infected Sf9 insect cells after 80 mins in presence of [33P]ATP by microbeta scintillation counting analysis
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[PMID: 27171036] |
| Sf9 | IC50 |
94 nM
Compound: 57
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Inhibition of recombinant human His/GST-tagged CDK2/Cyclin A expressed in baculovirus infected Sf9 cells using Histone H1 as substrate after 80 mins in presence of [33P]ATP by microbeta scintillation counting analysis
Inhibition of recombinant human His/GST-tagged CDK2/Cyclin A expressed in baculovirus infected Sf9 cells using Histone H1 as substrate after 80 mins in presence of [33P]ATP by microbeta scintillation counting analysis
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[PMID: 27171036] |
| Sf9 | IC50 |
94 nM
Compound: 57
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Inhibition of recombinant human His/GST-tagged CDK5/p35 expressed in baculovirus infected Sf9 insect cells using Rb-CTF as substrate after 80 mins in presence of [33P]ATP by microbeta scintillation counting analysis
Inhibition of recombinant human His/GST-tagged CDK5/p35 expressed in baculovirus infected Sf9 insect cells using Rb-CTF as substrate after 80 mins in presence of [33P]ATP by microbeta scintillation counting analysis
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[PMID: 27171036] |
In Vitro
AZ5576 (1 μM, 24 h) reduces the mRNA and protein expressions of Mcl-1 and MYC, inhibits DNA synthesis of Diffuse large B-cell lymphoma (DLBCL) cells, causes the S phase reduction, and induces apoptosis[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:primary DLBCL cell
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Concentration:1 μM
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Incubation Time:24 h
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Result:Induced apoptosis.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:VAL or OCI-LY3 xenograft mouse models[2]
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Dosage:60 mg/kg
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Administration:po, twice weekly for 30 days
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Result:Inhibited tumor growth.
Chemical Information
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CAS No. 2751721-40-9
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Appearance Solid
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Molecular Weight 385.43
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Formula C21H24FN3O3
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Color White to off-white
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SMILES
O=C([C@@H]1C[C@H](NC(C)=O)CCC1)NC2=NC=CC(C3=CC=C(F)C=C3OC)=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Nat Genet
2026 Apr;58(4):854-868. PMID: 41957181 -
Solvent & Solubility
In Vitro:
DMSO : 125 mg/mL (324.31 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)
In Vivo:
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 (5.40 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.
In Vivo Dissolution Calculator
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.
Protocols
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Kinase activity and phosphorylation assays
Kinase activity assays measure the ability of kinases to transfer phosphate groups from ATP to specific substrates, while phosphorylation assays detect the presence and levels of phosphorylated proteins. Common methods include radiolabeled ATP incorporation (e. g. ,), ADP release detection via bioluminescence (e. g. ,[3]), enzyme-linked immunosorbent assays (ELISA) for phospho-specific epitopes (e. g. ,[6]), and microtiter-based formats for high-throughput screening (e. g. ,[8]). The ADP-Glo assay quantifies kinase activity by measuring ADP produced during phosphorylation using a luciferase-based system. Radiometric assays involve autoradiography or scintillation counting after incorporation of 32P-labeled ATP into substrate proteins. ELISA-based approaches rely on phospho-specific antibodies to detect activated kinases in cell lysates or purified samples.
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Western Blot
Western blotting (WB) is a commonly used experimental method in molecular biology, biochemistry, and immunogenetics for identifying and quantifying target proteins. It combines gel electrophoresis with immunoassay, enabling researchers to analyze protein expression, post-translational modifications, and molecular weight.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Protocol for Kinase activity and phosphorylation assays
Kinase activity assays measure transfer of phosphate from ATP to a protein or peptide substrate, generating phosphorylated substrate, ADP, or incorporated radiolabeled phosphate as the readout; phosphorylation assays measure site-specific phosphorylation in cells or tissues as a proxy for kinase-pathway activation, inhibition, or substrate regulation. Phosphorylation can be detected by phospho-specific Western blot, immunoprecipitation kinase assay, phospho-immunofluorescence, phospho-flow cytometry, luminescent ADP detection, radiolabeled ATP incorporation, or reporter-based pathway assays, and these readouts can be applied to cancer cells, primary neurons, mouse tumors, organoids, inflammatory macrophages, ferroptosis studies, and mitophagy studies when the kinase target is biologically relevant.
Purity & Documentation
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Data Sheet (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Bernard Barlaam, et al. Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies. [Content Brief]
[2]. Hashiguchi T, et al., Cyclin-Dependent Kinase-9 Is a Therapeutic Target in MYC-Expressing Diffuse Large B-Cell Lymphoma. Mol Cancer Ther. 2019 Sep;18(9):1520-1532. [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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5945 mL | 12.9725 mL | 25.9450 mL | 64.8626 mL |
| 5 mM | 0.5189 mL | 2.5945 mL | 5.1890 mL | 12.9725 mL | |
| 10 mM | 0.2595 mL | 1.2973 mL | 2.5945 mL | 6.4863 mL | |
| 15 mM | 0.1730 mL | 0.8648 mL | 1.7297 mL | 4.3242 mL | |
| 20 mM | 0.1297 mL | 0.6486 mL | 1.2973 mL | 3.2431 mL | |
| 25 mM | 0.1038 mL | 0.5189 mL | 1.0378 mL | 2.5945 mL | |
| 30 mM | 0.0865 mL | 0.4324 mL | 0.8648 mL | 2.1621 mL | |
| 40 mM | 0.0649 mL | 0.3243 mL | 0.6486 mL | 1.6216 mL | |
| 50 mM | 0.0519 mL | 0.2595 mL | 0.5189 mL | 1.2973 mL | |
| 60 mM | 0.0432 mL | 0.2162 mL | 0.4324 mL | 1.0810 mL | |
| 80 mM | 0.0324 mL | 0.1622 mL | 0.3243 mL | 0.8108 mL | |
| 100 mM | 0.0259 mL | 0.1297 mL | 0.2595 mL | 0.6486 mL |
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