AZD4573
Based on 14 publication(s) in Google Scholar
AZD4573 is a potent and highly selective CDK9 inhibitor (IC50 of <4 nM) that enables transient target engagement for the treatment of hematologic malignancies.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.98%
- No. CAS: 2057509-72-3
- Fòrmula: C22H28ClN5O2
- Peso molecular:429.94
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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) AZD4573
More- Cancer Res. 2025 May 14. [Abstract]
- Cancer Res. 2024 Jan 2;84(1):17-25. [Abstract]
- Acta Pharm Sin B. 2023 Sep;13(9):3694-3707. [Abstract]
- Med. 2025 Jan 5:100568. [Abstract]
- Clin Cancer Res. 2024 Sep 13;30(18):4179-4189. [Abstract]
- Cell Rep. 2020 Apr 7;31(1):107485. [Abstract]
- Int J Mol Sci. 2022 Feb 24;23(5):2493. [Abstract]
- Heliyon. 2024 Jul 8;10(14):e34289. [Abstract]
- PLoS One. 2020 Jun 19;15(6):e0232068. [Abstract]
- Curr Protoc. 2021 Feb;1(2):e51. [Abstract]
- Res Sq. 2025 Dec 18.
- University of California, Irvine. 2024.
- bioRxiv. 2024 Nov 6:2024.11.04.621884. [Abstract]
- Freie Universität Berlin. 2023 Nov 29.
Customer Validation & Images
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RT-PCR
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IF
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WB
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Cell Proliferation/Viability Assay
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In Vivo Efficacy Study
Actividad biológica
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CDK9 4 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| 4T1 | IC50 |
8.29 nM
Compound: AZD4573
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Inhibition of cell viability in mouse 4T1 cells incubated for 4 days by WST-8 assay
Inhibition of cell viability in mouse 4T1 cells incubated for 4 days by WST-8 assay
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[PMID: 38885173] |
| BT-549 | IC50 |
9.57 nM
Compound: AZD4573
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Inhibition of cell viability in human BT-549 cells incubated for 4 days by WST-8 assay
Inhibition of cell viability in human BT-549 cells incubated for 4 days by WST-8 assay
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[PMID: 38885173] |
| MDA-MB-468 | IC50 |
13.57 nM
Compound: AZD4573
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Inhibition of cell viability in human MDA-MB-468 cells incubated for 4 days by WST-8 assay
Inhibition of cell viability in human MDA-MB-468 cells incubated for 4 days by WST-8 assay
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[PMID: 38885173] |
| MM1.S | IC50 |
6.03 nM
Compound: AZD4573
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Inhibition of cell viability in human MM1.S cells incubated for 4 days by WST-8 assay
Inhibition of cell viability in human MM1.S cells incubated for 4 days by WST-8 assay
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[PMID: 38885173] |
| OPM-2 | GI50 |
23 nM
Compound: 16; AZD-4573
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Growth inhibition of human OPM-2 cells incubated for 24 hrs
Growth inhibition of human OPM-2 cells incubated for 24 hrs
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[PMID: 32866383] |
| T-cell | IC50 |
<4 nM
Compound: 54; AZD-4573
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Inhibition of CDK9/Cyclin T (unknown origin) in presence of ATP by Kinomescan assay
Inhibition of CDK9/Cyclin T (unknown origin) in presence of ATP by Kinomescan assay
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[PMID: 35485642] |
Short-term treatment with AZD4573 led to a rapid dose- and time-dependent decrease in cellular pSer2-RNAPII, resulting in activation of caspase 3 and cell apoptosis in a broad range of haematological cancer cell lines (e.g. caspase activation EC50 13.7 nM in an acute myeloid leukemia model MV4-11) [1].
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2057509-72-3
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Appearance Solid
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Peso molecular 429.94
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Fòrmula C22H28ClN5O2
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Color White to off-white
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SMILES
ClC1=CN=C(NC([C@H]2CCC[C@@H](NC(C)=O)C2)=O)C=C1C3=C(CC(C)(C)C4)N4N=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 2 years -20°C 1 year
Publications (14)
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Journal Impact Factor
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Most Recent
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Cancer Res
SMARCA4 loss increases RNA Polymerase II pausing and elevates R-loops to inhibit BRCA1-mediated repair in ovarian cancer. [Abstract]2025 May 14. PMID: 40366633 -
Cancer Res
Targeting transcriptional regulation with a CDK9 inhibitor suppresses growth of endocrine- and palbociclib-resistant ER+ breast cancers. [Abstract]2024 Jan 2;84(1):17-25. PMID: 37801608
AZD4573 purchased from MedChemExpress. Usage Cited in: Cancer Res. 2024 Jan 2;84(1):17-25. [Abstract]
At the indicated concentrations. Cell viability was assessed using CellTiter-Glo (day 7). Data represent percentage NVP-2/AZD4573–treated viable cells compared with vehicle control.
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Acta Pharm Sin B
2023 Sep;13(9):3694-3707. PMID: 37719386 -
Med
Inactivation of TACC2 epigenetically represses CDKN1A and confers sensitivity to CDK inhibitors. [Abstract]2025 Jan 5:100568. PMID: 39793578 -
Clin Cancer Res
CDK9 inhibition by dinaciclib is a therapeutic vulnerability in epithelioid hemangioendothelioma. [Abstract]2024 Sep 13;30(18):4179-4189. PMID: 39052240
AZD4573 purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2024 Sep 13;30(18):4179-4189. [Abstract]
qPCR data showing the expression levels of TC target genes after AZD4573 (300 nM) treatment.
AZD4573 purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2024 Sep 13;30(18):4179-4189. [Abstract]
AZD4573 (300 nM) displayed a significant reduction in TC nuclear immunofluorescence.
AZD4573 purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2024 Sep 13;30(18):4179-4189. [Abstract]
AZD4573 (300 nM) reduced TC levels by Immunoblotting.
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Cell Rep
2020 Apr 7;31(1):107485. PMID: 32268092
AZD4573 purchased from MedChemExpress. Usage Cited in: Cell Rep. 2020 Apr 7;31(1):107485. [Abstract]
Survival analysis of atuveciclib and AZD4573 (20 mg/kg, i.p.)-treated cohorts versus vehicle control.
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Int J Mol Sci
Cyclin-Dependent Kinases (CDKs) and the Human Cytomegalovirus-Encoded CDK Ortholog pUL97 Represent Highly Attractive Targets for Synergistic Drug Combinations. [Abstract]2022 Feb 24;23(5):2493. PMID: 35269635 -
Heliyon
Cyclin dependent kinase 9 inhibition reduced programmed death-ligand 1 expression and improved treatment efficacy in hepatocellular carcinoma. [Abstract]2024 Jul 8;10(14):e34289. PMID: 39100490 -
PLoS One
Multiple myeloma: Combination therapy of BET proteolysis targeting chimeric molecule with CDK9 inhibitor. [Abstract]2020 Jun 19;15(6):e0232068. PMID: 32559187 -
Curr Protoc
Human Plasma In-Cell Western Assays-An In vitro Predictor for In vivo Pharmacology in Oncology Drug Discovery. [Abstract]2021 Feb;1(2):e51. PMID: 33587334 -
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bioRxiv
PAIRWISE: Deep Learning-based Prediction of Effective Personalized Drug Combinations in Cancer. [Abstract]2024 Nov 6:2024.11.04.621884. PMID: 39574568 -
Solvente y solubilidad
DMSO : 50 mg/mL (116.30 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, 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 (4.84 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 (4.84 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.
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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, 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 |
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| DMSO | 1 mM | 2.3259 mL | 11.6295 mL | 23.2591 mL | 58.1476 mL |
| 5 mM | 0.4652 mL | 2.3259 mL | 4.6518 mL | 11.6295 mL | |
| 10 mM | 0.2326 mL | 1.1630 mL | 2.3259 mL | 5.8148 mL | |
| 15 mM | 0.1551 mL | 0.7753 mL | 1.5506 mL | 3.8765 mL | |
| 20 mM | 0.1163 mL | 0.5815 mL | 1.1630 mL | 2.9074 mL | |
| 25 mM | 0.0930 mL | 0.4652 mL | 0.9304 mL | 2.3259 mL | |
| 30 mM | 0.0775 mL | 0.3877 mL | 0.7753 mL | 1.9383 mL | |
| 40 mM | 0.0581 mL | 0.2907 mL | 0.5815 mL | 1.4537 mL | |
| 50 mM | 0.0465 mL | 0.2326 mL | 0.4652 mL | 1.1630 mL | |
| 60 mM | 0.0388 mL | 0.1938 mL | 0.3877 mL | 0.9691 mL | |
| 80 mM | 0.0291 mL | 0.1454 mL | 0.2907 mL | 0.7268 mL | |
| 100 mM | 0.0233 mL | 0.1163 mL | 0.2326 mL | 0.5815 mL |
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