Art. -Nr.: HY-112088

AZD4573

14 Cited Publications

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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.

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Reinheit: 99.98%
CAS. Nr.: 2057509-72-3
Formel: C₂₂H₂₈ClN₅O₂
Molecular Weight:429.94

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

AZD4573 Chemical Structure

CAS. Nr.: 2057509-72-3

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (14)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

AZD4573 is a potent and highly selective CDK9 inhibitor (IC₅₀ of <4 nM) that enables transient target engagement for the treatment of hematologic malignancies^[1].

IC₅₀ & Target^[1]

CDK9

4 nM (IC₅₀)

Alle CDK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
4T1	IC₅₀	8.29 nM Compound: AZD4573	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	[PMID: 38885173]
BT-549	IC₅₀	9.57 nM Compound: AZD4573	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	[PMID: 38885173]
MDA-MB-468	IC₅₀	13.57 nM Compound: AZD4573	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	[PMID: 38885173]
MM1.S	IC₅₀	6.03 nM Compound: AZD4573	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	[PMID: 38885173]
OPM-2	GI₅₀	23 nM Compound: 16; AZD-4573	Growth inhibition of human OPM-2 cells incubated for 24 hrs Growth inhibition of human OPM-2 cells incubated for 24 hrs	[PMID: 32866383]
T-cell	IC₅₀	<4 nM Compound: 54; AZD-4573	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	[PMID: 35485642]

In Vitro

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.

In Vivo

AZD4573 exhibits a short half-life in multiple species (less than one hour in rat, dog and monkey) and good solubility for intravenous administration^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 2057509-72-3
Appearance Solid
Molecular Weight 429.94
Formel C₂₂H₂₈ClN₅O₂
Color White to off-white
SMILES

ClC1=CN=C(NC([C@H]2CCC[C@@H](NC(C)=O)C2)=O)C=C1C3=C(CC(C)(C)C4)N4N=C3
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (14)

All Cell Proliferation/Viability AssayRT-PCRIn Vivo Efficacy StudyIFWB

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Journal Impact Factor

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.
Acta Pharm Sin B

Predicting and overcoming resistance to CDK9 inhibitors for cancer therapy. [Abstract]

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.
Cell Rep

Super Elongation Complex as a Targetable Dependency in Diffuse Midline Glioma. [Abstract]

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.
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
Res Sq

2025 Dec 18.
University of California, Irvine

2024.
bioRxiv

PAIRWISE: Deep Learning-based Prediction of Effective Personalized Drug Combinations in Cancer. [Abstract]

2024 Nov 6:2024.11.04.621884. PMID: 39574568
Freie Universität Berlin

2023 Nov 29.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3259 mL

11.6295 mL

23.2591 mL

5 mM

0.4652 mL

2.3259 mL

4.6518 mL

10 mM

0.2326 mL

1.1630 mL

2.3259 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.84 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Bernard Barlaam, et al. Abstract 1650: Discovery of AZD4573, a potent and selective inhibitor of CDK9 that enables transient target engagement for the treatment of hematologic malignancies. Cancer Research. July 2018. 78(13): Supplement.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	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

Keywords

AZD4573

14 Cited Publications

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AZD4573

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Publications Citing Use of MedChemExpress (MCE) AZD4573

Alle CDK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (14)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AZD4573

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Publications Citing Use of MedChemExpress (MCE) AZD4573

Alle CDK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (14)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AZD4573 Related Classifications

HY-112088 Related Classifications