Art. -Nr.: HY-143584

AZ5576

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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.

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Reinheit: 99.86%
CAS. Nr.: 2751721-40-9
Formel: C₂₁H₂₄FN₃O₃
Molecular Weight:385.43

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

AZ5576 Chemical Structure

CAS. Nr.: 2751721-40-9

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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
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

CDK9

<5 nM ()

Alle CDK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
Sf9	IC₅₀	94 nM Compound: 57	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	[PMID: 27171036]
Sf9	IC₅₀	94 nM Compound: 57	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	[PMID: 27171036]
Sf9	IC₅₀	94 nM Compound: 57	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	[PMID: 27171036]
Sf9	IC₅₀	94 nM Compound: 57	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	[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.

Apoptosis Analysis^[2]

Cell Line:

primary DLBCL cell
Concentration:

1 μM
Incubation Time:

24 h
Result:

Induced apoptosis.

In Vivo

AZ5576 (60 mg/kg, po, twice weekly for 30 days) exhibits antitumor activity against VAL and OCI-LY3 in mouse models^[2].

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

Animal Model:

VAL or OCI-LY3 xenograft mouse models^[2]
Dosage:

60 mg/kg
Administration:

po, twice weekly for 30 days
Result:

Inhibited tumor growth.

Chemical Information

CAS. Nr. 2751721-40-9
Appearance Solid
Molecular Weight 385.43
Formel C₂₁H₂₄FN₃O₃
Color White to off-white
SMILES

O=C([C@@H]1C[C@H](NC(C)=O)CCC1)NC2=NC=CC(C3=CC=C(F)C=C3OC)=C2
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

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

2.5945 mL

12.9725 mL

25.9450 mL

5 mM

0.5189 mL

2.5945 mL

5.1890 mL

10 mM

0.2595 mL

1.2973 mL

2.5945 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, 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.

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 (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.

Protocol 2

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

Solubility: ≥ 2.08 mg/mL (5.40 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 (272 KB)
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)
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. 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]

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, 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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AZ5576

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Alle CDK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AZ5576

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Alle CDK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AZ5576 Related Classifications

HY-143584 Related Classifications