2. Cell Cycle/DNA Damage Apoptosis
  3. CDK Apoptosis
  4. AZ5576

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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AZ5576

AZ5576 Chemische Struktur

CAS. Nr. : 2751721-40-9

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Alle CDK Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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Beschreibung

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[1][2].

IC50 & Target[1]

CDK9

<5 nM ()

Cellular Effect
Cell Line Type Value Description References
Sf9 IC50
94 1
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 1
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 1
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 1
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 1
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]
Sf9 IC50
94 1
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 1
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 1
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 1
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.

AZ5576 Related Antibodies

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.
Molekulargewicht

385.43

Formel

C21H24FN3O3
CAS. Nr.
Appearance

Solid

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5945 mL 12.9725 mL 25.9450 mL
5 mM 0.5189 mL 2.5945 mL 5.1890 mL
View the 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.

  • Molaritätsrechner

  • Verdünnungsrechner

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Reinheit & Dokumentation
Verweise

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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AZ5576 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AZ55762751721-40-9AZ 5576AZ-5576CDKApoptosisCyclin dependent kinaseCDK9hematological Malignancyacute myeloid leukemiaAMlInhibitorinhibitorinhibit

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