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AZD4573 CDK9 Inhibitor

Name: AZD4573
Brand: Selleck Chemicals
SKU: S8719
Availability: InStock
Rating: 5 (16 reviews)

Cat.No.S8719

AZD4573 is a potent inhibitor of CDK9 (IC50 of <0.004 μM) with fast-off binding kinetics (t_1/2 = 16 min) and high selectivity versus other kinases, including other CDK family kinases.

Chemical Structure

Molecular Weight: 429.94

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.91%

99.91

Related Targets	DNA/RNA Synthesis Microtubule Associated Ras HSP PD-1/PD-L1 Aurora Kinase Casein Kinase Rho Serine/threonin kinase eIF Chk ROCK Myc Kinesin PLK DHFR PAK PERK DYRK RUNX PP2A PFKFB AP-1 MPS1 Wee1 p21 BMI-1 LIM kinase Nur77 APC
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Chemical Information, Storage & Stability

Molecular Weight	429.94	Formula	C₂₂H₂₈ClN₅O₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	2057509-72-3	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC(=O)NC1CCCC(C1)C(=O)NC2=NC=C(C(=C2)C3=C4CC(CN4N=C3)(C)C)Cl

Solubility

In vitro
Batch:

DMSO : 86 mg/mL (200.02 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 86 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.000mg/ml (9.30mM)	Taking the 1 mL working solution as an example, add 50 μL of 80 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	CDK9 ^[1] <0.004 μM
In vitro	Short-term treatment with AZD4573 leads 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 0.0137 μM in an acute myeloid leukemia model MV4-11)^[1]. In human cancer cell line panel screens, this compound demonstrates the ability to induce rapid caspase activation (6h) and loss of viability (24h) across a diverse set of hematological cancers (median caspase EC50 = 30 nM, GI50 = 11 nM) but with minimal effect on solid tumors (median EC50 & GI50 >30 μM)^[2].
In vivo	AZD4573 exhibits a short half-life in multiple preclinical species (less than one hour in rat, dog and monkey) and good solubility for intravenous administration^[1].
References	[1] http://cancerres.aacrjournals.org/content/78/13_Supplement/1650 [2] http://cancerres.aacrjournals.org/content/78/13_Supplement/310 [3] https://pubmed.ncbi.nlm.nih.gov/36026503/ [4] https://pubmed.ncbi.nlm.nih.gov/33306391/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05140382	Completed	Relapsed/Refractory Peripheral T-cell Lymphoma\|Relapsed/Refractory Classical Hodgkins Lymphoma	AstraZeneca	December 15 2021	Phase 2
NCT04630756	Active not recruiting	Advanced Haematological Malignancies	AstraZeneca\|Parexel	February 17 2021	Phase 1\|Phase 2
NCT03263637	Completed	Relapsed or Refractory Haematological Malignancies Including\|Acute Myeloid Leukemia\|Acute Lymphocytic Leukemia\|Chronic Lymphocytic Leukemia\|High Risk Myelodysplastic Syndrome\|Chronic Myelomonocytic Leukemia\|Richter''s Syndrome\|B-cell Non-Hodgkin Lymphoma\|T-cell Non-Hodgkin Lymphoma\|Small Lymphocytic Lymphoma\|Multiple Myeloma	AstraZeneca	October 24 2017	Phase 1

Tech Support

Handling Instructions

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