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Atuveciclib (Synonyms: BAY-1143572 Racemate)

Name: Atuveciclib
Brand: TargetMol
SKU: T10464L
Price: 45 USD
Availability: InStock
Rating: 5 (10 reviews)

Catalog No. T10464L Copy Product Info

Purity: 98.8%

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Atuveciclib (BAY 1143572) is a potent and highly selective PTEFb/CDK9 inhibitor with an IC50 value of 13 nm for CDK9/CycT1 and a selectivity ratio of 100 for CDK2, with highly bioavailable and orally available advantages.

Atuveciclib

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Catalog No. T10464L

Synonyms BAY-1143572 Racemate

Cas No. 1414943-88-6

Pack Size	Price	USA Stock	Global Stock
1 mg	$45	In Stock	In Stock
5 mg	$106	In Stock	In Stock
10 mg	$162	In Stock	In Stock
25 mg	$325	In Stock	In Stock
50 mg	$489	In Stock	In Stock
100 mg	$735	-	In Stock
1 mL x 10 mM (in DMSO)	$117	In Stock	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:98.8%

Appearance:Solid

Color:White

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COA LCMS

Product Introduction

Bioactivity

Description	Atuveciclib (BAY 1143572) is a potent and highly selective PTEFb/CDK9 inhibitor with an IC50 value of 13 nm for CDK9/CycT1 and a selectivity ratio of 100 for CDK2, with highly bioavailable and orally available advantages.
Targets&IC50	Antiproliferative:310 nM(MOLM-13 cells), Antiproliferative:920 nM(HeLa cells), P-TEFb/CDK9:13 nM, Apoptosis:385 nM(AML cell lines)
In vitro	Atuveciclib (BAY-1143572) exhibits a potent and highly selective inhibitory effect on PTEFb-kinase, specifically against PTEFb/CDK9, in the low nanomolar range, demonstrating at least 50-fold higher selectivity over other CDKs. The compound effectively inhibits the proliferation of seven AML cell lines, both with and without MLL rearrangements, evidenced by a median IC50 of 385 nM (ranging between 230-1100 nM), and it also triggers apoptosis[1]. Furthermore, Atuveciclib (BAY-1143572) differentiates itself by showing significant selectivity against a broad array of non-CDK kinases, coupled with wide-ranging antiproliferative effects across various tumor cell lines indicated by sub-micromolar IC50 values. Notably, it leads to the concentration-dependent inhibition of RNA polymerase II phosphorylation, subsequently diminishing MYC mRNA and protein levels[2].
In vivo	Atuveciclib (BAY-1143572) significantly enhances its effectiveness when used with various chemotherapeutics across different solid tumor models. Additionally, it reduces MYC mRNA levels in the blood cells of treated rats, suggesting the potential of using MYC as a pharmacodynamic marker during clinical trials. When administered orally once daily, Atuveciclib demonstrates efficacy as a single agent, achieving partial or complete remission in most AML (acute myeloid leukemia) xenograft models in both mice and rats, proving its potency and tolerability at certain doses.
Synonyms	BAY-1143572 Racemate

Chemical Properties

Molecular Weight	387.43
Formula	C₁₈H₁₈FN₅O₂S
Cas No.	1414943-88-6
Smiles	COc1cc(F)ccc1-c1ncnc(Nc2cccc(CS(C)(=N)=O)c2)n1
Relative Density.	1.36 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 100 mg/mL (258.11 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (10.32 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.5811 mL	12.9056 mL	25.8111 mL	129.0556 mL
5 mM	0.5162 mL	2.5811 mL	5.1622 mL	25.8111 mL
10 mM	0.2581 mL	1.2906 mL	2.5811 mL	12.9056 mL
20 mM	0.1291 mL	0.6453 mL	1.2906 mL	6.4528 mL
50 mM	0.0516 mL	0.2581 mL	0.5162 mL	2.5811 mL
100 mM	0.0258 mL	0.1291 mL	0.2581 mL	1.2906 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc