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THZ531

Name: THZ531
Brand: TargetMol
SKU: T4293
Price: 57 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T4293Cas No. 1702809-17-3

THZ531 is a covalent inhibitor of both CDK12(IC50=158 nM) and CDK13(IC50=69 nM).

THZ531

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Purity: 99.86%

Catalog No. T4293Cas No. 1702809-17-3

THZ531 is a covalent inhibitor of both CDK12(IC50=158 nM) and CDK13(IC50=69 nM).

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$57	In Stock	In Stock
2 mg	$83	In Stock	In Stock
5 mg	$113	In Stock	In Stock
10 mg	$155	In Stock	In Stock
25 mg	$347	In Stock	In Stock
50 mg	$497	In Stock	In Stock
100 mg	$723	In Stock	In Stock
500 mg	$1,490	-	In Stock
1 mL x 10 mM (in DMSO)	$139	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.86%

Color:White

Resource Download

COA HNMR HPLC

Product Introduction

Bioactivity

Description	THZ531 is a covalent inhibitor of both CDK12(IC50=158 nM) and CDK13(IC50=69 nM).
Targets&IC50	CDK12:158 nM, CDK13:69 nM, CDK9:10.5 μM, CDK7:8.5 μM
In vitro	In Jurkat cell, THZ531(IC50=50 nM) treatment leads to a dramatic and irreversible decrease proliferation.THZ531 potently inhibits CDK12(IC50=158 nM) and CDK13 (IC50=69 nM).
Kinase Assay	Cells are treated with THZ531 for 6 hours.After treatment cells are washed 2-fold with cold PBS and then lysed in the following lysis buffer: Hepes(50 mM, pH 7.4), NaCl（150 mM）, 1% Nonidet P40 substitute, EDTA（5 mM）, DTT（1 mM）, and protease/phosphatase cocktails.Lysates are treated with bio-THZ1 or bio-TH531 for pulldown overnight at 4°C.
Cell Research	Jurkat cells are plated in 96-well plates at 20,000 cells/well in fresh media and treated with THZ531 or DMSO at the indicated concentrations for 72 hours. HAP1 cells are seeded in 96-well plates at 12,000 cells/well in fresh media and 24 hours later are treated with THZ531 at the indicated concentrations for 72 hours. Anti-proliferative effect of THZ531 is assessed. To assess the effect of inhibitor washout on anti-proliferation of Jurkat cells, cells are treated with THZ531 or DMSO for 6 hrs. Inhibitor-containing medium is then removed and incubated with or without THZ531 for 66 hrs. Anti-proliferative effect of THZ531 is assessed. All proliferation assays are performed in biological triplicate. IC50s are determined using non-linear regression curve fit.

Chemical Properties

Molecular Weight	558.07
Formula	C₃₀H₃₂ClN₇O₂
Cas No.	1702809-17-3
Smiles	CN(C)C\C=C\C(=O)Nc1ccc(cc1)C(=O)N1CCC[C@H](C1)Nc1ncc(Cl)c(n1)-c1c[nH]c2ccccc12
Relative Density.	1.342 g/cm3 (Predicted)

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 8.17 mg/mL (14.64 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (1.79 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	1.7919 mL	8.9594 mL	17.9189 mL	89.5945 mL
5 mM	0.3584 mL	1.7919 mL	3.5838 mL	17.9189 mL
10 mM	0.1792 mL	0.8959 mL	1.7919 mL	8.9594 mL

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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