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BSJ-4-116

Name: BSJ-4-116
Brand: TargetMol
SKU: T9117
Price: 50 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T9117Cas No. 2519823-34-6

BSJ-4-116 is a highly potent and selective CDK12 degrader (PROTAC) with an IC50 of 6 nM. It downregulates DDR genes through a premature termination of transcription, primarily through increasing poly(adenylation).

BSJ-4-116

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Purity: 99.09%

Catalog No. T9117Cas No. 2519823-34-6

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$50	In Stock	In Stock
5 mg	$113	In Stock	In Stock
10 mg	$189	In Stock	In Stock
25 mg	$396	In Stock	In Stock
50 mg	$637	In Stock	In Stock
100 mg	$953	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$173	In Stock	In Stock

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

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Purity:99.09%

Appearance:Solid

Color:White

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COA HPLC HNMR

Product Introduction

Bioactivity

Description	BSJ-4-116 is a highly potent and selective CDK12 degrader (PROTAC) with an IC50 of 6 nM. It downregulates DDR genes through a premature termination of transcription, primarily through increasing poly(adenylation).
Targets&IC50	CDK12:6 nM
In vitro	BSJ-4-116 (50?nM; 6-24?hours) decreases the level of CDK12 protein, regardless of the mutational status of the cell line.BSJ-4-116 (10-10000 nM; 72 hours) exhibits potent antiproliferative effects in Kelly CDK12C1039F.BSJ-4-116 inhibits the growth of T-ALL cells (Jurkat and MOLT-4 cells) and sensitizes them to PARP inhibition. BSJ-4-116 regulates DDR genes via poly(adenylation). BSJ-4-116 overcomes CDK12C1039F mutation. BSJ-4-116 represents the first example of resistance to a bivalent degrader molecule that is a consequence of an acquired point mutation in the target protein.

Chemical Properties

Molecular Weight	837.38
Formula	C₄₀H₄₉ClN₈O₈S
Cas No.	2519823-34-6
Smiles	O=C1C=2C(C(=O)N1C3C(=O)NC(=O)CC3)=CC=CC2OCC(NCCCCCCCN4C[C@H](NC=5N=C(NC6=C(S(C(C)C)(=O)=O)C=CC=C6)C(Cl)=CN5)CCC4)=O
Relative Density.	1.368 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: 250 mg/mL (298.55 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (5.97 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	1.1942 mL	5.9710 mL	11.9420 mL	59.7100 mL
5 mM	0.2388 mL	1.1942 mL	2.3884 mL	11.9420 mL
10 mM	0.1194 mL	0.5971 mL	1.1942 mL	5.9710 mL
20 mM	0.0597 mL	0.2986 mL	0.5971 mL	2.9855 mL
50 mM	0.0239 mL	0.1194 mL	0.2388 mL	1.1942 mL
100 mM	0.0119 mL	0.0597 mL	0.1194 mL	0.5971 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