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TL12-186

Name: TL12-186
Brand: TargetMol
SKU: T34888
Price: 66 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T34888Cas No. 2250025-88-6

Alias TL12186, TL12 186

TL12-186 is a Cereblon-dependent kinase degrader that degrades CDK, BTK, FLT3, Aurora and other kinases.TL12-186 inhibits CDK2/cyclin A and CDK9/cyclin T1 with IC50s of 73 and 55 nM, respectively.

TL12-186

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Purity: 98.2%

Catalog No. T34888Alias TL12186, TL12 186Cas No. 2250025-88-6

TL12-186 is a Cereblon-dependent kinase degrader that degrades CDK, BTK, FLT3, Aurora and other kinases.TL12-186 inhibits CDK2/cyclin A and CDK9/cyclin T1 with IC50s of 73 and 55 nM, respectively.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$66	-	In Stock
2 mg	$96	-	In Stock
5 mg	$158	-	In Stock
10 mg	$248	-	In Stock
25 mg	$397	-	In Stock
50 mg	$569	-	In Stock
100 mg	$786	-	In Stock
200 mg	$1,080	-	In Stock
1 mL x 10 mM (in DMSO)	$272	-	In Stock

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

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Batch Information

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Purity:98.2%

Appearance:Solid

Color:Yellow

Resource Download

COA HNMR HPLC

Product Introduction

Bioactivity

Description	TL12-186 is a Cereblon-dependent kinase degrader that degrades CDK, BTK, FLT3, Aurora and other kinases.TL12-186 inhibits CDK2/cyclin A and CDK9/cyclin T1 with IC50s of 73 and 55 nM, respectively.
Targets&IC50	CDK2-CyclinA:73 nM (IC50), CRBN:12nM, CDK9-CyclinT1:55 nM (IC50)
In vitro	TL12-186 demonstrates over 90% inhibition against 193 kinases at a screening concentration of 1 μM[1]. Utilizing AlphaScreen binding assays, it exhibits potent binding to CRBN with an IC50 of 12 nM[1]. Displaying CRBN-dependent pharmacological effects, TL12-186 (1-10000 nM; 2 days) exerts 13 to 15 times stronger inhibition of cell survival in WT cells compared to CRBN-/- cells[1]. Moreover, at concentrations ranging from 10 to 10000 nM for 4 hours, TL12-186 selectively inhibits STAT1 phosphorylation without inducing degradation of JAK1/2[1].
Synonyms	TL12186, TL12 186

Chemical Properties

Molecular Weight	931.46
Formula	C₄₄H₅₁ClN₁₀O₉S
Cas No.	2250025-88-6
Smiles	O=C1NC(=O)C(N2C(=O)C=3C=CC=C(NCC(=O)NCCOCCOCCN4CCN(C5=CC=C(C=C5)NC6=NC=C(Cl)C(=N6)NC=7C=CC=CC7S(=O)(=O)C(C)C)CC4)C3C2=O)CC1
Relative Density.	no data available

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 200 mg/mL (214.72 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (5.37 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	1.0736 mL	5.3679 mL	10.7358 mL	53.6792 mL
5 mM	0.2147 mL	1.0736 mL	2.1472 mL	10.7358 mL
10 mM	0.1074 mL	0.5368 mL	1.0736 mL	5.3679 mL
20 mM	0.0537 mL	0.2684 mL	0.5368 mL	2.6840 mL
50 mM	0.0215 mL	0.1074 mL	0.2147 mL	1.0736 mL
100 mM	0.0107 mL	0.0537 mL	0.1074 mL	0.5368 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