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TL12-186

Name: TL12-186
Brand: TargetMol
SKU: T34888
Price: 90 USD
Availability: InStock
Rating: 5 (10 reviews)

🥰Excellent

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

🥰Excellent

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	$90	-	In Stock
5 mg	$222	-	In Stock
10 mg	$328	-	In Stock
25 mg	$575	-	In Stock
50 mg	$798	-	In Stock
100 mg	$1,090	-	In Stock
200 mg	$1,480	-	In Stock
1 mL x 10 mM (in DMSO)	$363	-	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:98.2%

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	CRBN:12nM, CDK9-CyclinT1:55 nM (IC50), CDK2-CyclinA:73 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
Color	Yellow
Appearance	Solid

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 mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

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