Shopping Cart

Your shopping cart is currently empty

Y06137

Name: Y06137
Brand: TargetMol
SKU: T13363
Price: 55 USD
Availability: InStock
Rating: 5 (10 reviews)

🥰Excellent

Catalog No. T13363Cas No. 2226534-49-0

Y06137 is an effective and selective BET inhibitor with a Kd of 81 nM for BRD4(1) bromodomain. Y06137 can be used for research on the treatment of castration-resistant prostate cancer.

Y06137

🥰Excellent

Purity: 99.85%

Catalog No. T13363Cas No. 2226534-49-0

Y06137 is an effective and selective BET inhibitor with a Kd of 81 nM for BRD4(1) bromodomain. Y06137 can be used for research on the treatment of castration-resistant prostate cancer.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$55	In Stock	In Stock
2 mg	$79	In Stock	In Stock
5 mg	$129	In Stock	In Stock
10 mg	$213	In Stock	In Stock
25 mg	$396	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$143	In Stock	In Stock

Add to Cart

Add to Quotation

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

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products. If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

Questions

Batch Information

Select Batch

Purity:99.85%

Appearance:Solid

Color:White

Resource Download

COA HNMR LCMS

Product Introduction

Bioactivity

Description	Y06137 is an effective and selective BET inhibitor with a Kd of 81 nM for BRD4(1) bromodomain. Y06137 can be used for research on the treatment of castration-resistant prostate cancer.
Targets&IC50	BRD4(1):81 nM (kd)
In vitro	Treatment of AR-positive prostate cancer cell lines 22Rv1 cells with Y06137 (1, 2, 4, 8, and 16 μM, 48 hours) results in significant down-regulation of both full-length (AR-fl) and AR variants levels. Y06137 (0.001-100 nM) exhibits low micromolar or nanomolar potencies in the four androgen receptor (AR)-positive prostate cancer cell lines LNCaP, C4-2B, 22Rv1, and VCaP cells with IC50s of 0.47, 0.84, 0.70, 0.29 μM, respectively[1].
In vivo	Y06137 (50 mg/kg, i.p., 100 μL) exhibited potent antitumor activity in a C4-2B CRPC xenograft tumor model in mice, achieving a tumor growth inhibition (TGI) of 51% during a 25-day treatment period[1].

Chemical Properties

Molecular Weight	444.57
Formula	C₂₇H₃₂N₄O₂
Cas No.	2226534-49-0
Smiles	C[C@H]1COCCN1c1ccc2nc(-c3ccc4onc(C)c4c3)n(CC3CCCCC3)c2c1
Relative Density.	1.31 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: 65 mg/mL (146.21 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.5 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	2.2494 mL	11.2468 mL	22.4936 mL	112.4682 mL
5 mM	0.4499 mL	2.2494 mL	4.4987 mL	22.4936 mL
10 mM	0.2249 mL	1.1247 mL	2.2494 mL	11.2468 mL
20 mM	0.1125 mL	0.5623 mL	1.1247 mL	5.6234 mL
50 mM	0.0450 mL	0.2249 mL	0.4499 mL	2.2494 mL
100 mM	0.0225 mL	0.1125 mL	0.2249 mL	1.1247 mL

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Molecular Weight Calculator

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