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BMS-986158

🥰Excellent
Catalog No. T14685Cas No. 1800340-40-2

BMS-986158 is a highly effective BET inhibitor, demonstrating IC50 values of 6.6 nM in NCI-H211 small cell lung cancer (SCLC) cells and 5 nM in MDA-MB231 triple negative breast cancer (TNBC) cells.

BMS-986158

BMS-986158

🥰Excellent
Purity: 98.78%
Catalog No. T14685Cas No. 1800340-40-2
BMS-986158 is a highly effective BET inhibitor, demonstrating IC50 values of 6.6 nM in NCI-H211 small cell lung cancer (SCLC) cells and 5 nM in MDA-MB231 triple negative breast cancer (TNBC) cells.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$79In StockIn Stock
5 mg$272In StockIn Stock
10 mg$490In StockIn Stock
25 mg$785In StockIn Stock
50 mg$1,080In StockIn Stock
100 mg$1,460-In Stock
1 mL x 10 mM (in DMSO)$297In StockIn 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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Purity:98.78%
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COA LCMS HNMR HPLC

Product Introduction

Bioactivity
Description
BMS-986158 is a highly effective BET inhibitor, demonstrating IC50 values of 6.6 nM in NCI-H211 small cell lung cancer (SCLC) cells and 5 nM in MDA-MB231 triple negative breast cancer (TNBC) cells.
Targets&IC50
BET:6.6 nM(in NCI-H211 SCLC cells), BET:5 nM (in MDA-MB231 TNBC) cells)
In vitro
BMS-986158 acts as an inhibitor targeting the bromodomain (BRD) and extra-terminal domain (BET) protein family, offering potential for cancer treatment. When administered, BMS-986158 attaches to the BRD's acetyl-lysine binding site on BET proteins, blocking their interaction with acetylated histones. This interruption hampers chromatin remodeling and curbs the expression of genes that promote growth, thereby inhibiting tumor cell proliferation[2].
Chemical Properties
Molecular Weight495.62
FormulaC30H33N5O2
Cas No.1800340-40-2
SmilesCc1nnn(C)c1-c1cnc2c(c1)n([C@@H](C1CCOCC1)c1ccccc1)c1cc(ccc21)C(C)(C)O
Relative Density.1.28 g/cm3 (Predicted)
ColorWhite
AppearanceSolid
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 60 mg/ml (121.06 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.04 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
1mg5mg10mg50mg
1 mM2.0177 mL10.0884 mL20.1767 mL100.8837 mL
5 mM0.4035 mL2.0177 mL4.0353 mL20.1767 mL
10 mM0.2018 mL1.0088 mL2.0177 mL10.0884 mL
20 mM0.1009 mL0.5044 mL1.0088 mL5.0442 mL
50 mM0.0404 mL0.2018 mL0.4035 mL2.0177 mL
100 mM0.0202 mL0.1009 mL0.2018 mL1.0088 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:
TargetMol | Animal experimentsFor 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 DMSOTargetMol | 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 DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2OTargetMol | 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.
1 Enter information below:
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2 Enter the in vivo formulation:
% DMSO
%
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Dose Conversion

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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

Keywords

InhibitorinhibitEpigeneticReaderDomainEpigenetic Reader DomainBMS-986158BMS986158BMS 986158BET
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