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BMS-986158 Epigenetic Reader Domain inhibitor

Name: BMS-986158
Brand: Selleck Chemicals
SKU: S9691
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S9691

BMS-986158 is a potent inhibitor of BET with IC50s of 6.6 nM and 5 nM in NCI-H211 small cell lung cancer (SCLC) cells and MDA-MB231 triple negative breast cancer (TNBC) cells, respectively.

Chemical Structure

Molecular Weight: 495.62

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S969101 DMSO]25 mg/mL]false]Ethanol]3 mg/mL]false]Water]Insoluble]false Purity: 99.96%

99.96

Related Targets	HDAC JAK Histone Methyltransferase AMPK PKC PARP HIF Histone Acetyltransferase Aurora Kinase Sirtuin PRMT Histone Demethylase EZH1/2 DNA Methyltransferase Pim LSD1 MLL JMJD G9a/GLP NSD FTO MicroRNA PAD SETD SMYD DOT1 COMT WDR5 HNMT SAM MTase
Related Products	Birabresib (OTX015) I-BET151 (GSK1210151A) Molibresib (I-BET-762) SGC-CBP30 EED226 Apabetalone (RVX-208) KG-501 CPI-203 compound 3i (666-15) PFI-3 AZD5153 6-hydroxy-2-naphthoic acid PFI-1 (PF-6405761) Mivebresib (ABBV-075) ABBV-744 UNC1215 I-BRD9 Bromosporine PLX51107 GSK1324726A (I-BET726) Pelabresib (CPI-0610) PF-CBP1 HCl INCB054329 MS436 GSK2801 UNC669 MZ-1 NEO2734 (EP31670) OF-1 CPI-637 GSK6853

Chemical Information, Storage & Stability

Molecular Weight	495.62	Formula	C₃₀H₃₃N₅O₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1800340-40-2	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C[N]1N=NC(=C1C2=CC3=C(N=C2)C4=C(C=C(C=C4)C(C)(C)O)[N]3C(C5CCOCC5)C6=CC=CC=C6)C

Solubility

In vitro
Batch:

DMSO : 25 mg/mL (50.44 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.250mg/ml (2.52mM)	Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.312mg/ml (0.63mM)	Taking the 1 mL working solution as an example, add 50 μL of 6.25 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	BET ^[1] (in NCI-H211 cells) 6.6 nM BET ^[1] (in MDA-MB231 cells) 5 nM
In vitro	BMS-986158 is a BET inhibitor. The IC50 in NCI-H211 small cell lung cancer (SCLC) cells and MDA-MB231 triple negative breast cancer (TNBC) cells is 6.6 nM and 5 nM, respectively.<sup><a class="sref" href="#s_ref">[1]</a></sup>
References	[1] https://pubmed.ncbi.nlm.nih.gov/32286255/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03936465	Active not recruiting	Solid Tumor Childhood\|Lymphoma\|Brain Tumor Pediatric	Dana-Farber Cancer Institute\|Stand Up To Cancer	September 27 2019	Phase 1
NCT02419417	Completed	Advanced Tumors	Bristol-Myers Squibb	June 19 2015	Phase 1\|Phase 2

Tech Support

Handling Instructions

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