Home Epigenetics Epigenetic Reader Domain inhibitor BMS-986158 For research use only.

BMS-986158

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.

BMS-986158 Chemical Structure

BMS-986158 Chemical Structure

CAS No. 1800340-40-2

Purity & Quality Control

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

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Signaling Pathway

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Epigenetic Reader Domain Signaling Pathway

Biological Activity

Description 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.
Targets
BET [1]
(in NCI-H211 cells)		 BET [1]
(in MDA-MB231 cells)
6.6  nM 5  nM
In vitro
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>
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

Chemical Information & Solubility

Molecular Weight 495.62 Formula

C30H33N5O2
CAS No. 1800340-40-2 SDF --
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
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 25 mg/mL ( (50.44 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble


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In vivo
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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.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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