Home GPCR & G Protein Hedgehog/Smoothened antagonist BMS-833923 For research use only.

BMS-833923

Synonyms: XL139

BMS-833923 (XL139) is an orally bioavailable Smoothened antagonist. Phase 2.

BMS-833923 Chemical Structure

BMS-833923 Chemical Structure

CAS No. 1059734-66-5

Purity & Quality Control

BMS-833923 Related Products

Signaling Pathway

Hedgehog/Smoothened Signaling Pathways

Hedgehog/Smoothened Signaling Pathway

Biological Activity

Description BMS-833923 (XL139) is an orally bioavailable Smoothened antagonist. Phase 2.
Targets
Smoothened [1]
In vitro
In vitro BMS-833923 reduces hedgehog pathway activity, decreases cell proliferation and induces apoptosis via the intrinsic pathway in esophageal adenocarcinoma (EAC) cell lines. [2] BMS-833923 dose-dependently affects canonical and prostate hedgehog signature gene transcription in vitro. [3]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01413906 Completed
Cancer
Bristol-Myers Squibb
 November 2011 Phase 1
NCT01218477 Completed
Leukemia
Bristol-Myers Squibb
 January 2011 Phase 1|Phase 2
NCT00927875 Completed
Small Cell Lung Carcinoma
Bristol-Myers Squibb|Exelixis
 February 2010 Phase 1
NCT00909402 Completed
Stomach Neoplasms|Esophageal Neoplasms
Bristol-Myers Squibb|Exelixis
 November 2009 Phase 1
NCT00670189 Completed
Hedgehog Pathway|Smoothened|Basal Cell Carcinoma (BCC)|Basal Cell Nevoid Syndrome (BCNS)
Bristol-Myers Squibb|Exelixis
 July 2008 Phase 1

Chemical Information & Solubility

Molecular Weight 473.57 Formula

C30H27N5O
CAS No. 1059734-66-5 SDF Download BMS-833923 SDF
Smiles CC1=C(C=C(C=C1)CNC)NC(=O)C2=CC=C(C=C2)NC3=NC4=CC=CC=C4C(=N3)C5=CC=CC=C5
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 95 mg/mL ( (200.6 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

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Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

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

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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
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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.

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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