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BMS-833923 Hedgehog/Smoothened antagonist

Cat.No.S7138

BMS-833923 (XL139) is an orally bioavailable Smoothened antagonist. Phase 2.
BMS-833923 Hedgehog/Smoothened antagonist Chemical Structure

Chemical Structure

Molecular Weight: 473.57

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Quality Control

Batch: Purity: 99.24%
99.24

Solubility

In vitro
Batch:

DMSO : 95 mg/mL (200.6 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : 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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 473.57 Formula

C30H27N5O

Storage (From the date of receipt)
CAS No. 1059734-66-5 Download SDF Storage of Stock Solutions

Synonyms XL139 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

Mechanism of Action

Targets/IC50/Ki
Smoothened
In vitro
BMS-833923 reduces hedgehog pathway activity, decreases cell proliferation and induces apoptosis via the intrinsic pathway in esophageal adenocarcinoma (EAC) cell lines. This compound dose-dependently affects canonical and prostate hedgehog signature gene transcription in vitro.
References

Clinical Trial Information

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

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

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