An orally bioavailable inhibitor of Smo; blocks binding of BODIPY cyclopamine (IC50 = 21 nM) and inhibits Gli activation in cell lines that express wild-type Smo or activated mutant forms of Smo (IC50s = 6-35 nM); inhibits Shh pathway activity and prevents tumor growth in cancer xenograft models

BMS 833923 – 50 mg

Brand:
Cayman
CAS:
1059734-66-5
Storage:
-20
UN-No:
De Minimis - 3077 / 9

Smoothened (Smo) is a cell surface receptor that, with Patched, mediates sonic hedgehog (Shh) signaling to regulate gene expression through the Gli transcription factors.{21774} BMS 833923 is an orally bioavailable inhibitor of Smo.{27708,27709} It blocks binding of BODIPY cyclopamine (IC50 = 21 nM) and inhibits Gli activation in cell lines that express wild-type Smo or activated mutant forms of Smo (IC50s = 6-35 nM). BMS 833923 robustly inhibits Shh pathway activity and prevents tumor growth in medulloblastoma and pancreatic carcinoma xenograft models.  

 

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Description

An orally bioavailable inhibitor of Smo; blocks binding of BODIPY cyclopamine (IC50 = 21 nM) and inhibits Gli activation in cell lines that express wild-type Smo or activated mutant forms of Smo (IC50s = 6-35 nM); inhibits Shh pathway activity and prevents tumor growth in cancer xenograft models

Formal name: N-[2-methyl-5-[(methylamino)methyl]phenyl]-4-[(4-phenyl-2-quinazolinyl)amino]-benzamide

Synonyms:  XL 139

Molecular weight: 473.6

CAS: 1059734-66-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cancer|Cell Signaling|Hedgehog Signaling||Research Area|Cancer|Transcription Factors||Research Area|Cell Biology|Cell Signaling|Hedgehog Signaling||Research Area|Epigenetics, Transcription, & Translation|Transcription Factors

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