BMS-833923_product_DataBase

Bioactivity

BMS-833923 (XL-139) is an orally bioavailable small-molecule inhibitor of Smoothened with potential antineoplastic activity; inhibits BODIPY cyclopamine binding to SMO in a dose-dependent manner with an IC50 of 21 nM.IC50 Value: 6-35 nM [1]Target: SmoothenedSMO antagonist BMS-833923 inhibits the sonic hedgehog (SHH) pathway protein SMO, which may result in a suppression of the SHH signaling pathway.in vitro: In vitro, BMS-833923 inhibits the expression of downstream effectors in the HH pathway (GLI1 and PTCH1) in cell lines that express wild-type SMO and those which express activated mutant forms of SMO (IC50values of 6-35 nM). In FACS-based binding assays, BMS-833923 inhibits BODIPY cyclopamine binding to SMO in a dose-dependent manner with an IC50 of 21 nM [1]. in vivo: Pharmacodynamic studies show that BMS-833923 robustly inhibits HH pathway activity with along duration of action after a single oral dose in medulloblastoma and pancreatic carcinoma xenograft models. The pharmacodynamic effects of BMS-833923 observed in these models translate into tumor growth inhibition at well-tolerated doses [1].Clinical trial: Dasatinib Combo With Smoothened (SMO) Antagonist (BMS-833923). Phase 2

Name

BMS-833923

CAS

1059734-66-5

Formula

C30H27N5O

Molar Mass

473.57

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Steven B, et al. Abstract B192: Preclinical characterization of BMS-833923 (XL139), a hedgehog (HH) pathway inhibitor in early clinical development. Molecular Cancer Therapeutics: December 2009; Volume 8, Issue 12, Supplement 1.

PeptideDB

BMS-833923

CAS: 1059734-66-5 F: C30H27N5O W: 473.57