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BMS-833923 (XL-139)

  Cat. No.:  DC7154   Featured
Chemical Structure
1059734-66-5
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Field of application
BMS 833923 is an orally bioavailable inhibitor of Smo. 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 inhi
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1059734-66-5
Chemical Name: N-[2-methyl-5-(methylaminomethyl)phenyl]-4-[(4-phenylquinazolin-2-yl)amino]benzamide
Synonyms: BMS 833923; BMS833923; XL-139; XL139; XL 139
SMILES: C(NC1=CC(CNC)=CC=C1C)(=O)C1=CC=C(NC2=NC(C3=CC=CC=C3)=C3C(=N2)C=CC=C3)C=C1
Formula: C30H27N5O
M.Wt: 473.57
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: 1. Lee, H.K., Kim, H.W., Lee, I.Y., et al. G-749, a novel FLT3 kinase inhibitor, can overcome drug resistance for the treatment of acute myeloid leukemia. Blood 123(14), 2209-2219 (2014).
Description: 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.BMS-833923 inhibits the sonic hedgehog (SHH) pathway protein SMO, which may result in a suppression of the SHH signaling pathway.
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
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].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
2018-0101
Cat. No. Product name Field of application
DC47944 MRT-81 MRT-81 is a potent antagonist of human and rodent smoothened Smo receptors, with an IC50 value of 41 nM in the Shh-light2 cells. MRT-81 has potent hedgehog inhibiting activity. MRT-81 can be used for the research of cancer.
DC8225 Smoothened Agonist (SAG) free base SAG is a potent Smoothened (Smo) receptor agonist (Kd = 59 nM); potently activates the Hedgehog signaling pathway in Shh-light 2 cells (EC50 ~ 3 nM).
DC7027 Glasdegib(PF-04449913) PF-04449913 is a potent and orally bioavailable inhibitor of smoothened with IC50 of 5 nM(Gli-luciferase reporter reporter in C3H10T1/2); the hedgehog pathway inhibitor
DC7154 BMS-833923 (XL-139) BMS 833923 is an orally bioavailable inhibitor of Smo. 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 inhi
DC8570 ALLO-1 ALLO-1 is a SMO antagonist that inhibits both wild-type (IC50 = 50 nM) and mutant SMO, including the D473H SMO mutant (IC50s = 300-1000 nM).
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