BMS
BMS kdorfman Fri, 03/25/2022 - 13:50BMS 833923
| ___ | ___ |
|---|---|
| CAS Registry No. | 1059734-66-5 |
| Formal Name: | N-[2-methyl-5-[(methylamino)methyl]phenyl]-4-[(4-phenyl-2-quinazolinyl)amino]-benzamide |
| Synonym | XL 139 |
| MF: | C30H27N5O |
| FW: | 473.6 |
| Purity: | ≥98%S |
| Stability: | ≥2 years at -20°C |
| Solubility | 0.1 mg/ml in a 1:7 solution of ethanol:PBS (dissolve in ethanol first!) Use aqueous solution within 1 day |
| Supplied as: | A crystalline solid |
| UV/Vis. | λmax: 315 nm |
Smoothened (Smo) is a cell surface receptor that, with Patched, mediates sonic hedgehog (Shh) signaling to regulate gene expression through the Gli transcription factors.1 BMS 833923 is an orally bioavailable inhibitor of Smo.2,3 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.
References
Ruiz-Gómez, A., Molnar, C., Holguín, H., et al. The cell biology of Smo signalling and its relationships with GPCRs. Biochim. Biophys. Acta1768(4), 901-912 (2007).
Sandhiya, S., Melvin, G., Kumar, S.S., et al. The dawn of hedgehog inhibitors: Vismodegib. J. Pharmacol. Pharmacother.4(1), 4-7 (2013).
Lin, T.L. and Matsui, W. Hedgehog pathway as a drug target: Smoothened inhibitors in development. OncoTargets and Therapy5, 47-58 (2012)