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LY3039478 (Crenigacestat) is a novel and orally active Notch and γ-secretase inhibitor, with an IC50 of 1 nM in most of the tumor cell lines tested. Crenigacestat (LY3039478) decreases expression of Myc and cyclin A1 (part of the NOTCH-driven proliferative signature) in murine and human model systems. Crenigacestat (LY3039478) treatment also leads to G0/G1 cell cycle arrest in CCRCC cells.
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Source | J Biol Chem (2017). Figure 6. LY3039478 |
| Method | qRT-PCR | |
| Cell Lines | CCRCC cell lines | |
| Concentrations | 1 μM | |
| Incubation Time | - | |
| Results | Treatment with a secretase inhibitor that is being tested in clinical trials, LY3039478, significantly inhibited the growth of 2 CCRCC cell lines in a concentrationdependent manner |
| Molecular Weight | 464.44 |
| Formula | C22H23F3N4O4 |
| CAS Number | 1421438-81-4 |
| Solubility (25°C) | DMSO ≥ 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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