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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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