LYN-1604 is a novel activator of ULK1, inducing cell death involved in ATF3, RAD21, and caspase3, accompanied by autophagy and apoptosis. LYN-1604 has an IC50 of 1.66 μM against MDA-MB-231 cells, and it binds to wild-type ULK1 with a binding affinity in the nanomole range (Kd=291.4 nM). The ULK1 (Y89A) mutant protein caused a sharp decrease in binding affinity with lower response and Kd than wild-type ULK1, ULK1 (K50A) and ULK1 (L53A) mutants.
| Cell Experiment | |
|---|---|
| Cell lines | MDA-MB-231 cells |
| Preparation method | Cells are dispensed in 96-well plates at a density of 5 × 104 cells per mL. After 24 h of incubation, cells are treated with different concentrations of compounds for the indicated time periods. Cell viability is measured by the MTT assay. |
| Concentrations | 0.5, 1.0 and 2.0 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | MDA-MB-231 xenograft model (BALB/c nude mice) |
| Formulation | - |
| Dosages | 25 mg/kg, 50 mg/kg, 100 mg/kg |
| Administration | intragastric administration |
| Molecular Weight | 657.54 |
| Formula | C33H45Cl4N3O2 |
| CAS Number | 2088939-99-3 |
| Solubility (25°C) | Water 90 mg/mL DMSO 45 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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