Alpelisib (Byl-719) is an effective, selective PI3Kα inhibitor with oral activity. Alpelisib (Byl-719) was targeted to PIK3CA mutated carcinoma. The IC50 of Alpelisib (Byl-719) against P110 α, P110 γ, p110δ and P110 β were 5 nM, 250 nM, 290 nM and 1200 nM, respectively. It has antitumor activity.
Cancer Res Commun. 2022 Aug.
Pharmacological inhibition of SHP2 blocks both PI3K and MEK signaling in low-epiregulin HNSCC via GAB1
BYL-719 purchased from AbMole
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Source | Int J Cancer (2015). Figure 1. BYL719 |
| Method | Caspase 3/7 activity assay | |
| Cell Lines | HOS and MOS-J cells | |
| Concentrations | 25 μM | |
| Incubation Time | 24 and 48 hr | |
| Results | After 72 hr of treatment, BYL719 significantly inhibited the cell growth of all osteosarcoma cell lines tested in a dosedependent manner with an IC50 ranging from 6 to 15 μM and with the IC90 from 24 to 42 μM at 72 hr. |
| Molecular Weight | 441.47 |
| Formula | C19H22F3N5O2S |
| CAS Number | 1217486-61-7 |
| Solubility (25°C) | DMSO 72 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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