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
BYL719 purchased from AbMole
|Source||Int J Cancer (2015). Figure 1. BYL719|
|Method||Caspase 3/7 activity assay|
|Cell Lines||HOS and MOS-J cells|
|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.|
|Solubility (25°C)||DMSO 72 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Related PI3K Products|
EDI048 is an orally active Cryptosporidium PI4K inhibitor for the research of cryptosporidiosis.
PI3Kδ-IN-13 is a PI3Kδ inhibitor (IC50=2.6 nM).
PI3Kα-IN-13 is a PI3Kα inhibitor (IC50: 2.5 nM).
FD2056 is a potent and orally active PI3K inhibitor.
Acetyl-Exenatideyes is an acetylated derivative of Exenatide.
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