ME-401 (PWT-143, P110δ-IN-1) is an oral, potent and selective inhibitor of Phosphatidylinositol 3-Kinase (PI3K) P110δ with IC50 of 0.6 nM in cellular assay.
|Solubility (25°C)||DMSO 20 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.
 Hideki Goto, et al. Int J Hematol. Zandelisib (ME-401) in Japanese patients with relapsed or refractory indolent non-Hodgkin's lymphoma: an open-label, multicenter, dose-escalation phase 1 study
 Ofir Moreno, et al. Target Oncol. Absorption, Distribution, and Binding Profile of ME-401, a Potent and Selective Oral Small-Molecule Inhibitor of Phosphatidylinositol 3-Kinase δ (PI3Kδ) in Animal and B-Cell Lymphoma Models
 Krish Patel, et al. Curr Hematol Malig Rep. Exploring a Future for PI3K Inhibitors in Chronic Lymphocytic Leukemia
 Ofir Moreno, et al. Clin Ther. Safety, Pharmacokinetics, and Pharmacodynamics of ME-401, an Oral, Potent, and Selective Inhibitor of Phosphatidylinositol 3-Kinase P110δ, Following Single Ascending Dose Administration to Healthy Volunteers
 N P Gupta, et al. J Endourol. Vapor resection: a good alternative to standard loop resection in the management of prostates >40 cc
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|Selective PI3Kδ Inhibitor 1 (compound 7n)
Selective PI3Kδ Inhibitor 1 (compound 7n) is an inhibitor of PI3Kδ with an IC50 of 0.9 nM and >1000-fold selectivity against other class I PI3K isoforms [PI3K α/γ/β=3670/1460/21300 nM].
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