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ME-401

Cat. No. M20796
ME-401 Structure
Synonym:

PWT-143, P110δ-IN-1

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Biological Activity

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.

Chemical Information
Molecular Weight 604.77
Formula C31H40N8O3S
CAS Number 1595129-71-7
Solubility (25°C) DMSO 20 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] 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

[2] 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

[3] Krish Patel, et al. Curr Hematol Malig Rep. Exploring a Future for PI3K Inhibitors in Chronic Lymphocytic Leukemia

[4] 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

[5] 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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Keywords: ME-401, PWT-143, P110δ-IN-1 supplier, PI3K, inhibitors, activators
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