Zandelisib (ME-401)

Catalog No.S8917 Synonyms: PWT-143, P110δ-IN-1, PW 143, ACC-524

For research use only.

Zandelisib (ME-401, PWT-143, P110δ-IN-1, PW 143, ACC-524) is an oral, potent and selective inhibitor of Phosphatidylinositol 3-Kinase (PI3K) P110δ with IC50 of 0.6 nM in cellular assay.

Zandelisib (ME-401) Chemical Structure

CAS No. 1595129-71-7

Purity & Quality Control

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Biological Activity

Description Zandelisib (ME-401, PWT-143, P110δ-IN-1, PW 143, ACC-524) is an oral, potent and selective inhibitor of Phosphatidylinositol 3-Kinase (PI3K) P110δ with IC50 of 0.6 nM in cellular assay.
Targets
P110δ [1]
(Cell-free assay)
0.6 nM
In vivo

ME-401 is an oral, once-daily, selective PI3Kδ inhibitor with an optimized pharmacologic profile that is in clinical development for the treatment of B-cell malignancies. ME-401 can be orally absorbed, distribute to target tissues, enter and accumulate in target cells, and bind to the target with high affinity to exert its mechanism of action.[2]

Protocol (from reference)

Animal Research:

[2]

  • Animal Models: CD-1 mice, Sprague Dawley (SD) rats, Female BALB/c mice, Beagle dogs, Cynomolgus monkeys
  • Dosages: 10 mg/kg for mice, 5 mg/kg for rats, 2 mg/kg for dogs and monkeys
  • Administration: Oral gavage

Solubility (25°C)

In vitro

DMSO 20 mg/mL
(33.07 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 604.77
Formula

C31H40N8O3S

CAS No. 1595129-71-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)(CC1=CC=CC=C1C2CCN(CC2)C)NC3=NC(=NC(=N3)N4CCOCC4)N5C6=CC=CC=C6N=C5S(=O)(=O)C

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04533581 Active not recruiting Drug: ME-401 Indolent B-cell Non-Hodgkin''s Lymphoma Kyowa Kirin Co. Ltd. September 17 2020 Phase 2
NCT03985189 Active not recruiting Drug: ME-401 Relapsed or Refractory Indolent B-cell Non-Hodgkin''s Lymphoma Kyowa Kirin Co. Ltd. April 29 2019 Phase 1
NCT03768505 Recruiting Drug: Zandelisib (ME-401) Follicular Lymphoma (FL)|Non Hodgkin Lymphoma|Marginal Zone Lymphoma MEI Pharma Inc. December 15 2018 Phase 2
NCT02914938 Recruiting Drug: ME-401|Drug: Rituximab|Drug: Zanubrutinib Chronic Lymphocytic Leukemia (CLL)|Small Lymphocytic Lymphoma (SLL)|Follicular Lymphoma (FL)|Marginal Zone B Cell Lymphoma|Diffuse Large B-cell Lymphoma (DLBCL)|High Grade Non-Hodgkin''s Lymphoma|Mantle Cell Lymphoma (MCL) MEI Pharma Inc. October 2016 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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