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ASP3026 ALK inhibitor

Cat.No.S8054

ASP3026 is a novel and selective inhibitor for ALK with IC50 of 3.5 nM. Phase 1.
ASP3026 ALK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 580.74

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Chemical Information, Storage & Stability

Molecular Weight 580.74 Formula

C29H40N8O3S

 Storage (From the date of receipt)
CAS No. 1097917-15-1 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC(C)S(=O)(=O)C1=CC=CC=C1NC2=NC(=NC=N2)NC3=C(C=C(C=C3)N4CCC(CC4)N5CCN(CC5)C)OC

Solubility

In vitro
Batch:

DMSO : 14 mg/mL (24.1 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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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.
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Mechanism of Action

Features
ALK-selective inhibitor that has been tested in Phase I clinical trials for treatment of solid tumors and B-cell lymphoma.
Targets/IC50/Ki
ALK [1]
3.5 nM
In vitro
ASP3026 shows more selective ALK inhibition in a Tyr-kinase panel than PF02341066. This compound inhibits the growth of NCI-H2228, a human NSCLC tumor cell line endogenously expressing EML4-ALK variant 3, with an IC50 value of 64.8 nM. [1]
In vivo
ASP3026, administered to mice bearing subcutaneous NCI-H2228 tumor xenografts as twice daily oral dosing for 14 days, induces dose dependent anti-tumor effects starting at 1 mg/kg with strong regression at 10, 30 and 100 mg/kg. [1]
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01401504 Completed
Solid Tumor
Astellas Pharma Inc
 May 2011 Phase 1
NCT01284192 Completed
Advanced Malignancies|Positive for Anaplastic Lymphoma Kinase|Positive for Proto-Oncogene Tyrosine-Protein Kinase ROS|Solid Tumor|B-Cell Lymphoma
Astellas Pharma Inc
 December 2010 Phase 1

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