Home Protein Tyrosine Kinase ALK inhibitor ASP3026 For research use only.

ASP3026

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

ASP3026 Chemical Structure

ASP3026 Chemical Structure

CAS No. 1097917-15-1

Purity & Quality Control

ASP3026 Related Products

Signaling Pathway

ALK Signaling Pathways

ALK Signaling Pathway

Biological Activity

Description ASP3026 is a novel and selective inhibitor for ALK with IC50 of 3.5 nM. Phase 1.
Features ALK-selective inhibitor that has been tested in Phase I clinical trials for treatment of solid tumors and B-cell lymphoma.
Targets
ALK [1]
3.5 nM
In vitro
In vitro ASP3026 shows more selective ALK inhibition in a Tyr-kinase panel than PF02341066. ASP3026 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
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]
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

Chemical Information & Solubility

Molecular Weight 580.74 Formula

C29H40N8O3S
CAS No. 1097917-15-1 SDF Download ASP3026 SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 14 mg/mL ( (24.1 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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.

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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