ASP3026

Catalog No.S8054

ASP3026 Chemical Structure

Molecular Weight(MW): 580.74

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

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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

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 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]

Protocol

Solubility (25°C)

In vitro DMSO 14 mg/mL (24.1 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 580.74
Formula

C29H40N8O3S

CAS No. 1097917-15-1
Storage powder
Synonyms N/A

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Clinical Trial Information

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

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

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID