ASP3026 | 99.99%(HPLC) | In Stock

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

ASP3026 Chemical Structure

CAS: 1097917-15-1

Selleck's ASP3026 has been cited by 3 publications

Purity & Quality Control

Batch: Purity: 99.99%

99.99

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Signaling Pathway

ALK Signaling Pathway

Choose Selective ALK Inhibitors

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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
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

References
[1] Sadao Kuromitsu, et al. AACR 102nd Annual Meeting, 2011.

References

[1] Sadao Kuromitsu, et al. AACR 102nd Annual Meeting, 2011.

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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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

Preparing Stock Solutions

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In vivo Formulation Calculator (Clear solution)

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

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% DMSO + % + % Tween 80 + % ddH₂O

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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.
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
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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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