ASP3026 ALK inhibitor

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Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	EGFR VEGFR PDGFR FGFR c-Met Src MEK CSF-1R FLT3 HER2
Other ALK Inhibitors	TAE684 (NVP-TAE684) GSK1838705A Repotrectinib (TPX-0005) AZD3463 Ensartinib dihydrochloride AP26113-analog (ALK-IN-1) NVL-655 (Neladalkib) Envonalkib Belizatinib (TSR-011) HG-14-10-04

Chemical Information, Storage & Stability

Molecular Weight	580.74	Formula	C₂₉H₄₀N₈O₃S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1097917-15-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
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
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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.

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 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 tumour cell line endogenously expressing EML4-ALK variant 3, with an IC50 value of 64.8 nM.
In vivo	ASP3026, administered to mice bearing subcutaneous NCI-H2228 tumour xenografts as twice daily oral dosing for 14 days, induces dose dependent anti-tumour effects starting at 1 mg/kg with strong regression at 10, 30 and 100 mg/kg.
References	[1] http://cancerres.aacrjournals.org/cgi/content/meeting_abstract/71/8_MeetingAbstracts/2821

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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Chemical Structure

Molecular Weight: 580.74