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Postion:Product Catalog >Biochemical Engineering>Inhibitors>protein tyrosine kinase>AZD-3463
AZD-3463
  • AZD-3463

AZD-3463 NEW

Price $48 $72 $125
Package 5mg 10mg 25mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-19

Product Details

Product Name: AZD-3463 CAS No.: 1356962-20-3
Purity: 99.13% Supply Ability: 10g
Release date: 2024/11/19

Product Introduction

Bioactivity

NameAZD-3463
DescriptionAZD-3463 (ALK/IGF1R inhibitor), an orally bioavailable ALK inhibitor (Ki: 0.75 nM), can inhibit IGF1R with equivalent potency.
Kinase AssayHDAC enzymatic assays: Tubastatin A is dissolved and diluted in assay buffer (50 mM HEPES, pH 7.4, 100 mM KCl, 0.001% Tween-20, 0.05% BSA, and 20 μM tris(2-carboxyethyl)phosphine) to 6-fold of the final concentration. HDAC enzymes are diluted to 1.5-fold of the final concentration in assay buffer and pre-incubated with Tubastatin A for 10 minutes before the addition of the substrate. The amount of FTS (HDAC1, HDAC2, HDAC3, and HDAC6) or MAZ-1675 (HDAC4, HDAC5, HDAC7, HDAC8, and HDAC9) used for each enzyme is equal to the Michaelis constant (Km), as determined by a titration curve. FTS or MAZ-1675 is diluted in assay buffer to 6-fold the final concentration with 0.3 μM sequencing grade trypsin. The substrate/trypsin mix is added to the enzyme/compound mix and the plate is shaken for 60 seconds and then placed into a SpectraMax M5 microtiter plate reader. The enzymatic reaction is monitored for release of 7-amino-4-methoxy-coumarin over 30 minutes, after deacetylation of the lysine side chain in the peptide substrate, and the linear rate of the reaction is calculated.
In vitroIn vivo, AZD-3463 is equally effective against both the mutated L1196M and the wild-type ALK. When acting on transplanted tumors in vivo, AZD-3463 dose-dependently inhibits pALK, leading to the stagnation (H3122) or reduction (DEL, H2228) of tumor volume.
In vivoIn various in vitro models resistant to Crizotinib, AZD3463 exhibits antiproliferative efficacy against five out of six cell lines, with a potency four times greater than that of the parent H3122 cells. AZD3463 is effective across tumor cell lines with ALK fusion, including DEL (ALCL NPM-ALK), H2228 (NSCLC EML4-ALK), and H3122 (NSCLC EML4-ALK), by inhibiting ALK and reducing its autophosphorylation.
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationEthanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 23 mg/mL (51.2 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
KeywordsAnaplastic lymphoma kinase (ALK) | Anaplastic lymphoma kinase | Apoptosis | neuroblastoma | kinase | ALK | AZD3463 | receptor | PI3K/AKT/mTOR. pathway | crizotinib | CD246 | AZD-3463 | IGF-1R | resistance | ALK tyrosine kinase receptor | Inhibitor | inhibit | AZD 3463 | Cluster of differentiation 246 | tyrosine | Autophagy
Inhibitors RelatedStavudine | 5-Fluorouracil | Sodium 4-phenylbutyrate | L-Ascorbic acid | Hydroxychloroquine | Guanidine hydrochloride | Taurine | Tributyrin | Curcumin | Paeonol | Naringin | Gefitinib
Related Compound LibrariesBioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Inhibitor Library | NO PAINS Compound Library | Stem Cell Differentiation Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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