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AZD-3463

Catalog No. T1967 CAS 1356962-20-3

Synonyms: ALK/IGF1R inhibitor

AZD-3463 (ALK/IGF1R inhibitor) , an orally bioavailable ALK inhibitor (Ki: 0.75 nM), can inhibit IGF1R with equivalent potency.

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AZD-3463, CAS 1356962-20-3

Pack Size	Availability	Price/USD
5 mg	In stock	$ 48.00
10 mg	In stock	$ 72.00
25 mg	In stock	$ 125.00
50 mg	In stock	$ 207.00
100 mg	In stock	$ 369.00
1 mL * 10 mM (in DMSO)	In stock	$ 53.00

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Purity: 99.13%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	AZD-3463 (ALK/IGF1R inhibitor) , an orally bioavailable ALK inhibitor (Ki: 0.75 nM), can inhibit IGF1R with equivalent potency.
Targets&IC50	ALK:0.75 nM(Ki)
In vitro	In 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 vivo	In 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.
Kinase Assay	HDAC 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.

Synonyms	ALK/IGF1R inhibitor
Molecular Weight	448.95
Formula	C24H25ClN6O
CAS No.	1356962-20-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 23 mg/mL (51.2 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. 104th AACR meeting, 2013, Abst 919.

Related compound libraries

This product is contained In the following compound libraries：

Tyrosine Kinase Inhibitor Library Kinase Inhibitor Library Inhibitor Library Cytokine Inhibitor Library NO PAINS Compound Library Bioactive Compound Library Anti-Pancreatic Cancer Compound Library Metabolism Compound Library Angiogenesis related Compound Library Anti-Aging Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

AZD-3463 1356962-20-3 Angiogenesis Apoptosis Autophagy Tyrosine Kinase/Adaptors ALK IGF-1R Anaplastic lymphoma kinase (ALK) Anaplastic lymphoma kinase neuroblastoma kinase AZD3463 receptor PI3K/AKT/mTOR. pathway crizotinib CD246 resistance ALK tyrosine kinase receptor Inhibitor inhibit AZD 3463 ALK/IGF1R inhibitor Cluster of differentiation 246 tyrosine inhibitor

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