AZD-3463

SKU: orb1306938

Description

AZD-3463 is a potent, orally active small molecule inhibitor of ALK (Ki=0.75 nM) and IGF1R. It is utilized in preclinical research to investigate targeted therapies, particularly in oncology models studying ALK- and IGF1R-driven cancers in both cellular and animal studies.

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1356962-20-3
• MW: 448.95
• Purity: 99.13% (May vary between batches)
• Formula: C₂₄H₂₅ClN₆O
• SMILES: COc1cc(ccc1Nc1ncc(Cl)c(n1)-c1c[nH]c2ccccc12)N1CCC(N)CC1
• Target: Autophagy,IGF-1R,Apoptosis,ALK
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.45 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:23 mg/mL (51.23 mM)

Bioactivity

• Target IC50:
  ALK:0.75 nM(Ki)
• 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.
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

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

Compound Identifiers

PubChem CID

56599293