Alectinib

SKU: orb1307053

Description

Alectinib is a potent, selective, and orally bioavailable ATP-competitive inhibitor of ALK (IC50=1.9 nM). It demonstrates robust antitumor activity in both cellular assays and animal models, underpinning its clinical application in ALK-positive non-small cell lung cancer (NSCLC) research.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1256580-46-7
• MW: 482.62
• Purity: 99.97% (May vary between batches)
• Formula: C₃₀H₃₄N₄O₂
• SMILES: CCc1cc2C(=O)c3c([nH]c4cc(ccc34)C#N)C(C)(C)c2cc1N1CCC(CC1)N1CCOCC1
• Target: Tyrosine Kinases,VEGFR,ALK
• Solubility: DMSO:4.83 mg/mL (10.01 mM);H2O:2.1 mM

Bioactivity

• Target IC50:
  ALK (F1174L):1 nM|ALK (R1275Q):3.5 nM|ALK:1.9 nM
• In Vivo:
  METHODS: To detect antitumor activity in vivo, Alectinib (25 mg/kg) was administered intraperitoneally to TH-MYCN transgenic mice every two days for 11 doses. RESULTS: Treatment with Alectinib resulted in reduced tumor growth in TH-MYCN transgenic mice.Alectinib induced PARP and Caspase 3 cleavage and blocked PI3K/Akt/mTOR signaling in TH-MYCN tumor tissue. Alectinib exposure prolonged the survival of TH-MYCN transgenic mice compared to DMSO treatment.
• In Vitro:
  METHODS: Six neuroblastoma (NB) cell lines were treated with Alectinib (0.001-50 µM) for 72 h and cell viability was measured by CCK-8 assay. RESULTS: Six NB cell lines were selected, including three ALK-WT cell lines (IMR-32, NB-19, and SK-N-AS) and three ALK-mutant cell lines (Kelly, SH-SY5Y, and LA-N-6.) Alectinib treatment dramatically reduced cell viability, with IC50s for the cell lines tested ranging from 3.181-9.6 µM. METHODS: NSCLCA cells NCI-H2228 were treated with Alectinib (10-1000 nM) for 2 h, and the expression levels of target proteins were detected by Western Blot. RESULTS: Alectinib prevented the autophosphorylation of ALK in NCI-H2228 NSCLC cells expressing EML4-ALK, and Alectinib also led to a substantial inhibition of the phosphorylation of STAT3 and AKT, but not ERK1/2.
• Cell Research:
  Cells including NSCLC, A549 and HCC827 are seeded in 96-well plates overnight and incubated with various concentrations of CH5424802 for the indicated time. For spheroid cell growth inhibition assay, cells are seeded on spheroid plates, incubated overnight, and then treated with compound for the indicated times. The viable cells are measured by the Luminescent Cell Viability Assay. Caspase-3/7 assay is evaluated using the Caspase-Glo 3/7 Assay Kit.(Only for Reference)

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

RG 7853, RG7853, RG-7853, RO 5424802, RO5424802, RO-5424802, VEGFR2 (KDR), Tyrosine Kinases, TyrosineKinases, inhibit, Inhibitor, INSR, Anaplastic lymphoma kinase, Anaplastic lymphoma kinase (ALK), Alectinib, ALK, ALK (F1174L), ALK (R1275Q), ALK tyrosine kinase receptor, AF 802, AF802, AF-802, CD246, Cluster of differentiation 246, CH 5424802, CH5424802, CH-5424802

Compound Identifiers

PubChem CID

49806720