Entrectinib

SKU: orb1303916

Description

Entrectinib

Research Area

Cardiovascular Research, Cell Biology, Immunology & Inflammation, Signal Transduction

Key Properties

• CAS Number: 1108743-60-7
• MW: 560.64
• Purity: 99.35%
• Formula: C₃₁H₃₄F₂N₆O₂
• SMILES: N(C(=O)C1=C(NC2CCOCC2)C=C(C=C1)N3CCN(C)CC3)C=4C=5C(NN4)=CC=C(CC6=CC(F)=CC(F)=C6)C5
• Target: Autophagy,Trk receptor,ALK,ROS,ROS Kinase
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:10 mg/mL (17.84 mM);DMSO:260 mg/mL (463.76 mM);Ethanol:67 mg/mL (119.51 mM)

Bioactivity

• Target IC50:
  TrkA:1.7 nM|TrkB:0.1 nM|TrkC:0.1 nM|ALK:1.6 nM
• In Vivo:
  METHODS: To assay anti-tumor activity in vivo, Entrectinib (30-60 mg/kg) was administered orally to SCID mice bearing Karpas-299 xenografts twice daily for ten days. RESULTS: Both dose levels were effective in inducing regression of all tumors to a nonpalpable extent. During the observation period after cessation of treatment at the 60 mg/kg dose, tumor eradication was sustained in four of seven mice at day 80 after the end of treatment, while tumor regeneration was observed in all animals treated with the 30 mg/kg dose.
• In Vitro:
  METHODS: Human lung cancer cells HCC78 were treated with Entrectinib (0.1-10 µM) for 72 h, and cell viability was measured by CCK-8 assay. RESULTS: Entrectinib effectively inhibited cell survival, and the IC50 value of inhibition of HCC78 was 450 nM. METHODS: Colorectal cancer cells KM12 were treated with Entrectinib (10-250 nmol/L) for 2 h, and the expression levels of target proteins were detected by Western Blot. RESULTS: Entrectinib eliminated the autophosphorylation of TPM3-TRKA and completely inhibited the phosphorylation of PLCγ1, AKT and MAPK after 2 h of treatment.
• Cell Research:
  NLF, NLF-TrkB, SY5Y or SY5Y-TrkB cells are plated in 96 well plates, and they are exposed to drug at different concentrations (1, 5, 10, 20, 30, 50 and 100 nM of entrectinib, 1.5 μM Irino and 50 μM TMZ, respectively) for one hr followed by addition of 100 ng/mL of BDNF. Plates are harvested at 24, 48, and 72 hr following addition of drug. The plates are processed and cell viability is analyzed using a standard SRB assay protocol.

Storage & Handling

• Storage: store at low temperature | 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

CD246, Cluster of differentiation 246, ALK, ALK tyrosine kinase receptor, Anaplastic lymphoma kinase (ALK), Anaplastic lymphoma kinase, Autophagy, NMS-E 628, NMS-E628, NMS-E-628, inhibit, Inhibitor, Entrectinib, RXDX 101, RXDX101, RXDX-101, ROS Kinase, ROS1, ROSKinase, ROS, Tropomyosin related kinase receptor, Trkreceptor, TrkC, Trk receptor, TrkA, TrkB, Trk Receptor

Compound Identifiers

PubChem CID

25141092