Ceritinib dihydrochloride

SKU: orb1307438

Description

Ceritinib dihydrochloride

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1380575-43-8
• MW: 631.06
• Purity: 99.99%
• Formula: C₂₈H₃₈Cl₃N₅O₃S
• SMILES: Cl.Cl.CC(C)Oc1cc(C2CCNCC2)c(C)cc1Nc1ncc(Cl)c(Nc2ccccc2S(=O)(=O)C(C)C)n1
• Target: IGF-1R,ALK
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (5.23 mM);H2O:5 mg/mL (7.92 mM);DMSO:95 mg/mL (150.54 mM)

Bioactivity

• Target IC50:
  IGF-1R:8 nM |ALK:0.2 nM |Insulin receptor:7 nM |STK22D:23 nM
• In Vivo:
  Ceritinib significantly improved the survival of CLP-induced polymicrobial septic mice, which was paralleled by reduced organ injury, decreased release of inflammatory cytokines and decreased recruitment of MDSCs to the spleen.Importantly, Ceritinib inhibited the migration of MDSCs to the spleen by blocking the CLP-mediated upregulation of CC chemokine receptor 2 (CCR2), a chemokine receptor critical for the recruitment of MDSCs.Mechanistically, Ceritinib treatment blocked the CLP-induced CCR2 upregulation of MDSCs via partially inhibiting the phosphorylation of p38 and G-protein-coupled receptor kinase-2 (GRK2) in bone marrow MDSCs of septic mice.
• In Vitro:
  In vitro experiments also showed that lipopolysaccharide (LPS)-induced migration of MDSCs was similarly owing to the activation of GRK2 and upregulation of CCR2 by LPS, whereas the treatment with LDK378 partially blocked the LPS-induced phosphorylation of p38 and GRK2 and decreased the expression of CCR2 on the cell surface, therefore leading to the suppression of MDSC migration.

Storage & Handling

• Storage: store at low temperature,store under nitrogen | 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

IGF-1R, IGF1R, Inhibitor, Insulin Receptor, LDK 378, LDK 378 Dihydrochloride, LDK378, LDK-378, LDK378 Dihydrochloride, LDK378 dihydrochloride, LDK-378 Dihydrochloride, inhibit, Ceritinib, Ceritinib dihydrochloride, Ceritinib Dihydrochloride, CD246, Cluster of differentiation 246, Anaplastic lymphoma kinase (ALK), Anaplastic lymphoma kinase, ALK, ALK tyrosine kinase receptor

Compound Identifiers

PubChem CID

67973512