CEP-28122 mesylate salt (1022958-60-6 free base)

SKU: orb1309847

Description

CEP-28122 mesylate salt, derived from the free base (CAS 1022958-60-6), is a potent and orally bioavailable inhibitor of ALK with high selectivity, demonstrating an IC50 of 1.9 nM in enzymatic assays. This compound is a valuable research tool for investigating ALK-driven pathologies, such as non-small cell lung cancer, in both cellular and animal models.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• MW: 635.17
• Purity: 99.19% (May vary between batches)
• Formula: C₂₉H₃₉ClN₆O₆S
• SMILES: COC1=C(C=CC2=C1CC[C@H](CC2)N3CCOCC3)NC4=NC=C(C(N[C@@H]5[C@@H]6C[C@H]([C@@H]5C(N)=O)C=C6)=N4)Cl.CS(=O)(O)=O
• Target: ALK
• Solubility: DMSO:6.4 mg/mL (10.08 mM)

Bioactivity

• Target IC50:
  ALK:1.9 nM
• In Vivo:
  CEP-28122 displays dose-dependent inhibition of ALK tyrosine phosphorylation in tumor xenografts in mice, with substantial target inhibition (>90%) for more than12 hours following single oral dosing at 30 mg/kg. Dose-dependent antitumor activity was observed in ALK-positive ALCL, NSCLC, and neuroblastoma tumor xenografts in mice administered CEP-28122 orally, with complete/near-complete tumor regressions observed following treatment at doses of 30 mg/kg twice daily or higher.
• In Vitro:
  CEP-28122 is a potent inhibitor of recombinant ALK activity and cellular ALK tyrosine phosphorylation. CEP-28122 also inhibits Flt4 (IC50: 46 nM). CEP-28122 induces concentration-dependent growth inhibition/cytotoxicity of ALK-positive anaplastic large-cell lymphoma (ALCL), neuroblastoma cells, and non-small cell lung cancer (NSCLC).

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ALK, 1022958-60-6, 1022958-60-6 free base, CEP 28122 mesylate salt (1022958 60 6 free base), CEP 28122 Mesylate, CEP28122 Mesylate, CEP-28122 Mesylate, CEP-28122 mesylate salt, CEP28122 mesylate salt (1022958606 free base)

Compound Identifiers

PubChem CID

91885507