CEP37440

SKU: orb1223322

Description

CEP-37440 is an orally available dual kinase inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) and focal adhesion kinase (FAK), with potential antineoplastic activity. Upon administration, ALK-FAK inhibitor CEP-37440 selectively binds to and inhibits ALK kinase and FAK kinase. The inhibition leads to disruption of ALK- and FAK-mediated signal transduction pathways and eventually inhibits tumor cell growth in ALK- and FAK-overexpressing tumor cells. ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development; its dysregulation and gene rearrangements are associated with a variety of tumors.

Key Properties

• CAS Number: 1391712-60-9
• MW: 580.12
• Purity: >98% (HPLC)
• Formula: C₃₀H₃₈ClN₇O₃
• SMILES: CNC(=O)c1ccccc1Nc1nc(ncc1Cl)Nc1c(c2c(C[C@H](CCC2)N2CCN(CC2)CCO)cc1)OC
• Target: HCV
• Solubility: DMSO : ≥ 41 mg/mL. 70.68 mM

Bioactivity

• In Vitro:
  Cell Viability Assay Cell line: FC-IBC02, KPL4, SUM190, MDA-IBC03 and SUM149 cells. Concentration: 0, 300, 1000, 2000 and 3000 nM. Incubation time: 0, 24, 48, 72, 96, 120, 144, 168, and 192 hours. Result: Reduced the proliferation of three out of five IBC cell lines at low concentration. Inhibited the proliferation almost completely at 3000 nM concentration. Western blot analysis. Cell line: FC-IBC02, SUM 190, and KPL4 cells. Concentration: 1000 nM. Incubation time: 0, 48, 72, 96 and 120 hours. Result: Decreased phospho-FAK1 by half in FC-IBC02, SUM190, and KPL4 cells after 48 hours.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CEP37440 | CEP 37440 | CEP-37440

Quick Database Links

Gene Symbol

HCV