HKI-357

CAS No. 848133-17-5

HKI-357 ( —— )

Catalog No. M26249 CAS No. 848133-17-5

HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 (IC50s: 34 nM and 33 nM). HKI-357 suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
5MG 140 Get Quote
10MG 215 Get Quote
25MG 438 Get Quote
50MG 626 Get Quote
100MG 888 Get Quote
200MG Get Quote Get Quote
500MG Get Quote Get Quote
1G Get Quote Get Quote

Biological Information

  • Product Name
    HKI-357
  • Note
    Research use only, not for human use.
  • Brief Description
    HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 (IC50s: 34 nM and 33 nM). HKI-357 suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation.
  • Description
    HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 (IC50s: 34 nM and 33 nM). HKI-357 suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation.(In Vitro):HKI-357 also is effective in suppressing EGFR autophosphorylation (measured at residue Y1068), and AKT and MAPK phosphorylation in parental NCI-H1650 cells harboring the delE746-A750 EGFR mutation. HKI-357 (0.01-10 μM) is effective in suppressing ligand-induced EGFR autophosphorylation and its downstream signaling, as determined by AKT and MAPK phosphorylation in NCI-H1975 cells.
  • Synonyms
    ——
  • Pathway
    Angiogenesis
  • Target
    EGFR
  • Recptor
    PEGs
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    848133-17-5
  • Formula Weight
    574.1
  • Molecular Formula
    C31H29ClFN5O3
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    CCOc1cc2ncc(C#N)c(Nc3ccc(OCc4cccc(F)c4)c(Cl)c3)c2cc1NC(=O)\C=C\CN(C)C
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562
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