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
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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.
  • In Vitro
    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.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. Western Blot Analysis Cell Line:NCI-H1975 bronchoalveolar cell line Concentration:0.01, 0.01, 0.1, 1 and 10 μM Incubation Time:Result:Suppressed ligand-induced EGFR autophosphorylation and its downstream signaling AKT and MAPK phosphorylation.
  • In Vivo
    ——
  • Synonyms
    ——
  • Pathway
    Angiogenesis
  • Target
    EGFR
  • Recptor
    PEGs
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    848133-17-5
  • Formula Weight
    574.05
  • Molecular Formula
    C31H29ClFN5O3
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 100 mg/mL (174.20 mM)
  • 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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