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PKI-166

CAS No. 187724-61-4

PKI-166( —— )

Catalog No. M33468 CAS No. 187724-61-4

PKI-166 is an oral inhibitor of EGF-R tyrosine kinase (IC50:0.7 nM) that is both effective and selective. PKI-166 can effectively inhibit the growth and metastasis of various human cancer cells including pancreatic cancer.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 53 Get Quote
5MG 116 Get Quote
10MG 188 Get Quote
25MG 364 Get Quote
50MG 609 Get Quote
100MG 954 Get Quote
200MG 1278 Get Quote
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Biological Information

  • Product Name
    PKI-166
  • Note
    Research use only, not for human use.
  • Brief Description
    PKI-166 is an oral inhibitor of EGF-R tyrosine kinase (IC50:0.7 nM) that is both effective and selective. PKI-166 can effectively inhibit the growth and metastasis of various human cancer cells including pancreatic cancer.
  • Description
    PKI-166 is a potent, selective and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 0.7 nM.
  • In Vitro
    Pretreatment with PKI-166 (0-0.5 μM; 1 hour) inhibits EGFR autophosphorylation in human pancreatic cancer cells.PKI-166 (0.03μ M; 6 days) enhanced the cytotoxicity mediated by gemcitabine.:Western Blot Analysis Cell Line:L3.6pl cells Concentration:0.01 μM, 0.05 μM, 0.5 μM Incubation Time:1 hour Result:Inhibited EGFR autophosphorylation in a dose-dependent manner.Cell Cytotoxicity Assay Cell Line:L3.6pl cells Concentration: 0.03 μM Incubation Time:6 days Result:Enhanced the cytotoxicity mediated by gemcitabine.
  • In Vivo
    PKI-166 (100 mg/kg; p.o.; daily; day 7-day 35 after xenograft) inhibits of pancreatic cancer growth.Animal Model:Male athymic nude mice with L3.6pl cells xenograft (8–12 weeks)Dosage:100 mg/kg Administration:Oral administration; daily; from day 7 to day 35 after xenograft Result:Significantly decreased median tumor volume.
  • Synonyms
    ——
  • Pathway
    Angiogenesis
  • Target
    VEGFR
  • Recptor
    VEGFR
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    187724-61-4
  • Formula Weight
    330.38
  • Molecular Formula
    C20H18N4O
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : ≥ 125 mg/mL (378.35 mM )
  • SMILES
    C[C@@H](Nc1ncnc2[nH]c(cc12)-c1ccc(O)cc1)c1ccccc1
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1. Bruns CJ, et al. Blockade of the epidermal growth factor receptor signaling by a novel tyrosine kinase inhibitor leads to apoptosis of endothelial cells and therapy of human pancreatic carcinoma. Cancer Res. 2000 Jun 1;60(11):2926-35.?
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