PKI-166

Research use only, not for human use.

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.

PKI-166 is a potent, selective and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 0.7 nM.

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.

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.

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Angiogenesis

VEGFR

VEGFR

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187724-61-4

330.38

C20H18N4O

>98% (HPLC)

In Vitro:?DMSO : ≥ 125 mg/mL (378.35 mM )

C[C@@H](Nc1ncnc2[nH]c(cc12)-c1ccc(O)cc1)c1ccccc1

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(-20℃)

With Ice Pack

≥ 2 years