PKI 166 hydrochloride

Modify Date: 2024-01-23 00:42:04

PKI 166 hydrochloride Structure
PKI 166 hydrochloride structure
Common Name PKI 166 hydrochloride
CAS Number 2230253-82-2 Molecular Weight 366.84
Density N/A Boiling Point N/A
Molecular Formula C20H19ClN4O Melting Point N/A
MSDS N/A Flash Point N/A

 Use of PKI 166 hydrochloride


PKI-166 hydrochloride is a potent, selective and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 0.7 nM[1].

 Names

Name PKI-166 hydrochloride

 PKI 166 hydrochloride Biological Activity

Description PKI-166 hydrochloride is a potent, selective and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 0.7 nM[1].
Related Catalog
Target

IC50: 0.7 nM (EGFR tyrosine kinase)[1]

In Vitro Pretreatment with PKI-166 hydrochloride (0-0.5 μM; 1 hour) inhibits EGFR autophosphorylation in human pancreatic cancer cells[1]. PKI-166 hydrochloride (0.03 μM; 6 days) enhances the cytotoxicity mediated by gemcitabine[1]. Western Blot Analysis[1] 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[1] Cell Line: L3.6pl cells Concentration: 0.03 μM Incubation Time: 6 days Result: Enhanced the cytotoxicity mediated by gemcitabine.
In Vivo PKI-166 hydrochloride (100 mg/kg; p.o.; daily; day 7-day 35 after xenograft) inhibits of pancreatic cancer growth[1]. Animal Model: Male athymic nude mice with L3.6pl cells xenograft (8–12 weeks)[1] Dosage: 100 mg/kg Administration: Oral administration; daily; from day 7 to day 35 after xenograft Result: Significantly decreased median tumor volume.
References

[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.

 Chemical & Physical Properties

Molecular Formula C20H19ClN4O
Molecular Weight 366.84