PKI-166

SKU: orb1706783

Description

PKI-166 is a potent and selective oral EGF-R tyrosine kinase inhibitor (IC50: 0.7 nM). It has demonstrated efficacy in inhibiting the growth and metastasis of various human cancer cell lines, including pancreatic cancer, in both in vitro and in vivo preclinical studies.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 187724-61-4
• MW: 330.38
• Purity: 99.80%
• Formula: C₂₀H₁₈N₄O
• SMILES: C[C@@H](Nc1ncnc2[nH]c(cc12)-c1ccc(O)cc1)c1ccccc1
• Target: EGFR,VEGFR
• Solubility: DMSO:27.5 mg/mL (83.24 mM)

Bioactivity

• Target IC50:
  EGFR tyrosine kinase:0.7 nM
• In Vivo:
  PKI-166 (100 mg/kg; p.o.; daily; day 7-day 35 after xenograft) suppresses pancreatic cancer growth.
• In Vitro:
  PKI-166 (0–0.5 μM; 1 hour) pretreatment suppresses EGFR autophosphorylation in human pancreatic cancer cells. PKI-166 (0.03μ M; 6 days) increased the cytotoxicity mediated by gemcitabine.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

EGFR tyrosine kinase, PKI 166, PKI166, PKI-166, VEGFR

Compound Identifiers

PubChem CID

6918403