PKI 166

Synonym(s):(R)-4-[4-[(1-Phenylethyl)amino]-1H-pyrrolo[2,3-d]pyrimidin-6-yl]-phenol;(R)-6-(4-Hydroxyphenyl)-4-[(1-phenylethyl)amino]-7H-pyrrolo[2,3-d]pyrimidine;4-[4-(((R)-1-Phenylethyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]phenol;4-[4-[[(1R)-1-Phenylethyl]amino]-1H-pyrrolo[2,3-d]pyrimidin-6-yl]-phenol (9CI);

CAS NO.：187724-61-4
Empirical Formula: C20H18N4O
Molecular Weight: 330.38
MDL number: MFCD09970842
SAFETY DATA SHEET (SDS)
Update Date: 2026-01-13 11:20:46

What is PKI 166?

Biological Activity

PKI-166 is a potent, selective and orally bioactive EGFR tyrosine kinase inhibitor with 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 (0.03 μM; 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
Conce ntration:	0.03 μM
Incubation Time:	6 days
Result:	Enhanced the cytotoxicity mediated by gemcitabine.

in vivo

PKI-166 (100 mg/kg; po; 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.

Properties of PKI 166

Density	1.324±0.06 g/cm3(Predicted)
storage temp.	2-8°C
solubility	DMSO: soluble10mg/mL, clear
form	powder
pka	9.67±0.15(Predicted)
color	white to beige

Safety information for PKI 166

Signal word	Danger
Pictogram(s)	Skull and Crossbones Acute Toxicity GHS06
GHS Hazard Statements	H301:Acute toxicity,oral
Precautionary Statement Codes	P301+P310:IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

Computed Descriptors for PKI 166

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