PKI-166

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

Product information

CAS Number: 187724-61-4

Molecular Weight: 330.38

Formula: C20H18N4O

Chemical Name: 4-(4-{[(1R)-1-phenylethyl]amino}-7H-pyrrolo[2, 3-d]pyrimidin-6-yl)phenol

Smiles: C[C@@H](NC1N=CN=C2NC(=CC=12)C1C=CC(O)=CC=1)C1C=CC=CC=1

InChiKey: XRYJULCDUUATMC-CYBMUJFWSA-N

InChi: InChI=1S/C20H18N4O/c1-13(14-5-3-2-4-6-14)23-19-17-11-18(24-20(17)22-12-21-19)15-7-9-16(25)10-8-15/h2-13,25H,1H3,(H2,21,22,23,24)/t13-/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

In Vivo:

PKI-166 (100 mg/kg; p.o.; daily; day 7-day 35 after xenograft) inhibits of pancreatic cancer growth.

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.

Products are for research use only. Not for human use.