For research use only. Not for therapeutic Use.
PKI-166 is a potent, selective and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 0.7 nM[1].
Pretreatment with PKI-166 (0-0.5 μM; 1 hour) inhibits EGFR autophosphorylation in human pancreatic cancer cells[1].
PKI-166 (0.03μ M; 6 days) enhanced the cytotoxicity mediated by gemcitabine[1].
PKI-166 (100 mg/kg; p.o.; daily; day 7-day 35 after xenograft) inhibits of pancreatic cancer growth[1].
| Catalog Number | I008784 |
| CAS Number | 187724-61-4 |
| Synonyms | 4-[4-[[(1R)-1-phenylethyl]amino]-7H-pyrrolo[2,3-d]pyrimidin-6-yl]phenol |
| Molecular Formula | C20H18N4O |
| Purity | ≥95% |
| 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 |
| InChIKey | XRYJULCDUUATMC-CYBMUJFWSA-N |
| SMILES | CC(C1=CC=CC=C1)NC2=NC=NC3=C2C=C(N3)C4=CC=C(C=C4)O |
| Reference | [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. |
