PD-089828

PD-089828 is an ATP competitive inhibitor of FGFR-1, PDGFR-β and EGFR (IC50s=0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of c-Src tyrosine kinase (IC50=0.18 µM). PD-089828 also inhibits MAPK with an IC50 of 7.1 µM. PD-089828 inhibits PDGF-, EGF- and bFGF-mediated tyrosine kinase receptor autophosphorylation in vitro. PD-089828 has a long-lasting cellular activity.

Product information

CAS Number: 179343-17-0

Molecular Weight: 405.28

Formula: C18H18Cl2N6O

Chemical Name: 1-[2-amino-6-(2, 6-dichlorophenyl)pyrido[2, 3-d]pyrimidin-7-yl]-3-tert-butylurea

Smiles: CC(C)(C)NC(=O)NC1=NC2=NC(N)=NC=C2C=C1C1C(Cl)=CC=CC=1Cl

InChiKey: RRWSNCZYJCOEFX-UHFFFAOYSA-N

InChi: InChI=1S/C18H18Cl2N6O/c1-18(2,3)26-17(27)25-15-10(13-11(19)5-4-6-12(13)20)7-9-8-22-16(21)24-14(9)23-15/h4-8H,1-3H3,(H4,21,22,23,24,25,26,27)

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:

PD-089828 (0.5-20 µM; 2 hours) inhibits PDGFR autophosphorylation with an IC50 of 0.82 µM. PD-089828 (1-50 µM; 2 hours) inhibits EGFR autophosphorylation with an IC50 value of 10.9 µM. In A121(p) cells, PD 089828 potently inhibits the phosphorylation of FGFR-1 with an IC50 value of 0.63 µM. PD-089828 (10 µM; 8 days) produces a concentration-related inhibition of serum-stimulated cell growth with an IC50 value of 1.8 µM. PD-089828 inhibits increases in DNA synthesis stimulated by all three growth factors, with IC50 values of 0.8 for PDGF-, 1.7 for EGF- and 0.48 µM for bFGF-induced mitogenesis.

References:

1. Dahring TK, et al. Inhibition of growth factor-mediated tyrosine phosphorylation in vascular smooth muscle by PD 089828, a new synthetic protein tyrosine kinase inhibitor. J Pharmacol Exp Ther. 1997 Jun;281(3):1446-56.

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