WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406476
Description: PD089828 is a potent FGFR inhibitor, which inhibits human full-length fibroblast growth factor (FGF) receptor-1 (FGFR-1), platelet-derived growth factor (PDGF) receptor beta subunit (PDGFR-beta), Src nonreceptor tyrosine kinase (c-Src) and epidermal growth factor (EGF) receptor (EGFR) tyrosine kinases with half-maximal inhibitory potencies (IC50 values) of 0.15 +/- 0.02 (n = 4), 0.18 +/- 0.04 (n = 3), 1.76 +/- 0.28 (n = 4) and 5.47 +/- 0.78 (n = 6) microM, respectively. The results highlight the biological characteristics of PD 089828 as a novel, broadly active protein tyrosine kinase inhibitor with long-lasting but reversible cellular effects. The potential therapeutic use of these broadly acting, nonselective inhibitors as antiproliferative and antimigratory agents could extend to such diseases as cancer, atherosclerosis and restenosis in which redundancies in growth-signaling pathways are known to exist.
MedKoo Cat#: 406476
Chemical Formula: C18H18Cl2N6O
Exact Mass: 404.09191
Molecular Weight: 405.28112
Elemental Analysis: C, 53.34; H, 4.48; Cl, 17.50; N, 20.74; O, 3.95
Synonym: PD089828; PD089828; PD 089828.
IUPAC/Chemical Name: 1-(2-amino-6-(2,6-dichlorophenyl)pyrido[2,3-d]pyrimidin-7-yl)-3-(tert-butyl)urea
InChi Key: RRWSNCZYJCOEFX-UHFFFAOYSA-N
InChi Code: 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)
SMILES Code: O=C(NC(C)(C)C)NC1=NC2=NC(N)=NC=C2C=C1C3=C(Cl)C=CC=C3Cl
Appearance: solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 405.28112 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: Hamby JM, Connolly CJ, Schroeder MC, Winters RT, Showalter HD, Panek RL, Major TC, Olsewski B, Ryan MJ, Dahring T, Lu GH, Keiser J, Amar A, Shen C, Kraker AJ, Slintak V, Nelson JM, Fry DW, Bradford L, Hallak H, Doherty AM. Structure-activity relationships for a novel series of pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors. J Med Chem. 1997 Jul 18;40(15):2296-303. PubMed PMID: 9240345.
2: Dahring TK, Lu GH, Hamby JM, Batley BL, Kraker AJ, Panek RL. 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. PubMed PMID: 9190882.