PD-161570 is a selective FGFR inhibitor (IC50 values are 40, 262 and 3700 nM for FGFR, PDGFR and EGFR respectively). PD 161570 had about 5- and 100-fold greater selectivity toward the FGF-1 receptor (IC50 = 40 nM) compared with the PDGFbeta receptor (IC50 = 262 nM) or EGF receptor (IC50 = 3.7 microM) tyrosine kinases, respectively. In addition, PD 161570 suppressed constitutive phosphorylation of the FGF-1 receptor in both human ovarian carcinoma cells (A121(p)) and Sf9 insect cells overexpressing the human FGF-1 receptor and blocked the growth of A121(p) cells in culture. The results demonstrate a novel synthetic inhibitor with nanomolar potency and specificity towards the FGF-1 receptor tyrosine kinase.
CAS Number: 192705-80-9
Molecular Weight: 532.51
Chemical Name: N-[6-(2,6-Dichlorophenyl)-2-[[4-(diethylamino)butyl]amino]pyrido[2,3-d]pyrimidin-7-yl]-N'-(1,1-dimethylethyl)urea
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: ≥12 months 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
PD-161570 (Compound 6c; 0.1-1 µM; 1-8 days; VSMCs) treatment inhibits PDGF-stimulated vascular smooth muscle cell proliferation in a dose dependent fashion with an IC50 of 0.3 µM on day 8. PD-161570 suppresses constitutive phosphorylation of the FGF-1 receptor in both human ovarian carcinoma cells (A121(p)) and Sf9 insect cells overexpressing the human FGF-1 receptor and blocked the growth of A121(p) cells in culture. PD-161570 can potently inhibit basic fibroblast growth factor (bFGF)-mediated angiogenesis.
- Stevens DA, Harvey CB, Scott AJ, O'Shea PJ, Barnard JC, Williams AJ, Brady G, Samarut J, Chassande O, Williams GR. Thyroid hormone activates fibroblast growthfactor receptor-1 in bone. Mol Endocrinol. 2003 Sep;17(9):1751-66. PubMed PMID:12805413.
- Wolfe A, O'Clair B, Groppi VE, McEwen DP. Pharmacologic characterization of akinetic in vitro human co-culture angiogenesis model using clinically relevantcompounds. J Biomol Screen. 2013 Dec;18(10):1234-45. doi:10.1177/1087057113502085. PubMed PMID: 24019254.
- Batley BL, Doherty AM, Hamby JM, Lu GH, Keller P, Dahring TK, Hwang O,Crickard K, Panek RL. Inhibition of FGF-1 receptor tyrosine kinase activity by PD161570, a new protein-tyrosine kinase inhibitor. Life Sci. 1998;62(2):143-50.PubMed PMID: 9488112.
Products are for research use only. Not for human use.
Payment & Security
Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.