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.
Chemical Formula: C26H35Cl2N7O
Exact Mass: 531.228
Molecular Weight: 532.514
Elemental Analysis: C, 58.64; H, 6.63; Cl, 13.31; N, 18.41; O, 3.00
Chemical Name: N-[6-(2,6-Dichlorophenyl)-2-[[4-(diethylamino)butyl]amino]pyrido[2,3-d]pyrimidin-7-yl]-N'-(1,1-dimethylethyl)urea
InChi Code: InChI=1S/C26H35Cl2N7O/c1-6-35(7-2)14-9-8-13-29-24-30-16-17-15-18(21-19(27)11-10-12-20(21)28)23(31-22(17)32-24)33-25(36)34-26(3,4)5/h10-12,15-16H,6-9,13-14H2,1-5H3,(H3,29,30,31,32,33,34,36)
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
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
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.
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.
Saksena S, Priyamvada S, Kumar A, Akhtar M, Soni V, Anbazhagan AN, Alakkam A, Alrefai WA, Dudeja PK, Gill RK. Keratinocyte growth factor-2 stimulates P-glycoprotein expression and function in intestinal epithelial cells. Am JPhysiol Gastrointest Liver Physiol. 2013 Mar 15;304(6):G615-22. doi:10.1152/ajpgi.00445.2012. PubMed PMID: 23328208; PubMed Central PMCID:PMC3602685.
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.
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.
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]pyrimidinetyrosine kinase inhibitors. J Med Chem. 1997 Jul 18;40(15):2296-303. PubMed PMID: 9240345.
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