PD-161570 - CAS 192705-80-9
Category: Inhibitor
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Molecular Formula:
C26H35Cl2N7O
Molecular Weight:
532.51
COA:
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Targets:
FGFR
Description:
PD-161570 is a selective inhibitor of human FGF-1 receptor tyrosine kinase, with IC50 values to be 40, 262 and 3700 nM for FGFR1, PDGFR and EGFR tyrosine kinases, respectively. In addintion, PD-161570 inhibits FGFR receptor phosphorylation (IC50 = 622 nM) and growth of A121 cells in vitro.
Appearance:
Solid powder
Synonyms:
N-[6-(2,6-Dichlorophenyl)-2-[[4-(diethylamino)butyl]amino]pyrido[2,3-d]pyrimidin-7-yl]-N'-(1,1-dimethylethyl)urea; PD-161570; PD 161570; PD161570.
Storage:
Store in a cool and dry place (or refer to the Certificate of Analysis).
MSDS:
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Density:
1.249±0.06 g/cm3
InChIKey:
MKVMEJKNLUWFSQ-UHFFFAOYSA-N
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)
Canonical SMILES:
O=C(NC(C)(C)C)NC1=NC2=NC(NCCCCN(CC)CC)=NC=C2C=C1C3=C(Cl)C=CC=C3Cl
1.Thyroid hormone activates fibroblast growth factor receptor-1 in bone.
Stevens DA;Harvey CB;Scott AJ;O'Shea PJ;Barnard JC;Williams AJ;Brady G;Samarut J;Chassande O;Williams GR Mol Endocrinol. 2003 Sep;17(9):1751-66. Epub 2003 Jun 12.
Thyroid hormone (T3) and the T3 receptor (TR) alpha gene are essential for bone development whereas adult hyperthyroidism increases the risk of osteoporotic fracture. We isolated fibroblast growth factor receptor-1 (FGFR1) as a T3-target gene in osteoblasts by subtraction hybridization. FGFR1 mRNA was induced 2- to 3-fold in osteoblasts treated with T3 for 6-48 h, and FGFR1 protein was stimulated 2- to 4-fold. Induction of FGFR1 was independent of mRNA half-life and abolished by actinomycin D and cycloheximide, indicating the involvement of an intermediary protein. Fibroblast growth factor 2 (FGF2) stimulated MAPK in osteoblasts, and pretreatment with T3 for 6 h induced a more rapid response to FGF that was increased in magnitude by 2- to 3-fold. Similarly, T3 enhanced FGF2-activated autophosphorylation of FGFR1, but did not modify FGF2-induced phosphorylation of the docking protein FRS2. These effects were abolished by the FGFR-selective inhibitors PD166866 and PD161570. In situ hybridization analyses of TRalpha-knockout mice, which have impaired ossification and skeletal mineralization, revealed reduced FGFR1 mRNA expression in osteoblasts and osteocytes, whereas T3 failed to stimulate FGFR1 mRNA or enhance FGF2-activated MAPK signaling in TRalpha-null osteoblasts.
2.Activation of the FGFR1 signalling pathway by the Epstein-Barr virus-encoded LMP1 promotes aerobic glycolysis and transformation of human nasopharyngeal epithelial cells.
Lo AK;Dawson CW;Young LS;Ko CW;Hau PM;Lo KW J Pathol. 2015 Oct;237(2):238-48. doi: 10.1002/path.4575. Epub 2015 Aug 3.
Non-keratinizing nasopharyngeal carcinoma (NPC) is closely associated with Epstein-Barr virus (EBV) infection. The EBV-encoded latent membrane protein 1 (LMP1) is believed to play an important role in NPC pathogenesis by virtue of its ability to activate multiple cell signalling pathways which collectively promote cell proliferation, transformation, angiogenesis, and invasiveness, as well as modulation of energy metabolism. In this study, we report that LMP1 increases cellular uptake of glucose and glutamine, enhances LDHA activity and lactate production, but reduces pyruvate kinase activity and pyruvate concentrations. LMP1 also increases the phosphorylation of PKM2, LDHA, and FGFR1, as well as the expression of PDHK1, FGFR1, c-Myc, and HIF-1α, regardless of oxygen availability. Collectively, these findings suggest that LMP1 promotes aerobic glycolysis. With respect to FGFR1 signalling, LMP1 not only increases FGFR1 expression, but also up-regulates FGF2, leading to constitutive activation of the FGFR1 signalling pathway. Furthermore, two inhibitors of FGFR1 (PD161570 and SU5402) attenuate LMP1-mediated aerobic glycolysis, cellular transformation (proliferation and anchorage-independent growth), cell migration, and invasion in nasopharyngeal epithelial cells, identifying FGFR1 signalling as a key pathway in LMP1-mediated growth transformation.
3.Inhibition of FGF-1 receptor tyrosine kinase activity by PD 161570, a new protein-tyrosine kinase inhibitor.
Batley BL;Doherty AM;Hamby JM;Lu GH;Keller P;Dahring TK;Hwang O;Crickard K;Panek RL Life Sci. 1998;62(2):143-50.
Through direct synthetic efforts we discovered a small molecule which is a 40 nanomolar inhibitor of the human FGF-1 receptor tyrosine kinase. 1-Tert-butyl-3-[6-(2,6-dichloro-phenyl)-2-(4-diethylamino-butylamino)-py rido[2,3-d]pyrimidin-7-yl]-urea (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.
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CAS 192705-80-9 PD-161570

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