受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C20H24N6O3 |
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分子量 | 396.44 | CAS No. | 192705-79-6 | ||||
Solubility (25°C)* | 体外 | DMSO (warmed with 50ºC water bath) | 21 mg/mL (52.97 mM) | ||||
Ethanol (warmed with 50ºC water bath) | 4 mg/mL (10.08 mM) | ||||||
Water | Insoluble | ||||||
体内 (毎回新しく調製した物を用意してください) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | PD-166866 is a synthetic molecule inhibiting the tyrosin kinase action of FGFR1, shows a very high selectivity towards FGFR1 and inhibits the auto-phosphorylation activity of FGRF1. |
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in vitro | The treatment with PD166866 apparently causes a mitochondrial deficit and an oxidative stress[1]. PD 166866 inhibits human full-length FGFR-1 tyrosine kinase with an IC50 value of 52.4 ± 0.1 nM but has no effect on c-Src, platelet-derived growth factor receptor-β, epidermal growth factor receptor or insulin receptor tyrosine kinases or on mitogen-activated protein kinase, protein kinase C and CDK4 at concentrations as high as 50 μM. PD 166866 is a potent inhibitor of basic fibroblast growth factor (bFGF)-mediated receptor autophosphorylation in NIH 3T3 cells expressing endogenous FGFR-1 and in L6 cells overexpressing the human FGFR-1 tyrosine kinase, confirming a tyrosine kinase-mediated mechanism. PD 166866 does not inhibit platelet-derived growth factor, epidermal growth factor or insulin-stimulated receptor autophosphorylation in vascular smooth muscle, A431 or NIHIR cells, respectively, further supporting its specificity for the FGFR-1. Besides, PD 166866 is found to be a potent inhibitor of microvessel outgrowth (angiogenesis) from cultured artery fragments of human placenta. Phosphorylated 44- and 42-kDa MAPK isoforms are inhibited in L6 cells by PD 166866 with IC50 values of 4.3 and 7.9 nM, respectively[2]. PD166866 induces autophagy through repressing Akt/mTOR signaling pathway[3]. |
細胞アッセイ | 細胞株 | HeLa cells |
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濃度 | 50 μM | |
反応時間 | 24 h | |
実験の流れ | HeLa cells are treated with PD166866 for 24 hours, the growth medium is removed, the cells are washed with PBS and fixed for 1 hour at 25°C adding a freshly made paraformaldheyde solution (4% in PBS). Samples are washed again with PBS and the endogenous oxidases were blocked for 2 minutes in the dark. Further washes with PBS followed and blocking the unspecific sites is done for 1 hour at 25℃. PARP is evidenced by immunolocalization utilizing a polyclonal antibody, directed against the N-terminal proteolytic fragment. Immuno-reaction is revealed by a secondary anti-rabbit antibody after incubation for 16 hours at 4°C. After exhaustive washing with PBS the samples are incubated for 30 minutes in solution ABC. Eventually, DAB (3,3'-Diaminobenzidine) is added and the samples are incubated for 10 minutes in the dark. The samples are washed again the plates are sealed and ready for microscopic observation. | |
動物実験 | 動物モデル | Female nude mice |
投薬量 | 20 mg/kg | |
投与方法 | i.p. |
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Paradoxical cancer cell proliferation after FGFR inhibition through decreased p21 signaling in FGFR1-amplified breast cancer cells [ Breast Cancer Res, 2024, 26(1):54] | PubMed: 38553760 |
Targeting FAPα-expressing hepatic stellate cells overcomes resistance to anti-angiogenics in colorectal cancer liver metastasis models [ J Clin Invest, 2022, e157399] | PubMed: 35951441 |
FGF8-FGFR1 signaling regulates human GnRH neuron differentiation in a time- and dose-dependent manner [ Dis Model Mech, 2022, 15(8)dmm049436] | PubMed: 35833364 |
Regulation of STUB1 expression and its biological significance in mouse Sertoli cells [ Syst Biol Reprod Med, 2022, 1-15] | PubMed: 35343345 |
Probing the signaling requirements for naive human pluripotency by high-throughput chemical screening [ Cell Rep, 2021, 35(11):109233] | PubMed: 34133938 |
The Roles of FGF21 and ALCAT1 in Aerobic Exercise-Induced Cardioprotection of Postmyocardial Infarction Mice [ Oxid Med Cell Longev, 2021, 2021:8996482] | PubMed: 34777697 |
Activation of Serum/Glucocorticoid Regulated Kinase 1/Nuclear Factor-κB Pathway Are Correlated with Low Sensitivity to Bortezomib and Ixazomib in Resistant Multiple Myeloma Cells [ Biomedicines, 2021, 9(1)E33] | PubMed: 33406639 |
Identification of testicular Foxq1 as a critical modulator of lactate metabolism in mouse Sertoli cells [ Histochem Cell Biol, 2021, 156(3):227-237] | PubMed: 34091745 |
Rab8 and Rabin8-Mediated Tumor Formation by Hyperactivated EGFR Signaling via FGFR Signaling [ Int J Mol Sci, 2020, 21(20)E7770] | PubMed: 33092268 |
Effect of fibroblast growth factor 2 on degenerative endplate chondrocyte: From anabolism to catabolism [ Exp Mol Pathol, 2020, S0014-4800(20)30867-4] | PubMed: 33285208 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。