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Synonyms | SU-5271 (AG1517) HCl ,ZM 252868 HCl | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C16H14BrN3O2.HCl |
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分子量 | 396.67 | CAS No. | 183322-45-4 | ||||
Solubility (25°C)* | 体外 | 4-Methylpyridine (warmed with 50ºC water bath) | 5 mg/mL (12.6 mM) | ||||
DMSO | 0.5 mg/mL (1.26 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 | PD153035 HCl (SU-5271 HCl, AG1517 HCl, ZM 252868 HCl) is a potent and specific inhibitor of EGFR with Ki and IC50 of 5.2 pM and 29 pM in cell-free assays; little effect noted against PGDFR, FGFR, CSF-1, InsR and Src. |
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in vitro | PD 153035 shows a potent and selective inhibitory effect on tyrosine phosphorylation induced with EGF with IC50 of 15 nM and 14 nM in Swiss 3T3 fibroblast and A-431 human epidermoid carcinoma cells, respectively. [1] PD153035 shows growth inhibitory effects in cultures of EGF receptor-overexpressing human cancer cell lines including A431, Difi, DU145, MDA-MB-468 and ME180 cells with IC50 of 0.22 μM, 0.3μM, 0.4 μM, 0.68 μM and 0.95 μM, respectively. [2] PD153035 induces a dose-dependent growth inhibition in nasopharyngeal carcinoma (NPC) cells including NPC-TW01, NPC-TW04, and HONE1 cell lines with IC50 of 12.9 μM, 9.8 μM and 18.6μM, respectively. [3] A recent study shows that PD153035 abolishes COX-2 expression induced by the PAR(2)-activating peptide 2-furoyl-LIGRLO-NH(2) (2fLI) in Caco-2 colon cancer cells. [4] |
in vivo | In A431 human epidermoid tumors grown as xenografts in immunodeficient nude mice, PD153035 at 80 mg/kg inhibit EGF receptor tyrosine kinase activity. [5] PD153035 improves glucose tolerance, insulin sensitivity, and signaling and reduces subclinical inflammation in HFD-fed mice. [6] Pretreatment of EGFR inhibitors by 24 hours significantly enhances the cytotoxic effect of doxorubicin, paclitaxel, cisplatin, and 5-fluororuacil in NPCTW04 cells. [3] |
キナーゼアッセイ | Inhibition of EGF receptor tyrosine kinase | |
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Enzyme reactions are performed in a total volume of 0.1 mL containing 25 mM Hepes (pH 7.4), 5 mM MgCl2, 2 mM MnCl2, 50 μM sodium vanadate, 0.5 to 1.0 ng of enzyme (which also contains enough EGF to make the final concentrations 2 μg/mL), 10 μM ATP containing 1 μCi of [32P]ATP, varying concentrations of PD153035, and 200 μM of a substrate peptide based on a portion of phospholipase C-γl having the sequence Lys-His-Lys-Lys-Leu-Ala-Glu-Gly-Ser-Ala-Tyr472-Glu-Glu-Val. The reaction is initiated by the addition of ATP. After 10 minutes at room temperature, the reaction is terminated by addition of 2 mL of 75 mM phosphoric acid, and the solution is passed through a 2.5-cm phosphocellulose filter disk that binds the peptide. The filter is washed five times with 75 mM phosphoric acid and placed in a vial with 5 mL of scintillation fluid. The uninhibited control activity produces approximately 100,000 cpm. | ||
細胞アッセイ | 細胞株 | A431, Difi, DU145, MDA-MB-468 and ME180 |
濃度 | 0-3 μM | |
反応時間 | 72 hours | |
実験の流れ | Cells are seeded in sixwell plates. The next day, cells are changed to medium containing 0.5% FBS for 18 hours, and then PD153035 is added at various concentrations to the cultures. After 72 hours of treatment, cells are washed once with PBS, harvested with 0.1% human trypsin-l mM EDTA in PBS, and counted with a Coulter counter. The CMK cells grow in suspension and, therefore, do not require trypsinization. | |
動物実験 | 動物モデル | A431 cells are injected into the outbred nude mice. |
投薬量 | ≤80 mg/kg | |
投与方法 | Administered via i.p. |
Data from [J Immunol, 2012, 188(9), 4581-4589 ]
, 2010, Dr. Zhang of Tianjin Medical University
Data from [Data independently produced by , , Oncotarget, 2016, 7(24):36168-36184.]
Receptor-kinase EGFR-MAPK adaptor proteins mediate the epithelial response to Candida albicans via the cytolytic peptide toxin, candidalysin [ J Biol Chem, 2022, 298(10):102419] | PubMed: 36037968 |
Hemodynamic Forces Regulate Cardiac Regeneration-Responsive Enhancer Activity during Ventricle Regeneration [ Int J Mol Sci, 2021, 22(8)3945] | PubMed: 33920448 |
Identification of chemical compounds regulating PD-L1 by introducing HiBiT-tagged cells [ FEBS Lett, 2021, 595(5):563-576] | PubMed: 33421110 |
Identification of chemical compounds regulating PD-L1 by introducing HiBiT-tagged cells [ FEBS Lett, 2021, 10.1002/1873-3468.14032] | PubMed: 33421110 |
RAB31 marks and controls an ESCRT-independent exosome pathway [ Cell Res, 2020, 10.1038/s41422-020-00409-1] | PubMed: 32958903 |
AREG mediates the epithelial‑mesenchymal transition in pancreatic cancer cells via the EGFR/ERK/NF‑κB signalling pathway. [ Oncol Rep, 2020, 43(5):1558-1568] | PubMed: 32323797 |
Epidermal growth factor receptor inhibition attenuates non-alcoholic fatty liver disease in diet-induced obese mice [ PLoS One, 2019, 14(2):e0210828] | PubMed: 30735525 |
Intelectin contributes to allergen-induced IL-25, IL-33, and TSLP expression and type 2 response in asthma and atopic dermatitis. [ Mucosal Immunol, 2017, 10(6):1491-1503] | PubMed: 28224996 |
[ Oncotarget, 2016, ] | PubMed: 27556697 |
SK3/TRPC1/Orai1 complex regulates SOCE-dependent colon cancer cell migration: a novel opportunity to modulate anti-EGFR mAb action by the alkyl-lipid Ohmline. [Guéguinou M, et al. Oncotarget, 2016, 7(24):36168-36184] | PubMed: 27102434 |
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。
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