PD153035 HCl

製品コードS1079 バッチS107901

印刷

化学情報

Chemical Structure 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
化学式

C16H14BrN3O2.HCl
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）
Clear solution
30%propylene glycol 5%Tween80 65%D5W

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 30.000mg/ml (75.63mM) Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified propylene glycol stock solution to 50 μL of Tween 80, mix evenly to clarify it; then continue to add 650 μL of D5W to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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.

溶剤液（一定の濃度）を調合する

生物活性

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.
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]

プロトコル(参考用のみ)

キナーゼアッセイ Inhibition of EGF receptor tyrosine kinase
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.

参考

  • https://pubmed.ncbi.nlm.nih.gov/8066447/
  • https://pubmed.ncbi.nlm.nih.gov/9815602/
  • https://pubmed.ncbi.nlm.nih.gov/16037687/
  • https://pubmed.ncbi.nlm.nih.gov/22517768/
  • https://pubmed.ncbi.nlm.nih.gov/8824347/
  • https://pubmed.ncbi.nlm.nih.gov/19696185/

カスタマーフィードバック

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.]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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
CD147 promotes collective invasion through cathepsin B in hepatocellular carcinoma [ J Exp Clin Cancer Res, 2020, 39(1):145] PubMed: 32727598
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

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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