PD168393

製品コードS7039 バッチS703902

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C17H13BrN4O
分子量 369.22 CAS No. 194423-15-9
Solubility (25°C)* 体外 DMSO 73 mg/mL (197.71 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
3.0mg/ml Taking the 1 mL working solution as an example, add 50 μL 60 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O 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 PD168393 is an irreversible EGFR inhibitor with IC50 of 0.70 nM, irreversibly alkylate Cys-773; inactive against insulin, PDGFR, FGFR and PKC.
in vitro PD 168393 is docked into the ATP binding pocket of EGFR TK. PD168393 completely suppresses EGF-dependent receptor autophosphorylation in A431 cells during continuous exposure, with continous suppression even after 8 hr in compound-free medium. PD168393 inhibits heregulin-induced tyrosine phosphorylation in MDA-MB-453 cells with IC50 of 5.7 nM. PD168393 is inactive against insulin, PDGF and basic FGFR TKs as well as PKC. PD168393 inhibits EGF-mediated tyrosine phosphorylation in HS-27 human fibroblasts with IC50 of 1-6 nM but has little effect on FGF- or PDGF-mediated tyrosine phosphorylation. [1] PD168393 shows rapid and potent inhibition of Her2-induced tyrosine phosphorylation with IC50 of ~100 nM in 3T3-Her2 cells. D168393 also inhibits phosphorylation of PLCγ1/Stat1/Dok1/δ-catenin in 3T3-Her2 cells, except for Fyb. [2]
in vivo PD 168393 produces tumor growth inhibition of 115% in A431 human epidermoid carcinoma xenograft in nude mice, with 50% reduced phosphotyrosine content of EGFR. PD 168393 also shows a low plasma concentration. [1]
特徴 Preclinical compound used in the design of CI-1033.

プロトコル(参考用のみ)

キナーゼアッセイ Enzyme Assays
The enzyme assay is performed in 96-well filte plates. The total volume is 0.1 mL containing 20 mM HEPES, pH 7.4, 50 μM sodium vanadate, 40 mM magnesium chloride, 10 μM ATP containing 0.5 μCi of [32P]ATP, 20 μg of polyglutamic acid/tyrosine, 1 ng of EGF receptor tyrosine kinase, and appropriate dilutions of inhibitor and/or ATP. All components except the ATP are added to the well, and the plate is incubated with shaking for 10 min at 25 °C. The reaction is started by adding [32P]ATP, and the plate is incubated with shaking at 25 °C for 10 min. The reaction is terminated by the addition of 0.1 mL of 20% TCA, and the plate is kept at 4 °C for at least 15 min to allow the substrate to precipitate. The wells are then washed five times with 0.125 mL of 10% TCA, and [32P] incorporation is determined with a Wallac beta plate counter. To assess the type of inhibition, kinetic data are fitted by nonlinear regression computer programs.
動物実験 動物モデル Athymic nude mice with A431 human epidermoid carcinoma
投薬量 58 mg/kg
投与方法 i.p.

カスタマーフィードバック

Data from [Data independently produced by , , Theranostics, 2017, 7(3):664-676.]

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：

The EGF/EGFR axis and its downstream signaling pathways regulate the motility and proliferation of cultured oral keratinocytes [ FEBS Open Bio, 2023, 10.1002/2211-5463.13653] PubMed: 37243482
Schwann cell precursors generate sympathoadrenal system during zebrafish development [ J Neurosci Res, 2021, 10.1002/jnr.24909] PubMed: 34184294
Cbfα1 hinders autophagy by DSPP upregulation in odontoblast differentiation. [ Int J Biochem Cell Biol, 2019, 115:105578] PubMed: 31374250
miR-17-3p Contributes to Exercise-Induced Cardiac Growth and Protects against Myocardial Ischemia-Reperfusion Injury. [Shi J, et al. Theranostics, 2017, 7(3):664-676] PubMed: 28255358
[ Oncotarget, 2016, ] PubMed: 27322144

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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