| 名稱 | PD153035 hydrochloride |
| 描述 | PD153035 hydrochloride (ZM 252868) is a effective and selective inhibitor of EGFR (Ki: 5.2 pM, IC50: 29 pM); few influence against FGFR, PGDFR, InsR, CSF-1, and Src. |
| 細(xì)胞實(shí)驗(yàn) | 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.(Only for Reference) |
| 激酶實(shí)驗(yàn) | 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. |
| 體外活性 | 作用于HFD-fed小鼠時(shí),PD153035促進(jìn)耐糖量、胰島素敏感性和信號(hào),并使亞臨床炎癥降低.作用于攜帶A431人體表皮樣癌細(xì)胞移植瘤的免疫缺陷裸鼠,PD153035（80 mg/kg）對EGF受體酪氨酸激酶活性有抑制作用. |
| 體內(nèi)活性 | PD153035劑量依賴性地抑制鼻咽癌細(xì)胞系HONE1（IC50：18.6 μM）,NPC-TW04（IC50：9.8 μM）和NPC-TW01（IC50：12.9 μM）。PD153035抑制A-431人扁平上皮癌相關(guān)的表皮生長因子受體酪氨酸激酶（Ki：5.2 pM,IC50：29 pM）。作用于Caco-2結(jié)腸癌細(xì)胞時(shí),PD153035可使PAR(2)激活肽2-呋喃甲?；?LIGRLO-NH(2)(2fLI)誘導(dǎo)的COX-2表達(dá)沉默。作用于Swiss 3T3成纖維細(xì)胞和A-431人扁平上皮癌細(xì)胞時(shí),PD153035可選擇性抑制EGF誘導(dǎo)的酪氨酸磷酸化（IC50：15 nM和14 nM）。作用于過量表達(dá)EGF受體的人癌細(xì)胞系時(shí),PD153035抑制包括A431, DU145, Difi, ME180和MDA-MB-468在內(nèi)的細(xì)胞生長,IC50分別為0.22 μM, 0.4 μM, 0.3 μM, 0.95 μM和0.68 μM。 |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 4 mg/mL (10 mM), Heating is recommended.
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| 關(guān)鍵字 | Inhibitor | SU-5271 | HER1 | PD-153035 | ErbB-1 | PD153035 hydrochloride | ZM-252868 | PD153035 Hydrochloride | PD-153035 Hydrochloride | Epidermal growth factor receptor | PD153035 | SU5271 | PD 153035 | Tyrphostin AG-1517 | ZM252868 | EGFR | inhibit | PD 153035 Hydrochloride | AG1517 | PD-153035 hydrochloride | AG-1517 | Tyrphostin AG1517 |
| 相關(guān)產(chǎn)品 | Lapatinib | Neratinib | Chalcone | Gefitinib | Erlotinib | Osimertinib | Erlotinib hydrochloride | Afatinib Dimaleate | Lidocaine Hydrochloride hydrate | Genistein | Khellin | Osimertinib mesylate |
| 相關(guān)庫 | 抑制劑庫 | 血管生成庫 | 經(jīng)典已知活性庫 | 抗癌活性化合物庫 | 已知活性化合物庫 | 抗胰腺癌化合物庫 | 激酶抑制劑庫 | 臨床前化合物庫 | 膜蛋白靶向化合物庫 | 酪氨酸激酶分子庫 |