| 名稱 | CL-387785 |
| 描述 | CL-387785 (WAY-EKI 785)(EKI785; WAY-EKI 785) is an irreversible inhibitor of EGFR(IC50： 370+/-120 pM); is able to overcome resistance caused by the T790M mutation on a functional level. |
| 細胞實驗 | MTS assays are performed with the CellTiter 96@ AQueous One solution proliferation kit. A total of 10,000 cells per well in 96-well ?at-bottomed plates are incubated with various concentrations of inhibitors for 48 h. The IC50 is determined from dose–response curves using XL?t4.(Only for Reference) |
| 激酶實驗 | Liquid scintillation: Stock solutions of 500 μM CL-387785 (prepared in 100% DMSO) are diluted to the desired concentration with 30 mM HEPES, pH 7.4. Ten microliters of CL-387785 at various concentrations are incubated with 3 μL of recombinant enzyme (1:120 dilution in 100 mM HEPES, pH 7.4) on ice for 10 min. Then, 5 μL peptide (400 μM final concentration of RR-SRC composed of Arg-Arg-Leu-Ile-Glu-Asp-Ala-Glu-Tyr-Ala-Ala-Arg-Gly), 10 μL of 4× reaction buffer containing 50 mM HEPES, pH 7.4, 80 μM ATP, 40 mM MnCl2, and 200 μM sodium orthovanadate. 0.30 μL [33P]ATP ( >2500 Ci/mmol), and 12 μL Water are added. After incubation for 90 min at room temperature, the entire volume is spotted onto precut P81 filter papers. The filter discs are washed two times with 0.5% phosphoric acid, and radioactivity is measured using a liquid scintillation counter. Under these conditions, the specific activity of EGF-R kinase is approximately 0.50 pmol/mg/min. |
| 體外活性 | CL-387785（50 mg/kg）對HCT-116誘導的異種移植瘤生長具有明顯抑制作用.在表達EGF-R的裸鼠體內,CL-387785（80 mg/kg/day,p.o.）有效抑制腫瘤生長.在常染色體隱性遺傳性多囊腎疾病小鼠模型中,CL-387785（90 mg/kg,i.p.）處理Balb/c-bpk/bpk (BPK)小鼠,可使集合小管囊性病變顯著降低,改善腎功能,使膽管上皮細胞異常降低,延長生存期.CL-387785（25 mg/kg）能夠降低HCA-7誘導的異種移植瘤生長,100 mg/kg時可完全抑制腫瘤生長. |
| 體內活性 | CL-387785可使細胞中EGF-介導的受體自磷酸化被阻斷（IC50：5 nM）。在過表達EGF-R或c-erbB-2的細胞系中,CL-387785主要以細胞抑制劑的方式抑制細胞增殖（IC50：31 nM）。 |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 60 mg/mL (157.39 mM), Sonication is recommended.
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 1 mg/mL (insoluble or slightly soluble)
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| 關鍵字 | EKI785 | ErbB-1 | HER1 | CL 387785 | EGFR | WAY-EKI-785 | WAY-EKI785 | CL387785 | inhibit | Inhibitor | EKI 785 | Epidermal growth factor receptor | CL-387785 |
| 相關產(chǎn)品 | Lapatinib | Neratinib | Chalcone | Gefitinib | Erlotinib | Osimertinib | Erlotinib hydrochloride | Afatinib Dimaleate | Lidocaine Hydrochloride hydrate | Genistein | Khellin | Osimertinib mesylate |
| 相關庫 | 抑制劑庫 | 經(jīng)典已知活性庫 | 抗癌活性化合物庫 | 已知活性化合物庫 | 激酶抑制劑庫 | 高選擇性抑制劑庫 | 抗卵巢癌化合物庫 | 膜蛋白靶向化合物庫 | 酪氨酸激酶分子庫 | 共價抑制劑庫 |