Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CL-387785 (WAY-EKI 785) 是一种不可逆的EGFR 抑制剂,IC50为 370 pM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 278 | 现货 | ||
2 mg | ¥ 393 | 现货 | ||
5 mg | ¥ 655 | 现货 | ||
10 mg | ¥ 987 | 现货 | ||
25 mg | ¥ 1,930 | 现货 | ||
50 mg | ¥ 3,190 | 现货 | ||
100 mg | ¥ 4,730 | 现货 | ||
500 mg | ¥ 9,870 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 722 | 现货 |
产品描述 | 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. |
靶点活性 | EGFR:370+/-120 pM |
体外活性 | CL-387785(50 mg/kg)对HCT-116诱导的异种移植瘤生长具有明显抑制作用.在表达EGF-R的裸鼠体内,CL-387785(80 mg/kg/day,p.o.)有效抑制肿瘤生长.在常染色体隐性遗传性多囊肾疾病小鼠模型中,CL-387785(90 mg/kg,i.p.)处理Balb/c-bpk/bpk (BPK)小鼠,可使集合小管囊性病变显著降低,改善肾功能,使胆管上皮细胞异常降低,延长生存期.CL-387785(25 mg/kg)能够降低HCA-7诱导的异种移植瘤生长,100 mg/kg时可完全抑制肿瘤生长. |
体内活性 | CL-387785可使细胞中EGF-介导的受体自磷酸化被阻断(IC50:5 nM)。在过表达EGF-R或c-erbB-2的细胞系中,CL-387785主要以细胞抑制剂的方式抑制细胞增殖(IC50:31 nM)。 |
激酶实验 | 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. |
细胞实验 | 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) |
别名 | WAY-EKI 785, EKI-785 |
分子量 | 381.23 |
分子式 | C18H13BrN4O |
CAS No. | 194423-06-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 59 mg/mL (154.8 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.6231 mL | 13.1154 mL | 26.2309 mL | 65.5772 mL |
5 mM | 0.5246 mL | 2.6231 mL | 5.2462 mL | 13.1154 mL | |
10 mM | 0.2623 mL | 1.3115 mL | 2.6231 mL | 6.5577 mL | |
20 mM | 0.1312 mL | 0.6558 mL | 1.3115 mL | 3.2789 mL | |
50 mM | 0.0525 mL | 0.2623 mL | 0.5246 mL | 1.3115 mL | |
100 mM | 0.0262 mL | 0.1312 mL | 0.2623 mL | 0.6558 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
CL-387785 194423-06-8 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR WAY-EKI 785 EKI785 ErbB-1 HER1 CL 387785 WAY-EKI-785 WAY-EKI785 CL387785 inhibit EKI-785 Inhibitor EKI 785 Epidermal growth factor receptor inhibitor