keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Oritinib (SH-1028) 是一种 EGFR 抑制剂,对 EGFR (wt)、EGFR (L858R)、EGFR (L861Q)、EGFR (L858R/T790M)、EGFR (d746-750) 的 IC50 分别为 18、0.7、4、0.1、1.4 和 0.89 nM , EGFR (d746-750/T790M), 分别。奥瑞替尼可用于治疗非小细胞肺癌的研究。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,650 | 现货 | ||
5 mg | ¥ 3,920 | 现货 | ||
10 mg | ¥ 5,590 | 现货 | ||
25 mg | ¥ 8,630 | 现货 | ||
50 mg | ¥ 11,600 | 现货 | ||
100 mg | ¥ 15,700 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 4,560 | 现货 |
产品描述 | Oritinib (SH-1028) is an inhibitor of EGFR with IC50s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM for EGFR (wt), EGFR (L858R), EGFR (L861Q), EGFR (L858R/T790M), EGFR (d746-750), EGFR (d746-750/T790M), respectively. Oritinib can be used in studies about the treatment of non-small cell lung cancer. |
体外活性 | Oritinib (0.001, 0.01, 0.1, 1, and 10 μM) selectively inhibits EGFR-mutated NCI-H1975, H3255 and PC-9 cells, with IC50s of 3.932, 9.39 and 7.63 nM, respectively. Oritinib (0.1 μM) continuously inhibits the phosphorylation of EGFR in PC-9 and NCI-H1975 cells[1]. |
体内活性 | In female mice bearing NCI-H1975 and A431 xenograft models, Oritinib (2.5, 5, and 15 mg/kg; oral) significantly inhibits proliferation of tumor cells with no TKI-induced weight loss. In NCI-H1975 tumor-bearing mice, Oritinib (2.5, 5, and 15 mg/kg; oral) shows good bioavailability(Tmax = 1.5-2 h) and extensive distribution from the plasma to the tissues. The AUC0–t values in plasma are 118, 300 and 931 ng×h/mL on Day 1, while 272, 308 and 993 ng×h/ml on Day 14, respectively[1]. |
别名 | SH-1028 |
分子量 | 539.67 |
分子式 | C31H37N7O2 |
CAS No. | 2035089-28-0 |
keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 120 mg/mL (222.36 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.853 mL | 9.2649 mL | 18.5298 mL | 46.3246 mL |
5 mM | 0.3706 mL | 1.853 mL | 3.706 mL | 9.2649 mL | |
10 mM | 0.1853 mL | 0.9265 mL | 1.853 mL | 4.6325 mL | |
20 mM | 0.0926 mL | 0.4632 mL | 0.9265 mL | 2.3162 mL | |
50 mM | 0.0371 mL | 0.1853 mL | 0.3706 mL | 0.9265 mL | |
100 mM | 0.0185 mL | 0.0926 mL | 0.1853 mL | 0.4632 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。
Oritinib 2035089-28-0 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR pharmacodynamics non-small cell lung cancer EGFR-T790M EGFR TKI Irreversible mutant-selective SH1028 HER1 inhibit SH-1028 Inhibitor Epidermal growth factor receptor SH 1028 ErbB-1 third-generation inhibitor