Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Tafetinib (SIM-010603) 是一种新型有效且可口服的酪氨酸激酶抑制剂,具有抗血管生成和抗肿瘤活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,750 | 现货 | ||
5 mg | ¥ 4,360 | 现货 | ||
10 mg | ¥ 6,220 | 现货 | ||
25 mg | ¥ 9,390 | 现货 | ||
50 mg | ¥ 12,600 | 现货 | ||
100 mg | ¥ 16,900 | 现货 | ||
500 mg | ¥ 34,300 | 现货 |
产品描述 | Tafetinib (SIM-010603) is a novel potent and orally available tyrosine kinase inhibitor with anti-angiogenic and anti-tumour activity. |
体内活性 | SIM010603, a promising multi-targeted receptor tyrosine kinase (RTK) inhibitor, is now being considered for evaluation in a phase clinical trial. In this work, the subchronic toxicity of SIM010603 in SD rats and beagle dogs has been characterized. Rats and dogs received SIM010603 orally (0-20 and 0-10mg/kg/day, respectively) on a consecutive daily dosing schedule for 28 days following a 14-day recovery period. Sunitinib was used as a positive control. The No Observed Adverse Effect Level (NOAEL) of SIM010603 was 5mg/kg/day for rats, and undefined for dogs. The treatment resulted in unscheduled mortality in dogs receiving 10mg/kg of SIM010603 or Sunitinib. The adverse effects of SIM010603 on rats and dogs mainly included gastrointestinal toxicity, skeletal toxicity, myelosuppression, thymus atrophy, bronchopneumonia, cardiovascular dysfunction, and pancreatic toxicity. Similar observations have also been noted with this class of RTK signaling inhibitors and are consistent with pharmacologic perturbations of physiologic/angiogenic processes associated with the intended molecular targets. Most treatment-induced effects were reversible or showed ongoing recovery upon discontinuation of treatment. SIM010603 has shown a comparable toxicity effect on beagle dogs, while better tolerability on SD rats when compared to Sunitinib.[2] |
别名 | SIM-010603, SIM010603, SIM 010603 |
分子量 | 424.51 |
分子式 | C24H29FN4O2 |
CAS No. | 1032265-57-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
Tafetinib 1032265-57-8 Tyrosine Kinase/Adaptors Tyrosine Kinases SIM-010603 SIM010603 SIM 010603 Inhibitor inhibitor inhibit