Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Hypothemycin is a fungal polyketide and is a multikinase inhibitor (Kis: 10/70 nM, 17/38 nM, 90 nM, 900 nM/1.5 μM, and 8.4/2.4 μM for VEGFR2/VEGFR1, MEK1/MEK2, FLT-3, PDGFRβ/PDGFRα, and ERK1/ERK2, respectively).
产品描述 | Hypothemycin is a fungal polyketide and is a multikinase inhibitor (Kis: 10/70 nM, 17/38 nM, 90 nM, 900 nM/1.5 μM, and 8.4/2.4 μM for VEGFR2/VEGFR1, MEK1/MEK2, FLT-3, PDGFRβ/PDGFRα, and ERK1/ERK2, respectively). |
靶点活性 | MEK2:38 nM (ki), PDGFRβ:900 nM (ki), PDGFRα:1.5 μM (ki), ERK2:2.4 μM (ki), FLT3:90 nM (ki), MEK1:17 nM (ki), ERK1:8.4 μM (ki), VEGFR1:70 nM (ki), VEGFR2:10 nM (ki) |
体外活性 | Hypothemycin inhibits eosinophilic EOL1 cell carrying mutations in FIP1L1-PDGFRα, acute myeloid leukemia MV-4-11 cell carrying mutations in FLT3-ITD, and melanoma COLO829 cell carrying mutations in BRAF V600E. It has an IC50s of 0.4 nM, 6 nM, and 50 nM, respectively. Hypothemycin also inhibits HUVEC cell carrying mutations in VEGFR, mastocytoma P815 cell carrying mutations in c-KIT D814Y, NSCLC A459 cell carrying mutations in KRAS, and ovarian SKOV-3 cell carrying mutations in HER2 (IC50s: 70 nM, 370 nM, 6.0 μM, and 7.0 μM, respectively)[2]. |
体内活性 | Hypothemycin (10 mg/kg) kills T. brucei in infected mice. However, it completely curing the infection in one third of animals, although high doses of Hypothemycin (>10 mg/kg) leads to side effects. |
分子量 | 378.37 |
分子式 | C19H22O8 |
CAS No. | 76958-67-3 |
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。
Hypothemycin 76958-67-3 Others Inhibitor inhibitor inhibit