Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SGI7079 是 ATP-竞争性 Axl 抑制剂,能够显著抑制 SUM149 (IC50:0.43 μM)和 KPL-4 (IC50:0.16 μM)细胞增殖。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 306 | 现货 | ||
2 mg | ¥ 482 | 现货 | ||
5 mg | ¥ 796 | 现货 | ||
10 mg | ¥ 1,270 | 现货 | ||
25 mg | ¥ 2,570 | 现货 | ||
50 mg | ¥ 3,170 | 现货 | ||
100 mg | ¥ 4,650 | 现货 | ||
500 mg | ¥ 9,920 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 788 | 现货 |
产品描述 | SGI-7079 is a new selective Axl inhibitor. SGI-7079 can be a dose-dependent manner inhibited growth of tumors. It is also a potential therapeutic target for EGFR inhibitor resistance. |
体外活性 | SGI-7079 exhibits a Ki = 5.7 nM for AXL ,and in HEK293T cells (EC50 = 100 nM) inhibits Gas6 ligand-induced tyrosine phosphorylation of human AXL expressed . Similar to AXL, SGI-7079 inhibits TAM family members such as MER and Tyro3, and shows effective inhibition of Syk, Flt1, Flt3, Jak2, TrkA, TrkB, PDGFRβ and Ret kinases. Mesenchymal cells, which have the increase of the receptor tyrosine kinase Axl, show a trend that has greater sensitivity to the Axl inhibitor SGI-7079. |
体内活性 | SGI-7079 can be in a dose-dependent manner inhibits tumor growth. And at the maximum dose, 67% tumor can be inhibited growth. Mesenchymal cells showed a trend towards a greater sensitivity to the Axl inhibitor SGI-7079, while the combination of SGI-7079 with erlotinib reversed erlotinib resistance in mesenchymal lines expressing Axl and in a xenograft model of mesenchymal NSCLC. |
激酶实验 | In phospho-GEF-H1 cellular assay, TR-293-KDG cells are incubated for 3 hours with PF-3758309. TR-293-KDG cells were captured on an anti-HA antibody-coated plate, which is detected with an anti-phospho-S810-GEF-H1 antibody, and quantified with a horseradish peroxidase-goat anti-rabbit antibody conjugate. TR-293-KDG cells are constructed from HEK293 cells, which is transfected with tetracycline-inducible PAK4-kinase domain (amino acids 291-591) and expressed HA-tagged GEFH1ΔDH (amino acids 210-921). |
细胞实验 | SGI-7079 show inhibition of Axl activation in HEK-293 cells, which were transiently transfected by electroporation with 1 mg FLAG-tagged plasmid containing the human Axl gene and incubated in standard media + 10% FBS for 24 hours.Cells are treated with SGI-7079( concentrations : 0.03, 0.1, 0.3, 1, 3 μmol/L) for 10 minutes. Five minutes before lysis, the cells are stimulated by WI38 conditioned media containing Gas6. |
动物实验 | Animal Models: Mouse(NCr-nu/nu female mice) xenograft model of NSCLC using the mesenchymal NSCLC cell line A549Formulation: 0.1N citrate bufferDosages: 10, 25, 50 mg/kgAdministration: p.o. |
分子量 | 455.53 |
分子式 | C26H26FN7 |
CAS No. | 1239875-86-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 84 mg/mL (184.4 mM)
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 | 2.1952 mL | 10.9762 mL | 21.9525 mL | 54.8811 mL |
5 mM | 0.439 mL | 2.1952 mL | 4.3905 mL | 10.9762 mL | |
10 mM | 0.2195 mL | 1.0976 mL | 2.1952 mL | 5.4881 mL | |
20 mM | 0.1098 mL | 0.5488 mL | 1.0976 mL | 2.7441 mL | |
50 mM | 0.0439 mL | 0.2195 mL | 0.439 mL | 1.0976 mL | |
100 mM | 0.022 mL | 0.1098 mL | 0.2195 mL | 0.5488 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。
SGI-7079 1239875-86-5 Angiogenesis Apoptosis Tyrosine Kinase/Adaptors c-RET c-Met/HGFR FLT TAM Receptor Src Tyro3 inhibit Inhibitor Axl Mer SGI7079 SGI 7079 inhibitor