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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。
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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 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 248 | 现货 | |
5 mg | ¥ 579 | 现货 | |
10 mg | ¥ 993 | 现货 | |
25 mg | ¥ 1,980 | 现货 | |
50 mg | ¥ 2,570 | 现货 | |
100 mg | ¥ 3,730 | 现货 | |
500 mg | ¥ 7,850 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 637 | 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对AXL的Ki值为5.7 nM,并能在HEK293T细胞中(EC50=100 nM)抑制由Gas6配体诱导的人类AXL的酪氨酸磷酸化。与AXL相似,SGI-7079还能抑制TAM家族成员如MER和Tyro3,同时有效抑制Syk、Flt1、Flt3、Jak2、TrkA、TrkB、PDGFRβ和Ret激酶。表达受体酪氨酸激酶Axl增加的间充质细胞对Axl抑制剂SGI-7079表现出更高的敏感性。 |
体内活性 | SGI-7079能够依剂量依赖性抑制肿瘤生长,在最大剂量下,可抑制67%的肿瘤生长。间充质细胞对Axl抑制剂SGI-7079显示出更高的敏感性,同时,SGI-7079与erlotinib的联合使用能够逆转表达Axl的间充质细胞系及间充质非小细胞肺癌(NSCLC)异种移植模型中的erlotinib抗药性。 |
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 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 84 mg/mL (184.4 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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