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CAS No.: 1239875-86-5

SGI-7079 Catalog No. CSN17238

SGI-7079, a selective Axl inhibitor, inhibits tumor growth in a dose dependent manner and is a potential therapeutic target for overcoming EGFR inhibitor resistance.

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400-920-2911

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生物活性

实验方案

技术信息

生物活性

描述The AXL protein, classified as a RTK (Receptor tyrosine kinase), belongs to the TAM (TYRO3, AXL, and MER) subfamily. Overexpression or overactivation of the AXL has been correlated with the promotion of multiple tumorigenic processes. SGI-7079 is a relatively potent AXL inhibitor (IC₅₀ = 58 nM, in cell-free assays) in preclinical development. It inhibits GAS6-stimulated AXL signaling in inflammatory breast cancer cells (IC₅₀ < 1 μM), resulting in decreased cell proliferation and invasion^[3]. Mesenchymal cell lines expressing Axl were highly sensitive to SGI-7079 alone. In a mouse xenograft model of NSCLC (non-small cell lung cancer), SGI-7079 inhibited tumor growth in a dose dependent manner, and at the maximum dose, inhibited tumor growth by 67%, compared to control. Notably, SGI-7079 + erlotinib (25/100 mg/kg) reduced the tumor growth by 82%^[4].
参考文献

[1] Myers SH, Brunton VG, et al. AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective. J Med Chem. 2016 Apr 28;59(8):3593-608.
[2] Byers LA, Diao L, et al. An epithelial-mesenchymal transition gene signature predicts resistance to EGFR and PI3K inhibitors and identifies Axl as a therapeutic target for overcoming EGFR inhibitor resistance. Clin Cancer Res. 2013 Jan 1;19(1):279-90.
[3] Myers SH, Brunton VG, Unciti-Broceta A. AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective. J Med Chem. 2016;59(8):3593-3608
[4] Byers LA, Diao L, Wang J, et al. An epithelial-mesenchymal transition gene signature predicts resistance to EGFR and PI3K inhibitors and identifies Axl as a therapeutic target for overcoming EGFR inhibitor resistance. Clin Cancer Res. 2013;19(1):279-290

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1952 mL
- 10.9762 mL
- 21.9525 mL
- 5 mM
- 0.4390 mL
- 2.1952 mL
- 4.3905 mL
- 10 mM
- 0.2195 mL
- 1.0976 mL
- 2.1952 mL

技术信息

CAS号

1239875-86-5

储存条件

粉末: Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H26FN7

运输

蓝冰

分子量

455.53

别名

溶解度

DMSO	91.0 mg/mL (199.8 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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