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SGI-7079

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Chemical Structure| 1239875-86-5 同义名 : -
CAS号 : 1239875-86-5
货号 : A771421
分子式 : C26H26FN7
纯度 : 99%+
分子量 : 455.53
MDL号 : MFCD28963942
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(76.83 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.20mL

0.44mL

0.22mL

10.98mL

2.20mL

1.10mL

21.95mL

4.39mL

2.20mL
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