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首页-小分子抑制剂&激动剂-Tyrosine Kinase-TAM Receptor (Tyro3-Axl-Mer)-SGI-7079
SGI-7079

Chemical Structure : SGI-7079

CAS No.: 1239875-86-5

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SGI-7079 (SGI7079;SGI 7079)

货号: PC-43298Not For Human Use, Lab Use Only.

SGI-7079 is a potent, selective Axl inhibitor with Ki of 5.7 nM, inhibits Gas6 ligand-induced tyrosine phosphorylation of human AXL expressed in HEK293T cells with EC50 of 100 nM.

规格 价格 库存 数量
2 mg (Free Sample) ￥180 In stock
5 mg ￥880 In stock
10 mg ￥1280 In stock
25 mg ￥2180 In stock
50 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

SGI-7079 is a potent, selective Axl inhibitor with Ki of 5.7 nM, inhibits Gas6 ligand-induced tyrosine phosphorylation of human AXL expressed in HEK293T cells with EC50 of 100 nM.
SGI-7079 inhibits proliferation of inflammatory breast cancer cells SUM149 and KPL-4 with IC50 of 0.43 and 0.15 uM.
SGI-7079 inhibits TAM family members MER and Tyro3, also shows potent, low nM inhibition of Syk, Flt1, Flt3, Jak2, TrkA, TrkB, PDGFRβ and Ret kinases.
SGI-7079 decreases invasion, halts the cell cycle in the G1 phase, and synergistically increases the potency of erlotinib.
SGI-7079 inhibits tumor growth mouse xenograft model of NSCLC, reverses erlotinib resistance combined with erlotinib.

物理化学性质&存储条件

分子量 455.5299
分子式 C26H26FN7
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: ≥ 34 mg/mL
Chemical Name/SMILES

Benzeneacetonitrile, 3-[2-[[3-fluoro-4-(4-methyl-1-piperazinyl)phenyl]amino]-5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-

参考文献

1. Byers LA, et al. Clin Cancer Res. 2013 Jan 1;19(1):279-90.

2. Myers SH, et al. J Med Chem. 2016 Apr 28;59(8):3593-608.

3. Wang X, et al. Cancer Res. 2013 Nov 1;73(21):6516-25.

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