货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
S57057-1ml促销	10mM in DMSO	￥789.00 ￥630.00 S57057-1ml ￥630.00 现货	9 9	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

S57057-1ml促销

10mM in DMSO

￥789.00 ￥630.00

产品描述：

Axl 抑制剂;Axl Inhibitors;;InformationSGI-7079 SGI-7079, a novel selective Axl inhibitor with an IC50 of 58 nM in vitro, inhibits tumor growth in a dose dependent manner and is a potential therapeutic target for overcoming EGFR inhibitor resistance.TargetsMet ; Mer ; YES ; RET ; FLT3 16051,;In vitroSGI-7079 exhibits a Ki = 5.7 nM for AXL and inhibits Gas6 ligand-induced tyrosine phosphorylation of human AXL expressed in HEK293T cells (EC50 = 100 nM). It inhibits TAM family members MER and Tyro3 similarly as AXL, and shows potent, low nM inhibition of Syk, Flt1, Flt3, Jak2, TrkA, TrkB, PDGFRβ and Ret kinases. Mesenchymal cells express increased levels of the receptor tyrosine kinase Axl and show a trend toward greater sensitivity to the Axl inhibitor SGI-7079.In vivoSGI-7079 inhibits tumor growth in a dose-dependent manner, and at the maximum dose, inhibits tumor growth by 67%, compared with control. the combination of SGI-7079 with erlotinib reverses erlotinib resistance in mesenchymal lines expressing Axl and in a xenograft model of mesenchymal NSCLC.Cell Research(from reference)Cell lines：HEK-293 cells Concentrations：0.03, 0.1, 0.3, 1, 3 μmol/L Incubation Time：10 min

体内研究：

SGI-7079 (50 mg/kg；口服；每周 5 天，持续 2 周) 在小鼠的 SUM149 炎症性乳腺癌皮下移植瘤模型中显著抑制肿瘤生长并延长生存期。
SGI-7079 (50 mg/kg；口服；每周 5 天，持续 2 周) 与抗 PD-1 抗体联用在小鼠 ID8 卵巢癌腹腔模型中诱导肿瘤根除，1/3 小鼠长期存活。

参考文献：

1. Wang X, et al. TIG1 promotes the development and progression of inflammatory breast cancer through activation of Axl kinase. Cancer Res. 2013 Nov 1;73(21):6516-25.
2. Wang SC, et al. Chidamide and mitomycin C exert synergistic cytotoxic effects against bladder cancer cells in vitro and suppress tumor growth in a rat bladder cancer model. Cancer Lett. 2022 Apr 1;530:8-15
3. Guo Z, et al. Axl inhibition induces the antitumor immune response which can be further potentiated by PD-1 blockade in the mouse cancer models. Oncotarget. 2017 Sep 21;8(52):89761-89774.

保存条件：

-80℃（运输条件：冰袋低温运输）

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.195 ml	10.976 ml	21.952 ml
5 mM	0.439 ml	2.195 ml	4.39 ml
10 mM	0.22 ml	1.098 ml	2.195 ml
50 mM	0.044 ml	0.22 ml	0.439 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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