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首页-小分子抑制剂&激动剂-Tyrosine Kinase-c-Met (HGFR)-Foretinib
Foretinib

Chemical Structure : Foretinib

CAS No.: 849217-64-7

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Foretinib (XL880;GSK1363089;GSK089;EXEL-2880)

货号: PC-42535Not For Human Use, Lab Use Only.

Foretinib (XL880, GSK1363089, GSK089, EXEL-2880) is a potent, multikinase inhibitor that inhibits c-Met and VEGFR, also KIT, Flt-3, PDGFRβ, and Tie-2.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Foretinib (XL880, GSK1363089, GSK089, EXEL-2880) is a potent, multikinase inhibitor that inhibits c-Met and VEGFR, also inhibits KIT, Flt-3, PDGFRβ, and Tie-2.
Foretinib inhibits HGFR family tyrosine kinases with IC50 of 0.4 nM for Met and 3 nM for Ron, also inhibits KDR, Flt-1, and Flt-4 with IC50 of 0.9, 6.8, and 2.8 nM, respectively.
Foretinib exhibits modest activity against FGFR1 and EGFR, no activity against 50 serine/threonine kinases, including CDKs and PKC isoforms.
Foretinib inhibits cellular HGF-induced Met phosphorylation and VEGF-induced ERK phosphorylation and prevents both HGF-induced responses of tumor cells and HGF/VEGF-induced responses of endothelial cells.
Foretinib exhibits significant inhibition of tumor burden in animal model of lung metastasis.

物理化学性质&存储条件

分子量 632.6537
分子式 C34H34F2N4O6
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: ≥ 38 mg/mL
Chemical Name/SMILES

1,1-Cyclopropanedicarboxamide, N-[3-fluoro-4-[[6-methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinolinyl]oxy]phenyl]-N'-(4-fluorophenyl)-

参考文献

1. Qian F, et al. Cancer Res. 2009 Oct 15;69(20):8009-16.

2. Liu L, et al. Cancer Res. 2009 Sep 1;69(17):6871-8.

3. Eder JP, et al. Clin Cancer Res. 2010 Jul 1;16(13):3507-16.

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