CAS number：928037-13-2 molecular formula：C33H37F2N7O4
Golvatinib (E7050)是c-Met和VEGFR-2双重抑制剂，IC50分别为14 nM和16 nM，不抑制bFGF刺激的HUVEC生长(浓度高达1000 nM)。Golvatinib也能抑制多种肿瘤细胞的生长,包括MKN45\EBC-1\Hs746T和SNU-5.除此之外,golvatinib有效抑制HGF或VEGF诱导的生长,IC50值为17 nM和84 nM. 在MKN45\Hs746T\SUN-5和EBC-1肿瘤细胞系异种移植小鼠模型上,golvatinib显著抑制肿瘤的生长.在VEGF过表达的人胰腺癌细胞系KP-1 /VEGF异种移植小鼠模型中,E7050单一给药,可减少VEGFR-2的磷酸化,随后通过抑制VEGF/VEGFR-2介导的肿瘤血管生成从而抑制肿瘤的生长。
| Chinese alias | - | ||
| English alias | AKOS015998189 | FT-0700410 | N~1~-{2-fluoro-4-[(2-{[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]amino}pyridin-4-yl)oxy]phenyl}-N'~1~-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | s2859 | UNII-516Z3YP58E | 1-N'-[2-fluoro-4-[2-[[4-(4-methylpiperazin- | ||
| CAS number | 928037-13-2 | molecular formula | C33H37F2N7O4 |
| molecular weight | 633.69 g/mol | Exact mass | - |
| PSA | 119.000 Ų | logp | 4.1 |
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