SU14813
产品说明书
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同义名 : | SU 014813 |
| CAS号 : | 627908-92-3 | |
| 货号 : | A748613 | |
| 分子式 : | C23H27FN4O4 | |
| 纯度 : | 99%+ | |
| 分子量 : | 442.48 | |
| MDL号 : | MFCD16495822 | |
| 存储条件： |
Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
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| 描述 | SU14813 is a multi-targeted receptor tyrosine kinases inhibitor with IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT. SU14813 inhibits the growth of U-118MG with an IC50 of 50 to 100 nM. SU14813 inhibited VEGFR (vascular endothelial growth factor receptor)-2, PDGFR (platelet-derived growth factor receptor)-beta, and FLT3 (fms-like tyrosine kinase 3) phosphorylation in xenograft tumors in a dose- and time-dependent fashion. SU14813 inhibited target RTK (Receptor tyrosine kinases) activity in vivo in association with reduction in angiogenesis, target RTK-mediated proliferation, and survival of tumor cells, leading to broad and potent antitumor efficacy. Treatment in combination with docetaxel significantly enhances both the inhibition of primary tumor growth and the survival of the tumor-bearing mice compared with administration of either agent alone[3]. SU14813 has manageable safety and tolerability and allows once-daily continuous oral dosing. SU14813 shows dose-proportional pharmacokinetics, with target plasma concentrations achieved at doses ≥ 100 mg/day[4]. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.26mL 0.45mL 0.23mL |
11.30mL 2.26mL 1.13mL |
22.60mL 4.52mL 2.26mL |
| 参考文献 |
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