5-[(5-氟-1,2-二氢-2-氧代-3H-吲哚-3-亚基)甲基]-N-[(2S)-2-羟基-3-(4-吗啉基)丙基]-2,4-二甲基-1H-吡咯-3-甲酰胺
SU14813(SU14813)
CAS: 627908-92-3
化学式: C23H27FN4O4
| 中文名 | SU14813 |
| 英文名 | SU14813 |
| 别名 | SU-14813游离态 受体酪氨酸激酶抑制剂(SU14813) 5-((5-氟-2-氧代吲哚-3-亚基)甲基)-N-(2-羟基-3-吗啉代丙基)-2,4-二甲基-1H-吡咯-3-甲酰胺 5-[(5-氟-1,2-二氢-2-氧代-3H-吲哚-3-亚基)甲基]-N-[(2S)-2-羟基-3-(4-吗啉基)丙基]-2,4-二甲基-1H-吡咯-3-甲酰胺 5-[(5-氟-1,2-二氢-2-氧代-3H-吲哚-3-亚烷基)甲基]-N-[(2S)-2-羟基-3-(4-吗啉基)丙基]-2,4-二甲基-1H-吡咯-3-甲酰胺 |
| 英文别名 | SU14813 CS-1149 SU-14813 SU 14813 SU14813(Random Configuration) 5-[(Z)-(5-Fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-N- [ 2-hydroxy-3-(4-morpholinyl)propyl]-2,4-dimethyl-1H-pyrrole-3-carb 5-[(5-Fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-N-[(2S)-2-hydroxy-3-(4-morpholinyl)propyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide 1H-Pyrrole-3-carboxamide, 5-[(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-N-[(2S)-2-hydroxy-3-(4-morpholinyl)propyl]-2,4-dimethyl- |
| CAS | 627908-92-3 |
| 化学式 | C23H27FN4O4 |
| 分子量 | 442.48 |
| 密度 | 1.341 |
| 沸点 | 685.6±55.0 °C(Predicted) |
| 溶解度 | DMSO: 44 mg/mL (99.44 mM)，需超声 ( < 1 mg/mL指产品微溶或不溶) |
| 酸度系数 | 11.24±0.20(Predicted) |
| 存储条件 | -20℃ |
| 靶点 | VEGFR1; VEGFR2; PDGFRβ; KIT; VEGFR Kinases; Tyrosine |
| 体外研究 | SU14813 inhibits ligand-dependent and ligand-independent proliferation, migration, and survival of endothelial cells and/or tumor cells expressing these targets. SU14813 inhibits cellular ligand-dependent phosphorylation of VEGFR-2 (transfected NIH 3T3 cells), PDGFR-β (transfected NIH 3T3 cells), KIT (Mo7e cells), and FLT3-internal tandem duplication (FLT3-ITD; MV4;11 cells) as well as FMS/CSF1R (transfected NIH 3T3 cells). SU14813 inhibits VEGFR-2, PDGFR-β, and KIT phosphorylation in porcine aorta endothelial cells overexpressing these targets, with cellular IC 50 values of 5.2, 9.9, and 11.2 nM, respectively. SU14813 inhibits the growth of U-118MG with an IC 50 of 50 to 100 nM. |
| 体内研究 | SU14813 inhibits VEGFR-2, PDGFR-β, and FLT3 phosphorylation in xenograft tumors in a dose- and time-dependent fashion. The plasma concentration required for in vivo target inhibition is estimated to be 100 to 200 ng/mL. Used as monotherapy, SU14813 exhibits broad and potent antitumor activity resulting in regression, growth arrest, or substantially reduces growth of various established xenografts derived from human or rat tumor cell lines. 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. |
5-[(5-氟-1,2-二氢-2-氧代-3H-吲哚-3-亚基)甲基]-N-[(2S)-2-羟基-3-(4-吗啉基)丙基]-2,4-二甲基-1H-吡咯-3-甲酰胺 - 配置溶液浓度参考
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.26 ml | 11.3 ml | 22.599 ml |
| 5 mM | 0.452 ml | 2.26 ml | 4.52 ml |
| 10 mM | 0.226 ml | 1.13 ml | 2.26 ml |
| 5 mM | 0.045 ml | 0.226 ml | 0.452 ml |
最后更新：2024-01-02 23:10:35
![5-[(5-氟-1,2-二氢-2-氧代-3H-吲哚-3-亚基)甲基]-N-[(2S)-2-羟基-3-(4-吗啉基)丙基]-2,4-二甲基-1H-吡咯-3-甲酰胺](http://res.chembk.com/assets/images/structure/309254.gif)
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