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BGJ398 CAS NO.872511-34-7
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- Min.Order: 100 Gram
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≥98.0%(100-500)Gram≥98.0%(1000-5000)Gram
- Product Details
Keywords
- BGJ398
- 3-(2,6-Dichloro-3,5-dimethoxyphenyl)-1-[6-[[4-(4-ethylpiperazin-1-yl)phenyl]amino]pyrimidin-4-yl]-1-methylurea;NVP-BGJ398;BGJ 398;BGJ-398;BGJ398 (NVP-BGJ398);3-(2,6-Dichloro-3,5-dimethoxyphenyl)-1-[6-
- 872511-34-7
Quick Details
- ProName: BGJ398
- CasNo: 872511-34-7
- Molecular Formula: C26H31Cl2N7O3
- Appearance: White crystal
- Application: CAS：872511-34-7；3-(2,6-Dichloro-3,5-di...
- DeliveryTime: 3 months
- PackAge: 100g,500g,1kg,25kg
- Port: shang hai
- ProductionCapacity: 1000 Metric Ton/Month
- Purity: 98%
- Storage: Dry seal
- Transportation: shipping
- LimitNum: 100 Gram
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Details
| BGJ398 (NVP-BGJ398) |
| 生物活性 体外研究 体内研究 |
| 中文名称: | BGJ398 (NVP-BGJ398) |
| 中文同义词: | 3-(2,6-二氯-3,5-二甲氧基苯基)-1-[6-[[4-(4-乙基哌嗪-1-基)苯基]氨基]嘧啶-4-基]-1-甲基脲 |
| 英文名称: | BGJ398 (NVP-BGJ398) |
| 英文同义词: | 3-(2,6-Dichloro-3,5-dimethoxyphenyl)-1-[6-[[4-(4-ethylpiperazin-1-yl)phenyl]amino]pyrimidin-4-yl]-1-methylurea;NVP-BGJ398;BGJ 398;BGJ-398;BGJ398 (NVP-BGJ398);3-(2,6-Dichloro-3,5-dimethoxyphenyl)-1-[6-[[4-(4-ethylpiperazin-1-yl)phenyl]amino]pyrimidin-4-yl]-1-methylurea NVP-BGJ398;NVP-BGJ398 3-(2,6-Dichloro-3,5-dimethoxyphenyl)-1-[6-[[4-(4-ethylpiperazin-1-yl)phenyl]amino]pyrimidin-4-yl]-1-methylurea;Urea, N'-(2,6-dichloro-3,5-dimethoxyphenyl)-N-[6-[[4-(4-ethyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]-N-methyl-, methanesulfonate |
| CAS号: | 872511-34-7 |
| 分子式: | C26H31Cl2N7O3 |
| 分子量: | 560.47544 |
| EINECS号: | |
| 相关类别: | 信号转导通路激酶抑制剂;Inhibitor;小分子抑制剂;Inhibitors;小分子抑制剂，天然产物 |
| Mol文件: | 872511-34-7.mol |
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| BGJ398 (NVP-BGJ398) 性质 |
| 密度 | 1.354 |
| BGJ398 (NVP-BGJ398) 用途与合成方法 |
| 生物活性 | BGJ398 (NVP-BGJ398)是一种有效的，选择性的FGFR抑制剂，作用于FGFR1/2/3，IC50为0.9 nM/1.4 nM/1 nM，作用于FGFR比作用于FGFR4和VEGFR2选择性高40倍以上，对Abl， Fyn， Kit， Lck， Lyn和Yes几乎没有抑制活性。Phase 2。 |
| 体外研究 | BGJ398抑制FGFR3-K650E，IC50 为4.9 nM。此外, BGJ398 也抑制VEGFR2。BGJ398 抑制其他激酶，包括ABL, FYN, KIT, LCK, LYN 和 YES，IC50分别为2.3 μM, 1.9 μM, 0.75 μM, 2.5 μM, 0.3 μM和1.1 μM。在细胞水平, BGJ398 抑制FGFR1-, FGFR2-Q, 和FGFR3-依赖的BaF3 细胞增殖，IC50分别为2.9 μM, 2.0μM和2 μM。BGJ398在特定酪氨酸残基，包括FGFR-WT, FGFR2-WT, FGFR3-K650E, FGFR3-S249C 和 FGFR4-WT处，干扰自磷酸化，IC50分别为4.6 nM, 4.9 nM, 5 nM, 5 nM 和168 nM。BGJ398 抑制过量表达野生型(WT)FGFR3的癌细胞，如RT112, RT4, SW780 和JMSU1 的增殖，IC50分别为5 nM, 30 nM, 32 nM 和15 nM。 |
| 体内研究 | BGJ398按10和30 mg/kg剂量, 分别处理原位移植膀胱癌模型，持续12天，则抑制肿瘤生长，和引起淤血。BGJ398按10 mg/kg剂量处理实验动物，体重没有改变，按30 mg/kg剂量处理，则体重增加10%。BGJ398磷酸盐按 4.25和8.51 mg/kg剂量口服处理给药携带RT112肿瘤的雌性Rowett大鼠。BGJ398显著降低 pFRS2 和pMAPK水平，这种作用存在剂量依赖性。BGJ398显著抑制bFGF刺激的血管生成，这种作用存在剂量依赖性。然而, BGJ398不损害VEGF诱导的血管形成 |