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ERK5-IN-2 是具有口服活性,亚微摩尔效力,选择性ERK5抑制剂,对ERK5和ERK5 MEF2D 的IC50s 分别是 0.82 和 3 μM。它抑制肿瘤异种移植生长和碱性成纤维细胞生长因子驱动的基质胶塞血管生成。


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ERK5-IN-2 是具有口服活性,亚微摩尔效力,选择性ERK5抑制剂,对ERK5和ERK5 MEF2D 的IC50s 分别是 0.82 和 3 μM。它抑制肿瘤异种移植生长和碱性成纤维细胞生长因子驱动的基质胶塞血管生成。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 432 | In stock | |
| 5 mg | ¥ 927 | In stock | |
| 10 mg | ¥ 1,730 | In stock | |
| 25 mg | ¥ 2,980 | In stock | |
| 50 mg | ¥ 4,480 | In stock | |
| 100 mg | ¥ 6,290 | In stock | |
| 200 mg | ¥ 8,490 | In stock | |
| 1 mL x 10 mM (in DMSO) | ¥ 849 | In stock |
ERK5-IN-2 相关产品
| 产品描述 | ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively. |
| 靶点活性 | ERK5 MEF2D:3 μM, ERK5:0.82 μM |
| 体内活性 | ERK5-IN-2(口服;100mg/kg;CD1小鼠服用7天及CD1裸鼠(nu/nu)服用10天)显示出抗血管生成效应并降低血红蛋白浓度。ERK5-IN-2(静脉注射或口服;10mg/kg,持续0.083-24小时)在人类和小鼠的caco-2细胞渗透性实验中表现出低内在清除率、高通量以及低外排比率(ER)。 |
| 分子量 | 388.19 |
| 分子式 | C17H11BrFN3O2 |
| CAS No. | 1888305-96-1 |
| Smiles | Fc1cccc(Br)c1C(=O)c1c[nH]c(c1)C(=O)Nc1cccnc1 |
| 密度 | 1.628 g/cm3 (Predicted) |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| 溶解度信息 | DMSO: 10 mg/mL (25.76 mM), Sonication is recommended. | |||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.58 mM), Sonication is recommended. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 | |||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||
DMSO
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