生物活性
BIX 02189是选择性双重MEK5和ERK5（或BMK1）激酶抑制剂，对于MEK5，ERK5，TGFbR1和其他紧密相关的激酶，IC50值分别为1.5、59、580和> 6200 nM。
Targets
| Target | Value |
| MEK5 | IC50: 1.5nM |
| ERK5 | IC50: 59nM |
| TGFβR1 | IC50: 580nM |
| MEK1 | IC50: >6.2μM |
| MEK2 | IC50: >6.2μM |
| ERK1 | IC50: >6.2μM |
| JNK2 | IC50: >6.2μM |
| EGFR | IC50: >6.3μM |
| STK16 | IC50: >6.3μM |
化学数据
| 目录号 | A10151 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 440.5 |
| Formula | C27H28N4O2 |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated.
In lyophilized form, the chemical is stable for36 months.
In solution, store at -20ºC and use within3 monthsto prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles. |
| CAS No. | 1094614-85-3 |
| Synonyms | BIX02189, BIX-02189 |
| SMILES | CN(C)CC1=CC(=CC=C1)N/C(=C\2/C3=C(C=C(C=C3)C(=O)N(C)C)NC2=O)/C4=CC=CC=C4 |
溶解度
| In vitro (25°C) | DMSO | Warmed: 56 mg/mL (127.11 mM) |
| Water | Insoluble |
| Ethanol | 75 mg/mL (170.24 mM) |
| In vivo | 2% DMSO+30% PEG 300+5% Tween 80+ddH2O | 9 mg/mL |
*<1 mg/ml means slightly soluble or insoluble.
*Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
储备液配制
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
| 0.1 mM | 22.7 mL | 113.51 mL | 227.01 mL |
| 0.5 mM | 4.54 mL | 22.7 mL | 45.4 mL |
| 1 mM | 2.27 mL | 11.35 mL | 22.7 mL |
| 5 mM | 0.45 mL | 2.27 mL | 4.54 mL |
*The above data is based on the productmolecular weight 440.5 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
