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.