504433-23-2GW441756

产品属性：

Cas No.504433-23-2

别名

化学名 (3Z)-3-[(1-methylindol-3-yl)methylidene]-1H-pyrrolo[3,2-b]pyridin-2-one

分子式 C17H13N3O

分子量 275.3

溶解度 ≥ 13.75mg/mL in DMSO

储存条件 Store at -20°C
General tips  For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition     Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述：
GW441756 is an inhibitor of TrkA kinase and LRRK2 with IC50 value of 320nM and 2nM, respectively [1].

The activity of TrkA kinase can affect its downstream signaling and involves in many biological processes including proliferation, differentiation and apoptosis. Thereby the inhibitor of TrkA is developed for the treatment of cancers. GW441756 belongs to the oxindole series and is found to be a potent inhibitor of TrkA. It is also selective against TrkA. The IC50 values of it for cRaf1 and CDK2 are above 12μM and 7μM, respectively. In human muscle sarcoma cancer cell line HTB114, treatment of GW441756 dose-dependently suppresses neoplastic proliferation and induces apoptosis [1, 2].

In addition, GW441756 is also found to be an LRRK2 inhibitor. It inhibits the Ser935 phosphorylation of LRRK2 in cellular TR-FRET assay with IC50 value of 2.2μM. It shows no significant cytotoxicity with IC50 value of >20μM [3].