| Bioactivity | R406 free base is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a Ki of 30 nM, potently inhibits Syk kinase activity in vitro with an IC50 of 41 nM, measured at an ATP concentration corresponding to its Km value. R406 free base reduces immune complex-mediated inflammation[1]. R406 free base also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM)[2]. | ||||||||||||
| Invitro | R406 inhibits adenosine A3 receptor (IC50=0.081 µM), adenosine transporter (IC50=1.84 µM), and monoamine transporter (IC50=2.74 µM)[1].R406 inhibits Huh7 hepatocyte, A549 epithelial, and H1299 lung cancer lines with EC50s of 15.1, 2.9 and 6.3 µM, respectively[1].R406 inhibits phosphorylation of Syk substrate LAT in mast cells and BLNK/SLP65 in B cells[1]. Western Blot Analysis[1] Cell Line: | ||||||||||||
| Name | R406 free base | ||||||||||||
| CAS | 841290-80-0 | ||||||||||||
| Formula | C22H23FN6O5 | ||||||||||||
| Molar Mass | 470.45 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|