Sample solution is provided at 25 µL, 10mM.
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|Description||XMD17-109 is a novel, specific inhibitor of ERK-5 with an EC50 value of 4.2 μM in HEK293 cells.|
|IC50||4.2±0.69 μM(EC50, in HEK 293 cells)|
|Cas No.||1435488-37-1||SDF||Download SDF|
|Solubility||Soluble in DMSO||Storage||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.Stock solution can be stored below -20℃ for several months.|
|Shipping Condition||Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
XMD17-109 is a new inhibitor of ERK5, IC50 value in HeLa cell is 0.09 ± 0.03 μM, and in vitro, Enzymatic IC50 value is 0.162 ± 0.006 μM.
XMD17-109 is capable of inhibiting the ERK5 autophosphorylation in cells.
Through intravenous injection and oral delivery of XMD17-109 in mice, the pharmacokinetic properties of this compound are as bellows: the T1/2 (half time) is 8.2 h, the plasma clearance is 8.64 mL/min/Kg (data of intravenous injection), the AUC (area under the curve) of oral delivery is 15745 h*ng/mL and the oral bioavailability is 90%.
1. Deng, X., et al., Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones. European Journal of Medicinal Chemistry, 2013. 70: p. 758-767.