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XMD17-109ERK-5 inhibitor

XMD17-109

Catalog No. A3942
Size Price Stock Qty
10mM (in 1mL DMSO) $197.00 In stock
5mg $105.00 In stock
25mg $335.00 In stock
100mg $699.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

XMD17-109

Biological Activity

Description XMD17-109 is a novel, specific inhibitor of ERK-5 with an EC50 value of 4.2 μM in HEK293 cells.
Targets ERK-5          
IC50 4.2±0.69 μM(EC50, in HEK 293 cells)          

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Chemical Properties

Cas No. 1435488-37-1 SDF Download SDF
Synonyms XMD17 109
Canonical SMILES CN1CCN(C2CCN(C(C3=CC(OCC)=C(NC4=NC=C5C(N(C6CCCC6)C(C=CC=C7)=C7C(N5C)=O)=N4)C=C3)=O)CC2)CC1
Formula C36H46N8O3 M.Wt 638.8
Solubility >32mg/mL in DMSO Storage Store at -20°C
General tips N/A
Shipping Condition N/A

Background

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.[1]

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%.

Reference:
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.