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Medchemexpress LLC ERK5-IN-2 | 1888305-96-1 | 99.0% | 50 MG
Supplier: Medchemexpress LLC HY12834150MG
ERK5-IN-2 is an orally active, selective ERK5 inhibitor (IC50s of 0.82 μM for ERK5 and 3 μM for ERK5 MEF2D) that does not interact with the BRD4 bromodomain. It has been shown to suppress tumor xenograft growth and bFGF-driven angiogenesis. This compound exhibits favorable pharmacokinetic properties including low intrinsic clearance and high oral bioavailability.
- Selective ERK5 inhibitor with sub-micromolar IC50s
- Does not interact with the BRD4 bromodomain
- Suppresses tumor xenograft growth
- Suppresses basic fibroblast growth factor (bFGF) driven angiogenesis
- Exhibits low intrinsic clearance and high flux
- Demonstrates low efflux ratio in caco-2 cell permeability assays
- Significantly reduces tumor volumes in animal models
- Features an oral bioavailability of 68%
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