1. MAPK/ERK Pathway
    Stem Cell/Wnt
  2. ERK
  3. ERK5-IN-2

ERK5-IN-2 

Cat. No.: HY-128341
Handling Instructions

ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively. ERK5-IN-2 does not interact with the BRD4 bromodomain. ERK5-IN-2 suppresses both tumor xenograft growth and basic fibroblast growth factor (bFGF) driven Matrigel plug angiogenesis.

For research use only. We do not sell to patients.

ERK5-IN-2 Chemical Structure

ERK5-IN-2 Chemical Structure

CAS No. : 1888305-96-1

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Description

ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively. ERK5-IN-2 does not interact with the BRD4 bromodomain. ERK5-IN-2 suppresses both tumor xenograft growth and basic fibroblast growth factor (bFGF) driven Matrigel plug angiogenesis[1].

IC50 & Target[1]

ERK5

0.82 μM (IC50)

ERK5 MEF2D

3 μM (IC50)

In Vivo

ERK5-IN-2 (compound 46) (p.o.; 100 mg/kg; CD1 mice for 7 days and CD1 nude (nu/nu) mice for 10 days) has an anti-angiogenic effect and low concentrations of haemoglobin[1].
ERK5-IN-2 (i.v. or p.o.; 10 mg/kg for 0.083-24 hours) exhibits low intrinsic clearance and has high flux and a low efflux ratio (ER) in a caco-2 cell permeability assay in both human and mouse[1].

Animal Model: Female CD1 mice (8-10 weeks old) with Matrigel inoculation and female CD1 nude (nu/nu) mice (8-10 weeks old) bearing A2780 human ovarian carcinoma xenografts[1]
Dosage: 100 mg/kg
Administration: P.o.; twice-daily; CD1 mice for 7 days and CD1 nude (nu/nu) mice for 10 days
Result: Tumor volumes were significantly reduced.
Animal Model: Female CD1 mice at 8-10 weeks of age[1]
Dosage: 10 mg/kg
Administration: I.v. or p.o.; 0.083-24 hours
Result: The terminal plasma half-life was 38 min, with a plasma clearance of 27 mL/min/kg, and oral bioavailability of 68%.
Molecular Weight

388.19

Formula

C₁₇H₁₁BrFN₃O₂

CAS No.

1888305-96-1

SMILES

FC1=CC=CC(Br)=C1C(C2=CNC(C(NC3=CC=CN=C3)=O)=C2)=O

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Please store the product under the recommended conditions in the Certificate of Analysis.

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ERK5-IN-2
Cat. No.:
HY-128341
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