1888305-96-1
1888305-96-1 structure
- Name: ERK5-IN-2
- Chemical Name: ERK5-IN-2
- CAS Number: 1888305-96-1
- Molecular Formula: C17H11BrFN3O2
- Molecular Weight: 388.19
- Catalog: Signaling Pathways MAPK/ERK Pathway ERK
- Create Date: 2019-08-04 10:56:58
- Modify Date: 2024-01-09 17:20:55
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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].
| Name | ERK5-IN-2 |
|---|
| 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]. |
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| Related Catalog | |
| Target |
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%. |
| References |
| Molecular Formula | C17H11BrFN3O2 |
|---|---|
| Molecular Weight | 388.19 |