CAS NO.：1888305-96-1 Product Name：Erk5-IN-2 Synonyms：ERK5-IN-2;4-(2-bromanyl-6-fluoranyl-phenyl)carbonyl-~{N}-pyridin-3-yl-1~{H}-pyrrole-2-carboxamide;4-(2-Bromo-6-fluorobenzoyl)-N-(pyridin-3-yl)-1H-pyrrole-2-carboxamide;9N8 EINEC: Molecular Formula：C17H11BRFN3O2 Molecular Weight：388.1905
Target:
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%.
In Vitro
Kinase Assay
Cell Assay
Animal Administration
References
[1]. Myers SM, et al. Identification of a novel orally bioavailable ERK5 inhibitor with selectivity over p38α and BRD4. Eur J Med Chem. 2019 May 25;178:530-543.
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