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| Cas No.: | 1888305-96-1 |
| Chemical 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 |
| SMILES: | BrC1=C([H])C([H])=C([H])C(=C1C(C1=C([H])N([H])C(C(N([H])C2=C([H])N=C([H])C([H])=C2[H])=O)=C1[H])=O)F |
| Formula: | C17H11BrFN3O2 |
| M.Wt: | 388.1905 |
| Purity: | >98% |
| 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]. |
| 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: | [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. |