ERK5-IN-2

Modify Date: 2024-01-09 17:20:55

ERK5-IN-2 structure	Common Name	ERK5-IN-2
	CAS Number	1888305-96-1	Molecular Weight	388.19
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₁₇H₁₁BrFN₃O₂	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of ERK5-IN-2

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].
Related Catalog	Research Areas >> Cancer Research Areas >> Cardiovascular Disease Signaling Pathways >> MAPK/ERK Pathway >> ERK Signaling Pathways >> Stem Cell/Wnt >> ERK
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	[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.

Molecular Formula	C₁₇H₁₁BrFN₃O₂
Molecular Weight	388.19

DC Chemicals Limited
China
Product Name: ERK5-IN-2
Price: $600.0/100mg $1100.0/250mg $2200.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

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