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.
Product information
CAS Number: 1888305-96-1
Molecular Weight: 388.19
Formula: C17H11BrFN3O2
Chemical Name: 4-(2-bromo-6-fluorobenzoyl)-N-(pyridin-3-yl)-1H-pyrrole-2-carboxamide
Smiles: O=C(C1C(F)=CC=CC=1Br)C1C=C(NC=1)C(=O)NC1C=NC=CC=1
InChiKey: ATKCERYALDNMPL-UHFFFAOYSA-N
InChi: InChI=1S/C17H11BrFN3O2/c18-12-4-1-5-13(19)15(12)16(23)10-7-14(21-8-10)17(24)22-11-3-2-6-20-9-11/h1-9,21H,(H,22,24)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 250 mg/mL (644.01 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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. 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.
Products are for research use only. Not for human use.
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