ERK5-IN-2

SKU: orb1220762

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.

Research Area

Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1888305-96-1
• MW: 388.19
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₁BrFN₃O₂
• SMILES: Fc1cccc(Br)c1C(=O)c1c[nH]c(c1)C(=O)Nc1cccnc1
• Target: ERK
• Solubility: In Vitro: DMSO : 250 mg/mL (644.01 mM)

Bioactivity

• In Vivo:
  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. 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. 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%.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

ERK