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ERK5-IN-2

Cat. No. M9688
ERK5-IN-2 Structure
Size Price Availability
10mg USD 248  USD248 4-7 Days
25mg USD 496  USD496 4-7 Days
50mg USD 843  USD843 4-7 Days
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Quality Control
  • Current batch:
  • Purity >98.5%
  • COA
  • MSDS
Biological Activity

ERK5-IN-2 is a selective, orally active, sub-micromolar 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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 388.19
Formula C17H11BrFN3O2
CAS Number 1888305-96-1
Purity >98.5%
Solubility DMSO ≥ 100 mg/mL
Storage 2-8°C, protect from light, dry, sealed
References

[1] Stephanie M Myers, et al. Eur J Med Chem. Identification of a novel orally bioavailable ERK5 inhibitor with selectivity over p38α and BRD4

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: ERK5-IN-2 supplier, ERK, inhibitors

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