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EHT 1864 2HCl

Cat. No. M6704
EHT 1864 2HCl Structure
Size Price Availability Quantity
10mg USD 126  USD140 In stock
50mg USD 522  USD580 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

EHT 1864 is a inhibitor of Rac family GTPases. Blocks activation by direct binding to Rac1, Rac1b, Rac2 and Rac3 (KD values are 40, 50, 60 and 250 nM respectively). Inhibits Rac, Ras and Tiam-induced growth transformation of NIH-3T3 fibroblasts. Reduces β-amyloid peptide production in vivo.

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 581.47
Formula C25H27F3N2O4S.2HCl
CAS Number 754240-09-0
Purity >99%
Solubility Water ≥ 90 mg/mL
DMSO ≥ 30 mg/mL
Storage at -20°C
References

Plumbagin (5-hydroxy-2-methyl-1,4-napthoquinone) induces apoptosis and cell cycle arrest in A549 cells through p53 accumulation via c-Jun NH2-terminal kinase mediated phosphorylation at serine 15 in vitro and in vivo.
Hsu, et al. J Pharmacol Exp Ther. 2006;318: 484. PMID: 16632641.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: EHT 1864 2HCl supplier, Ras, inhibitors

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