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A 484954

Cat. No. M6368
A 484954 Structure
Size Price Availability
10mg USD 200  USD200 1-2 Weeks
25mg USD 400  USD400 1-2 Weeks
50mg USD 600  USD600 1-2 Weeks
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Quality Control & Documentation
Biological Activity

A 484954 is a inhibitor of eukaryotic elongation factor-2 (eEF-2) kinase (IC50 = 0.28 μM in enzymatic assay). Reduces eEF-2 phosphorylation with little effect on cancer cell growth.

Chemical Information
Molecular Weight 289.29
Formula C13H15N5O3
CAS Number 142557-61-7
Form Solid
Solubility (25°C) DMSO 2.89 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Qiantao Wang, et al. Using docking and alchemical free energy approach to determine the binding mechanism of eEF2K inhibitors and prioritizing the compound synthesis

[2] Crhistian L Bender, et al. NH125 reduces the level of CPEB3, an RNA binding protein, to promote synaptic GluA2 expression

[3] Satoshi Kameshima, et al. Eukaryotic elongation factor 2 kinase mediates monocrotaline-induced pulmonary arterial hypertension via reactive oxygen species-dependent vascular remodeling

[4] T Usui, et al. Eukaryotic elongation factor 2 kinase controls proliferation and migration of vascular smooth muscle cells

[5] Zehan Chen, et al. 1-Benzyl-3-cetyl-2-methylimidazolium iodide (NH125) induces phosphorylation of eukaryotic elongation factor-2 (eEF2): a cautionary note on the anticancer mechanism of an eEF2 kinase inhibitor

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  Catalog
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