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EHT 1610

Cat. No. M14888
EHT 1610 Structure
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Biological Activity

EHT 1610 is a strong inhibitor of DYRK’s family kinases, with IC50s of 0.36, 0.59 nM for DYRK1A and DYRK1B, respectively.

<span style='color:#ff0000;'><strong>*The compound is unstable in solutions, freshly prepared is recommended</strong></span>


Chemical Information
Molecular Weight 383.4
CAS Number 1425945-60-3
Solubility (25°C) DMSO 5 mg/mL
Storage -20°C, protect from light, sealed
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] Apirat Chaikuad, et al. An Unusual Binding Model of the Methyl 9-Anilinothiazolo[5,4-f] quinazoline-2-carbimidates (EHT 1610 and EHT 5372) Confers High Selectivity for Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases

[2] Alicia Foucourt, et al. Design and synthesis of thiazolo[5,4-f]quinazolines as DYRK1A inhibitors, part II

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