EHT-1610
EHT-1610 is a potent and selective DYRK1A inhibitor. DYRK1B (also called Mirk for minibrain-related kinase) is potentially an attractive cancer target that is highly expressed in quiescent cancer cells while it is expressed at very low levels in normal tissue. It has been hypothesized that pharmacological DYRK1B inhibition would enable cancer cells to escape from quiescence, triggering apoptosis, and resensitize cancer cells to conventional chemotherapeutic agents.
1: Chaikuad A, Diharce J, Schröder M, Foucourt A, Leblond B, Casagrande AS, Desire L, Bonnet P, Knapp S, Besson T. 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. J Med Chem. 2016 Oct 21. [Epub ahead of print] PubMed PMID: 27766861.
2: Coutadeur S, Benyamine H, Delalonde L, de Oliveira C, Leblond B, Foucourt A, Besson T, Casagrande AS, Taverne T, Girard A, Pando MP, Désiré L. A novel DYRK1A (dual specificity tyrosine phosphorylation-regulated kinase 1A) inhibitor for the treatment of Alzheimer's disease: effect on Tau and amyloid pathologies in vitro. J Neurochem. 2015 May;133(3):440-51. doi: 10.1111/jnc.13018. PubMed PMID: 25556849.
3: Foucourt A, Hédou D, Dubouilh-Benard C, Girard A, Taverne T, Casagrande AS, Désiré L, Leblond B, Besson T. Design and synthesis of thiazolo[5,4-f]quinazolines as DYRK1A inhibitors, part II. Molecules. 2014 Sep 26;19(10):15411-39. doi: 10.3390/molecules191015411. PubMed PMID: 25264830.
2: Coutadeur S, Benyamine H, Delalonde L, de Oliveira C, Leblond B, Foucourt A, Besson T, Casagrande AS, Taverne T, Girard A, Pando MP, Désiré L. A novel DYRK1A (dual specificity tyrosine phosphorylation-regulated kinase 1A) inhibitor for the treatment of Alzheimer's disease: effect on Tau and amyloid pathologies in vitro. J Neurochem. 2015 May;133(3):440-51. doi: 10.1111/jnc.13018. PubMed PMID: 25556849.
3: Foucourt A, Hédou D, Dubouilh-Benard C, Girard A, Taverne T, Casagrande AS, Désiré L, Leblond B, Besson T. Design and synthesis of thiazolo[5,4-f]quinazolines as DYRK1A inhibitors, part II. Molecules. 2014 Sep 26;19(10):15411-39. doi: 10.3390/molecules191015411. PubMed PMID: 25264830.
| Chemical | |
|---|---|
| CAS Num | 1425945-60-3 |
| Chemical Formula | C18H14FN5O2S |
| Molecular Weight | 383.4014 |
| IUPAC Chemical Name | methyl 9-((2-fluoro-4-methoxyphenyl)amino)thiazolo[5,4-f]quinazoline-2-carbimidate |
| Exact Mass | 383.0852 |
| Elemental Analysis | C, 56.39; H, 3.68; F, 4.96; N, 18.27; O, 8.35; S, 8.36 |
| Synonym | EHT-1610; EHT 1610; EHT1610. |
| Solubility | Soluble in DMSO |
| SMILES Code | N=C(C(S1)=NC2=C1C3=C(NC4=CC=C(OC)C=C4F)N=CN=C3C=C2)OC |
| Biological | |
| Targets and Effects | N/A |
| Pathways | Apoptosis |
| Physical | |
| Appearance | Solid powder |
| Purity | >98% (or refer to the Certificate of Analysis) |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| Storage Condition | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Shelf Life | >2 years if stored properly |
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