Synonym
EHT-1610; EHT 1610; EHT1610; EHT5372; EHT 5372; EHT-5372;
IUPAC/Chemical Name
methyl 9-((2-fluoro-4-methoxyphenyl)amino)thiazolo[5,4-f]quinazoline-2-carbimidate
InChi Key
RYBNARZBIXTFJS-UHFFFAOYSA-N
InChi Code
InChI=1S/C18H14FN5O2S/c1-25-9-3-4-11(10(19)7-9)23-17-14-12(21-8-22-17)5-6-13-15(14)27-18(24-13)16(20)26-2/h3-8,20H,1-2H3,(H,21,22,23)
SMILES Code
N=C(C(S1)=NC2=C1C3=C(NC4=CC=C(OC)C=C4F)N=CN=C3C=C2)OC
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).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.03.00
Preparing Stock Solutions
The following data is based on the
product
molecular weight
383.40
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
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.
