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MedKoo Cat#: 526966 | Name: EHT-5372

Description:

WARNING: This product is for research use only, not for human or veterinary use.

EHT-5372 is a potent and selective DYRK1A inhibitor (IC50 = 0.22 nM). EHT-5372 shows high degree of selectivity over 339 kinases. EHT 5372 inhibits DYRK1A-induced Tau phosphorylation at multiple AD-relevant sites in biochemical and cellular assays. EHT 5372 also normalizes both Aβ-induced Tau phosphorylation and DYRK1A-stimulated Aβ production. EHT 5372 inhibits DYRK1A-induced Tau phosphorylation, Aβ production and Aβ effects on phospho-Tau, including Tau aggregation.

Chemical Structure

EHT-5372
EHT-5372
CAS#1425945-63-6

Theoretical Analysis

MedKoo Cat#: 526966

Name: EHT-5372

CAS#: 1425945-63-6

Chemical Formula: C17H11Cl2N5OS

Exact Mass: 403.0061

Molecular Weight: 404.27

Elemental Analysis: C, 50.51; H, 2.74; Cl, 17.54; N, 17.32; O, 3.96; S, 7.93

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
No Data
Synonym
EHT-5372; EHT 5372; EHT5372.
IUPAC/Chemical Name
methyl 9-((2,4-dichlorophenyl)amino)thiazolo[5,4-f]quinazoline-2-carbimidate
InChi Key
QSGKPYRFWJINEH-UHFFFAOYSA-N
InChi Code
InChI=1S/C17H11Cl2N5OS/c1-25-15(20)17-24-12-5-4-11-13(14(12)26-17)16(22-7-21-11)23-10-3-2-8(18)6-9(10)19/h2-7,20H,1H3,(H,21,22,23)
SMILES Code
N=C(C(S1)=NC2=C1C3=C(NC4=CC=C(Cl)C=C4Cl)N=CN=C3C=C2)OC
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).
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
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 404.27 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.

Recalculate based on batch purity %
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.