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| 5mg |
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| 25mg |
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Purity: ≥98%
EHT-1610 is a novel, potent and selective DYRK kinase inhibitor with IC50s of 0.22, 0.28 nM for DYRK1A and DYRK1B, respectively. DYRK1B, also called minibrain-related kinase (Mirk) is a protein that is highly expressed in quiescent cancer cells but expressed at very low levels in normal tissue, making it a potentially appealing cancer target.
| Targets |
DYRK1B; DYRK1A
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|---|---|
| ln Vitro |
Arabinoblast batches can be assembled by primary ALL cells induced by EHT 1610 [2]. In primary human pediatric cells and B and T cell lines, EHT 1610 dose-sensitively induces Frankfurt [2]. B cells are specifically killed when 1610 (72 hours) suppresses DYRK1A, which causes the loss of DYRK1A-mediated FOXO1 and STAT3 signaling [3]. EHT 1610 (2.5-10 μM; 4-5 hours) inhibits the phosphorylation of cyclin D3, STAT3, and FOXO1, consequently controlling DNA damage, mitochondrial ROS, and late cell cycle progression, in that order [3].
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| Cell Assay |
Western Blot analysis[3]
Cell Types: MHH-CALL-4 cells Tested Concentrations: 0, 2.5, 5, 10 μM Incubation Duration: 4, 5 hrs (hours) Experimental Results: p-cyclin D3 (Thr283) and p-FOXO1 protein levels were dose-dependent diminished sexual behavior. |
| Animal Protocol |
Animal/Disease Models: Mouse B-ALL xenograft model (12-14 weeks old) [3]
Doses: 20 mg/kg Route of Administration: intraperitoneal (ip) injection; twice a day for 5 days, 2 days off; 3-week Experimental Results: The leukemia burden is diminished by about 8% and has a certain survival advantage. |
| References |
[1]. Chaikuad A, 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. J Med Chem. 2016 Nov 23;59(22):10315-10321.
[2]. Thompson B J, et al. The Chromosome 21 Kinase DYRK1A Controls Cell Cycle Exit and Survival During Lymphoid Development and Is a Novel Therapeutic Target In Acute Lymphoblastic Leukemia[C]// Ash Meeting & Exposition. 2013. l [3]. Bhansali RS, et al. DYRK1A regulates B cell acute lymphoblastic leukemia through phosphorylation of FOXO1 and STAT3. J Clin Invest. 2021 Jan 4;131(1):e135937. [4]. Foucourt A, et al. Design and synthesis of thiazolo[5,4-f]quinazolines as DYRK1A inhibitors, part II. Molecules. 2014 Sep 26;19(10):15411-39. |
| Molecular Formula |
C18H14FN5O2S
|
|---|---|
| Molecular Weight |
383.399465084076
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| Exact Mass |
383.09
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| Elemental Analysis |
C, 56.39; H, 3.68; F, 4.96; N, 18.27; O, 8.35; S, 8.36
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| CAS # |
1425945-60-3
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| Related CAS # |
1425945-60-3
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| Appearance |
Solid powder
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| SMILES |
COC1=CC(=C(C=C1)NC2=NC=NC3=C2C4=C(C=C3)N=C(S4)C(=N)OC)F
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| InChi Key |
RYBNARZBIXTFJS-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
methyl 9-(2-fluoro-4-methoxyanilino)-[1,3]thiazolo[5,4-f]quinazoline-2-carboximidate
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| Synonyms |
EHT-1610; EHT1610; EHT 1610; EHT 5372; EHT-5372; EHT5372
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| HS Tariff Code |
2934.99.03.00
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~5 mg/mL (~13.0 mM)
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|---|
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6082 mL | 13.0412 mL | 26.0824 mL | |
| 5 mM | 0.5216 mL | 2.6082 mL | 5.2165 mL | |
| 10 mM | 0.2608 mL | 1.3041 mL | 2.6082 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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