| Identification | Back Directory | [Name]
EHT 5372 | [CAS]
1425945-60-3 | [Synonyms]
EHT1610
CS-2911
EHT 5372
Methyl 9-((2-fluoro-4-methoxyphenyl)amino)thiazolo[5,4-f]quinazoline-2-carbimidate
methyl 9-[(2-fluoro-4-methoxyphenyl)amino]-[1,3]thiazolo[5,4-f]quinazoline-2-carboximidate
Thiazolo[5,4-f]quinazoline-2-carboximidic acid, 9-[(2-fluoro-4-methoxyphenyl)amino]-, methyl ester | [Molecular Formula]
C18H14FN5O2S | [MOL File]
1425945-60-3.mol | [Molecular Weight]
383.4 |
| Chemical Properties | Back Directory | [Boiling point ]
507.8±60.0 °C(Predicted) | [density ]
1.51±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C,unstable in solution, ready to use. | [solubility ]
DMSO: 25 mg/mL (65.21 mM); Water: < 0.1 mg/mL (insoluble) | [form ]
Solid | [pka]
3.84±0.50(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
EHT 1610 is a potent inhibitor of DYRK, with IC50s of 0.36 nM (DYRK1A), 0.59 nM (DYRK1B), respectively. EHT 1610 exhibits antileukemia effect, regulates cell cycle and induces cell apoptosis[1]-[4]. | [in vivo]
EHT 1610 (20 mg/kg/d; i.p.; twice a day; 3 weeks) shows antileukemia activity against in leukemic aggressive model in mice[3].
| Animal Model: | Xenograft models of B-ALL in mice (12-14 weeks old)[3] | | Dosage: | 20 mg/kg | | Administration: | Intraperitoneal injection; twice a day, 5 days on, 2 days off; 3 weeks | | Result: | Reduced leukemic burden by approximately 8% and conferred a modest survival advantage.
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| [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): DOI:10.1021/acs.jmedchem.6b01083
[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. DOI:10.1172/JCI135937
[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. DOI:10.3390/molecules191015411 |
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Cckinase, Inc.
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+1 (732)236-3202 |
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www.cckinase.com |
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cjbscvictory
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13348960310 13348960310 |
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https://www.weikeqi-biotech.com/ |
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InvivoChem
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13549236410 |
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https://www.invivochem.cn/ |
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