QUALITÀ & PUREZZAMoligand™?Moligand™ — Aladdin's line of ligands and bioactive small molecules. Use for receptor, pathway, and binding studies needing defined small-molecule tools.≥98%
Moligand™,≥98% Moligand™ per flussi di lavoro cromatografici e analitici sensibili che richiedono un'interferenza minima della linea di base.
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Stoccaggio e spedizione
Protected from light,Store at -20°C,Argon charged Spedizione Ice chest + Ice pads. Consultare il COA specifico del lotto per le specifiche esatte.
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Documenti di qualità
SDS, COA, scheda tecnica e scheda delle specifiche disponibili per il download. COA specifico del lotto accessibile tramite ricerca per numero di lotto.
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Prova documentale
Citato in 0 pubblicazioni peer-reviewed su cromatografia, sintesi organica e reazioni di accoppiamento incrociato.
Panoramica
EHT 1610 is a potent inhibitor of DYRK , with IC 50 s of 0.36 nM ( DYRK1A ), 0.59 nM ( DYRK1B ), respectively. EHT 1610 exhibits antileukemia effect, regulates cell cycle and induces cell apoptosis.
In Vitro
EHT 1610 induces apoptosis of primary ALL cells that were resistant to cytarabine. EHT 1610 dose-dependently induces apoptosis in B- and T-cell lines and primary human pediatric. EHT 1610 (; 72 h) inhibits DYRK1A, results loss of DYRK1A-mediated FOXO1 and STAT3 signaling, leading to preferential cell death in leukemic B cells. EHT 1610 (2.5-10 μM; 4-5 h) inhibits phosphorylation of FOXO1, STAT3 and cyclin D3, thus regulates late cell-cycle progression, mitochondrial ROS and DNA damage, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: MHH-CALL-4 cells Concentration: 0, 2.5, 5, 10 μM Incubation Time: 4, 5 hours Result: Reduced p-cyclin D3 (Thr283), and p-FOXO1 protein level in a dose-dependent manner.
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Xenograft models of B-ALL in mice (12-14 weeks old)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.
EHT 1610 is a potent inhibitor of DYRK , with IC 50 s of 0.36 nM ( DYRK1A ), 0.59 nM ( DYRK1B ), respectively. EHT 1610 exhibits antileukemia effect, regulates cell cycle and induces cell apoptosis- .
Condizioni di conservazione di stoccaggio
Protected from light,Store at -20°C,Argon charged
Spedito in
Ice chest + Ice pads
Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.
This compound belongs to the class of organic compounds known as quinazolinamines. These are heterocyclic aromatic compounds containing a quianazoline moiety substituted by one or more amine groups.
External Descriptors
Not available
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.
Certificati (CoA, COO, BSE/TSE e tabella di analisi)
C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:
Proprietà chimiche e fisiche
Solubilità
DMSO : 5 mg/mL (13.04 mM; Need ultrasonic)
Peso molecolare
383.400 g/mol
XLogP3
4.200
Hydrogen Bond Donor Count
2
Hydrogen Bond Acceptor Count
9
Rotatable Bond Count
5
Exact Mass
383.085 Da
Monoisotopic Mass
383.085 Da
Topological Polar Surface Area
121.000 Ų
Heavy Atom Count
27
Formal Charge
0
Complexity
544.000
Isotope Atom Count
0
Defined Atom Stereocenter Count
0
Undefined Atom Stereocenter Count
0
Defined Bond Stereocenter Count
0
Undefined Bond Stereocenter Count
0
The total count of all stereochemical bonds
0
Covalently-Bonded Unit Count
1
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Recensioni
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