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Art. -Nr.: HY-124633

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NEU-1953

NEU-1953 is a parasite inhibitor. NEU-1953 inhibits Abl, EGFR, and KDR tyrosine kinases. NEU-1953 inhibits Aurora A, MNK2, and MAP4K4 serine/threonine kinases. NEU-1953 can be used for research on malaria, human African trypanosomiasis, schistosomiasis, Chagas disease, and leishmaniasis.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 2218480-85-2
Formel: C₂₂H₂₂N₈
Molecular Weight:398.47

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

NEU-1953 Chemical Structure

CAS. Nr.: 2218480-85-2

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

Abl

EGFR

KDR

Aurora A

MNK2

MAP4K4

Alle Bcr-Abl Isoform-spezifische Produkte anzeigen :

Abl
Bcr-Abl

Alle EGFR Isoform-spezifische Produkte anzeigen :

Alle VEGFR Isoform-spezifische Produkte anzeigen :

Alle Aurora Kinase Isoform-spezifische Produkte anzeigen :

Alle MNK Isoform-spezifische Produkte anzeigen :

Alle MAP4K Isoform-spezifische Produkte anzeigen :

Alle Parasite Isoform-spezifische Produkte anzeigen :

In Vitro

NEU-1953 (compound 40) is a potent inhibitor of P. falciparum D6 (EC₅₀: 0.026 μM) with low toxicity against HepG2 cells (TC₅₀: >4 μM)^[1].
NEU-1953 (compound 1) (50 μM; 48 h) exhibits moderate anti-trypanosome potency against T. b. brucei strain 427 with an EC₅₀ of 0.43 μM^[2].
NEU-1953 (5 μM) significantly inhibits seven human kinases (Aurora A, MNK2, MAP4K4, EGFR, Abl, and KDR) at 5 μM^[1].
NEU-1953 (compound 3) has 87.0% human plasma protein binding^[3].
NEU-1953 has an intrinsic clearance of 180 μL/min/mg protein in human liver microsomes^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 2218480-85-2
Molecular Weight 398.47
Formel C₂₂H₂₂N₈
SMILES

N=1C=CN=C(C1)NC=2C=CN=C3C=C(C=CC32)C=4C=NC(=NC4)N5CCN(C)CC5
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Mehta N, et al. Optimization of Physicochemical Properties for 4-Anilinoquinoline Inhibitors of Plasmodium falciparum Proliferation. ACS infectious diseases. 2018 Apr 13;4(4):577-591.

[2]. Bachovchin KA, et al. Improvement of Aqueous Solubility of Lapatinib-Derived Analogues: Identification of a Quinolinimine Lead for Human African Trypanosomiasis Drug Development. Journal of medicinal chemistry. 2019 Jan 24;62(2):665-687.

[3]. Buskes MJ, et al. Structure–bioactivity relationships of lapatinib derived analogs against Schistosoma mansoni. ACS Medicinal Chemistry Letters. 2020 Jan 10;11(3):258.

[4]. Singh B, et al. Scaffold and Parasite Hopping: Discovery of New Protozoal Proliferation Inhibitors. ACS medicinal chemistry letters. 2020 Mar 12;11(3):249-257.

[5]. Bachovchin KA. Chemical Modifications for Activity and Property Optimization: Drug Discovery Efforts for Neglected Tropical Diseases (Doctoral dissertation, et al.

[6]. Klug DM. Hit-to-lead optimization of small molecules for neglected tropical disease therapeutics (Doctoral dissertation, et al.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

MOQ

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100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise

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NEU-1953

Alle Bcr-Abl Isoform-spezifische Produkte anzeigen

Alle EGFR Isoform-spezifische Produkte anzeigen

Alle VEGFR Isoform-spezifische Produkte anzeigen

Alle Aurora Kinase Isoform-spezifische Produkte anzeigen

Alle MNK Isoform-spezifische Produkte anzeigen

Alle MAP4K Isoform-spezifische Produkte anzeigen

Alle Parasite Isoform-spezifische Produkte anzeigen