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Cat. No.: 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.

For research use only. We do not sell to patients.

CAS No.: 2218480-85-2
Formula: C₂₂H₂₂N₈
Molecular Weight:398.47

Storage:

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

NEU-1953 Chemical Structure

CAS No.: 2218480-85-2

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Use of MCE Products

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

IC₅₀ & Target

^[1]

Abl

EGFR

KDR

Aurora A

MNK2

MAP4K4

All Bcr-Abl Isoforms :

Abl
Bcr-Abl

All EGFR Isoforms :

All VEGFR Isoforms :

All Aurora Kinase Isoforms :

All MNK Isoforms :

All MAP4K Isoforms :

All Parasite Isoforms :

In Vitro

Parasitic InfectionOthers

Parasitic Infection

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].

Others

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 No. 2218480-85-2
Molecular Weight 398.47
Formula C₂₂H₂₂N₈
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[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.

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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.

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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NEU-1953

All Bcr-Abl Isoforms

All EGFR Isoforms

All VEGFR Isoforms

All Aurora Kinase Isoforms

All MNK Isoforms

All MAP4K Isoforms

All Parasite Isoforms