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ARQ 621

Names

[ CAS No. ]:
1095253-39-6

[ Name ]:
ARQ 621

[Synonym ]:
Benzamide, N-(3-aminopropyl)-3-chloro-N-[(1R)-1-[7-chloro-3,4-dihydro-4-oxo-3-(phenylamino)-2-quinazolinyl]-3-butyn-1-yl]-2-fluoro-
N-(3-amino-propyl)-3-chloro-N-[(R)-1-(7-chloro-4-oxo-3-phenylamino-3,4-dihydro-quinazolin-2-yl)-but-3-ynyl]-2-fluoro-benzamide
ARQ-621
(R)-N-(3-aminopropyl)-3-chloro-N-(1-(7-chloro-4-oxo-3-(phenylamino)-3,4-dihydroquinazolin-2-yl)but-3-ynyl)-2-fluorobenzamide
N-(3-Aminopropyl)-N-[(1R)-1-(3-anilino-7-chloro-4-oxo-3,4-dihydro-2-quinazolinyl)-3-butyn-1-yl]-3-chloro-2-fluorobenzamide
ARQ 621

Biological Activity

[Description]:

ARQ 621 is an allosteric, potent and selective inhibitor of Eg5, a microtubule-based ATPase motor protein involved in cell division. Anti-tumor activity[1]. ARQ 621 is a kinesin inhibitor[2].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Cell Cycle/DNA Damage >> Kinesin
Signaling Pathways >> Cytoskeleton >> Kinesin

[Target]

Eg5


[In Vitro]

Over-expression of Eg5 causes genomic instability and tumor formation in mice; therefore, Eg5 is a potential anti-cancer target[1].

[References]

[1]. L. C. Chen, et al. First-in-human study with ARQ 621, a novel inhibitor of Eg5: Final results from the solid tumors cohort.J Clin Oncol. 2011, May (20): 3076-3076.

[2]. Lindsay S Roberts, et al. Mapping Novel Metabolic Nodes Targeted by Anti-Cancer Drugs that Impair Triple-Negative Breast Cancer Pathogenicity. ACS Chem Biol. 2017 Apr 21;12(4):1133-1140.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
730.6±70.0 °C at 760 mmHg

[ Molecular Formula ]:
C28H24Cl2FN5O2

[ Molecular Weight ]:
552.427

[ Flash Point ]:
395.7±35.7 °C

[ Exact Mass ]:
551.129089

[ PSA ]:
93.25000

[ LogP ]:
4.18

[ Vapour Pressure ]:
0.0±2.4 mmHg at 25°C

[ Index of Refraction ]:
1.638

[ Storage condition ]:
-20℃


Related Compounds

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