rac-CCT 250863

Names

[ Name ]:
rac-CCT 250863

[Synonym ]:
MFCD30474714
4-(2-Amino-5-{4-[(dimethylamino)methyl]-2-thienyl}-3-pyridinyl)-2-{[(3Z)-5,5,5-trifluoro-3-penten-2-yl]oxy}benzamide
Benzamide, 4-[2-amino-5-[4-[(dimethylamino)methyl]-2-thienyl]-3-pyridinyl]-2-[[(2Z)-4,4,4-trifluoro-1-methyl-2-buten-1-yl]oxy]-

Biological Activity

[Description]:

(Rac)-CCT 250863 (compound rac-21) is a selective and reversible NEK 2 inhibitor with an IC50 of 0.073 µM. (Rac)-CCT 250863 shows good effects of inducing cell cycle arrest and also can antiproliferative in cells (Pomalidomide sensitive/resistant). (Rac)-CCT 250863 induces apoptosis when combines with Pomalidomide[1][2].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

[Target]

IC50: 0.073 µM (NEK 2), 8.0 μΜ (H929), 7.1 μΜ (AMOl), 8.7 μΜ (K12PE)[1][2].

[References]

[1]. Innocenti P, et al. Design of potent and selective hybrid inhibitors of the mitotic kinase Nek2: structure-activity relationship, structural biology, and cellular activity. J Med Chem. 2012 Apr 12;55(7):3228-41.

[2]. Ahsan A, et al. Methods for treating cancer with combination therapies. WO2021262962A1.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
582.9±50.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₄H₂₅F₃N₄O₂S

[ Molecular Weight ]:
490.541

[ Flash Point ]:
306.3±30.1 °C

[ Exact Mass ]:
490.165039

[ LogP ]:
4.42

[ Vapour Pressure ]:
0.0±1.6 mmHg at 25°C

[ Index of Refraction ]:
1.591

Related Compounds

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