R-116010

Names

[ Name ]:
R-116010

[Synonym ]:
1,2-Benzenediamine, N1-2-benzothiazolyl-4-[(1S)-1-(1H-imidazol-1-yl)propyl]-N2,N2-dimethyl-
N1-(1,3-Benzothiazol-2-yl)-4-[(1S)-1-(1H-imidazol-1-yl)propyl]-N2,N2-dimethyl-1,2-benzenediamine

Biological Activity

[Description]:

A potent CYP26A1 inhibitor with IC50 of 10 nM, potently inhibits all-trans-retinoic acid metabolism in intact T47D cells with IC50 of 8.7 nM; enhances the ATRA-mediated antiproliferative activity in a concentration-dependent manner, significantly inhibits the growth of murine oestrogen-independent TA3-Ha mammary tumour in vivo.

[References]

References 1. Thatcher JE, et al. Mol Pharmacol. 2011 Aug;80(2):228-39. 2. Van Heusden J, et al. Br J Cancer. 2002 Feb 12;86(4):605-11. View Related Products by Target Cytochrome P450 (CYPs)

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
569.7±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₁H₂₃N₅S

[ Molecular Weight ]:
377.506

[ Flash Point ]:
298.4±32.9 °C

[ Exact Mass ]:
377.167419

[ LogP ]:
4.19

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

[ Index of Refraction ]:
1.669

Related Compounds

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