MU 380

Names

[ Name ]:
MU 380

[Synonym ]:
Pyrazolo[1,5-a]pyrimidin-7-amine, 6-bromo-5-[(3R)-3-piperidinyl]-3-[1-(trifluoromethyl)-1H-pyrazol-4-yl]-
6-Bromo-5-[(3R)-3-piperidinyl]-3-[1-(trifluoromethyl)-1H-pyrazol-4-yl]pyrazolo[1,5-a]pyrimidin-7-amine

Biological Activity

[Description]:

A novel potent, selective CHK1 inhibitor 2 nM, >80-fold selectivity over CHK2; sensitizes a variety of tumor cell lines to hydroxyurea or gemcitabine up to 10 times; shows extended inhibitory effects in cells, and unlike SCH900776, does not undergo in vivo N-dealkylation to the significantly less selective metabolite; causes higher accumulation of DNA damage in tumor cells and subsequent enhanced cell death, and is more efficacious in the A2780 xenograft mouse model.

[References]

References 1. Samadder P, et al. Mol Cancer Ther. 2017 Sep;16(9):1831-1842. View Related Products by Target Checkpoint Kinase (Chk)

Chemical & Physical Properties

[ Density]:
1.9±0.1 g/cm3

[ Molecular Formula ]:
C₁₅H₁₅BrF₃N₇

[ Molecular Weight ]:
430.226

[ Exact Mass ]:
429.052429

[ LogP ]:
1.78

[ Index of Refraction ]:
1.750

Related Compounds

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