2109805-78-7

2109805-78-7 structure

Name: MU 380
Chemical Name: 6-Bromo-5-[(3R)-3-piperidinyl]-3-[1-(trifluoromethyl)-1H-pyrazol-4-yl]pyrazolo[1,5-a]pyrimidin-7-amine
CAS Number: 2109805-78-7
Molecular Formula: C₁₅H₁₅BrF₃N₇
Molecular Weight: 430.226
Create Date: 2020-01-11 07:35:33
Modify Date: 2024-01-06 10:02:03
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.

Name	6-Bromo-5-[(3R)-3-piperidinyl]-3-[1-(trifluoromethyl)-1H-pyrazol-4-yl]pyrazolo[1,5-a]pyrimidin-7-amine
Synonyms	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

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)