《Design and optimization leading to an orally active TTK protein kinase inhibitor with robust single agent efficacy》 was written by Riggs, Jennifer R.; Elsner, Jan; Cashion, Dan; Robinson, Dale; Tehrani, Lida; Nagy, Mark; Fultz, Kimberly E.; Krishna Narla, Rama; Peng, Xiaohui; Tran, Tam; Kulkarni, Ashutosh; Bahmanyar, Sogole; Condroski, Kevin; Pagarigan, Barbra; Fenalti, Gustavo; LeBrun, Laurie; Leftheris, Katerina; Zhu, Dan; Boylan, John F.. Application of 90213-66-4This research focused ontriple neg breast cancer antitumor TTK protein kinase pharmacokinetics. The article conveys some information:
Triple neg. breast cancer (TNBC) is an aggressive disease with high relapse rates and few treatment options. Outlined in previous publications, we identified a series of potent, dual TTK/CLK2 inhibitors with strong efficacy in TNBC xenograft models. Pharmacokinetic properties and kinome selectivity were optimized, resulting in the identification of a new series of potent, selective, and orally bioavailable TTK inhibitors. We describe here the structure-activity relationship of the 2,4-disubstituted-7H-pyrrolo[2,3-d]pyrimidine series, leading to significant single agent efficacy in a TNBC xenograft model without body weight loss. The design effort evolving an iv-dosed TTK/CLK2 inhibitor to an orally bioavailable TTK inhibitor is described. The results came from multiple reactions, including the reaction of 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4Application of 90213-66-4)
2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4) belongs to pyrimidine. Pyrimidine nucleotide derivatives have a wide range of biological applications. For example, pyrimidine derivatives are useful in DNA repair studies involving cancer and epigenetics. Application of 90213-66-4
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia