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Novel bis-ortho-alkoxy-para-piperazinesubstituted-2,4-dianilinopyrimidines (KRCA-0008) as Potent and Selective ALK Inhibitors for Anticancer Treatment

Chi Hoon Park, Hyeonjeong Choe, In-Young Jang, So Yeong Kwon, Muhammad Latif, Heung Kyoung Lee, Hyeon Ji Lee, Eun Hye Yang, Jeong In Yun, Chong Hak Chae, Sung Yun Cho, Sang Un Choi, Jae Du Ha, Heejung Jung, etc.

Bioorg Med Chem Lett. 2013 Nov 15;23(22):6192-6.

PMID: 24095090

Abstract:

The synthesis of bis-ortho-alkoxy-para-piperazinesubstituted-2,4-dianilinopyrimidines is described and their structure-activity-relationship to anaplastic lymphoma kinase (ALK) is presented. KRCA-0008 is selective and potent to ALK and Ack1, and displays drug-like properties without hERG liability. KRCA-0008 demonstrates in vivo efficacy comparable to Crizotinib in xenograft mice model.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP1472795202 KRCA-0008 KRCA-0008 1472795-20-2 Price
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