Ribociclib

CAT#: H205513

CAS#: 1211441-98-3


Description: Ribociclib Free Base, also known as LEE011, is an orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic activity. CDK4/6 inhibitor LEE011 specifically inhibits CDK4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, thereby arresting the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth. Overexpression of CDK4/6, as seen in certain types of cancer, causes cell cycle deregulation.

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Synthetic Routes

Ribociclib - Synthetic Route 1

Ribociclib route01

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Ribociclib - Synthetic Route 2

Ribociclib route02

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Ribociclib - Synthetic Route 3

Ribociclib route03

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Ribociclib - Synthetic Route 4

Ribociclib route04

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Ribociclib - Synthetic Route 5

Ribociclib route05

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Ribociclib - Synthetic Route 6

Ribociclib route06

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Ribociclib - Synthetic Route 7

Ribociclib route07

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Chen, Linghao. Process for synthesis of Ribociclib. Assignee Qingdao Chenda Biotechnology Co., Ltd., Peop. Rep. China. CN 106928236 A (2017).

Ribociclib - Synthetic Route 8

Ribociclib route08

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Sokhi, Sarbjot Singh; Singh, Govind; Lahiri, Saswata; Pandey, Maneesh Kumar; Tiwari, Raj Narayan; Shukla, Sonu; Musmade, Sachin; Dua, Heena; Cabri, Walter. An improved process for the preparation of Ribociclib and its salts. Assignee Fresenius Kabi Oncology Ltd., India. WO 2019082143 A1 (2019).

Ribociclib - Synthetic Route 9

Ribociclib route09

Synthetic reference

Wu, Ke; He, Wei; Peng, Lei; Wang, Longlin; Jiang, Guangding; Yang, Fan. Method for preparing Ribociclib. Assignee Chongqing Sansheng Industrial Co., Ltd., Peop. Rep. China. CN 109400612 A. (2019).

Ribociclib - Synthetic Route 10

Ribociclib route010

Synthetic reference

Song, Lei. Method for rapidly synthesizing Ribociclib. Assignee Southwest University for Nationalities, Peop. Rep. China. CN 108623599 A. (2018).