Idelalisib

CAT#: H200586

CAS#: 870281-82-6

Description: Idelalisib, also known as CAL-101, is a PI3K-delta inhibitor with potential immunomodulating and antineoplastic activities. CAL-101 inhibits the production of the second messenger phosphatidylinositol-3,4,5-trisphosphate (PIP3), preventing the activation of the PI3K signaling pathway and thus inhibiting tumor cell proliferation, motility, and survival. Unlike other isoforms of PI3K, PI3K-delta is expressed primarily in hematopoietic lineages. The targeted inhibition of PI3K-delta is designed to preserve PI3K signaling in normal, non-neoplastic cells. CAL-101 has [EC(50)] = 8nM.

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Synthetic Routes

Idelalisib - Synthetic Route 1

Idelalisib route01

Synthetic reference

Cai, Duo-Te; Zhang, Yue-Bin; Chen, Ken; Xiong, Qi-Xing; Luo, Wen-Juan; Gao, Zhi-Gang. Synthesis and evaluation of a novel heterocyclic compound against pediatric hepatoblastoma cells. Latin American Journal of Pharmacy. Volume 36. Issue 10. Pages 2022-2027. Journal. (2017).

Idelalisib - Synthetic Route 2

Idelalisib route02

Synthetic reference

Liu, Jian; Huang, Yu; Chang, Xiao-hui; Liu, Xiang-kui; Jiang, Hui-juan; Zhu, Xue-yan. A Novel Method of Preparing (S)​-​5-​Fluoro-​3-​phenyl-​2-​[1-​(9H-​purin-​6-​ylamino)​propyl]​-​3H-​quinazolin-​4-​one. Organic Preparations and Procedures International. Volume 48. Issue 4. Pages 337-341. Journal; Online Computer File. (2016).

Idelalisib - Synthetic Route 3

Idelalisib route03

Synthetic reference

Idelalisib - Synthetic Route 4

Idelalisib route04

Synthetic reference

Kompella, Amala; Rachakonda, Sreenivas; Gampa, Venugopala Krishna; Kusumba, Subhash; Konakanchi, Durga Prasad; Muddasani, Pulla Reddy; Nannapaneni, Venkaiah Chowdary. Process for the preparation of amorphous idelalisib. Assignee Natco Pharma Limited, India. WO2018198131. (2018).

Idelalisib - Synthetic Route 5

Idelalisib route05

Synthetic reference

Thennati, Rajamannar; Dwivedi, Shriprakash Dhar; Jadav, Kanaksinh Jesingbhai; Patel, Vimeshkumar Maganlal; Joshi, Krunalkumar Chetanbhai. Process for the preparation of Idelalisib. Assignee Sun Pharmaceutical Industries Limited, India. WO 2017221272. (2017).

Idelalisib - Synthetic Route 6

Idelalisib route06

Synthetic reference

Oruganti, Srinivas; Sen, Saikat; Dahanukar, Vilas Hareshwar. Processes for preparation of idelalisib and intermediates thereof. Assignee Dr. Reddy\'s Laboratories Limited, India. IN 2014CH06844. (2016).