CAL101
CAL101 is an inhibitor of p110δ PI3K that is clinically used to treat leukemias such as mantle cell lymphoma and chronic lymphocytic leukemia (CLL). CAL101 exhibits anticancer chemotherapeutic and immunosuppressive activities. In mantle cell lymphoma cells, CAL101 induces G1 phase cell cycle arrest and apoptosis. In non-Hodgkin lymphoma and CLL cells, CAL101 inhibits downstream phosphorylation of Akt and induces apoptosis. Additionally, this compound inhibits cell chemotaxis, decreases chemokine production, inhibits migration, and prevents ERK- and Akt-dependent B-cell receptor signaling in CLL cells.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18846431
| Cas No. |
870281-82-6 |
|---|---|
| Purity |
≥98% |
| Formula |
C22H18FN7O |
| Formula Wt. |
415.42 |
| IUPAC Name |
5-fluoro-3-phenyl-2-[(1S)-1-(7H-purin-6-ylamino)propyl]quinazolin-4-one |
| Synonym |
Idelalisib, GS1101, CAL-101 |
| Appearance |
White Crystal Powder |
Sanford DS, Wierda WG, Burger JA, et al. Three Newly Approved Drugs for Chronic Lymphocytic Leukemia: Incorporating Ibrutinib, Idelalisib, and Obinutuzumab into Clinical Practice. Clin Lymphoma Myeloma Leuk. 2015 Feb 19. [Epub ahead of print]. PMID: 25817936.
Chiron D, Martin P, Di Liberto M, et al. Induction of prolonged early G1 arrest by CDK4/CDK6 inhibition reprograms lymphoma cells for durable PI3Kδ inhibition through PIK3IP1. Cell Cycle. 2013 Jun 15;12(12):1892-900. PMID: 23676220.
Meadows SA, Vega F, Kashishian A, Johnson D, et al. PI3Kδ inhibitor, GS-1101 (CAL-101), attenuates pathway signaling, induces apoptosis, and overcomes signals from the microenvironment in cellular models of Hodgkin lymphoma. Blood. 2012 Feb 23;119(8):1897-900. PMID: 22210877.
Hoellenriegel J, Meadows SA, Sivina M, et al. The phosphoinositide 3-kinase delta inhibitor, CAL-101, inhibits B-cell receptor signaling and chemokine networks in chronic lymphocytic leukemia. Blood. 2011 Sep 29;118(13):3603-12. PMID: 21803855.
