Idelalisib (CAL-101)
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. TFA approved this drug on July 23, 2014. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).
Synonym: CAL101; CAL 101; CAL-101; GS1101; GS 1101; GS-1101, Idelalisib.
IUPAC/Chemical Name: (S)-2-(1-((9H-purin-6-yl)amino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one
THEORETICAL ANALYSIS
MedKoo Cat#: 200586
Name: Idelalisib (CAL-101)
CAS#: 870281-82-6
Chemical Formula: C22H18FN7O
Exact Mass: 415.1557
Molecular Weight: 415.423
Elemental Analysis: C, 63.61; H, 4.37; F, 4.57; N, 23.60; O, 3.85
TECHNICAL DATA
REFERENCES
1: Meadows SA, Vega F, Kashishian A, Johnson D, Diehl V, Miller LL, Younes A, Lannutti BJ. 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. doi: 10.1182/blood-2011-10-386763. Epub 2011 Dec 30. PubMed PMID: 22210877.
2: Byrd JC, Woyach JA, Johnson AJ. Translating PI3K-Delta Inhibitors to the Clinic in Chronic Lymphocytic Leukemia: The Story of CAL-101 (GS1101). Am Soc Clin Oncol Educ Book. 2012;32:691-694. doi: 10.14694/EdBook_AM.2012.32.691. PubMed PMID: 24451820.
3: Castillo JJ, Furman M, Winer ES. CAL-101: a phosphatidylinositol-3-kinase p110-delta inhibitor for the treatment of lymphoid malignancies. Expert Opin Investig Drugs. 2012 Jan;21(1):15-22. doi: 10.1517/13543784.2012.640318. Epub 2011 Nov 24. Review. PubMed PMID: 22112004.
4: Hoellenriegel J, Meadows SA, Sivina M, Wierda WG, Kantarjian H, Keating MJ, Giese N, O’Brien S, Yu A, Miller LL, Lannutti BJ, Burger JA. 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. doi: 10.1182/blood-2011-05-352492. Epub 2011 Jul 29. PubMed PMID: 21803855.
5: Lannutti BJ, Meadows SA, Herman SE, Kashishian A, Steiner B, Johnson AJ, Byrd JC, Tyner JW, Loriaux MM, Deininger M, Druker BJ, Puri KD, Ulrich RG, Giese NA. CAL-101, a p110delta selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability. Blood. 2011 Jan 13;117(2):591-4. doi: 10.1182/blood-2010-03-275305. Epub 2010 Oct 19. PubMed PMID: 20959606; PubMed Central PMCID: PMC3694505.
6: Herman SE, Gordon AL, Wagner AJ, Heerema NA, Zhao W, Flynn JM, Jones J, Andritsos L, Puri KD, Lannutti BJ, Giese NA, Zhang X, Wei L, Byrd JC, Johnson AJ. Phosphatidylinositol 3-kinase-δ inhibitor CAL-101 shows promising preclinical activity in chronic lymphocytic leukemia by antagonizing intrinsic and extrinsic cellular survival signals. Blood. 2010 Sep 23;116(12):2078-88. doi: 10.1182/blood-2010-02-271171. Epub 2010 Jun 3. PubMed PMID: 20522708; PubMed Central PMCID: PMC2951855.
