Activity of MZ1, birabresib and cisMZ1 in ABC DLBCL cell lines
Cell line | MZ1 (nmol/L) | Birabresib (nmol/L) | CisMZ1 (nmol/L) | |||
---|---|---|---|---|---|---|
IC50 | AUC | IC50 | AUC | IC50 | AUC | |
HBL1 | 61.68 | 17,036 | 292.38 | 43,057 | > 2,000 | 89,050 |
OCI-LY-10 | 4.39 | 1,302 | 125.91 | 33,067 | > 2,000 | 94,936 |
OCI-LY-3 | 22.76 | 3,934 | 98.35 | 26,973 | > 2,000 | 89,072 |
RI-1 | 134.88 | 32,997 | 394.42 | 50,586 | > 2,000 | 86,715 |
SU-DHL-2 | 48.95 | 14,789 | 68.42 | 17,690 | > 2,000 | 88,269 |
TMD8 | 39.10 | 6,847 | 106.92 | 19,826 | > 2,000 | 99,547 |
U2932 | 109.03 | 24,749 | 470.57 | 53,025 | > 2,000 | 96,221 |
Median IC50 | 48.95 | 125.91 | n.a. | |||
95% CI | 10.16–126.76 | 77.83–446.64 | n.a. | |||
Median AUC | 14,789 | 33,067 | 89,072 | |||
95% CI | 1,302–32,997 | 17,690–53,025 | 86,715–99,547 |
Seven ABC DLBCL lymphoma cell lines were exposed to increasing concentrations of MZ1, birabresib or cisMZ1 for 72 h. Table shows the IC50 and AUC values for each cell line, 95% CI of median IC50 and AUC for each drug. n.a.: not avalable
The supplementary Figures for this article are available at: https://www.explorationpub.com/uploads/Article/file/100265_sup_1.pdf. The supplementary Tables for this article are available at: https://www.explorationpub.com/uploads/Article/file/100265_sup_2.xlsx.
The authors would like to thank the Colleagues at BigOmics Analytics SA (Viganello, Switzerland) for their support in using their on-line tool.
Conception and design: CT, AC, FB. Development of methodology: CT, EG, AT, CM, AC, FB. Analysis and interpretation of data (e.g., statistical analysis, biostatistics, computational analysis): CT, LC, FB. Writing, review, and/or revision of the manuscript: CT, EZ, AS, AC, FB. Administrative, technical, or material support (i.e., reporting or organizing data, constructing databases): CT, FB. Study supervision: FB. Others (performed experiments): CT, HE, CM, EG, EC, CR, SN, AR. All authors have approved the submitted version and have agreed to both be personally accountable for the author’s own contributions and to ensure that questions related to the accuracy or integrity of any part of the work, even ones in which the author was not personally involved, are appropriately investigated.
EZ: institutional research funds from Celgene, Roche, and Janssen; advisory board fees from Celgene, Roche, Mei Pharma, Astra Zeneca, and Celltrion Healthcare; travel grants from Abbvie and Gilead; expert statements provided to Gilead, Bristol-Myers Squibb, and MSD. AS: institutional research funds from: Bayer, Merck, Pfizer, Novartis, Roche, MEI Pharma, ADC-Therapeutics; travel grant from AbbVie and PharmaMar. AC: scientific founder, director, consultant and shareholder of Amphista Therapeutics; institutional research funds from Amphista therapeutics, Boehringer Ingelheim, Eisai, and Nurix, Inc. and One Pharma. FB: institutional research funds from Acerta, ADC Therapeutics, Bayer AG, Cellestia, CTI Life Sciences, EMD Serono, Helsinn, ImmunoGen, Menarini Ricerche, NEOMED Therapeutics 1, Nordic Nanovector ASA, Oncology Therapeutic Development, PIQUR Therapeutics AG; consultancy fee from Helsinn, Menarini; expert statements provided to HTG; travel grants from Amgen, Astra Zeneca, Jazz Pharmaceuticals, PIQUR Therapeutics AG. The other authors have nothing to disclose.
Mice maintenance and animal experiments were performed under the institutional guidelines established for the Animal Facility and with study protocols approved by the local Cantonal Veterinary Authority (license TI-23/2015).
Not applicable.
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All transcriptome data are available at GEO (http://www.ncbi.nlm.nih.gov/geo).
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© The Author(s) 2021.