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Fig. 6 | Journal of Hematology & Oncology

Fig. 6

From: Activity of the novel BCR kinase inhibitor IQS019 in preclinical models of B-cell non-Hodgkin lymphoma

Fig. 6

Improved in vitro and in vivo activity of IQS019 vs the Btk inhibitor ibrutinib. a A panel of eight B-NHL cell lines was incubated with increasing concentrations of IQS019 or ibrutinib for 24, 48, and 72 h and IC50 was calculated as previously. b IQS019 has improved anti-migratory activity. UPN-1 cells were exposed to 5 μM IQS019 or ibrutinib for 90 min followed by evaluation of CXCL12-dependent cell chemotaxis, as described in methods section. Statistical significance: ** p < 0.01. c Orally administered IQS019 impairs tumor outgrowth more efficiently than ibrutinib. SCID mice were inoculated with UPN-1 cells subcutaneously and, at day 10 post-inoculation, started to be dosed p.o., 5 days a week, for two weeks, with 25 mg/kg IQS019-2MeSO3H, 25 mg/kg ibrutinib or equal volume of vehicle (n = 10 animals per group). Tumor volumes were recorded as above. Statistical significance: * p < 0.05, ** p < 0.01. d Western blot analysis of phospho-Lyk, phospho-Syk and (e) cytofluorimetric analysis of phospho-Btk in UPN-1 and UPN-IbruR cells treated for 6 h with indicated doses of IQS019 or ibrutinib. For phospho-Btk analysis, cells were exposed to a single dose of each agent (5 μM) 90 min prior to IgM stimulation and cell labeling. Indicated are the r values observed after treatment with IQS019 (grey curves) or ibrutinib (red curves), and referred to control IgM-stimulated cells (black curves). Isotype controls are represented by grey filled histograms. Shown are representative experiments from two replicates

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