IndraLab

Statements

Imatinib inhibits KCNH2. 9 / 9
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"The results demonstrated that hERG1 was highly detected in K562 cells and primary CML cells, and down-regulated by imatinib at mRNA and protein levels."
22161019
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"Furthermore, imatinib markedly reduced hERG currents in HEK293T-hERG cells, this effect was accompanied by inhibition of CML cell proliferation and apoptosis, as well as suppression of vascular endothelial growth factor (VEGF) secretion."
22161019
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"Imatinib markedly diminishes hERG current in cells, alongside suppressing the growth and apoptosis of CML cells and the release of VEGF, emphasizing the hERG1 K channel as a treatment target for CML therapy."
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"It has been documented that hERG1 is significantly overexpressed in primary CML cells and K562 cells, and imatinib can downregulate hERG1 by modulating mRNA and protein levels."
39027429
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"However, ponatinib and imatinib significantly decreased the polarization of the hERG channel."
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"The study demonstrated that dasatinib, imatinib, and nilotinib inhibit hERG currents in vitro with IC50 values of 14.3, 15.6, and 0.66 μM, respectively."
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"According to the formal studies, imatinib could preferentially block the open HERG channel, contributing to QT interval prolongation [XREF_BIBR]."
29876021
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"8 Imatinib was reported to suppress hERG K + channels expressed in HEK293 cells with an IC 50 value of 9.63 μg/mL (19.51 μM), 11 whereas its peak free plasma concentration after a single administratio[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
36184120
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"Meanwhile, imatinib did not alter the T peak -T end , suggesting that imatinib may hardly inhibit hERG K + channel in vivo."
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