WebDec 8, 2024 · Conclusions: INCB053914 monotherapy demonstrated preliminary safety in Part 1; elevated ALT/AST were the most common treatment-related TEAEs and DLTs, and … INCB053914 is a recently described pan-PIM kinase inhibitor that exhibits potent activity against PIM1, PIM2, and PIM3 (biochemical 50% inhibitory concentration [IC 50] values of 0.24, 30, and 0.12 nM, respectively). 40 To assess the effects of INCB053914 on JAK2 V617F-driven cell growth, we determined the concentration for 50% of maximal ...
Uzansertib phosphate (INCB053914 phosphate) PIM Inhibitor ...
WebDec 7, 2024 · Together, these data suggest that the pan-PIM inhibitor INCB053914 may provide a highly effective novel anti-MPN therapeutic, particularly in combination with ruxolitinib. INCB053914 is currently under investigation in a Phase 1/2 study in patients with advanced hematological malignancies (ClinicalTrials.gov: NCT02587598). WebOct 30, 2024 · Based on the up-regulation of the proviral integration site of the Moloney murine leukemia virus (Pim) kinase family (Pim1, 2, and 3) observed in several types of leukemias and lymphomas, the development of pan-Pim inhibitors is an attractive therapeutic strategy. While only PIM447 and AZD1208 have entered the clinical stages. To … granite countertops conroe tx
The pan-PIM inhibitor INCB053914 displays potent ... - ScienceDirect
WebAug 1, 2015 · The in vitro and in vivo activity of INCB053914, a pan-PIM kinase inhibitor, was determined in a panel of acute myelogenous leukemia (AML) cell lines. Greater than half of all AML cell lines... WebDescription: INCB053914, also known as Uzansertib, is a novel, potent, and selective adenosine triphosphate-competitive pan-PIM kinase inhibitor. In vitro, INCB053914 inhibited proliferation and the phosphorylation of downstream substrates in cell lines from multiple hematologic malignancies. WebUzansertib (INCB053914) phosphate is an orally active, ATP-competitive pan- PIM kinase inhibitor with IC50 s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. … granite countertops company georgetown