VS-II-173 is a potent pan-Pim kinase inhibitor, exhibiting IC50 values of 0.07 μM for Pim1 and 0.02 μM for Pim3, with a residual activity of 46% at 1 μM for Pim2. This compound selectively targets acute myeloid leukemia (AML) cells, demonstrating significant inhibition of key phosphorylation events, including Stat5 (Y694) and MDM2 (S166), which disrupts pro-survival signaling pathways and promotes apoptosis. VS-II-173 shows enhanced anti-AML efficacy when used in combination with Daunorubicin and is especially relevant for research involving AML characterized by FLT3-ITD and NPM1 mutations. Its minimal toxicity to non-malignant cells makes it a valuable tool in cancer research.
VS-II-173 is a potent pan-Pim kinase inhibitor, exhibiting IC50 values of 0.07 μM for Pim1 and 0.02 μM for Pim3, with a residual activity of 46% at 1 μM for Pim2. This compound selectively targets acute myeloid leukemia (AML) cells, demonstrating significant inhibition of key phosphorylation events, including Stat5 (Y694) and MDM2 (S166), which disrupts pro-survival signaling pathways and promotes apoptosis. VS-II-173 shows enhanced anti-AML efficacy when used in combination with Daunorubicin and is especially relevant for research involving AML characterized by FLT3-ITD and NPM1 mutations. Its minimal toxicity to non-malignant cells makes it a valuable tool in cancer research.
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