In Vitro: VTP50469 more potently ａnd rapidly inhibits cell proliferation in a concentration-dependent manner in MLL-r cell lines carrying (MOLM13 (IC₅₀ of 13 nM), THP1 (IC₅₀ of 37 nM), NOMO1 (IC₅₀ of 30 nM), ML2 (IC₅₀ of 16 nM), EOL1 (IC₅₀ of 20 nM), ａnd murine MLL-AF9 cells (IC₅₀ of 15 nM)) ａnd ALL (KOPN8 (IC₅₀ of 15 nM), HB11;19 (IC₅₀ of 36 nM), MV4;11 (IC₅₀ of 17 nM), SEMK2 (IC50 of 27 nM), ａnd RS4;11 (IC₅₀ of 25 nM)) cell lines.
At early timepoints MLL-r B cell ALL (B-ALL) cell lines, but not MLL-r AML cell lines, underwent apoptosis in response to VTP50469 in a dose-dependent manner. MLL-r AML cell lines underwent dose-dependent differentiation starting at 4-6 days of exposure to VTP50469.
VTP50469 displaces Menin from protein complexes ａnd inhibits chromatin occupancy of MLL at ｓelect genes. Loss of MLL binding led to changes in gene expression, differentiation, ａnd apoptosis.

In Vivo: VTP50469 (15-60 mg/kg; oral administration; twice a day; for 28 days; NSG mice) treatment is highly efficacious across all dosage levels ａnd all treatment groups have a significant survival advantage. Mice dosed at 30 ａnd 60 mg/kg VTP50469 extends survival advantage.

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更新时间：2024/1/2 10:12:11

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