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VTP50469 fumarate

CAS No. : 2169919-29-1

MCE 站：VTP50469 fumarate

产品活性：VTP50469 fumarate 是一种有效的，高选择性和口服活性的 Menin-MLL 相互作用抑制剂，K_i 为 104 pM。VTP50469 fumarate 具有高效的抗白血病活性。

研究领域：Epigenetics  |  Apoptosis

作用靶点：Epigenetic Reader Domain  |  Apoptosis

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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