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MI-3454

CAS No. : 2134169-43-8

MCE 站：MI-3454

产品活性：MI-3454 是一种具有口服活性，高效和选择性的 Menin-MLL1 相互作用抑制剂，IC₅₀ 为 0.51 nM。MI-3454 通过下调涉及白血病发生的关键基因，在 MLL1 重排或 NPM1 突变的白血病小鼠模型中抑制细胞增殖，诱导分化并完全缓解或消退白血病。

研究领域：Epigenetics

作用靶点：Epigenetic Reader Domain

In Vitro: MI-3454 (0.001-10 μM; 7 days) strongly reduces murine bone marrow cells transformed with MLL-AF9 or Hoxa9/Meis1 proliferation.
MI-3454 (50 nM; 6 days) leads to downregulated expression of HOXA9 ａnd MEIS1 in Human leukemic cell lines MV-4-11 cells or MOLM13.
MI-3454 markedly reduces the viability of leukemic cells harboring various MLL fusion proteins (MLL-AF9, MLL-AF4, MLL-ENL), with GI₅₀ values ranging from 7 to 27 nM. MI-3454 blocks the interaction of menin with an MLL1_4–43 fragment encompassing the entire menin binding motif.
MI-3454 does not potently inhibit cytochromes P450 (<50% inhibition at 10 μM).

In Vivo: MI-3454 induces complete remission or regression of leukemia in mouse models of mixed lineage leukemia 1 (MLL1)-rearranged or nucleophosmin 1 (NPM1)-mutated leukemia.
MI-3454 (p.o.; 120 mg/kg; one or twice daily for 7 consecutive days) sufficiently blocks leukemia progression by a once-daily treatment.
MI-3454 (p.o.; 100 mg/kg; b.i.d.; for 19 consecutive days) effectively blocks leukemia progression during the treatment period ａnd markedly prolongs survival of MOLM13 xenotransplantation model mice. MI-3454 induces complete remission or blocks leukemia progression in patient-derived xenograft (PDX) models of MLL leukemia.
MI-3454 (100 mg/kg of PO or 15 mg/kg of IV) has a T_1/2 of 3.2 hours, a C_max of 4698 mg/mL for PO.
MI-3454 exhibits favorable stability in murine ａnd human liver microsomes (t_1/2=20.4 minutes ａnd 37.1 minutes, respectively).
MI-3454 demonstrates lower levels in brain ａnd cerebrospinal fluid, suggesting limited ability to cross the blood-brain barrier.

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