| Identification | Back Directory | [Name]
Benzamide, N-ethyl-5-fluoro-2-[[5-[2-[(1R)-4-[(2-methoxyethyl)methylamino]-1-(1-methylethyl)butyl]-2,6-diazaspiro[3.4]oct-6-yl]-1,2,4-triazin-6-yl]oxy]-N-(1-methylethyl)- | [CAS]
2654081-35-1 | [Synonyms]
Bleximenib/Menin-MLL inhibitor 24
Benzamide, N-ethyl-5-fluoro-2-[[5-[2-[(1R)-4-[(2-methoxyethyl)methylamino]-1-(1-methylethyl)butyl]-2,6-diazaspiro[3.4]oct-6-yl]-1,2,4-triazin-6-yl]oxy]-N-(1-methylethyl)- | [Molecular Formula]
C32H50FN7O3 | [MOL File]
2654081-35-1.mol | [Molecular Weight]
599.78 |
| Chemical Properties | Back Directory | [Boiling point ]
698.3±65.0 °C(Predicted) | [density ]
1.19±0.1 g/cm3(Predicted) | [form ]
Oil | [pka]
9.14±0.20(Predicted) | [color ]
Colorless to light yellow |
| Hazard Information | Back Directory | [Uses]
Bleximenib (JNJ-75276617; Menin-MLL inhibitor 24) is a potent, selective and orally active menin-KMT2A protein-protein interaction inhibitor with IC50 values of 0.1, 0.045, ≤0.066 nM for human, mouse, dog, respectively. Bleximenib shows antiproliferative activity and induces apoptosis. Bleximenib has the potential for the research of Acute myeloid leukemia (AML)[1][2]. | [in vivo]
Bleximenib (30, 50, 100 mg/kg; PO; daily for 5 weeks) shows antitumor activity[1]. | Animal Model: | 6- to 8-week-old immune-compromised mice (MOLM-14 AML)[1] | | Dosage: | 30, 50, 100 mg/kg | | Administration: | PO; daily for 5 weeks | | Result: | Induced tumor regressions of 70%, 97%, and 99% at 30, 50, and 100 mg/kg, respectively. |
| [References]
[1] Kwon MC, et al. Preclinical efficacy of the potent, selective menin-KMT2A inhibitor JNJ-75276617 (bleximenib) in KMT2A- and NPM1-altered leukemias. Blood. 2024 Sep 12;144(11):1206-1220. DOI:10.1182/blood.2023022480
[2] Hogeling SM, et al. Bleximenib, the novel menin-KMT2A inhibitor JNJ-75276617, impairs long-term proliferation and immune evasion in acute myeloid leukemia. Haematologica. 2024 Dec 19. DOI:10.3324/haematol.2024.285616 |
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