| Chemical Properties | Back Directory | [form ]
Solid | [color ]
Light yellow to yellow | [InChIKey]
OYKHOVACUSUKFI-OSMNJKESNA-N | [SMILES]
[C@H](N1CC2(CCN(C3=NC=NN=C3OC3C=CC(=CC=3C(=O)N(CC)C(C)C)F)C2)C1)(C(C)C)CCCN(C)CCOC.C(=O)(O)C(=O)O |&1:0,r| |
| Hazard Information | Back Directory | [Uses]
Bleximenib (JNJ-75276617; Menin-MLL inhibitor 24) oxalate 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 oxalate shows antiproliferative activity and induces apoptosis. Bleximenib oxalate 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) oxalate 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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