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Bleximenib oxalate

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Bleximenib oxalate Basic information

Product Name:
Bleximenib oxalate
Synonyms:
  • Bleximenib oxalate
  • (R)-N-Ethyl-5-fluoro-N-isopropyl-2-((5-(2-(6-((2-methoxyethyl)(methyl)amino)-2-methylhexan-3-yl)-2,6-diazaspiro[3.4]octan-6-yl)-1,2,4-triazin-6-yl)oxy)benzamide oxalate
  • 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)-, ethanedioate (1:1)
  • Bleximenib
CAS:
2866179-95-3
MF:
C32H50FN7O3.C2H2O4
MW:
689.82
Mol File:
2866179-95-3.mol
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Bleximenib oxalate Chemical Properties

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|
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Bleximenib oxalate Usage And Synthesis

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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