Icovamenib

Icovamenib (BMF-219) is a selective, orally active, irreversible Menin inhibitor. Icovamenib forms a stable and irreversible covalent bond with Menin. Icovamenib promotes selective and controlled proliferation of beta cells and improvement of beta cell function in ex vivo human islet cultures. Icovamenib enhances glycemic control in animal diabetic models. Icovamenib induces a dose-dependent enhancement in insulin secretion potentiated by the GLP-1 RA. Icovamenib can be used for the study of multiple hematologic malignancies, solid tumors, and diabetes mellitus, such as diffuse large B-cell lymphoma (DLBCL), multiple myeloma (MM) and chronic lymphocytic leukemia and type 2 diabetes[1][2][3][4][5].

Product Specifications

CAS Number

[2448172-22-1]

Product Name Alternative

BMF-219; Menin-MLL inhibitor 21

UNSPSC

12352005

Target

Epigenetic Reader Domain

Type

Reference compound

Related Pathways

Epigenetics

Applications

COVID-19-immunoregulation

Field of Research

Cancer; Metabolic Disease; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/menin-mll-inhibitor-21.html

Purity

98.96

Solubility

DMSO : 25 mg/mL (ultrasonic)

Smiles

O=C(C1=CC(CN2C[C@@H](CCC2)NC(C=C)=O)=CC=N1)NC3=CC=C(C=C3)C4=CC5=C(N6CCOCC6)N=CN=C5N4

Molecular Formula

C31H34N8O3

Molecular Weight

566.65

References & Citations

[1]Thomas Butler, et al. Irreversible inhibitors of menin-mll interaction.WO2020142557 A1.|[2]Jeffrey Lancet MD, et al. Dovalent Menin Inhibitor Bmf-219 in Patients with Relapsed or Refractory (R/R) Acute Leukemia (AL) : Preliminary Phase 1 Data from the Covalent-101 Study. Blood. Volume 142, Supplement 1, 2 November 2023, Page 2916. |[3]Mo J, et al. Design, synthesis, and evaluation of Menin-targeting compounds for the treatment of acute Myelocytic leukemia (AML) . Eur J Med Chem. 2025 Jun 12;296:117847.|[4]Mini Balakrishnan, et al., Combination of Icovamenib and GLP-1-based Therapeutic Agents Improves Beta Cell Function and Insulin Secretion. Metabolism - Clinical and Experimental, Volume 168, 156226.|[5]Carraway, H. E., et al., (2025) . Complete remission of NUP98 fusion-positive acute myeloid leukemia with the covalent menin inhibitor BMF-219, icovamenib. Haematologica, 110 (4), 1041–1046.