M-808 

M-808 is a highly potent and efficacious covalent Menin-MLL interaction inhibitor, with a binding IC₅₀ value of 2.6 nM^[1].

IC50: 1 nM (Menin-MLL in MV4;11 cells), 4 nM (Menin-MLL in MOLM-13 cells)^[1].

M808 exhibits IC₅₀ values of 1 nM, 4 nM and 2.8 nM in MV4;11 cells, MOLM-13 cells and HL60 cells, respectively^[1].
M808 forms a covalent bond between its acrylamide and the sulfur atom of Cys329 in menin^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

M-808 (16) is well tolerated in severe combined immunodeficiency (SCID) mice with intravenous administration of 10 mg/kg (or 25 mg/kg) every other day dosing (three times a week) for one week. M-808 (25 mg/kg) achieves a maximum tumor growth inhibition (TGI) of 97% during treatment (day 35) and reduces the average tumor volume from 92 mm³ at the beginning of the treatment to 59 mm³ at day 35, with no significant toxicity^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

819.08

C₄₅H₆₃FN₆O₅S

2377335-74-3

O=S(C(C=C1)=CC=C1N(C2)CC2CN(CC3)CCC3[C@@]([C@@]4([H])CCC[C@@H]4NC(OC)=O)(CN5CCC5)C6=CC(F)=CC=C6)(C7CN(C(/C=C/CN8CCCCC8)=O)C7)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Shilin Xu, et al. Discovery of M-808 as a Highly Potent, Covalent, Small-Molecule Inhibitor of the Menin-MLL Interaction With Strong In Vivo Antitumor Activity. J Med Chem. 2020 May 14;63(9):4997-5010.  [Content Brief]