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M-808

Chemical Structure : M-808

CAS No.: 2377335-74-3

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M-808 (M808)

Catalog No.: PC-20564Not For Human Use, Lab Use Only.

M-808 (M808) is a highly potent, selective and covalent inhibitor of menin-MLL interaction with binding IC50 of 2.6 nM, forms a covalent bond with Cys329 in menin.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

M-808 (M808) is a highly potent, selective and covalent inhibitor of menin-MLL interaction with binding IC50 of 2.6 nM, forms a covalent bond with Cys329 in menin.
M-808 effectively inhibits leukemia cell growth of MV4;11 and MOLM13 cell lines carrying MLL fusion with IC50 of 1 and 4 nM, respectively.
M-808 (25 mg/kg, i.v. qD) exhibits partial tumor regression in the MV4;11 leukemia xenograft tumor model in mice, suppresses expression of HOXA9 and MEIS1 genes in MV4;11 xenograft tumors.

Physicochemical Properties

M.Wt 819.09
Formula C45H63FN6O5S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

O=C(OC)N[C@@H]1[C@@H]([C@@](C2CCN(CC3CN(C4=CC=C(S(=O)(C5CN(C(/C=C/CN6CCCCC6)=O)C5)=O)C=C4)C3)CC2)(C7=CC=CC(F)=C7)CN8CCC8)CCC1

References

1. Xu S, et al. J Med Chem. 2020 May 14;63(9):4997-5010.

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