M-808 is a small-molecule inhibitor of the Menin–MLL interaction with strong in vivo anti tumor activity. M-808 effectively inhibits leukemia cell growth at low nanomolar concentrations and is capable of achieving partial tumor regression in an MV4;11 xenograft tumor model in mice at a well-tolerated dose schedule. Determination of the co-crystal structure of M-808 in complex with menin provides a structural basis for their high-affinity, covalent interactions. M-808 represents a promising, covalent menin inhibitor for further optimization and evaluation toward developing a new therapy for the treatment of MLL leukemia.
MedKoo Cat#: 593182
Name: M-808
CAS#: 2377335-74-3
Chemical Formula: C45H63FN6O5S
Exact Mass: 818.4565
Molecular Weight: 819.09
Elemental Analysis: C, 65.99; H, 7.75; F, 2.32; N, 10.26; O, 9.77; S, 3.91
The following data is based on the product molecular weight 819.09 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |