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  3. M-808

M-808 

Cat. No.: HY-133738
Handling Instructions

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

For research use only. We do not sell to patients.

M-808 Chemical Structure

M-808 Chemical Structure

CAS No. : 2377335-74-3

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Description

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

IC50 & Target

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

In Vitro

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].

In Vivo

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].

Molecular Weight

819.08

Formula

C₄₅H₆₃FN₆O₅S

CAS No.

2377335-74-3

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

M-808M808M 808Epigenetic Reader DomainMLLleukemialowtoxicityInhibitorinhibitorinhibit

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