产品
编 号:F715396
分子式:C45H63FN6O5S
分子量:819.08
产品类型
结构图
CAS No: 2377335-74-3
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产品详情
生物活性:
M-808 is a highly potent and efficacious covalent Menin-MLL interaction inhibitor, with a binding IC50 value of 2.6 nM.
体内研究:
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.
体外研究:
M808 exhibits IC50 values of 1 nM, 4 nM and 2.8 nM in MV4;11 cells, MOLM-13 cells and HL60 cells, respectively.M808 forms a covalent bond between its acrylamide and the sulfur atom of Cys329 in menin.