M-808

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

M-808 

M-808 是强效的、共价的 Menin-MLL 互作抑制剂,其 binding IC50 值为 2.6 nM。

M-808

M-808 Chemical Structure

CAS No. : 2377335-74-3

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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[1].

IC50 & Target

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

体外研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

819.08

Formula

C45H63FN6O5S

CAS 号

2377335-74-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

参考文献
  • [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.

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