aladdin 阿拉丁 M413841 MI-463 1628317-18-9 99%

中文名：MI-463

英文名：MI-463

纯度：≥99%

货号：M413841

Cas号：1628317-18-9

存储温度：-20°C储存

运输条件：超低温运输

产品介绍：

Information

MI-463 MI-463 is a potent inhibitor of Menin-MLL interaction with an IC50 value of 15.3 nM.

Targets

Menin-MLL interaction (Cell-free assay) 15.3 nM

In vitro

MI-463 demonstrates profound on-target activity in MLL leukemia cells. MI-463 results in substantial growth inhibition, with half-maximal growth inhibitory concentration (GI50) values of 0.23 μM, measured after 7 days of treatment in MLL leukemia cells. MI-463 is effective in inducing differentiation of MLL leukemia cells. Treatment with sub-micromolar concentrations of MI-463 also leads to markedly reduced expression of Hoxa9 and Meis1, downstream targets of MLL fusion proteins substantially upregulated in MLL leukemias.

In vivo

MI-463 shows substantial survival benefit in mouse models of MLL leukemia. It has very favorable druglike properties, including metabolic stability and PK profile in mice. MI-463 achieves high levels in peripheral blood following a single intravenous or oral dose, while also showing high oral bioavailability(∼45%). In a mouse xenograft model using MV4;11 human MLL leukemia cells implanted into BALB/c nude mice, MI-463 induces strong inhibition of tumor growth with once-daily intraperitoneal (i.p.) administration. It does not impair normal hematopoiesis in vivo.

Cell Research(from reference)

Cell lines：leukemia cells 

Incubation Time：6 or 7 days 

查看阿拉丁官网此产品相关对应页面：https://www.aladdin-e.com/zh_cn/M413841.html