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MELK-8a hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MELK-8a hydrochloride图片
CAS NO:2096992-20-8
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
MELK-8a hydrochloride 是一种有效的母体胚胎亮氨酸拉链激酶抑制剂,IC50 为 2 nM。

产品描述

MELK-8a hydrochloride is a potent inhibitor of maternal embryonic leucine zipper kinase (MELK, IC50 = 2 nM).

体外活性

MELK-8a hydrochloride inhibits the growth of MDA-MB-468 cells and MCF-7 cells with an IC50 of approximately 0.06 and 1.2 μM, respectively. MELK-8a hydrochloride remains very potent with an IC50 of 140 nM when the ATP concentration in the biochemical assay is shifted from 20 μM to 2 mM. MELK-8a hydrochloride only inhibits seven off-target kinases in addition to MELK with >85% inhibition of binding at 1 μM demonstrating great selectivity. MELK-8a hydrochloride is at least 90-fold more selective in targeting MELK in all cases. MELK-8a hydrochloride is fairly soluble (0.22 g/L at pH 6.8) and shows a good permeability in the Caco-2 assay[1].

体内活性

In C57BL/6 mice, MELK-8a hydrochloride (30 mg/kg; s.c.) results in good plasma exposure. The compound adsorption into the systemic circulation is rapid (Tmax=0.4 h) and peak plasma concentration reaches 6.6 μM. An ascending dose PK study in female athymic nude mice shows that the rate of compound release is maximal at 120 mg/kg and all clearance mechanisms can be saturated at 240 mg/kg. However, MELK-8a hydrochloride (10 mg/kg; oral) shows very poor PK (3.6% oral bioavailability) consistent with very high in vivo clearance[1].

Cas No.

2096992-20-8

分子式

C25H33ClN6O

分子量

469.02

储存和溶解度

DMSO:8 mg/mL (17.06 mM),Need ultrasonic and warming
H2O:100 mg/mL (213.21 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years