MELK-8a hydrochloride

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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。

CAS NO:

2096992-20-8

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
1mg	电议
5mg	电议
10mg	电议
50mg	电议
100mg	电议
200mg	电议
500mg	电议

产品名称

NVS-MELK8a hydrochloride

产品介绍

MELK-8a hydrochloride是一种新颖的母体胚胎亮氨酸拉链激酶（MELK）抑制剂，其IC₅₀值为2 nM。

生物活性

MELK-8a hydrochloride is a novel maternal embryonic leucine zipper kinase (MELK) inhibitor with anIC₅₀of 2 nM.

IC₅₀& Target

IC50: 2 nM (MELK)^[1]

体外研究
(In Vitro)

MELK-8a remains very potent (IC₅₀=140 nM) when the ATP concentration in the biochemical assay is shifted from 20 μM to 2 mM. Its potency is well tracked between full-length MELK versus catalytic domain construct (5 nM versus 2 nM). It only inhibits seven off-target kinases in addition to MELK with >85% inhibition of binding at 1 μM demonstrating great selectivity. The compound is at least 90-fold more selective in targeting MELK in all cases. MELK-8a is fairly soluble (0.22 g/L at pH 6.8) and shows a good permeability in the Caco-2 assay. MELK-8a inhibits the growth of MDA-MB-468 cells and MCF-7 cells with an IC₅₀of approximately 0.06 and 1.2 μM, respectively^[1].

体内研究
(In Vivo)

Subcutaneous administration of MELK-8a at 30 mg/kg in C57BL/6 mice results in good plasma exposure. The compound adsorption into the systemic circulation is rapid (T_max=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, when administered orally at 10 mg/kg in C57BL/6 male mice, it shows very poor PK (3.6% oral bioavailability) consistent with very highin vivoclearance^[1].

分子量

469.02

性状

Solid

Formula

C₂₅H₃₃ClN₆O

CAS 号

2096992-20-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

H₂O : ≥ 100 mg/mL(213.21 mM)

DMSO : 8.6 mg/mL(18.34 mM;Need ultrasonic and warming)

*"≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	2.1321 mL	10.6605 mL	21.3211 mL
5 mM	0.4264 mL	2.1321 mL	4.2642 mL
10 mM	0.2132 mL	1.0661 mL	2.1321 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.
请依序添加每种溶剂： PBS
Solubility: 50 mg/mL (106.61 mM); Clear solution; Need ultrasonic

*以上所有助溶剂都可在本网站选购。