MELK-8a hydrochloride

目录号: GC32736纯度: >98.00%同义词: NVS-MELK8a hydrochloride

A MELK inhibitor

Cas No.: 2096992-20-8

规格	价格	库存	数量	操作
5mg	¥2,520.00	现货	1
10mg	¥3,690.00	现货	1

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本产品暂无引用记录;以下为 GlpBio 产品在 Nature / Cell / Science 等顶刊的客户引用样例

Nature
641, 529–536 (2025)
Nature
628, 630–638 (2024)
Nature
632, 686–694 (2024)
Nature
618, 1017–1023 (2023)
Nature
610, 366–372 (2022)
Cell
187(9):2288-2304 (2024)
Cell
183(7):1867-1883 (2020)
Science
388(6745) (2025)
Science
387(6739) (2025)
Science
387(6734) (2025)
Cell Research
35, 97–116 (2025)
Cell Research
34, 683–706 (2024)
Cell Research
33, 273–287 (2023)
Cell Research
33, 546–561 (2023)
Cell Research
33, 904–922 (2023)
Cell Research
31, 1291–1307 (2021)

产品描述 Description

MELK-8a is an inhibitor of maternal embryonic leucine zipper kinase (MELK; IC₅₀ = 0.002 ?M).¹ It is selective for MELK over FLT3, haspin, KIT, and PDGFRα, (IC₅₀s = 0.18, 0.19, >10, and 0.42 ?M, respectively), as well as a panel of 456 kinases at 1 ?M. MELK-8a inhibits the proliferation of MDA-MB-468 and MCF-7 breast cancer cells (IC₅₀s = 0.11 and 3.68 ?M).

1.Touré, B.B., Giraldes, J., Smith, T., et al.Toward the validation of maternal embryonic leucine zipper kinase: Discovery, optimization of highly potent and selective inhibitors, and preliminary biology insightJ. Med. Chem.59(10)4711-4723(2016)

实验参考方法 Experimental Reference Method

Cell experiment:

MDA-MB-468 and MCF7 cells are seeded in growth medium into 96-well plates at 1000 and 4000 cells/well, respectively. Sixteen hours after plating, MELK-8a are added and incubated for 7 days. For each well, ATPLite reagent is added and incubated. Luminescence is measured on an multilabel plate reader[1].

Animal experiment:

Mice: For pharmacokinetic studies, the intravenous and oral dose is prepared in a solution containing 5% ethanol, 100% PG, 5% CremophorEL, and 80% PBS. The subcutaneous dose is formulated in 10% PG and 25% (20%, v/v) Solutol. Plasma samples are collected at specified time points and stored frozen (−20 °C) until MELK-8a analysis. An LC−MS/MS method is used to quantitate MELK-8a drug levels in plasma[1].

References:

[1]. Touré BB, et al. Toward the Validation of Maternal Embryonic Leucine Zipper Kinase: Discovery, Optimization of Highly Potent and Selective Inhibitors, and Preliminary Biology Insight. J Med Chem. 2016 May 26;59(10):4711-23.

产品文档 Product Documents

Purity:>98.00%

化学性质Chemical Properties

CAS 号

2096992-20-8

同义词

NVS-MELK8a hydrochloride

SMILES

CN(CC1)CCN1C2=CC=C(N3C=C(C4=CC=NC=C4OCC5CCNCC5)C=N3)C=C2.Cl

分子式

C₂₅H₃₃ClN₆O

分子量

469.02 g/mol

溶解性

Water : ≥ 100 mg/mL (213.21 mM);DMSO : 8.6 mg/mL (18.34 mM)

保存条件

Store at -20°C

General tips

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°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。

Shipping Condition

评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

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