MELK-8a hydrochloride
(Synonyms: NVS-MELK8a hydrochloride) 目录号 : GC32736
A MELK inhibitor
Cas No.:2096992-20-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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. | |
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)
| Cas No. | 2096992-20-8 | SDF | |
| 别名 | NVS-MELK8a hydrochloride | ||
| Canonical 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 |
| 溶解度 | Water : ≥ 100 mg/mL (213.21 mM);DMSO : 8.6 mg/mL (18.34 mM) | 储存条件 | 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℃，然后在超声波浴中震荡一段时间。 |
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| 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。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。