LDN 209929 dihydrochloride
目录号 : GC14901haspin kinase inhibitor
Cas No.:1784281-97-5
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Target: haspin kinase
IC50: 55 nM
LDN 209929 dihydrochloride is a selective and potent haspin kinase inhibitor with IC50 value of 55 nM [1]. LDN 209929 dihydrochloride displays 180-fold selectivity on haspin kinase over DYRK2 [1].
Haspin, also known as Germ Cell-Specific Gene-2 (Gsg2), is a serine/threonine kinase expressed in several tissues (e.g., testis, thymus, bone narrow, and spleen), proliferating cells and neoplasms, including diffuse large B cell lymphomas and Burkitt’s lymphoma. Haspin’s kinase activity is required for completion of normal mitosis. Therefore, Haspin has emerged as a potential therapeutic target in oncology [1].
DYRKs (Dual-specificity Tyrosine-regulated Kinases), belong to the CMGC family of eukaryotic protein kinase, can be divided into class 1 kinases (DYRK1A and 1B) and class 2 kinases (DYRK2, 3, and 4), which are predominantly cytosolic. DYRKs participate in regulation of several signaling pathways, including Hedgehog signaling, caspase activity during apoptosis, cell cycle progression and mitosis, NFAT signaling in the brain and immune system, and p53 activation in response to DNA damage [1].
In vitro: N/A
In vivo: N/A
Reference:
1. Cuny GD, Robin M, Ulyanova NP, Patnaik D, Pique V, Casano G, et al. Structure-activity relationship study of acridine analogs as haspin and DYRK2 kinase inhibitors. Bioorg Med Chem Lett. 2010;20(12):3491-4.
Cas No. | 1784281-97-5 | SDF | |
化学名 | 3-((2-chloro-7-methoxyacridin-9-yl)thio)propan-1-amine | ||
Canonical SMILES | NCCCSC1=C2C(C=CC(OC)=C2)=NC3=CC=C(Cl)C=C31 | ||
分子式 | C17H17ClN2OS.2HCl | 分子量 | 405.77 |
溶解度 | <40.58mg/ml in Water; <40.58mg/ml in DMSO | 储存条件 | Desiccate at RT |
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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.4645 mL | 12.3223 mL | 24.6445 mL |
5 mM | 0.4929 mL | 2.4645 mL | 4.9289 mL |
10 mM | 0.2464 mL | 1.2322 mL | 2.4645 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。