OSIP-486823 (OSIP 486823)
(Synonyms: OSIP 486823; OSIP486823; CP248) 目录号 : GC33163
OSIP-486823 (OSIP 486823) 是一种新型微管干扰剂，对蛋白激酶 G (PKG) 和微管具有独特的生物学效应。
Cas No.:200803-37-8
Sample solution is provided at 25 µL, 10mM.
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OSIP-486823 is a novel microtubule-interfering agent with distinct biological effects on both protein kinase G (PKG) and microtubules.
OSIP486823 inhibits growth and induce apoptosis in SW480 human colon cancer cells, with IC50 of 0.1 μM. OSIP-486823 (OSIP486823) causes depolymerization of microtubules in interphase cells, inhibit spindle formation in mitotic cells, and induce multinucleated cells. Exisulind and the potent synthetic derivative OSIP-486823 are members of a new class of drugs known as selective apoptotic antineoplastic drugs that target cyclic guanosine 3′,5′-monophosphate phosphodiesterases (cGMP-PDE). OSIP-486823 also disrupts microtubule polymerization, perturbs mitotic spindle function, and arrests cells in mitosis in human glioma cells[1].
[1]. Xiao D, et al. The sulindac derivatives OSI-461, OSIP486823, and OSIP487703 arrest colon cancer cells in mitosis by causing microtubule depolymerization. Mol Cancer Ther. 2006 Jan;5(1):60-7.
Cell experiment: | The SW480 human colon adenocarcinoma and NIH3T3 mouse fibroblast cell lines are seeded in six-well plates at a density of 3×104 per well, grown for 36 to 48 hours, and then exposed to increasing concentrations of each compound (e.g., OSIP-486823; 1, 2 and 4 μM) for 48 hours. Cell numbers are determined using a Coulter counter and results are expressed as a percentage of the control culture. All assays are done in triplicate. Data are analyzed in Excel and the IC50s are determined graphically from cell survival curves[1]. |
References: [1]. Xiao D, et al. The sulindac derivatives OSI-461, OSIP486823, and OSIP487703 arrest colon cancer cells in mitosis by causing microtubule depolymerization. Mol Cancer Ther. 2006 Jan;5(1):60-7. | |
| Cas No. | 200803-37-8 | SDF | |
| 别名 | OSIP 486823; OSIP486823; CP248 | ||
| Canonical SMILES | O=C(NCC1=CC=CC=C1)CC(C2=C/3C=CC(F)=C2)=C(C)C3=C\C4=CC(OC)=C(OC)C(OC)=C4 | ||
| 分子式 | C29H28FNO4 | 分子量 | 473.54 |
| 溶解度 | Soluble in DMSO | 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 | 2.1118 mL | 10.5588 mL | 21.1175 mL |
| 5 mM | 0.4224 mL | 2.1118 mL | 4.2235 mL |
| 10 mM | 0.2112 mL | 1.0559 mL | 2.1118 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet