Lith-O-Asp
目录号 : GC31385
Lith-O-Asp是唾液酸转移酶(ST)的抑制剂，其IC50值在12-37μM之间。
Cas No.:881179-02-8
Sample solution is provided at 25 µL, 10mM.
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Lith-O-Asp is a sialytransferase (ST) inhibitor, with IC50s of 12-37 μM.
The results indicate that Lith-O-Asp shows no apparent growth inhibition effect toward different cancer cell lines at the tested doses of 10, 30, and 60 μM. By in vitro activity assay, it is revealed that the ability of Lith-O-Asp to inhibit the activities of ST3Gal I, ST3Gal III, and ST6GalI. The IC50 values ranged from 12 to 37 μM. Flow cytometry shows a significant decrease in the expression of cell surface a-2,3- and a-2,6-sialylated antigens on The results indicates that Lith-O-Asp decreased the activity of both a-2,3- and a-2,6-sialyltransferases, and thus inhibit the transfer of sialic acids to the targeted glycoproteins[1].
A significant amount of secondary metastatic cancer cells are observed in lung tissues of DMSO control mice detected using IVIS in vivo imaging system after 26 days of fat pad inoculation. However, Lith-O-Asp-treated mice show fewer lung metastases. All DMSO-treated mice confirm secondary lung metastasis, but only 3 of 8 Lith-O-Asp-treated mice show lung metastasis. Average tumor nodules per mouse are 11±9 nodules in DMSO-treated group, and 2±4 nodules in Lith-O-Asp-treated group. Additionally, significantly stronger 4T1-Luc illumination signals are shown in control mice than in those injected with Lith-O-Asp-treated cancer cells on days 7 and 9[1].
[1]. Chen JY, et al. A novel sialyltransferase inhibitor suppresses FAK/paxillin signaling and cancer angiogenesis and metastasis pathways. Cancer Res. 2011 Jan 15;71(2):473-83.
Cell experiment: | About 3x104 of the CL1-0, CL1-5, A549, and H1299 lung cancer cells are seeded on 12-well culture dishes in DMEM containing 10% FBS. Different concentrations of Lith-O-Asp (10, 30, and 60 μM) are added into each plate and incubated for 48 hr. Cell viabilities under different concentrations of compound treatment are determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. In the untreated control, 0.1% DMSO-containing medium is used[1]. |
Animal experiment: | Mice[1]The BALB/c mice are used. Highly metastatic murine 4T1-Luc breast cancer cells (5 x105) are subcutaneously injected into the mammary fat pad of mice. Mice receive 3 mg/kg of Lith-O-Asp intraperitoneally on every other day. DMSO treatment is used as control. The growth and the spontaneous metastasis of the tumors are observed under IVIS50 in vivo imaging system with endotoxin-free luciferase substrate injection. The metastasized tumor tissues are dissected on day 26[1]. |
References: [1]. Chen JY, et al. A novel sialyltransferase inhibitor suppresses FAK/paxillin signaling and cancer angiogenesis and metastasis pathways. Cancer Res. 2011 Jan 15;71(2):473-83. | |
| Cas No. | 881179-02-8 | SDF | |
| Canonical SMILES | C[C@@]12-;@[C@](-;@C-;@C-;@[C@]-;@2([H])[C@H](C)CCC(O)=O)([H])-;@[C@@]3([H])-;@[C@](-;@[C@@]4(-;@[C@](-;@C-;@[C@H](OC([C@@H](N)CC(O)=O)=O)-;@C-;@C-;@4)([H])-;@C-;@C-;@3)C)([H])-;@C-;@C-;@1 | ||
| 分子式 | C28H45NO6 | 分子量 | 491.66 |
| 溶解度 | DMSO : ≥ 106 mg/mL (215.60 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 | 2.0339 mL | 10.1696 mL | 20.3393 mL |
| 5 mM | 0.4068 mL | 2.0339 mL | 4.0679 mL |
| 10 mM | 0.2034 mL | 1.017 mL | 2.0339 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