OTX008
(Synonyms: Calixarene 0118; PTX008) 目录号 : GC18756
An inhibitor of Gal-1
Cas No.:286936-40-1
Sample solution is provided at 25 µL, 10mM.
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OTX008 is a selective inhibitor of galectin-1.
Growth inhibitory concentrations (GI50) of OTX008 in a large panel of human solid tumour cell lines ranges from 3 to 500 μM. A significant correlation between OTX008 GI50 values and Gal1 mRNA (LGALS1) and protein expression levels in the panel of cancer cells is observed. In SQ20B and A2780-1A9 cells, OTX008 inhibits Gal1 expression and ERK1/2 and AKT-dependent survival pathways, and induces G2/M cell cycle arrest through CDK1. OTX008 enhances the anti-proliferative effects of Semaphorin-3A (Sema3A) in SQ20B cells and reverses invasion induced by exogenous Gal1[1]. OTX008 affects endothelial cell proliferation, motility, invasiveness, and cord formation. Tumor cell proliferation is also inhibited, with differences in sensitivity among cell lines (IC50 from 1 to 190 μM)[2].
OTX008 inhibits growth of A2780-1A9 xenografts. OTX008 treatment is associated with down-regulation of Gal1 and Ki67 in treated tumours, as well as decreased microvessel density and VEGFR2 expression. Finally, combination studies show OTX008 synergy with several cytotoxic and targeted therapies, principally when OTX008 is administered first[1].
References:
[1]. Astorgues-Xerri L, et al. OTX008, a selective small-molecule inhibitor of galectin-1, downregulates cancer cell proliferation, invasion and tumour angiogenesis. Eur J Cancer. 2014 Sep;50(14):2463-77.
[2]. Zucchetti M, et al. Pharmacokinetics and antineoplastic activity of galectin-1-targeting OTX008 in combination with sunitinib. Cancer Chemother Pharmacol. 2013 Oct;72(4):879-87.
Animal experiment: | Mice[1]A total of 8×106 A2780-1A9 ovarian cells are injected subcutaneously into the right lateral flank of female nu/nu athymic mice. Once tumours are palpable (50 mm3), mice are randomised to receive treatment intraperitoneally with either PBS (3 times/week), 5 mg/kg OTX008 (3 times/week), 6 mg/kg cisplatin (days 1, 8 and 15) or 10 mg/kg docetaxel (days 1, 8 and 15). Tumour size was measured twice weekly with calipers and tumour volume is calculated as 3.14×(width2)/length[1]. |
References: [1]. Astorgues-Xerri L, et al. OTX008, a selective small-molecule inhibitor of galectin-1, downregulates cancer cell proliferation, invasion and tumour angiogenesis. Eur J Cancer. 2014 Sep;50(14):2463-77. | |
| Cas No. | 286936-40-1 | SDF | |
| 别名 | Calixarene 0118; PTX008 | ||
| 化学名 | 2,2',2'',2'''-[pentacyclo[19.3.1.13,7.19,13.115,19]octacosa-1(25),3,5,7(28),9,11,13(27),15,17,19(26),21,23-dodecaene-25,26,27,28-tetrayltetrakis(oxy)]tetrakis[N-[2-(dimethylamino)ethyl]-acetamide | ||
| Canonical SMILES | O=C(NCCN(C)C)COC1=C(C2)C=CC=C1CC3=CC=CC(CC4=CC=CC(CC5=CC=CC2=C5OCC(NCCN(C)C)=O)=C4OCC(NCCN(C)C)=O)=C3OCC(NCCN(C)C)=O | ||
| 分子式 | C52H72N8O8 | 分子量 | 937.2 |
| 溶解度 | DMF: 1 mg/ml,DMSO: 2 mg/ml,Ethanol: 5 mg/ml,PBS (pH 7.2): 0.5 mg/ml | 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 | 1.067 mL | 5.335 mL | 10.6701 mL |
| 5 mM | 0.2134 mL | 1.067 mL | 2.134 mL |
| 10 mM | 0.1067 mL | 0.5335 mL | 1.067 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
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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