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Thalidomide
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Thalidomide图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
200mg电议

产品介绍
Immunomodulatory agent,sedative drug,angiogenesis inhibitor

Cell lines

PBMCs

Preparation method

The solubility of this compound in DMSO is >11.8 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 ℃ for several months.

Reacting condition

0 ~ 100 μg/mL

Applications

Thalidomide dose-dependently increased the proliferative responses of PBMCs stimulated by immobilized anti-CD3. As the concentration of anti-CD3 increased, Thalidomide at a constant concentration of 10 μg/mL significantly induced the proliferative responses of PBMCs. However, Thalidomide exhibited no effect on the proliferative response in the absence of anti-CD3. These results indicated that Thalidomide was not mitogenic, Instead, it acted as a costimulator.

Animal models

Rabbits

Dosage form

200 mg/kg; p.o.

Applications

In rabbits, Thalidomide at the dose of 200 mg/kg inhibited the area of vascularized cornea, with a median inhibition of 36%. The inhibition of Thalidomide on angiogenesis was seen after only two doses. In addition, the rabbits did not show significant sedation, and there were no signs of toxicity or weight loss.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

产品描述

Thalidomide is initially promoted as a sedative, inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ~250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties.

Thalidomide is initially promoted as a sedative, has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties, and targets cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ~250 nM[1]. Thalidomide (50 μg/mL) potentiates the anti-tumor activity of icotinib against the proliferation of both PC9 and A549 cells, and this effect is correlated with apoptosis and cell migration. In addition, Thalidomide and icotinib inhibits the EGFR and VEGF-R2 pathways in PC9 cells[3].

Thalidomide (100 mg/kg, p.o.) inhibits the collagen deposition, down-regulates the mRNA expression level of α-SMA and collagen I, and significantly reduces the pro-inflammatory cytokines in RILF mice. Thalidomide alleviates RILF via suppression of ROS and down-regulation of TGF-β/Smad pathway dependent on Nrf2 status[2]. Thalidomide (200 mg/kg, p.o.) combined with icotinib shows synergistic anti-tumor effects in nude mice bearing PC9 cells, suppressing tumor growth and promoting tumor death[3].

References:
[1]. Fischer ES, et al. Structure of the DDB1-CRBN E3 ubiquitin ligase in complex with thalidomide. Nature. 2014 Aug 7;512(7512):49-53.
[2]. Bian C, et al. Thalidomide (THD) alleviates radiation induced lung fibrosis (RILF) via down-regulation of TGF-β/Smad3 signaling pathway in an Nrf2-dependent manner. Free Radic Biol Med. 2018 Dec;129:446-453.
[3]. Sun X, et al. Synergistic Inhibition of Thalidomide and Icotinib on Human Non-Small Cell Lung Carcinomas Through ERK and AKT Signaling. Med Sci Monit. 2018 May 15;24:3193-3203.