Department of Child and Adolescent Psychiatry, University Hospital of Marburg, Marburg, Germany;
Bio 21 Institute, CSL Limited Melbourne, Parkville, VIC, Australia.
In Vivo. 2021 Mar-Apr;35(2):721-729. doi: 10.21873/invivo.12313.
BACKGROUND/AIM: We evaluated the potential of the kinase inhibitors sorafenib, lenvatinib and selumetinib on increasing the uptake of technetium-99m into thyroid cancer cells.
Four established cell lines and three patient's cell cultures were treated with 0.1, 1 and 5 μM of sorafenib, lenvatinib and selumetinib for 72 hours. After incubation with 1 MBq of technetium-99m, the radioactivity uptake was measured.
The experiments showed heterogeneous results. Maximum technetium-99m uptake increases of 312% (sorafenib), 326% (lenvatinib) and 759% (selumetinib) were obtained using the highest applied concentrations. In some tests, an uptake reduction or no effect was observed.
Kinase inhibitors have a positive effect on technetium-99m uptake. Due to study limitations, a redifferentiating effect of the drugs could not be definitely proven. Unspecific cytotoxicity might have a confounding effect.
背景/目的:我们评估了激酶抑制剂索拉非尼、仑伐替尼和塞尔美替尼增加甲状腺癌细胞摄取锝-99m 的潜力。
用 0.1、1 和 5 μM 的索拉非尼、仑伐替尼和塞尔美替尼处理 4 种已建立的细胞系和 3 种患者细胞培养物 72 小时。孵育 1MBq 的锝-99m 后,测量放射性摄取。
实验结果存在异质性。最高应用浓度下,锝-99m 的摄取增加了 312%(索拉非尼)、326%(仑伐替尼)和 759%(塞尔美替尼)。在一些测试中,观察到摄取减少或无影响。
激酶抑制剂对锝-99m 的摄取有积极影响。由于研究的局限性,不能确定药物的再分化作用。非特异性细胞毒性可能有混杂影响。