參考文獻(xiàn)及鳴謝
[1] Yu, Y.; Zhao, Y.; Choi, J. et al. ERK Inhibitor Ulixertinib Inhibits High-Risk Neuroblastoma Growth In Vitro and In Vivo. Cancers 2022, 14 (22).
[2] Sigaud, R. Rosch, L. Gatzweiler, C. et al. The first-in-class ERK inhibitor ulixertinib shows promising activity in mitogen-activated protein kinase (MAPK)-driven pediatric low-grade glioma models. Neuro-oncology 2023, 25 (3), 566-579.
[3] Winkler, M. Friedrich, J. Boedicker, C. et al. Co-targeting MCL-1 and ERK1/2 kinase induces mitochondrial apoptosis in rhabdomyosarcoma cells. Translational oncology 2022, 16, 101313.
[4] Jiang, H. Xu, M. Li, L. et al. Concurrent HER or PI3K Inhibition Potentiates the Antitumor Effect of the ERK Inhibitor Ulixertinib in Preclinical Pancreatic Cancer Models. Molecular cancer therapeutics 2018, 17 (10), 2144-2155.
[5] Xiao, C. Fan, T. Wang, D. et al. RAD21-mediated epigenetic regulation promotes lung adenocarcinoma progression and sensitizes cancer cells to ERK-targeted therapy. Cancer letters 2025, 634, 218062.
[6] Tiong, T. Y.; Chan, M. L. Wang, C. H. et al. Exosomal miR-21 determines lung-to-brain metastasis specificity through the DGKB/ERK axis within the tumor microenvironment. Life sciences 2023, 329, 121945.
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細(xì)胞系：A375 cells
方法：Cells were serum-starved overnight, and treated with BVD-523 (2 µM) or PD184352 (10 µM) for 30 min. before to PMA stimulation (100 ng/ml) for another 30 min. Cells were lysed in RIPA buffer and CDK12 immunoprecipitates were washed thrice in lysis buffer followed by three washes in kinase buffer.
濃度：2 µM
處理時間：30 min
參考文獻(xiàn)：Nat Commun. 2022 Oct 29;13(1):6457.
* 上述方法來自公開文獻(xiàn)，僅供相同目的實(shí)驗(yàn)參考。如實(shí)驗(yàn)?zāi)康�、材料、方法不同，請參考其他文獻(xiàn)。
 
動物實(shí)驗(yàn)參考
動物模型：Nude mice
配制：BVD-523 was suspended in 1% (w/v) CMC at the desired concentration and homogenized on ice at 6,500 rpm for 50 minutes.
劑量：50-100 mg/kg
給藥處理：Oral gavage
參考文獻(xiàn)：Mol Cancer Ther. 2017 Nov;16(11):2351-2363.
* 上述方法來自公開文獻(xiàn)，僅供相同目的實(shí)驗(yàn)參考。如實(shí)驗(yàn)?zāi)康�、材料、方法不同，請參考其他文獻(xiàn)。
體內(nèi)實(shí)驗(yàn)的工作液，建議現(xiàn)用現(xiàn)配，當(dāng)天使用；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過超聲和（或）加熱的方式助溶。
切勿一次性將產(chǎn)品全部溶解。
建議制定動物給藥及實(shí)驗(yàn)方案時，盡量參考已發(fā)表的相關(guān)實(shí)驗(yàn)文獻(xiàn)（溶劑種類及配比眾多，簡單地溶解目的化合物，并不能解決動物給藥依從性、體內(nèi)生物利用度、組織分布等相關(guān)問題，未必能保證目的化合物在動物體內(nèi)充分發(fā)揮生物學(xué)效用）。