用逐渐增加浓度BEZ235处理PTEN-null细胞系PC3M和U87MG时,导致细胞增殖剂量依赖性减少。 参考文献:MairaSM, Stauffer F, Brueggen J, et al. Identification and characterization ofNVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammaliantarget of rapamycin inhibitor with potent in vivo ...
对于既往经CDK4/6抑制剂治疗后伴PIC3CA突变的HR阳性HER-2阴性晚期乳腺癌患者,BYLieve研究首次证实,CDK4/6抑制剂治疗后,接受Alpelisib联合芳香化酶抑制剂(aromatase inhibitor, AI)或氟维司群均可获益。同时,既往CDK4/6抑制剂治疗持续时...
参考文献 [1] Green LJ,Marder P,Ray C,et al. Development and validation of a drug activity biomarker that shows target inhibition in cancer patients receiving enzastaurin, a novel protein kinase C-h inhibitor. Clin Cancer Res 2006;12: 3408–15. [2] Dangelmaier C, Kunapuli S P. Protease...
PI3K/mTOR Inhibitor-2 PI3K/mTOR Inhibitor-2是一种有效的双重泛PI3K/mTOR抑制剂,具有抗肿瘤活性。 PI-103 PI-103 是一种多靶点 PI3K 抑制剂,在无细胞试验中作用于p110α/β/δ/γ的IC50为2 nM/3 nM/3 nM/15 nM,对 mTOR/DNA-PK的作用较小,IC50为30 nM/23 nM。PI-103 可诱导小鼠T细胞淋巴瘤的凋...
econazole was a new type of PI3K inhibitor, which inhibited the PI3K/AKT signaling pathway and reversed the resistance of breast cancer cells to doxorubicin137. Some studies showed that phenybutyl isoselenocyanate (ISC-4) treatment significantly inhibited PI3K/AKT activation in a dose-dependent manne...
BKM120, also known as NVP-BKM120, is another effective pan-class I PI3K inhibitor that exerts a strong inhibitory effect on p110-α and p110β enzymes, with IC50 values of 52 nM and 166 nM, respectively. It also effectively inhibits p110δ and p110γ enzymes, with IC50 values of...
5. Rugo HS, et al. Capivasertib and fulvestrant (F) for patients (pts) with aromatase inhibitor (AI)-resistant HR+/HER2- advanced breast cancer (ABC): second progression-free survival (PFS2) and time to first subsequent chemotherapy (TFSC) in the CAPItello-291 trial. 2024 ESMO BC. 183...
41.Mandal M, Kim S, Younes MN, Jasser SA, El-Naggar AK, Mills GB, Myers JN. The Akt inhibitor KP372-1 suppresses Akt activity and cell proliferation and induces apoptosis in thyroid cancer cells.Br J Cancer. 2005;92:1899-1905.[PubMed] ...
关键词 胰腺炎; 磷酸肌醇3-激酶类; 蛋白质丝氨酸苏氨酸激酶; Toll 样受体4; 胰岛素样生长因子Ⅰ;Wortmannin; 肿瘤坏死因子 α; 白细胞介素 6Effect of Agonist and Inhibitor of PI3K/AKT on Inflammatory Response in Macrophages WANG Jing 1 ,XUPing 1 ,YANG Zhiwen 2 ,XU Kai 1 ,LAI Yuexing 1 .1 ...
human cancer cellsin vitroandin vivo. Moreover, the combination of an inhibitor with various cytotoxic agents enhances the anti-tumor efficacy. Therefore, specific inhibition of the activation of Akt may be a valid approach to treating human malignancies and overcoming the resistance of cancer cells...