PI-103是PI 3-激酶β ±-亞型的選擇性抑制劑(IC 50:PI 3-κ ± = 8 nM PI 3-κ 2 = 88 nM PI 3-κ 2 = 48 nM PI 3-κ 2 = 150 nM)。它還抑制DNA-PK(IC 50 = 2 nM)和mTOR 1和mTOR 2(IC 50 = 20 - 83 nM)。PI-103在10 μ M時對多種蛋白激酶幾乎沒有活性。PI-103通過在體外和體內(nèi)阻斷PI 3-K/Akt通路來阻斷神經(jīng)膠質(zhì)瘤增殖。參考資料Powered by Bioz See more details on Bioz 1)Fan Q. 等(2006)中所述。“雙重PI 3激酶/mTOR抑制劑揭示了膠質(zhì)瘤的緊急療效。“Cancer Cell 9:341-349.2)Smit M. A. T. R.蓋革等人(2009年)。“Twist-Snail軸對TrkB誘導的上皮-間充質(zhì)轉(zhuǎn)化樣轉(zhuǎn)化失巢凋亡抵抗和轉(zhuǎn)移至關重要。“Mol Cell Biol 29(13):3722-37.3)Gursel D. B。 Y. S. Connell-Albert et al.(2011).“通過受體酪氨酸激酶/PI 3 K/AKT信號傳導軸控制星形細胞瘤細胞的增殖,并使用PI-103和TCN作為潛在的抗星形細胞瘤療法。神經(jīng)腫瘤學13(6):610-621。
產(chǎn)品描述
PI-103 is a selective inhibitor for the ?±-isoform of PI 3-Kinase (IC50: PI 3-K?± = 8 nM PI 3-K?2 = 88 nM PI 3-K?′ = 48 nM PI 3-K?3 = 150 nM). It is also inhibits DNA-PK (IC50 = 2 nM) and mTOR1 and mTOR2 (IC50 = 20 & 83 nM). PI-103 shows little activity against a wide array of protein kinases at 10??M. PI-103 blocks glioma proliferation by blocking the PI 3-K/Akt pathway in vitro and in vivo.References Powered by Bioz See more details on Bioz1) Fan Q. et al. (2006) ."A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma." Cancer Cell 9: 341-349.2) Smit M. A. T. R. Geiger et al. (2009). "A Twist-Snail axis critical for TrkB-induced epithelial-mesenchymal transition-like transformation anoikis resistance and metastasis." Mol Cell Biol 29(13): 3722-37.3) Gursel D. B. Y. S. Connell-Albert et al. (2011). "Control of proliferation in astrocytoma cells by the receptor tyrosine kinase/PI3K/AKT signaling axis and the use of PI-103 and TCN as potential anti-astrocytoma therapies." Neuro-Oncology 13(6): 610-621.