PI-103是PI 3-激酶β ±-亚型的选择性抑制剂（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）。它还抑制DNA-PK（IC 50 = 2 nM）和mTOR 1和mTOR 2（IC 50 = 20 - 83 nM）。PI-103在10 μ M时对多种蛋白激酶几乎没有活性。PI-103通过在体外和体内阻断PI 3-K/Akt通路来阻断神经胶质瘤增殖。参考资料Powered by Bioz See more details on Bioz 1）Fan Q. 等（2006）中所述。“双重PI 3激酶/mTOR抑制剂揭示了胶质瘤的紧急疗效。“Cancer Cell 9：341-349.2）Smit M. A. T. R.盖革等人（2009年）。“Twist-Snail轴对TrkB诱导的上皮-间充质转化样转化失巢凋亡抵抗和转移至关重要。“Mol Cell Biol 29（13）：3722-37.3）Gursel D. B。 Y. S. Connell-Albert et al.（2011）.“通过受体酪氨酸激酶/PI 3 K/AKT信号传导轴控制星形细胞瘤细胞的增殖，并使用PI-103和TCN作为潜在的抗星形细胞瘤疗法。神经肿瘤学13（6）：610-621。
产品描述
PI-103 is a selective inhibitor for the α-isoform of PI 3-Kinase (IC50: PI 3-Kα = 8 nM PI 3-Kβ = 88 nM PI 3-Kδ = 48 nM PI 3-Kγ = 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 10μM. 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.
