| 分子量(MW): | 410.39 | |
|---|---|---|
| 化学式: | C18H21F3N6O2 | |
| 溶解度: | DMSO ≥82mg/mL Water <1mg/mL Ethanol ≥25mg/mL | |
| 纯度: | >99% | |
| 稳定性: | at -20℃ 2 years | |
| CAS号: | 944396-07-0, 1312445-63-8 (HCl) |
BKM120 (NVP-BKM120) is a bioavailable specific oral pan-class I phosphatidylinositol 3-kinase (PI3K) kinase inhibitor. BKM120 inhibits tumor proliferation and survival by blocking the phosphatidylinositol-3-kinase (PI3K) pathway. BKM120 has shown significant cell growth inhibition and induction of apoptosis in a variety of tumor cell lines as well as in animal models. BKM120 specifically inhibits class I PIK3 in the PI3K/AKT kinase (or protein kinase B) signaling pathway in an ATP-competitive manner, thereby inhibiting the production of the secondary messenger phosphatidylinositol-3,4,5-trisphosphate and activation of the PI3K signaling pathway. This may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. Activation of the PI3K signaling pathway is frequently associated with tumorigenesis. Dysregulated PI3K signaling may contribute to tumor resistance to a variety of antineoplastic agents. [1][2][3]
| After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of BKM120 for 3h,followed by 20-minute stimolation of 100ng/ml EGF. |
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