目前临床肿瘤治疗中,PI3K/Akt/mTOR是重要的靶向治疗信号通路。然而,仅抑制mTORC1活性,不是所有的肿瘤都能得到预期控制.雷帕霉素虽然能抑制mTORC1,但也能反馈性地增加PI3K信号活跃度,从而影响治疗预后。近来发现的第二代抑制剂可以同时抑制mTORC1/2和PI3K活性,这种抑制剂被认为在肿瘤治疗上颇具前景.本综述着重阐述了PI...
NVP-BKM120 是一种 pan-class IPI3K抑制剂,作用于p110α/p110β/p110δ/p110γ,IC50分别为 52 nM/166 nM/116 nM/262 nM。 Fields of Application : BKM120 is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM, respectively. Reduced potency against ...
by inhibiting mTORC1 activity alone, not all tumors can be expected to be controlled. Although rapamycin can inhibit mTORC1, it can also feedbackally increase PI3K signal activity, which affects the treatment prognosis. Recently discovered second-generation inhibitors can simultaneously...
分子式:C1COCCN1C2=NC(=NC(=C2)C3=CN=C(C=C3C(F)(F)F)N)N4CCOCC4 品牌:上海惠诚生物唧电话021-60496554 包装规格:1 mg BKM120试剂CAS号:944396-07-0纯度:≥98%化学式:C18H21F3N6O2熔点:分子量:410.39保存温度:+4°C产品介绍:Buparlisib, NVP-BKM120Wachsberger PR, Lawrence YR, Liu Y, et...
Buparlisib is an orally bioavailable, pan-class I PI3K inhibitor. We evaluated the safety and efficacy of buparlisib in patients with metastatic triple-negative breast cancer. Methods This was a single-arm phase 2 study enrolling patients with triple-negative metastatic breast cancer. Patients ...
Interestingly, BKM120 at micromolar range also affects the mTOR activity by downregulating the levels of S6 protein kinase (p70S6K) and eIF4E-binding protein 1 (4EBP1), two well-known mTORC1 substrates27,28,29,36. Furthermore, it has been documented that BKM120 synergizes with well ...
BEZ235 and NVP-BGT226 and the combined mTORC1 and mTORC2 inhibitors Torin 1, PP242 and KU-0063794 using long-term cultures of ALL cells (ALL-LTC) ... S Badura,T Tesanovic,H Pfeifer,... - 《Plos One》 被引量: 89发表: 2013年 Activity of the mTOR inhibitor RAD001, the dual mTOR ...
Here, we have analyzed the therapeutic potential of the pan-PI3K inhibitor NVP-BKM120 (BKM120), an orally bioavailable 2,6-dimorpholino pyrimidine derivative, which has entered clinical trials for solid tumors, on both T-ALL cell lines and patient samples. BKM120 treatment resulted in G2/M ...