产品名称:PI3K alpha抑制剂(CNX-1351) 英文名称:CNX-1351 产品货号:M01143 产品规格:1mL(10mM)|5mg|10mg CNX-1351是PI3K_alpha_高效选择性抑制剂,IC50值为6.8nM,对其他PI3K亚型作用弱20-400倍。 注:本品仅可用于科研实验,严禁用于临床医疗及其他用途!
Fruman DA, Rommel C. PI3K and cancer: lessons, challenges and opportunities. Nat Rev Drug Discov. 2014;13(2):140-156. Edgar K, Hong R, Song K, et al. GDC-0077 is a selective PI3K alpha inhibitor with robust efficacy in PIK3CA mutant hormone-positive breast cancer models. Cancer Res. ...
PI3K alpha inhibitorEPHB6quinazolin-4(3H)-one analog(DFX24)Cell cycle arrestApoptosisNon-Small cell lung cancer (NSCLC)EPHB6 is a metastasis inhibitory gene that is frequently decreased or deficiency in non-small cell lung cancer (NSCLC), which contributed to the subsequent development of distant...
1. Christine Fritsch, etc. Characterization of the Novel and Specific PI3Ka Inhibitor NVP-BYL719 and Development of the Patient Stratification Strategy for Clinical Trials.Small Molecule Therapeutics, 2014, 13.2. Setiawan V. W., etc. Breast cancer risk factors defined by estrogen and progesterone r...
The discovery of the pan-PI3K inhibitor copanlisib with careful optimization of functionality around the scaffold. Article CAS PubMed PubMed Central Google Scholar Furet, P. et al. Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical ...
2.Seeking alpha in PI3K inhibition. 3.Pi3K inhibitors as new cancer therapeutics: implications for clinicaltrial design. 4.Novel Molecular-targeted Antitumor Drugs-PI3K Inhibitor. 2018年8月全球批准新药概况 乳腺癌最有潜力靶点——CDK4/6抑制剂盘点与解析 ...
体内：GDC-0077 (po) 在患者来源的PIK3CA-突变乳腺癌异种移植模型中以剂量依赖性方式导致肿瘤消退、细胞凋亡诱导和 pAKT、pPRAS40 和 pS6RP 减少<支持>[1]。参考文献：[1]. R Hong, Abstract PD4-14: GDC-0077 is a selective PI3Kalpha inhibitor that demonstrates robust efficacy in PIK3CA mutant breast ...
[5] Hong R., et al. GDC-0077 is a selective PI3K alpha inhibitor that demonstrates robust efficacy in PIK3CA mutant breast cancer models as a single agent and in combination with standard of care therapies. Cancer Res. 2018;78(4):4-14. ...
Alpelisib 对大鼠 (1 mg/kg, iv) 具有中等的终末消除半衰期 (t1/2=2.9±0.2 h) [1] .参考文献：[1]. Furet P, et al. Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation. Bioorg Med Chem Lett. 2013 Jul 1;23(13):...
[1]. Furet P, et al. Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation. Bioorg Med Chem Lett. 2013 Jul 1;23(13):3741-8. [2]. Fritsch C, et al. Characterization of the novel and specific PI3Kα inhibitor NVP-BY...