Buparlisib
Cat. No.:YN420281
产品名称: | Buparlisib |
CAS No.: | 944396-07-0 |
Chemical Name: | 5-(2,6-di-4-morpholinyl-4-pyrimidinyl)-4-(trifluoromethyl)-2-pyridinamine |
Synonyms: | 布帕尼西; BKM120; NVP-BKM120 |
分子量: | 410.39 |
分子式: | C₁₈H₂₁F₃N₆O₂ |
SMILES: | FC(F)(C1=C(C2=CC(N3CCOCC3)=NC(N4CCOCC4)=N2)C=NC(N)=C1)F |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | Buparlisib (BKM120; 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。 |
IC50和靶点: | [{name:"p110α:52 nM (IC50)"},{name: "p110β:166 nM (IC50)"},{name: "p110δ:116 nM (IC50)"},{name: "p110γ:262 nM (IC50)"},{name: "Vps34:2.4 μM (IC50)"},{name: "p110α-H1047R:58 nM (IC50)"},{name: "p110α-E545K:99 nM (IC50)"},{name: "mTOR:4.6 μM (IC50)"}] |
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Maira, S.M., Pecchi, S., Huang, A., et al.Identification and characterization of NVP-BKM120, an orally available pan-class I PI3-kinase inhibitorMol. Cancer Ther.11(2),317-328(2012)
Koul, D., Fu, J., Shen, R., et al.Antitumor activity of NVP-BKM120--a selective pan class I PI3 kinase inhibitor showed differential forms of cell death based on p53 status of glioma cellsClin. Cancer Res.18(1),184-195(2012)
Park, E., Park, J., Han, S.W., et al.NVP-BKM120, a novel PI3K inhibitor, shows synergism with a STAT3 inhibitor in human gastric cancer cells harboring KRAS mutationsInt. J. Oncol.40(4),1259-1266(2012)
de Gooijer, M.C., Zhang, P., Buil, L.C.M., et al.Buparlisib is a brain penetrable pan-PI3K inhibitorSci. Rep.8(1),10784(2018)