Taselisib
Cat. No.：YN420188
CAS No. ：1282512-48-4
规格
价格(RMB)
库存
| 产品名称: | Taselisib |
| CAS No.: | 1282512-48-4 |
| Chemical Name: | 4-[5,6-dihydro-2-[3-methyl-1-(1-methylethyl)-1H-1,2,4-triazol-5-yl]imidazo[1,2-d][1,4]benzoxazepin-9-yl]-α,α-dimethyl-1H-pyrazole-1-acetamide |
| Synonyms: | GDC-0032; RG-7604 |
| 分子量: | 460.53 |
| 分子式: | C₂₄H₂₈N₈O₂ |
| SMILES: | CC(C)N1C(C2=CN3C(C(C(OCC3)=C4)=CC=C4C5=CN(C(C)(C(N)=O)C)N=C5)=N2)=NC(C)=N1 |
| 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: | Taselisib (GDC-0032) 是一种有效的PI3K抑制剂，靶向作用于突变PI3KCA。Taselisib 抑制 PI3Kα，PI3Kβ 和 PI3Kγ，IC50分别为 0.29 nM，0.91 nM，0.97 nM。 |
| IC50和靶点: | [{name:"PI3Kδ:0.12 nM (Ki)"},{name: "PI3Kα:0.29 nM (Ki)"},{name: "PI3Kγ:0.97 nM (Ki)"},{name: "PI3Kβ:9.1 nM (Ki)"}] |
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Ndubaku, C.O., Heffron, T.P., Staben, S.T., et al.Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): A β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activityJ. Med. Chem.56(11),4597-45610(2013)
Lopez, S., Schwab, C.L., Cocco, E., et al.Taselisib, a selective inhibitor of PIK3CA, is highly effective on PIK3CA-mutated and HER2/neu amplified uterine serous carcinoma in vitro and in vivoGynecol. Oncol.135(2),312-317(2014)
Zumsteg, Z.S., Morse, S., Krigsfeld, G., et al.Taselisib (GDC-0032), a potent β-sparing small molecule inhibitor of PI3K, radiosensitizes head and neck squamous carcinomas containing activating PIK3CA alterationsClin. Cancer Res.22(8),2009-2019(2016)
