ETP-46321
Cat. No.:YN420124
产品名称: | ETP-46321 |
CAS No.: | 1252594-99-2 |
Chemical Name: | 5-[2-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-8-(4-morpholinyl)imidazo[1,2-a]pyrazin-6-yl]-2-pyrimidinamine |
Synonyms: | ETP-46321;ETP 46321;5-[2-[[4-(Methylsulfonyl)-1-piperazinyl]methyl]-8-(4-morpholinyl)imidazo[1,2-a]pyrazin-6-yl]-2-pyrimidinamine;5-(2-((4-(methylsulfonyl)piperazin-1-yl)methyl)-8-morpholinoimidazo[1,2-a]pyrazin-6-yl)pyrimidin-2-amine;5-[2-[(4-methylsulfo |
分子量: | 473.55 |
分子式: | C₂₀H₂₇N₉O₃S |
SMILES: | NC(N=C1)=NC=C1C2=CN3C=C(CN4CCN(S(=O)(C)=O)CC4)N=C3C(N5CCOCC5)=N2 |
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: | ETP-46321 是一种有效的PI3Kα和PI3Kδ抑制剂,Kiapp分别为 2.3 和 14.2 nM。 |
IC50和靶点: | [{name:"p110α:2.3 nM (Ki)"},{name: "PI3Kα-E545K:1.77 nM (Ki)"},{name: "PI3Kα-E542K:1.89 nM (Ki)"},{name: "PI3Kα-H1047R:2.33 nM (Ki)"},{name: "p110δ:14.2 nM (Ki)"},{name: "p110β:170 nM (Ki)"},{name: "p110γ:179 nM (Ki)"}] |
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González, S.M., Hernández, A.I., Varela, C., et al.Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitorBioorg. Med. Chem. Lett.22(10),3460-3466(2012)
Aragoneses-Fenoll, L., Montes-Casado, M., Ojeda, G., et al.ETP-46321, a dual p110α/δ class IA phosphoinositide 3-kinase inhibitor modulates T lymphocyte activation and collagen-induced arthritisBiochem. Pharmacol.106,56-69(2016)