Ibrutinib
Cat. No.:YN430041
产品名称: | Ibrutinib |
CAS No.: | 936563-96-1 |
Chemical Name: | 1-[(3R)-3-[4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinyl]-2-propen-1-one |
Synonyms: | 伊布替尼; PCI-32765 |
分子量: | 440.50 |
分子式: | C₂₅H₂₄N₆O₂ |
SMILES: | C=CC(N1C[C@H](N2N=C(C3=CC=C(OC4=CC=CC=C4)C=C3)C5=C(N)N=CN=C52)CCC1)=O |
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: | Ibrutinib (PCI-32765) 是一种不可逆的选择性Btk抑制剂,IC50值为 0.5 nM。Ibrutinib 可作为 Btk 配体,用于合成一系列 PROTAC 分子,如 P13I。P13I 作用于人 Burkitt’s 淋巴瘤 RAMOS 细胞,浓度为 10 和 100 nM 时,分别降解 73% 和 89% Btk。 |
IC50和靶点: | |
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Leslie, L.A., and Younes, A.Targeting oncogenic and epigenetic survival pathways in lymphomaLeuk. Lymphoma.54(11),2365-2376(2013)
Honigberg, L.A., Smith, A.M., Sirisawad, M., et al.The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancyProc. Natl. Acad. Sci. USA107(29),13075-13080(2010)
Herman, S.E.M., Gordon, A.L., Hertlein, E., et al.Bruton tyrosine kinase represents a promising therapeutic target for treatment of chronic lymphocytic leukemia and is effectively targeted by PCI-32765Blood117(23),6287-6296(2011)
Wu, M., Akinleye, A., and Zhu, X.Novel agents for chronic lymphocytic leukemiaJ. Hematol. Oncol.6,36(2013)