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Submit ReviewPF 06463922
说明： High affinity and selective ALK and ROS1 inhibitor
别名： Lorlatinib
化学名： (10R)-7-Amino-12-fluoro-10,15,16,17-tetrahydro-2,10,16-trimethyl-15-oxo-2H-4,8-methenopyrazolo[4,3-h][2,5,11]benzoxadiazacyclotetradecine-3-carbonitrile
纯度： ≥98% (HPLC)
生物活性 for PF 06463922
High affinity and selective ALK and ROS1 inhibitor (Ki values are <0.02, <0.07 and 0.7 nM for ROS1, wild-type ALK and ALK-L1196M, respectively). Exhibits >100-fold selectivity for ROS1 over a panel of 204 other kinases. Inhibits proliferation of BaF3 cells containing crizotinib-resistant ROS1 mutation in vitro. Inhibits tumor growth in relevant mouse models. Orally available and brain penetrant.
许可信息
Sold for research purposes under agreement from Pfizer Inc.
技术数据 for PF 06463922
| 分子量 | 406.41 |
| 公式 | C21H19FN6O2 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1454846-35-5 |
| PubChem ID | 71731823 |
| InChI Key | IIXWYSCJSQVBQM-LLVKDONJSA-N |
| Smiles | C[C@@H](O3)C4=C(C=CC(F)=C4)C(N(C)CC1=NN(C)C(C#N)=C1C2=CC3=C(N)N=C2)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
产品说明书 for PF 06463922
参考文献 for PF 06463922
参考文献是支持产品生物活性的出版物。
Johnson et al (2014) Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lympho J.Med.Chem. 57 4720 PMID: 24819116
Zou et al (2015) PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations. Proc.Natl.Acad.Sci.U.S.A. 112 3493 PMID: 25733882
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关键词: PF 06463922, PF 06463922 supplier, anaplastic, lymphoma, kinases, (ALK), inhibitors, inhibits, inhibition, ROS1, c-ros, oncogenes, cancer, PF06463922, Lorlatinib, ALK, 5640, Tocris Bioscience
1 篇 PF 06463922 的引用文献
引用文献是使用了 Tocris 产品的出版物。 PF 06463922 的部分引用包括：
Fadeev et al (2018) ALKALs are in vivo ligands for ALK family receptor tyrosine kinases in the neural crest and derived cells. Proc Natl Acad Sci U S A 115 E630 PMID: 29317532
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