Lorlatinib
Cat. No.：YN440198
CAS No. ：1454846-35-5
规格
价格(RMB)
库存
| 产品名称: | Lorlatinib |
| CAS No.: | 1454846-35-5 |
| Chemical Name: | (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 |
| Synonyms: | 劳拉替尼; PF-06463922 |
| 分子量: | 406.41 |
| 分子式: | C₂₁H₁₉FN₆O₂ |
| SMILES: | CN1C(C#N)=C2C(CN(C)C(C3=C([C@@H](C)OC4=C(N)N=CC2=C4)C=C(F)C=C3)=O)=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: | Lorlatinib (PF-06463922) 是一种具有口服活性，选择性，脑渗透性和 ATP 竞争性的ROS1/ALK抑制剂。Lorlatinib 对于 ROS1，野生型 ALK 和 ALKL1196M的Ki分别为 <0.025 nM，<0.07 nM 和 0.7 nM。Lorlatinib 具有抗癌活性。 |
| IC50和靶点: | |
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Johnson, T.W., Richardson, P.F., Bailey, S., et al.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 lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain exposure and broad-spectrum potency against ALK-resistant mutationsJ. Med. Chem.57(11),4720-4744(2014)
Awad, M.M., and Shaw, A.T.ALK inhibitors in non-small cell lung cancer: Crizotinib and beyondClin. Adv. Hematol. Oncol.12(7),429-439(2014)
Zou, H.Y., Li, Q., Engstrom, L.D., et al.PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutationsProc. Natl. Acad. Sci. USA112(11),3493-3498(2015)
Yamazaki, S., Lam, J.L., Zou, H.Y., et al.Translational pharmacokinetic-pharmacodynamic modeling for an orally available novel inhibitor of anaplastic lymphoma kinase and c-Ros oncogene 1J. Pharmacol. Exp. Ther.351,67-76(2014)
