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方案
≥98% (HPLC)
表单
powder
旋光性
[α]/D -95 to -115°, c = 0.5 in methanol
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
room temp
SMILES字符串
NC1=C(O[C@@H](C2=C3C=CC(F)=C2)C)C=C(C4=C(C#N)N(C)N=C4CN(C)C3=O)C=N1
InChI key
IIXWYSCJSQVBQM-LLVKDONJSA-N
生化/生理作用
ALK和ROS1的有效选择性抑制剂
Lorlatinib (PF-06463922)是变性淋巴瘤激酶（ALK）和c-ros癌基因1（ROS1）的一种有效的选择性脑可穿透抑制剂，其对在克唑替尼耐药的患者中发现的大部分已知ROS1的ALK和ROS1突变体具有很强的活性。 它正被用于治疗非小细胞肺癌（NSCLC）的临床试验中。
法律信息
根据辉瑞公司的协议出售，用于研究目的。
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Liang Dong et al.
BMC pulmonary medicine, 18(1), 13-13 (2018-01-25)
Crizotinib is recommended as first-line therapy in ROS1-driven lung adenocarcinoma. However, the optimal first-line therapy for this subgroup of lung cancer is controversial according to the available clinical data. Here, we describe a 57-year-old man who was diagnosed with stage
Ted W Johnson et al.
Journal of medicinal chemistry, 57(11), 4720-4744 (2014-05-14)
Although crizotinib demonstrates robust efficacy in anaplastic lymphoma kinase (ALK)-positive non-small-cell lung carcinoma patients, progression during treatment eventually develops. Resistant patient samples revealed a variety of point mutations in the kinase domain of ALK, including the L1196M gatekeeper mutation. In
Alice T Shaw et al.
The Lancet. Oncology, 18(12), 1590-1599 (2017-10-28)
Most patients with anaplastic lymphoma kinase (ALK)-rearranged or ROS proto-oncogene 1 (ROS1)-rearranged non-small-cell lung cancer (NSCLC) are sensitive to tyrosine kinase inhibitor (TKI) therapy, but resistance invariably develops, commonly within the CNS. This study aimed to analyse the safety, efficacy
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