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化驗
≥98% (HPLC)
形狀
powder
光學活性
[α]/D -95 to -115°, c = 0.5 in methanol
顏色
white to beige
溶解度
DMSO: 2 mg/mL, clear
儲存溫度
room temp
SMILES 字串
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
生化／生理作用
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。
法律資訊
根据辉瑞公司的协议出售，用于研究目的。
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
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
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
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