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Merck
CN

PZ0039

罗拉替尼

≥98% (HPLC), selective ALK and ROS1 inhibitor , powder

别名:

PF-06463922, PF-6463922, (10R)-7-氨基-12-氟-2,10,16-三甲基-15-氧代-10,15,16,17-四氢-2H.8,4-(甲基)吡唑并[4,3.h ] [2,5,11]-苯并二氮杂二环十四癸-3-甲腈

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选择尺寸

变更视图

关于此项目

经验公式(希尔记法):
C21H19FN6O2
化学文摘社编号:
分子量:
406.41
UNSPSC Code:
51111800
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
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产品名称

罗拉替尼, ≥98% (HPLC)

assay

≥98% (HPLC)

form

powder

optical activity

[α]/D -95 to -115°, c = 0.5 in methanol

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

room temp

SMILES string

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

Biochem/physiol Actions

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。


存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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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



全球贸易项目编号

货号GTIN
PZ0039-5MG04061835507634
PZ0039-25MG04061835507627