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Merck
CN

PZ0039

Lorlatinib

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

Synonym(s):

(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, PF-6463922

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About This Item

Empirical Formula (Hill Notation):
C21H19FN6O2
CAS Number:
1924207-18-0
Molecular Weight:
406.41
UNSPSC Code:
51111800
NACRES:
NA.77
MDL number:
MFCD28144520

Key Documents

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Product Name

Lorlatinib, ≥98% (HPLC)

InChI key

IIXWYSCJSQVBQM-LLVKDONJSA-N

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

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

Biochem/physiol Actions

Lorlatinib (PF-06463922) is a potent, selective brain-penetrable inhibitor of both anaplastic lymphoma kinase (ALK) and c-ros Oncogene 1 (ROS1) with strong activity against most known ALK and ROS1 mutants identified in patients with crizotinib-resistant disease. It is in clinical trials for the treatment of non–small cell lung cancer (NSCLC).
Potent, selective inhibitor of both ALK and ROS1

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000445475
0000445475
0000361297
0000361297
0000188851

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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

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