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Merck
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PZ0039

Sigma-Aldrich

Lorlatinib

≥98% (HPLC)

Sinónimos:

(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

Fórmula empírica (notación de Hill):
C21H19FN6O2
Número de CAS:
1924207-18-0
Peso molecular:
406.41
MDL number:
MFCD28144520
UNSPSC Code:
51111800
NACRES:
NA.77

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

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).

Legal Information

Sold for research purposes under agreement from Pfizer Inc.

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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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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