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PZ0039

Lorlatinib

Name: Lorlatinib
Brand: SIGMA

≥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

Assay:

≥98% (HPLC)

Form:

powder

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Properties

Product Name

Lorlatinib, ≥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

Description

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

0000361297

0000188851

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Long-term progression-free survival in an advanced lung adenocarcinoma patient harboring EZR-ROS1 rearrangement: a case report.

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

Discovery of (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), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain exposure and broad-spectrum potency against ALK-resistant mutations.

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

Lorlatinib in non-small-cell lung cancer with ALK or ROS1 rearrangement: an international, multicentre, open-label, single-arm first-in-man phase 1 trial.

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

Global Trade Item Number

SKU	GTIN
PZ0039-5MG	04061835507634
PZ0039-25MG	04061835507627