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PZ0271

Sigma-Aldrich

PF-06463922 acetate

≥98% (HPLC)

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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 acetate, Lorlatinib acetate
Empirical Formula (Hill Notation):
C21H19FN6O2 · CH3COOH
CAS Number:
1924207-18-0
Molecular Weight:
466.46
UNSPSC Code:
12352200
PubChem Substance ID:
329823805
NACRES:
NA.77

Quality Level

100

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 10 mg/mL, clear

storage temp.

room temp

SMILES string

CC(O)=O.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

1S/C21H19FN6O2.C2H4O2/c1-11-15-7-13(22)4-5-14(15)21(29)27(2)10-16-19(17(8-23)28(3)26-16)12-6-18(30-11)20(24)25-9-12;1-2(3)4/h4-7,9,11H,10H2,1-3H3,(H2,24,25);1H3,(H,3,4)/t11-;/m1./s1

InChI key

BLNAIBLTPYGILH-RFVHGSKJSA-N

Application

PF-06463922 acetate has been used as an inhibitor of anaplastic lymphoma kinase (ALK) to analyze the expression of adrenomedullin using qPCR.

Biochem/physiol Actions

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 all known ALK and ROS1 mutants identified in patients with crizotinib-resistant disease. PF-06463922 is in clinical trials for the treatment of non–small cell lung cancer (NSCLC).

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

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Early and late effects of pharmacological ALK inhibition on the neuroblastoma transcriptome
Shana Claeys
Oncotarget (2017)
Shana Claeys et al.
Oncotarget, 8(63), 106820-106832 (2018-01-02)
Neuroblastoma is an aggressive childhood malignancy of the sympathetic nervous system. Despite multi-modal therapy, survival of high-risk patients remains disappointingly low, underscoring the need for novel treatment strategies. The discovery of Here, we further dissected the transcriptional dynamic profiles of
Liying Chen et al.
The Journal of clinical investigation, 128(1), 446-462 (2017-12-05)
Pharmacologically difficult targets, such as MYC transcription factors, represent a major challenge in cancer therapy. For the childhood cancer neuroblastoma, amplification of the oncogene MYCN is associated with high-risk disease and poor prognosis. Here, we deployed genome-scale CRISPR-Cas9 screening of

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