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Merck

PZ0271

Sigma-Aldrich

PF-06463922 acetate

≥98% (HPLC)

Synonym(e):

(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

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About This Item

Empirische Formel (Hill-System):
C21H19FN6O2 · CH3COOH
CAS-Nummer:
Molekulargewicht:
466.46
UNSPSC-Code:
12352200
PubChem Substanz-ID:
NACRES:
NA.77

Qualitätsniveau

Assay

≥98% (HPLC)

Form

powder

Farbe

white to beige

Löslichkeit

DMSO: 10 mg/mL, clear

Lagertemp.

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

InChIKey

BLNAIBLTPYGILH-RFVHGSKJSA-N

Anwendung

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

Biochem./physiol. Wirkung

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).

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable


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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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