PZ0197

Sigma-Aldrich

Pelitinib

≥98% (HPLC)

Sinónimos:
EKB-569, (2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide, WAY-EKB-569, EKB 569
Empirical Formula (Hill Notation):
C24H23ClFN5O2
Número de CAS:
Peso molecular:
467.92
NACRES:
NA.77

Nivel de calidad

100

ensayo

≥98% (HPLC)

formulario

powder

manufacturer/tradename

Pfizer®

condiciones de almacenamiento

desiccated
protect from light

color

white to beige

solubilidad

DMSO: 5 mg/mL, clear (warmed)

emisor

Pfizer

temp. de almacenamiento

−20°C

InChI

1S/C24H23ClFN5O2/c1-4-33-22-12-20-17(11-21(22)30-23(32)6-5-9-31(2)3)24(15(13-27)14-28-20)29-16-7-8-19(26)18(25)10-16/h5-8,10-12,14H,4,9H2,1-3H3,(H,28,29)(H,30,32)/b6-5+

InChI key

WVUNYSQLFKLYNI-AATRIKPKSA-N

Categorías relacionadas

Envase

5, 25 mg in glass bottle

Acciones bioquímicas o fisiológicas

Pelitinib (EKB-569) is an orally active, potent, second generation irreversible epidermal growth factor receptor tyrosine kinase (EGFR TK) inhibitor. Pelitinib is selective for EGFR (ErbB-1) with an IC50 about 80 nM, but also covalently binds to ErbB-2 (HER2/c-neu) and ErbB-4 (Her 4) with much lower potency. Pelitinib has been shown to inhibit the growth of EGFR-overexpressing tumor cell lines.

Otras notas

Light sensitive
This compound was developed by Pfizer for Kinase Phosphatase Biology research. To learn more about Sigma′s partnership with Pfizer and view other authentic, high-quality Pfizer compounds, visit sigma.com/bsm-pfizer.

To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Información legal

Sold for research purposes under agreement from Pfizer Inc.
Pfizer is a registered trademark of Pfizer, Inc.

pictogramas

Skull and crossbones

Palabra de señalización

Danger

Frases de peligro

Consejos de prudencia

RIDADR

UN 2811 6.1 / PGIII

WGK Alemania

WGK 3

Punto de inflamabilidad F

Not applicable

Punto de inflamabilidad C

Not applicable

Certificado de Análisis
Molly F Kulesz-Martin et al.
Cancer biology & therapy, 14(2), 95-99 (2012-11-30)
Current therapies for Renal Cell Carcinoma favor vascular endothelial growth factor receptor (VEGF-R) tyrosine kinase (TK) inhibitors (TKIs). In theory, these are most applicable in tumors that have lost VHL-with subsequent stabilization of HIF and upregulation of VEGF. A subset...
Shan Bian et al.
Nature methods, 15(8), 631-639 (2018-07-25)
Brain tumors are among the most lethal and devastating cancers. Their study is limited by genetic heterogeneity and the incompleteness of available laboratory models. Three-dimensional organoid culture models offer innovative possibilities for the modeling of human disease. Here we establish...
Kenneth K W To et al.
British journal of pharmacology, 172(16), 4089-4106 (2015-05-20)
Pelitinib is a potent irreversible EGFR TK inhibitor currently in clinical trials for the treatment of lung cancer. Hyperthermia has been applied concomitantly with chemotherapy and radiotherapy to enhance treatment outcome. In this study, we investigated the ability of the...
Yeong Hoon Kim et al.
The Korean journal of parasitology, 55(5), 491-503 (2017-11-07)
The effects of tyrosine kinase inhibitors (TKIs) were evaluated on growth inhibition of intracellular Toxoplasma gondii in host ARPE-19 cells. The number of tachyzoites per parasitophorous vacuolar membrane (PVM) was counted after treatment with TKIs. T. gondii protein expression was...
Jean-Philippe Coppé et al.
Nature cell biology, 21(6), 778-790 (2019-06-05)
Phosphorylation networks intimately regulate mechanisms of response to therapies. Mapping the phospho-catalytic profile of kinases in cells or tissues remains a challenge. Here, we introduce a practical high-throughput system to measure the enzymatic activity of kinases using biological peptide targets...

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