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PZ0191

Sigma-Aldrich

Crizotinib

Crizotinib

≥98% (HPLC)

Sinonimo/i:

(R)-3-[1-(2,6-Dichloro-3-fluoro-phenyl)-ethoxy]-5-(1-piperidin-4-yl-1H-pyrazol-4-yl)-pyridin-2-ylamine, PF 2341066, PF-02341066, PF02341066, Xalkori

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5 MG
CHF 132.00

CHF 132.00

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CHF 132.00

About This Item

Formula empirica (notazione di Hill):
C21H22Cl2FN5O
Numero CAS:
877399-52-5
Peso molecolare:
450.34
Numero MDL:
MFCD12407409
Codice UNSPSC:
12352200
ID PubChem:
329823765
NACRES:
NA.77

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Saggio

≥98% (HPLC)

Stato

powder

Colore

white to tan

Temperatura di conservazione

room temp

Stringa SMILE

C[C@@H](Oc1cc(cnc1N)-c2cnn(c2)C3CCNCC3)c4c(Cl)ccc(F)c4Cl

InChI

1S/C21H22Cl2FN5O/c1-12(19-16(22)2-3-17(24)20(19)23)30-18-8-13(9-27-21(18)25)14-10-28-29(11-14)15-4-6-26-7-5-15/h2-3,8-12,15,26H,4-7H2,1H3,(H2,25,27)/t12-/m1/s1
KTEIFNKAUNYNJU-GFCCVEGCSA-N

Informazioni sul gene

human ... ALK(238) , MET(4233)

Applicazioni

Crizotinib has been used:
  • to investigate its effects on hepatocyte growth factor receptor (c-Met) expression, proliferation and apoptosis[1]
  • to block neurotrophic tyrosine kinase receptor type 1 (NTRK1) activity in epithelial cells[2]
  • to restore sensitivity to erlotinib[3]

Azioni biochim/fisiol

ATP-competitive c-MET / ALK Inhibitor
Crizotinib (PF-02341066) is an ATP-competitive inhibitor of the receptor tyrosine kinases (RTKs) c-Met (hepatocyte growth factor receptor) and anaplastic lymphoma kinase (ALK). Crizotinib is a highly specific inhibitor of c-Met and ALK among > 120 different RTKs surveyed. Crizotinib was approved for treatment of a subtype of nonsmall-cell lung cancer (NSCLC) with ALK fusion mutations.

Caratteristiche e vantaggi

This compound is a featured product for Kinase Phosphatase Biology research. Click here to discover more featured Kinase Phosphatase Biology products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

Note legali

Sold for research purposes under agreement from Pfizer Inc.

Avvertenze

Warning

Indicazioni di pericolo

H317,H319,H341,H400

Classi di pericolo

Aquatic Acute 1 - Eye Irrit. 2 - Muta. 2 - Skin Sens. 1

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable

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Certificati d'analisi (COA)

Lot/Batch Number
0000360769
0000360769
0000187253
034M4739V
091M4718V

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Shota Yamamoto et al.
Radiology, 272(2), 568-576 (2014-06-03)
To present a radiogenomic computed tomographic (CT) characterization of anaplastic lymphoma kinase (ALK)-rearranged non-small cell lung cancer (NSCLC) (ALK+). In this HIPAA-compliant institutional review board-approved retrospective study, CT studies, ALK status, and clinical-pathologic data in 172 patients with NSCLC from
Registered report: Widespread potential for growth factor-driven resistance to anticancer kinase inhibitors
Greenfield E, et al.
eLife, 3, e04037-e04037 (2014)
Zheng Liu et al.
Oncoimmunology, 9(1), 1758003-1758003 (2020-09-15)
Despite some of the oncogenic driver mutations that have been associated with increased expression of programmed death-ligand 1 (PD-L1), the correlation between PD-L1 expression and ROS1 fusion in NSCLC cells, especially for those with Crizotinib resistance has not been fully
Nicole R Infarinato et al.
Cancer discovery, 6(1), 96-107 (2015-11-12)
Neuroblastomas harboring activating point mutations in anaplastic lymphoma kinase (ALK) are differentially sensitive to the ALK inhibitor crizotinib, with certain mutations conferring intrinsic crizotinib resistance. To overcome this clinical obstacle, our goal was to identify inhibitors with improved potency that
Neurotrophic tyrosine kinase receptor 1 is a direct transcriptional and epigenetic target of IL-13 involved in allergic inflammation
Rochman M, et al.
Mucosal Immunology, 8(4), 785-785 (2015)
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