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產(chǎn)品名稱

PF 02341066 - Crizotinib | PF 2341066

產(chǎn)品貨號(hào)

Axon 1660 CAS [877399-52-5] MF C21H22Cl2FN5OMW 450.34 Purity: 99% Optical purity: Optically pure Soluble in DMSO Description Potent, selective and ATP-competitive inhibitor of c-Met/HGF receptor and the nucleophosmin-anaplastic lymphoma kinase (NPM-ALK), with IC50 values to be 4 and 25 nM for c-Met and ALK respectively. (R)-Crizotinib is superior to standard chemotherapy in patients with previously treated, advanced non-smal-cell lung cancer with ALK rearrangement. Notably, (S)-Crizotinib (Axon 2296) was recently found to potently inhibit the MTH1 phosphatase enzyme, whereas the (R) enantiomer is inactive (IC50 values of 72 nM and 1375 nM resp.). References Certificates Categories Extra info A.T. Shaw et al. Crizotinib versus chemotherapy in advanced ALK-positive lung cancer. N. Engl. J. Med. 2013, 368, 2385-2394. ? HY Zou et al. An Orally Available Small-Molecule Inhibitor of c-Met, PF-2341066, Exhibits Cytoreductive Antitumor Efficacy through Antiproliferative and Antiangiogenic Mechanisms. Cancer Res. 2007, 67, 4408. ? SH Ou et al. Activity of Crizotinib (PF02341066), a Dual Mesenchymal-Epithelial Transition (MET) and Anaplastic Lymphoma Kinase (ALK) Inhibitor, in a Non-small Cell Lung Cancer Patient with De Novo MET Amplification. J. Thor. Oncol. 2011, 6(5), 942-946. ? K.V. Huber et al. Stereospecific targeting of MTH1 by (S)-crizotinib as an anticancer strategy. Nature. 2014, doi: 10.1038/nature13194. [Epub ahead of print] Certificate of Analysis Material Safety Data Sheet Cell Signaling & Oncology c-MET p53-Tumor Suppression RTK class X; EC 2.7.10.1 ALK Pfizer Licensed Products ALK c-MET Inhibitor; NPM-ALK inhibitor Chemical name (R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine Source information Pfizer compound; Sold for research purposes under agreement from Pfizer Inc. Parent CAS No. [877399-52-5] Order Size Unit Price Stock 10 mg €80.00 In Stock

產(chǎn)品價(jià)格

現(xiàn)貨詢價(jià)，電話：010-67529703

產(chǎn)品規(guī)格

產(chǎn)品品牌

axonmedchem

產(chǎn)品概述

產(chǎn)品詳情

PF 02341066 - Crizotinib | PF 2341066

Based on 14 reference(s) in Google Scholar 8 10 14

Axon 1660

CAS [877399-52-5]

MF C21H22Cl2FN5O
MW 450.34

Purity: 99%
Optical purity: Optically pure
Soluble in DMSO

PF 02341066

Description

Potent, selective and ATP-competitive inhibitor of c-Met/HGF receptor and the nucleophosmin-anaplastic lymphoma kinase (NPM-ALK), with IC50 values to be 4 and 25 nM for c-Met and ALK respectively. (R)-Crizotinib is superior to standard chemotherapy in patients with previously treated, advanced non-smal-cell lung cancer with ALK rearrangement.
Notably, (S)-Crizotinib (Axon 2296) was recently found to potently inhibit the MTH1 phosphatase enzyme, whereas the (R) enantiomer is inactive (IC50 values of 72 nM and 1375 nM resp.).

A.T. Shaw et al. Crizotinib versus chemotherapy in advanced ALK-positive lung cancer. N. Engl. J. Med. 2013, 368, 2385-2394.

HY Zou et al. An Orally Available Small-Molecule Inhibitor of c-Met, PF-2341066, Exhibits Cytoreductive Antitumor Efficacy through Antiproliferative and Antiangiogenic Mechanisms. Cancer Res. 2007, 67, 4408.

SH Ou et al. Activity of Crizotinib (PF02341066), a Dual Mesenchymal-Epithelial Transition (MET) and Anaplastic Lymphoma Kinase (ALK) Inhibitor, in a Non-small Cell Lung Cancer Patient with De Novo MET Amplification. J. Thor. Oncol. 2011, 6(5), 942-946.

K.V. Huber et al. Stereospecific targeting of MTH1 by (S)-crizotinib as an anticancer strategy. Nature. 2014, doi: 10.1038/nature13194. [Epub ahead of print]

Certificate of Analysis
Material Safety Data Sheet

Cell Signaling & Oncology c-MET p53-Tumor Suppression RTK class X; EC 2.7.10.1 ALK Pfizer Licensed Products ALK

c-MET Inhibitor; NPM-ALK inhibitor

Chemical name

(R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine

Source information

Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.

Parent CAS No.

[877399-52-5]

產(chǎn)品資料

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