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Crizotinib
$35 – $209
Products Details
Product Description
– Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition[1][2][3].
Web ID
– HY-50878
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C21H22Cl2FN5O
Citations
– ACS Omega. 2023 Jun 14.|Biochem Pharmacol. 2021 Aug;190:114620.|Biochim Biophys Acta Mol Cell Res. 2020 Jul;1867(7):118712.|Biomed Chromatogr. 2019 Oct;33(10):e4611.|Blood Adv. 2023 Feb 10;bloodadvances.2022008384.|Blood. 2021 Oct 17;blood.2020008136.|Braz J Pharm Sci. 2015 Jun;51(2):2175-9790.|Cancer Discov. 2018 Mar;8(3):354-369.|Cancer Lett. 2018 May 28;422:19-28.|Cancer Med. 2020 Jun;9(12):4350-4359.|Cancer Res. 2015 Nov 1;75(21):4548-59. |Cancers (Basel). 2017 Oct 30;9(11). pii: E149. |Cell Rep Med. 2023 Jan 10;100911.|Dis Model Mech. 2016 Sep 1;9(9):941-52.|Eberhard Karls Universität Tübingen. 2023 Sep 18.|EBioMedicine. 2022 Dec 14;87:104410.|Eur J Drug Metab Pharmacokinet. 2021 Jul 18;1-11.|Eur J Med Chem. 2017 Oct 20;139:674-697.|Evid Based Complement Alternat Med. 2019 Nov 7;2019:4253846.|Exp Cell Res. 2020 Aug 1;393(1):112054.|Front Oncol. 2020 May 12;10:696.|Fundam Clin Pharmacol. 2021 Feb 1.|Harvard Medical School LINCS LIBRARY|Int J Mol Sci. 2022 Sep 17;23(18):10895.|Invest New Drugs. 2023 Apr 10.|J Cancer Res Clin Oncol. 2021 Jan;147(1):167-175.|J Exp Clin Cancer Res. 2022 Mar 29;41(1):113.|J Med Chem. 2021 Mar 11;64(5):2725-2738.|J Med Chem. 2021 Sep 21.|J Pharm Anal. 2021 Jun 19.|J Solution Chem. 2014 Jul;43(7):1282-1295.|J Transl Med. 2023 Aug 5;21(1):530.|Mol Oncol. 2017 Aug;11(8):996-1006.|Nat Biomed Eng. 2018 Aug;2(8):578-588.|Oncogene. 2018 Mar;37(11):1417-1429.|Oncotarget. 2014 May 15;5(9):2688-702.|Oncotarget. 2016 May 17;7(20):29011-22. |Oncotarget. 2019 Aug 13;10(48):4937-4950.|PLoS One. 2021 Jun 8;16(6):e0252907.|PLoS One. 2019 Feb 11;14(2):e0212048. |Proteomes. 2023 Jun 2, 11(2), 20.|Research Square Preprint. 2022 Feb.|Research Square Print. 26 Oct, 2022|Research Square Print. September 14th, 2022.|Saudi Pharm J. 2015 Jan;23(1):75-84. |Sci Signal. 2014 Oct 28;7(349):ra102. |Sci Signal. 2015 Dec 8;8(406):ra125. |Sci Transl Med. 1 Sep 2021.|Sci Transl Med. 2018 Jul 18;10(450):eaaq1093.|Spectrochim Acta A Mol Biomol Spectrosc. 2014 Oct 15;131:347-54.|Spectrochim Acta A Mol Biomol Spectrosc. 2021 Oct 5;259:119884.|Stem Cell Reports. 2017 Dec 12;9(6):1948-1960.|Talanta. 2019 Aug 15;201:217-225.|Technical University of Munich. 24.01.2018.|Transl Oncol. 2021 Jan;14(1):100887.|Transl Oncol. 2021 Nov 22;15(1):101272.|J Hematol Oncol. 2018 Aug 29;11(1):109.
References
– [1]Zou HY, 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(9), 4408-4417.|[2]Cui JJ, et al. Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). J Med Chem. 2011 Sep 22;54(18):6342-63.|[3]Cullinane C, et al. Differential (18)F-FDG and 3′-deoxy-3′-(18)F-fluorothymidine PET responses to pharmacologic inhibition of the c-MET receptor in preclinical tumor models. J Nucl Med. 2011 Aug;52(8):1261-7|[4]Christensen JG, et al. Cytoreductive antitumor activity of PF-2341066, a novel inhibitor of anaplastic lymphoma kinase and c-Met, in experimental models of anaplastic large-cell lymphoma. Mol Cancer Ther. 2007, 6(12 Pt 1), 3314-3322.|[5]Shen A, et al. c-Myc alterations confer therapeutic response and acquired resistance to c-Met inhibitors in MET-addicted cancers. Cancer Res. 2015 Nov 1;75(21):4548-59.|[6]Umapathy G, et al. The kinase ALK stimulates the kinase ERK5 to promote the expression of the oncogene MYCN in neuroblastoma. Sci Signal. 2014 Oct 28;7(349):ra102.|[7]Tucker ER, et al. Immunoassays for the quantification of ALK and phosphorylated ALK support the evaluation of on-target ALK inhibitors in neuroblastoma. Mol Oncol. 2017 Aug;11(8):996-1006.|[8]Liu H, et al. Identifying and Targeting Sporadic Oncogenic GeneticLiu H, et al. Identifying and Targeting Sporadic Oncogenic Genetic Aberrations in Mouse Models of Triple Negative Breast Cancer. Cancer Discov. 2018 Mar;8(3):354-369.
CAS Number
– 877399-52-5
Molecular Weight
– 450.34
Compound Purity
– 99.97
SMILES
– ClC1=C(F)C=CC(Cl)=C1[C@H](OC2=CC(C3=CN(N=C3)C4CCNCC4)=CN=C2N)C
Clinical Information
– Launched
Research Area
– Cancer
Solubility
– DMSO : 20 mg/mL (ultrasonic;warming;heat to 60°C)|H2O : < 0.1 mg/mL (ultrasonic)
Target
– Anaplastic lymphoma kinase (ALK);Autophagy;c-Met/HGFR;ROS Kinase
Pathway
– Autophagy;Protein Tyrosine Kinase/RTK
Product type
– Reference compound
Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.
