Crizotinib (hydrochloride)

Crizotinib (hydrochloride)

• CAS Number: 1415560-69-8
• UNSPSC Description: Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition[1][2][3].
• Target Antigen: Anaplastic lymphoma kinase (ALK); Autophagy; c-Met/HGFR; ROS Kinase
• Type: Reference compound
• Related Pathways: Autophagy;Protein Tyrosine Kinase/RTK
• Applications: Cancer-Kinase/protease
• Field of Research: Cancer
• Assay Protocol: https://www.medchemexpress.com/Crizotinib-hydrochloride.html
• Purity: 99.86
• Solubility: DMSO : ≥ 4.9 mg/mL|H2O : 50 mg/mL (ultrasonic)
• Smiles: ClC1=C(F)C=CC(Cl)=C1[C@H](OC2=CC(C3=CN(N=C3)C4CCNCC4)=CN=C2N)C.Cl
• Molecular Weight: 486.80
• References & Citations: [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]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.|[3]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.|[4]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):1261-7J Hematol Oncol. 2018 Aug 29;11(1):109. |ACS Omega. 2023 Jun 14.|Arch Biochem Biophys. 2024 Jan 26:109905.|Biochem Pharmacol. 2021 Aug;190:114620.|Biochim Biophys Acta Mol Cell Res. 2020 Jul;1867(7):118712.|Biomark Res. 2024 Jan 25;12(1):13.|Biomed Chromatogr. 2019 Oct;33(10):e4611.|Biomed Chromatogr. 2024 Oct;38(10):e5986.|bioRxiv. 2024 Nov 6:2024.11.04.621884.|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 Discov. 2023 Mar 1;13(3):598-615.|Cancer Discov. 2024 Sep 13:OF1-OF20.|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. |Cancers (Basel). 2024|Cell Rep Med. 2023 Jan 10;100911.|Cell Rep Med. 2024 Mar 19;5(3):101472.|Cell Rep Methods. 2023 Oct 23;3(10):100599.|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 Med Chem. 2024 Oct 3.|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.|Oncogene. 2024 Aug 29.|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.|Signal Transduct Target Ther. 2024 Mar 9;9(1):65.|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.
• Shipping Conditions: Room Temperature
• Storage Conditions: 4°C (Powder, sealed storage, away from moisture)
• Clinical Information: Launched