Crizotinib (hydrochloride)

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].

Product Specifications

CAS Number

[1415560-69-8]

Product Name Alternative

PF-02341066 (hydrochloride)

UNSPSC

12352005

Target

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 Formula

C21H23Cl3FN5O

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) :1261-7

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, sealed storage, away from moisture)

Scientific Category

Reference compound1

Clinical Information

Launched

Citation 01

Int J Antimicrob Agents. 2025 Jun;65 (6) :107470.|J Hematol Oncol. 2018 Aug 29;11 (1) :109. |MedComm (2020) . 2025 Jul 21;6 (8) :e70286.|ACS Omega. 2023 Jun 14;8 (25) :22603-22612.|Arch Biochem Biophys. 2024 Mar:753:109905.|Biochim Biophys Acta Mol Cell Res. 2020 Jul;1867 (7) :118712.|Bioengineering (Basel) . 2025 Oct 19;12 (10) :1121.|Biol Methods Protoc. 2025 Feb 13;10 (1) :bpaf012.|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 Aug 8;7 (15) :4049-4063.|Blood Adv. 2025 Jul 2:bloodadvances.2024015322.|Blood. 2022 Feb 3;139 (5) :717-731. |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. |Cancer Sci. 2025 Jul 23.|Cancers (Basel) . 2017 Oct 30;9 (11) . pii: E149. |Cancers (Basel) . 2024|Cell Rep Med. 2023 Feb 21;4 (2) :100911.|Cell Rep Med. 2024 Mar 19;5 (3) :101472.|Cell Rep Med. 2025 Apr 2:102053.|Cell Rep Methods. 2023 Oct 23;3 (10) :100599.|Clin Transl Med. 2025 May;15 (5) :e70338. |Dis Model Mech. 2016 Sep 1;9 (9) :941-52.|Eberhard Karls Universität Tübingen. 2023 Sep 18.|EBioMedicine. 2023 Jan:87:104410.|Eur J Drug Metab Pharmacokinet. 2021 Sep;46 (5) :625-635.|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 Oct;35 (5) :919-929.|Harvard Medical School LINCS LIBRARY|Int J Biol Macromol. 2025 Jun 4;318 (Pt 1) :144963.|Int J Mol Sci. 2022 Sep 17;23 (18) :10895.|Invest New Drugs. 2023 Apr;41 (2) :254-266.|J Cancer Res Clin Oncol. 2021 Jan;147 (1) :167-175.|J Exp Clin Cancer Res. 2022 Mar 29;41 (1) :113.|J Exp Clin Cancer Res. 2025 Jul 19;44 (1) :215.|J Med Chem. 2021 Mar 11;64 (5) :2725-2738.|J Med Chem. 2021 Oct 14;64 (19) :14344-14357.|J Med Chem. 2024 Oct 24;67 (20) :18098-18123.|J Pharm Anal. 2021 Dec;11 (6) :799-807.|J Solution Chem. 2014 Jul;43 (7) :1282-1295.|J Transl Med. 2023 Aug 5;21 (1) :530.|Leukemia. 2025 Aug 14.|Mol Cancer Ther. 2025 Jul 2;24 (7) :1005-1019.|Mol Oncol. 2017 Aug;11 (8) :996-1006.|Nat Biomed Eng. 2018 Aug;2 (8) :578-588.|Nat Commun. 2025 Jul 17;16 (1) :6587.|Oncogene. 2018 Mar;37 (11) :1417-1429.|Oncogene. 2024 Sep;43 (40) :2995-3002.|Oncotarget. 2014 May 15;5 (9) :2688-702.|Oncotarget. 2016 May 17;7 (20) :29011-22. |Oncotarget. 2019 Aug 13;10 (48) :4937-4950.|Patent. US20250269018A1.|PLoS One. 2021 Jun 8;16 (6) :e0252907.|PLoS One. 2025 Jan 21;20 (1) :e0308747.|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. 2018 Jul 18;10 (450) :eaaq1093.|Sci Transl Med. 2021 Sep;13 (609) :eabb3738.|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. 2022 Jan;15 (1) :101272.