Crizotinib hydrochloride
Based on 92 publication(s) in Google Scholar
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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity : 99.72%
- CAS No.: 1415560-69-8
- 화학식: C21H23Cl3FN5O
- 분자량:486.80
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
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HY-12215
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HY-15656A
Ceritinib dihydrochlorideALK Inhibitor -
HY-50878
CrizotinibALK/c-Met/ROS1 Inhibitor -
HY-12857
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HY-13011A
Alectinib HydrochlorideALK Inhibitor -
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Ensartinib dihydrochlorideALK/MET Inhibitor -
HY-50767
PalbociclibCDK4/6 Inhibitor -
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SelumetinibMEK1/2 Inhibitor -
HY-15656
CeritinibALK Inhibitor -
HY-15772
OsimertinibMutant-Selective EGFR Inhibitor -
HY-100549
(S)-CrizotinibSelective MTH1 Inhibitor
Publications Citing Use of MedChemExpress (MCE) Crizotinib hydrochloride
More- Signal Transduct Target Ther. 2024 Mar 9;9(1):65. [Abstract]
- Cancer Cell. 2026 May 11;44(5):983-994.e5. [Abstract]
- J Hematol Oncol. 2018 Aug 29;11(1):109. [Abstract]
- Cancer Discov. 2024 Dec 2;14(12):2367-2386. [Abstract]
- Cancer Discov. 2023 Mar 1;13(3):598-615. [Abstract]
- Cancer Discov. 2018 Mar;8(3):354-369. [Abstract]
- Nat Biomed Eng. 2018 Aug;2(8):578-588. [Abstract]
- Blood. 2022 Feb 3;139(5):717-731. [Abstract]
- Cancer Res. 2015 Nov 1;75(21):4548-59. [Abstract]
- Nat Commun. 2025 Jul 17;16(1):6587. [Abstract]
- J Am Chem Soc. 2026 Sep 9;148(35):37884-37908.
- Sci Transl Med. 2021 Sep;13(609):eabb3738. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Acta Pharm Sin B. 2026 Mar 2.
- Biomark Res. 2024 Jan 25;12(1):13. [Abstract]
- J Exp Clin Cancer Res. 2025 Jul 19;44(1):215. [Abstract]
- J Exp Clin Cancer Res. 2022 Mar 29;41(1):113. [Abstract]
- MedComm (2020). 2025 Jul 21;6(8):e70286. [Abstract]
- Cell Rep Med. 2025 Apr 15;6(4):102053. [Abstract]
- Cell Rep Med. 2024 Mar 19;5(3):101472. [Abstract]
- Cell Rep Med. 2023 Feb 21;4(2):100911. [Abstract]
- Cancer Lett. 2026 May 29:656:218624. [Abstract]
- Cancer Lett. 2018 May 28:422:19-28. [Abstract]
- EBioMedicine. 2023 Jan:87:104410. [Abstract]
- J Pharm Anal. 2021 Dec;11(6):799-807. [Abstract]
- J Transl Med. 2023 Aug 5;21(1):530. [Abstract]
- Oncogene. 2024 Sep;43(40):2995-3002. [Abstract]
- Oncogene. 2018 Mar;37(11):1417-1429. [Abstract]
- Leukemia. 2025 Aug 14. [Abstract]
- Int J Biol Macromol. 2025 Jun 4;318(Pt 1):144963. [Abstract]
- Clin Transl Med. 2025 May;15(5):e70338. [Abstract]
- Blood Adv. 2025 Jul 2:bloodadvances.2024015322. [Abstract]
- Blood Adv. 2023 Aug 8;7(15):4049-4063. [Abstract]
- J Med Chem. 2024 Oct 24;67(20):18098-18123. [Abstract]
- J Med Chem. 2021 Oct 14;64(19):14344-14357. [Abstract]
- J Med Chem. 2021 Mar 11;64(5):2725-2738. [Abstract]
- Sci Signal. 2015 Dec 8;8(406):ra125. [Abstract]
- Sci Signal. 2014 Oct 28;7(349):ra102. [Abstract]
- Mol Cancer Ther. 2025 Jul 2;24(7):1005-1019. [Abstract]
- Talanta. 2019 Aug 15:201:217-225. [Abstract]
- Eur J Med Chem. 2017 Oct 20:139:674-697. [Abstract]
- Anal Chim Acta. 2026 May 12;1412:345649.
- Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
- Pharmaceuticals (Basel). 2026 Feb 27;19(3):381. [Abstract]
- Int J Mol Sci. 2022 Sep 17;23(18):10895. [Abstract]
- Stem Cell Reports. 2017 Dec 12;9(6):1948-1960. [Abstract]
- ACS Omega. 2023 Jun 14;8(25):22603-22612. [Abstract]
- Int J Antimicrob Agents. 2025 Jun;65(6):107470. [Abstract]
- Cancer Sci. 2025 Jul 23. [Abstract]
- Transl Oncol. 2022 Jan;15(1):101272. [Abstract]
- Transl Oncol. 2021 Jan;14(1):100887. [Abstract]
- Cancers (Basel). 2024
- Spectrochim Acta A Mol Biomol Spectrosc. 2021 Oct 5:259:119884. [Abstract]
- Cancers (Basel). 2017 Oct 30;9(11):149. [Abstract]
- Spectrochim Acta A Mol Biomol Spectrosc. 2014 Oct 15:131:347-54. [Abstract]
- J Pharm Investig. 2025 Dec 29.
- Mol Oncol. 2017 Aug;11(8):996-1006. [Abstract]
- Bioengineering (Basel). 2025 Oct 19;12(10):1121. [Abstract]
- Proteomes. 2023 Jun 2;11(2):20. [Abstract]
- Biochim Biophys Acta Mol Cell Res. 2020 Jul;1867(7):118712. [Abstract]
- Saudi Pharm J. 2015 Jan;23(1):75-84. [Abstract]
- Dis Model Mech. 2016 Sep 1;9(9):941-52. [Abstract]
- Arch Biochem Biophys. 2024 Mar:753:109905. [Abstract]
- Exp Cell Res. 2020 Aug 1;393(1):112054. [Abstract]
- Cancer Med. 2020 Jun;9(12):4350-4359. [Abstract]
- Invest New Drugs. 2023 Apr;41(2):254-266. [Abstract]
- Front Oncol. 2020 May 12;10:696. [Abstract]
- J Cancer Res Clin Oncol. 2021 Jan;147(1):167-175. [Abstract]
- Food Chem Toxicol. 2026 Nov:217:116309.
- PLoS One. 2025 Jan 21;20(1):e0308747. [Abstract]
- PLoS One. 2021 Jun 8;16(6):e0252907. [Abstract]
- PLoS One. 2019 Feb 11;14(2):e0212048. [Abstract]
- Fundam Clin Pharmacol. 2021 Oct;35(5):919-929. [Abstract]
- Biol Methods Protoc. 2025 Feb 13;10(1):bpaf012. [Abstract]
- Eur J Drug Metab Pharmacokinet. 2021 Sep;46(5):625-635. [Abstract]
- Biomed Chromatogr. 2024 Oct;38(10):e5986. [Abstract]
- Biomed Chromatogr. 2019 Oct;33(10):e4611. [Abstract]
- J Solution Chem. 2014 Jul;43(7):1282-1295.
- Braz J Pharm Sci. 2015 Jun;51(2):2175-9790.
- Biomed Pharmacother. 2026 Sep:202:119803.
- bioRxiv. 2025 Dec 5.
- Patent. US20250269018A1.
- bioRxiv. 2024 Nov 6:2024.11.04.621884. [Abstract]
- Eberhard Karls Universität Tübingen. 2023 Sep 18.
- Research Square Print. 26 Oct, 2022
- Research Square Print. September 14th, 2022.
- Research Square Preprint. 2022 Feb.
- Evid Based Complement Alternat Med. 2019 Nov 7:2019:4253846. [Abstract]
- Oncotarget. 2019 Aug 13;10(48):4937-4950. [Abstract]
- Technical University of Munich. 24.01.2018.
- Oncotarget. 2016 May 17;7(20):29011-22. [Abstract]
- Oncotarget. 2014 May 15;5(9):2688-702. [Abstract]
Customer Validation & Images
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Biological Activity
제품 설명
IC50 & Target
IC50: 20 nM (ALK), 8 nM (c-Met)[3]
In Vitro
PF-2341066 displays similar potency against c-Met phosphorylation in mIMCD3 mouse or MDCK canine epithelial cells with IC50 of 5 nM and 20 nM, respectivly. PF-2341066 shows improved or similar activity against NIH3T3 cells engineered to express c-Met ATP-binding site mutants V1092I or H1094R or the P-loop mutant M1250T with IC50 of 19 nM, 2 nM and 15 nM, respectively, compared with NIH3T3 cells expressing wild-type receptor with IC50 of 13 nM. In contrast, a marked shift in potency of PF-2341066 is observed against cells engineered to express c-Met activation loop mutants Y1230C and Y1235D with IC50 of 127 nM and 92 nM, respectively, compared with wild-type receptor. PF-2341066 also potently prevents the phosphorylation of c-Met in NCI-H69 and HOP92 cells, with IC50 of 13 nM and 16 nM, respectively, which express the endogenous c-Met variants R988C and T1010I, respectively[1].
PF-2341066 also potently inhibits NPM-ALK phosphorylation in Karpas299 or SU-DHL-1 ALCL cells with an IC50 of 24 nM. PF-2341066 potently prevents cell proliferation, which is associated with G(1)-S-phase cell cycle arrest and induction of apoptosis in ALK-positive ALCL cells with IC50 of 30 nM, but not ALK-negative lymphoma cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Treatment of c-MET-amplified GTL-16 xenografts with 50 mg/kg PF-2341066 elicits tumor regression that is associated with a slow reduction in 18F-FDG uptake and decreases expression of the glucose transporter 1, GLUT-1[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
- Kinase activity and phosphorylation assays
- Western Blot
- ROS/oxidative-stress fluorescent staining
- Patient-Derived Xenograft (PDX)
- Patient-Derived Orthotopic Xenograft (PDOX)
- Protocol for Kinase activity and phosphorylation assays
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Directly Induced Neuron Culture
Chemical Information
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CAS No. 1415560-69-8
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Appearance Solid
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분자량 486.80
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화학식 C21H23Cl3FN5O
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Color Yellow to brown
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SMILES
ClC1=C(F)C=CC(Cl)=C1[C@H](OC2=CC(C3=CN(N=C3)C4CCNCC4)=CN=C2N)C.Cl
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Synonyms
PF-02341066 hydrochloride
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (92)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Tet methylcytosine dioxygenase 2 (TET2) deficiency elicits EGFR-TKI (tyrosine kinase inhibitors) resistance in non-small cell lung cancer. [Abstract]2024 Mar 9;9(1):65. PMID: 38461173 -
Cancer Cell
JYP0322, a highly selective and brain-penetrant ROS1 inhibitor, overcomes ROS1G2032R resistance mutation in NSCLC: The first-in-human phase 1 trial. [Abstract]2026 May 11;44(5):983-994.e5. PMID: 42030931 -
J Hematol Oncol
Mouse avatar models of esophageal squamous cell carcinoma proved the potential for EGFR-TKI afatinib and uncovered Src family kinases involved in acquired resistance. [Abstract]2018 Aug 29;11(1):109. PMID: 30157900
Crizotinib hydrochloride purchased from MedChemExpress. Usage Cited in: J Hematol Oncol. 2018 Aug 29;11(1):109. [Abstract]
Resistant cells are treated with 200 nM Afatinib alone or in combination with 1 μM Crizotinib for 48 h.
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Cancer Discov
NVL-655 Is a Selective and Brain-Penetrant Inhibitor of Diverse ALK-Mutant Oncoproteins, Including Lorlatinib-Resistant Compound Mutations. [Abstract]2024 Dec 2;14(12):2367-2386. PMID: 39269178 -
Cancer Discov
NVL-520 is a selective, TRK-sparing, and brain-penetrant inhibitor of ROS1 fusions and secondary resistance mutations. [Abstract]2023 Mar 1;13(3):598-615. PMID: 36511802 -
Cancer Discov
Identifying and Targeting Sporadic Oncogenic Genetic Aberrations in Mouse Models of Triple-Negative Breast Cancer. [Abstract]2018 Mar;8(3):354-369. PMID: 29203461
Crizotinib hydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2018 Mar;8(3):354-369. [Abstract]
At 50mg/kg, Crizotinib inhibits MET phosphorylation and downstream signaling pathway activation.
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Nat Biomed Eng
TLR7/8-agonist-loaded nanoparticles promote the polarization of tumour-associated macrophages to enhance cancer immunotherapy. [Abstract]2018 Aug;2(8):578-588. PMID: 31015631 -
Blood
Tyrosine phosphatases regulate resistance to ALK inhibitors in ALK+ anaplastic large cell lymphoma. [Abstract]2022 Feb 3;139(5):717-731. PMID: 34657149 -
Cancer Res
c-Myc alterations confer therapeutic response and acquired resistance to c-Met inhibitors in MET-addicted cancers. [Abstract]2015 Nov 1;75(21):4548-59. PMID: 26483207 -
Nat Commun
Engineering bi-directional chemically-modulated synthetic condensates for cellular control. [Abstract]2025 Jul 17;16(1):6587. PMID: 40675979 -
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Sci Transl Med
Oncogenic switch and single-agent MET inhibitor sensitivity in a subset of EGFR-mutant lung cancer. [Abstract]2021 Sep;13(609):eabb3738. PMID: 34516823 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
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Biomark Res
Simultaneous inhibition of FAK and ROS1 synergistically repressed triple-negative breast cancer by upregulating p53 signalling. [Abstract]2024 Jan 25;12(1):13. PMID: 38273343 -
J Exp Clin Cancer Res
MiR-181a-driven downregulation of cholesterol biosynthesis through SREBP2 inhibition suppresses uveal melanoma metastasis. [Abstract]2025 Jul 19;44(1):215. PMID: 40684202 -
J Exp Clin Cancer Res
The autocrine loop of ALK receptor and ALKAL2 ligand is an actionable target in consensus molecular subtype 1 colon cancer. [Abstract]2022 Mar 29;41(1):113. PMID: 35351152 -
MedComm (2020)
Crizotinib: A Novel Strategy to Reverse Immunosuppression in Melanoma by Targeting Lactate Transport. [Abstract]2025 Jul 21;6(8):e70286. PMID: 40692663 -
Cell Rep Med
CAN-Scan: A multi-omic phenotype-driven precision oncology platform identifies prognostic biomarkers of therapy response for colorectal cancer. [Abstract]2025 Apr 15;6(4):102053. PMID: 40187357 -
Cell Rep Med
STAT3 couples activated tyrosine kinase signaling to the oncogenic core transcriptional regulatory circuitry of anaplastic large cell lymphoma. [Abstract]2024 Mar 19;5(3):101472. PMID: 38508140 -
Cell Rep Med
Using patient-derived organoids to predict locally advanced or metastatic lung cancer tumor response: A real-world study. [Abstract]2023 Feb 21;4(2):100911. PMID: 36657446 -
Cancer Lett
Integrated clinical, genomic and functional characterization of a novel ALK variant in neuroblastoma. [Abstract]2026 May 29:656:218624. PMID: 42217560 -
Cancer Lett
CD74-ROS1 G2032R mutation transcriptionally up-regulates Twist1 in non-small cell lung cancer cells leading to increased migration, invasion, and resistance to crizotinib. [Abstract]2018 May 28:422:19-28. PMID: 29477381
Crizotinib hydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2018 May 28:422:19-28. [Abstract]
CD74-ROS1 or CD74-ROS1 G2032R mutation cells are treated with Crizotinib for 24 h, the expression of ROS1 or p-ROS1 is determined by western blot.
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EBioMedicine
Immunological profiles of human oligodendrogliomas define two distinct molecular subtypes. [Abstract]2023 Jan:87:104410. PMID: 36525723 -
J Pharm Anal
Synergistic effects of methyl 2-cyano-3,11-dioxo-18beta-olean-1,-12-dien-30-oate and erlotinib on erlotinib-resistant non-small cell lung cancer cells. [Abstract]2021 Dec;11(6):799-807. PMID: 35028186 -
J Transl Med
Epithelial cell adhesion molecule (EpCAM) regulates HGFR signaling to promote colon cancer progression and metastasis. [Abstract]2023 Aug 5;21(1):530. PMID: 37543570 -
Oncogene
Synergistic effects of combined BET and FAK inhibition against Vestibular Schwannomas in NF2-related Schwannomatosis. [Abstract]2024 Sep;43(40):2995-3002. PMID: 39209965 -
Oncogene
Activated ALK signals through the ERK-ETV5-RET pathway to drive neuroblastoma oncogenesis. [Abstract]2018 Mar;37(11):1417-1429. PMID: 29321660 -
Leukemia
Unraveling the impact of crizotinib to promote megakaryopoiesis for alleviating thrombocytopenia in myelodysplastic neoplasms. [Abstract]2025 Aug 14. PMID: 40813622 -
Int J Biol Macromol
Regulation of shelterin proteins TERF2IP and TRF2 by the MLL2-H3K4me3-p65 axis drives hyperglycemia-dependent endothelial senescence. [Abstract]2025 Jun 4;318(Pt 1):144963. PMID: 40480577 -
Clin Transl Med
2025 May;15(5):e70338. PMID: 40437874 -
Blood Adv
BH3 mimetic drugs overcome the microenvironment-induced resistance to crizotinib in ALK+ anaplastic large cell lymphoma. [Abstract]2025 Jul 2:bloodadvances.2024015322. PMID: 40601898 -
Blood Adv
Aberrant expression of GOLM1 protects ALK+ anaplastic large cell lymphoma from apoptosis by enhancing BCL-XL stability. [Abstract]2023 Aug 8;7(15):4049-4063. PMID: 36763539 -
J Med Chem
Discovery of Oral Degraders of the ROS1 Fusion Protein with Potent Activity against Secondary Resistance Mutations. [Abstract]2024 Oct 24;67(20):18098-18123. PMID: 39361251 -
J Med Chem
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors. [Abstract]2021 Oct 14;64(19):14344-14357. PMID: 34547896 -
J Med Chem
Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration. [Abstract]2021 Mar 11;64(5):2725-2738. PMID: 33619967 -
Sci Signal
Pleiotrophin promotes vascular abnormalization in gliomas and correlates with poor survival in patients with astrocytomas. [Abstract]2015 Dec 8;8(406):ra125. PMID: 26645582 -
Sci Signal
The kinase ALK stimulates the kinase ERK5 to promote the expression of the oncogene MYCN in neuroblastoma. [Abstract]2014 Oct 28;7(349):ra102. PMID: 25351247
Crizotinib hydrochloride purchased from MedChemExpress. Usage Cited in: Sci Signal. 2014 Oct 28;7(349):ra102. [Abstract]
Activation of ERK5 in neuroblastoma cell lines expressing activated ALK. (A to C) Immunoblotting for the indicated proteins in neuroblastoma cells CLB-BAR (A), CLB-GE (B), and IMR32 (C) cultured on six-well plates in complete growth medium and treated with inhibitors as indicated for 6 hours alone (A and B) or before (C) stimulation with mAb46 for 30 min.
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Mol Cancer Ther
2025 Jul 2;24(7):1005-1019. PMID: 40299789 -
Talanta
Development and comparative evaluation of two immunoassay platforms for bioanalysis of crizotinib: A potent drug used for the treatment of non-small cell lung cancer. [Abstract]2019 Aug 15:201:217-225. PMID: 31122414 -
Eur J Med Chem
Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR associated drug resistant mutants in NSCLC. [Abstract]2017 Oct 20:139:674-697. PMID: 28850922 -
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Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
Pharmaceuticals (Basel)
Synthesis and Development of 3-((2,4-Difluorophenyl)Amino)Propanoic Acid Derivatives as an Antiproliferative Medicinal Chemistry Scaffold Targeting Growth Factor Receptors. [Abstract]2026 Feb 27;19(3):381. PMID: 41901229 -
Int J Mol Sci
Doxorubicin-Induced TrkAIII Activation: A Selection Mechanism for Resistant Dormant Neuroblastoma Cells. [Abstract]2022 Sep 17;23(18):10895. PMID: 36142807 -
Stem Cell Reports
Inhibition of Farnesyltransferase Potentiates NOTCH-Targeted Therapy against Glioblastoma Stem Cells. [Abstract]2017 Dec 12;9(6):1948-1960. PMID: 29198824 -
ACS Omega
2023 Jun 14;8(25):22603-22612. PMID: 37387790 -
Int J Antimicrob Agents
A new perspective on the antimicrobial mechanism of linezolid against Staphylococcus aureus revealed by proteomics and metabolomics analysis. [Abstract]2025 Jun;65(6):107470. PMID: 40049374 -
Cancer Sci
APE1 Attenuates ALK Tyrosine Kinase Inhibitors Sensitivity in NPM1-ALK Positive Anaplastic Large Cell Lymphoma. [Abstract]2025 Jul 23. PMID: 40702700 -
Transl Oncol
2022 Jan;15(1):101272. PMID: 34823094 -
Transl Oncol
Anti-epidermal growth factor vaccine antibodies increase the antitumor activity of kinase inhibitors in ALK and RET rearranged lung cancer cells. [Abstract]2021 Jan;14(1):100887. PMID: 33129112 -
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Spectrochim Acta A Mol Biomol Spectrosc
Innovative use of σ and π electron acceptors in the development of three high throughput 96-microwell spectrophotometric assays for crizotinib. [Abstract]2021 Oct 5:259:119884. PMID: 33971436 -
Cancers (Basel)
Novel Mechanisms of ALK Activation Revealed by Analysis of the Y1278S Neuroblastoma Mutation. [Abstract]2017 Oct 30;9(11):149. PMID: 29084134 -
Spectrochim Acta A Mol Biomol Spectrosc
Charge-transfer reaction of 1,4-benzoquinone with crizotinib: spectrophotometric study, computational molecular modeling and use in development of microwell assay for crizotinib. [Abstract]2014 Oct 15:131:347-54. PMID: 24835938 -
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Mol Oncol
Immunoassays for the quantification of ALK and phosphorylated ALK support the evaluation of on-target ALK inhibitors in neuroblastoma. [Abstract]2017 Aug;11(8):996-1006. PMID: 28432815
Crizotinib hydrochloride purchased from MedChemExpress. Usage Cited in: Mol Oncol. 2017 Aug;11(8):996-1006. [Abstract]
Dose-response and time course comparison of ALK inhibition by Crizotinib or Ceritinib.
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Bioengineering (Basel)
Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]2025 Oct 19;12(10):1121. PMID: 41155119 -
Proteomes
Mass Spectrometry and Pharmacological Approaches to Measuring Cooption and Reciprocal Activation of Receptor Tyrosine Kinases. [Abstract]2023 Jun 2;11(2):20. PMID: 37368466 -
Biochim Biophys Acta Mol Cell Res
ZX-29, a novel ALK inhibitor, induces apoptosis via ER stress in ALK rearrangement NSCLC cells and overcomes cell resistance caused by an ALK mutation. [Abstract]2020 Jul;1867(7):118712. PMID: 32224191 -
Saudi Pharm J
Charge-transfer reaction of 2,3-dichloro-1,4-naphthoquinone with crizotinib: Spectrophotometric study, computational molecular modeling and use in development of microwell assay for crizotinib. [Abstract]2015 Jan;23(1):75-84. PMID: 25685046 -
Dis Model Mech
The ALK inhibitor PF-06463922 is effective as a single agent in neuroblastoma driven by expression of ALK and MYCN. [Abstract]2016 Sep 1;9(9):941-52. PMID: 27483357
Crizotinib hydrochloride purchased from MedChemExpress. Usage Cited in: Dis Model Mech. 2016 Sep 1;9(9):941-52. [Abstract]
CLB-BAR, CLB-GE neuroblastoma cells are treated for 6 h with either Crizotinib or PF-04643922. Cells are harvested and pre-cleared cell lysates are analyzed on SDS PAGE followed by western blotting for ALK, phospho-ALK-Y1278, phospho-ERK5, pan-ERK5 phospho-ERK1/2 and pan-ERK. Actin is employed as a loading control. Protein band intensities are quantified by Image Studio Lite 3.1 and normalized to untreated samples.
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Arch Biochem Biophys
Collagen I protects human keratinocytes HaCaT against UVB injury via restoring PINK1/parkin-mediated mitophagy. [Abstract]2024 Mar:753:109905. PMID: 38281543 -
Exp Cell Res
Network-based analysis with primary cells reveals drug response landscape of acute myeloid leukemia. [Abstract]2020 Aug 1;393(1):112054. PMID: 32376287 -
Cancer Med
The underlying mechanisms of lorlatinib penetration across the blood-brain barrier and the distribution characteristics of lorlatinib in the brain. [Abstract]2020 Jun;9(12):4350-4359. PMID: 32347012 -
Invest New Drugs
Iruplinalkib (WX‑0593), a novel ALK/ROS1 inhibitor, overcomes crizotinib resistance in preclinical models for non-small cell lung cancer. [Abstract]2023 Apr;41(2):254-266. PMID: 37036582 -
Front Oncol
Low-Dose Crizotinib, a Tyrosine Kinase Inhibitor, Highly and Specifically Sensitizes P-Glycoprotein-Overexpressing Chemoresistant Cancer Cells Through Induction of Late Apoptosis in vivo and in vitro. [Abstract]2020 May 12;10:696. PMID: 32528877 -
J Cancer Res Clin Oncol
MET canonical transcript expression is a predictive biomarker for chemo-sensitivity to MET-inhibitors in hepatocellular carcinoma cell lines. [Abstract]2021 Jan;147(1):167-175. PMID: 32980960 -
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PLoS One
Inhibition of the anti-apoptotic protein BCL2 in EML4-ALK cell models as a second proposed therapeutic target for non-small cell lung cancer. [Abstract]2025 Jan 21;20(1):e0308747. PMID: 39836700 -
PLoS One
A new method for the study of biophysical and morphological parameters in 3D cell cultures: Evaluation in LoVo spheroids treated with crizotinib. [Abstract]2021 Jun 8;16(6):e0252907. PMID: 34101765 -
PLoS One
Synthesis of hapten, generation of specific polyclonal antibody and development of ELISA with high sensitivity for therapeutic monitoring of crizotinib. [Abstract]2019 Feb 11;14(2):e0212048. PMID: 30742664 -
Fundam Clin Pharmacol
2021 Oct;35(5):919-929. PMID: 33523504 -
Biol Methods Protoc
Optimizing drug sensitivity assays in patient-derived tumor organoids: a comparison of IC50 estimation methods and experimental parameters. [Abstract]2025 Feb 13;10(1):bpaf012. PMID: 40060949 -
Eur J Drug Metab Pharmacokinet
Differential Inhibition of Equilibrative Nucleoside Transporter 1 (ENT1) Activity by Tyrosine Kinase Inhibitors. [Abstract]2021 Sep;46(5):625-635. PMID: 34275128 -
Biomed Chromatogr
Development and validation of an ultra-performance liquid chromatography-tandem mass spectrometry method to quantify the small molecule inhibitors adagrasib, alectinib, brigatinib, capmatinib, crizotinib, lorlatinib, selpercatinib, and sotorasib in human plasma. [Abstract]2024 Oct;38(10):e5986. PMID: 39136165 -
Biomed Chromatogr
Pharmacokinetics of cligosiban in dog plasma after oral administration by liquid chromatography electrospray ionization tandem mass spectrometry. [Abstract]2019 Oct;33(10):e4611. PMID: 31145820 -
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bioRxiv
PAIRWISE: Deep Learning-based Prediction of Effective Personalized Drug Combinations in Cancer. [Abstract]2024 Nov 6:2024.11.04.621884. PMID: 39574568 -
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Evid Based Complement Alternat Med
In a Rat Model of Acute Liver Failure, Icaritin Improved the Therapeutic Effect of Mesenchymal Stem Cells by Activation of the Hepatocyte Growth Factor/c-Met Pathway. [Abstract]2019 Nov 7:2019:4253846. PMID: 31915446
Crizotinib hydrochloride purchased from MedChemExpress. Usage Cited in: Evid Based Complement Alternat Med. 2019 Nov 7:2019:4253846. [Abstract]
Western blot analysis of cleaved caspase 3, Bax, and Bcl-2 expression after serum-free culture for 72 h with or without Crizotinib.
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Oncotarget
ALK mutation dynamics and clonal evolution in a neuroblastoma model exhibiting two ALK mutations. [Abstract]2019 Aug 13;10(48):4937-4950. PMID: 31452835 -
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Oncotarget
Brigatinib, an anaplastic lymphoma kinase inhibitor, abrogates activity and growth in ALK-positive neuroblastoma cells, Drosophila and mice. [Abstract]2016 May 17;7(20):29011-22. PMID: 27049722
Crizotinib hydrochloride purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 May 17;7(20):29011-22. [Abstract]
A, B. CLB-BAR (ALK-Δ4-11) and CLB-GE (ALK-F1174V), both ALK addicted cell lines, are treated with increasing doses of Brigatinib for 6 hours. Crizotinib (250 nM) is employed as a positive control. Cells lysates are resolved on SDS/PAGE followed by immunoblotting for pALK (Y1604) and additional downstream targets as indicated.
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Oncotarget
Activated Alk triggers prolonged neurogenesis and Ret upregulation providing a therapeutic target in ALK-mutated neuroblastoma. [Abstract]2014 May 15;5(9):2688-702. PMID: 24811913
Crizotinib hydrochloride purchased from MedChemExpress. Usage Cited in: Oncotarget. 2014 May 15;5(9):2688-702. [Abstract]
The Ret expression level is investigated by Western blot in MYCN/KI AlkR1279Q and MYCN/KI AlkF1178L treated tumors and controls using the anti-Ret antibody EPR2871. Actin is used as a standard for quantification.
용액&용해도
In Vitro:
H2O : 50 mg/mL (102.71 mM; Need ultrasonic)
DMSO : ≥ 4.9 mg/mL (10.07 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 55 mg/mL (112.98 mM); Clear solution; Need ultrasonic
순도&문서
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Data Sheet (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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 [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 2.0542 mL | 10.2712 mL | 20.5423 mL | 51.3558 mL |
| 5 mM | 0.4108 mL | 2.0542 mL | 4.1085 mL | 10.2712 mL | |
| 10 mM | 0.2054 mL | 1.0271 mL | 2.0542 mL | 5.1356 mL | |
| H2O | 15 mM | 0.1369 mL | 0.6847 mL | 1.3695 mL | 3.4237 mL |
| 20 mM | 0.1027 mL | 0.5136 mL | 1.0271 mL | 2.5678 mL | |
| 25 mM | 0.0822 mL | 0.4108 mL | 0.8217 mL | 2.0542 mL | |
| 30 mM | 0.0685 mL | 0.3424 mL | 0.6847 mL | 1.7119 mL | |
| 40 mM | 0.0514 mL | 0.2568 mL | 0.5136 mL | 1.2839 mL | |
| 50 mM | 0.0411 mL | 0.2054 mL | 0.4108 mL | 1.0271 mL | |
| 60 mM | 0.0342 mL | 0.1712 mL | 0.3424 mL | 0.8559 mL | |
| 80 mM | 0.0257 mL | 0.1284 mL | 0.2568 mL | 0.6419 mL | |
| 100 mM | 0.0205 mL | 0.1027 mL | 0.2054 mL | 0.5136 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Crizotinib hydrochloride Related Classifications
HY-50878A Related Classifications
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