Lorlatinib acetate
Based on 38 publication(s) in Google Scholar
Lorlatinib (PF-06463922) acetate is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib acetate has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALKL1196M, respectively. Lorlatinib acetate targets to EML4-ALK, and inhibits ALK phosphorylation with IC50s of 15-43 nM (ALKL1196), 14-80 nM (ALKG1269A), 38-50 nM (ALK1151Tins), 77-113 nM (ALKG1202R), respectively.
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- CAS No.: 1924207-18-0
- Formule: C23H23FN6O4
- Masse moléculaire:466.46
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Activité biologique
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Lorlatinib acetate
More- Cancer Cell. 2026 May 11;44(5):983-994.e5. [Abstract]
- Cancer Discov. 2024 Sep 13:OF1-OF20. [Abstract]
- Nat Cancer. 2022 Oct;3(10):1211-1227. [Abstract]
- Cancer Res. 2022 Feb 1;82(3):484-496. [Abstract]
- Nat Commun. 2024 Apr 23;15(1):3422. [Abstract]
- Nat Commun. 2017 Oct 30;8(1):1197. [Abstract]
- Leukemia. 2025 Aug 14. [Abstract]
- J Exp Med. 2024 Mar 4;221(3):e20232028. [Abstract]
- Cell Rep Med. 2023 Feb 21;4(2):100911. [Abstract]
- Cancer Lett. 2026 May 29:656:218624. [Abstract]
- EMBO Mol Med. 2020 Jul 7;12(7):e11099. [Abstract]
- Mol Syst Biol. 2024 Jan;20(1):28-55. [Abstract]
- Oncogene. 2022 Sep;41(40):4547-4559. [Abstract]
- Oncogene. 2022 May;41(20):2789-2797. [Abstract]
- J Med Chem. 2024 Oct 24;67(20):18098-18123. [Abstract]
- Mol Pharm. 2023 Jan 2;20(1):357-369. [Abstract]
- Cancers (Basel). 2026 May 14;18(10):1591. [Abstract]
- Cancers (Basel). 2021 Dec 29;14(1):151. [Abstract]
- iScience. 2024 Apr 23;27(5):109800. [Abstract]
- Sci Rep. 2024 Sep 27;14(1):22191. [Abstract]
- Bioengineering (Basel). 2025 Oct 19;12(10):1121. [Abstract]
- Cancer Res Commun. 2023 Dec 27;3(12):2608-2622. [Abstract]
- J Pharm Biomed Anal. 2021 Jan 30;193:113733. [Abstract]
- Cancer Med. 2020 Jun;9(12):4350-4359. [Abstract]
- Mol Pharmacol. 2022 Jun;101(6):381-389. [Abstract]
- J Chromatogr B Analyt Technol Biomed Life Sci. 2025 Aug 28:1267:124770. [Abstract]
- Fundam Clin Pharmacol. 2021 Oct;35(5):919-929. [Abstract]
- Eur J Drug Metab Pharmacokinet. 2021 Sep;46(5):625-635. [Abstract]
- J Anal Methods Chem. 2019 Mar 4:2019:7574369. [Abstract]
- Biomed Chromatogr. 2024 Oct;38(10):e5986. [Abstract]
- Biomed Chromatogr. 2023 Jun;37(6):e5628. [Abstract]
- bioRxiv. 2026 Jan 27.
- bioRxiv. 2026 Jan 23:2026.01.21.700721. [Abstract]
- bioRxiv. 2025 Dec 5.
- Maastricht University. 2023 Jun 1.
- Universitat Autònoma de Barcelona. 2022 Aug.
- Uppsala University. 2022 Feb.
- bioRxiv. October 28, 2021.
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In Vivo Efficacy Study
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Cell Proliferation/Viability Assay
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Cell Imaging/Staining
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WB
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Cell Proliferation/Viability Assay
Activité biologique
Lorlatinib (PF-06463922) acetate demonstrates significant cell activity against ALK and a large set of ALK clinical mutations with IC50 ranging from 0.2 nM-77 nM[1]. Lorlatinib acetate significantly inhibits cell proliferation and induces cell apoptosis in the HCC78 human NSCLC cells harboring SLC34A2-ROS1 fusions and the BaF3-CD74-ROS1 cells expressing human CD74-ROS1. Lorlatinib acetate also shows potent growth inhibitory activity and induces apoptosis in the NSCLC cells harboring either non-mutant ALK or mutant ALK fusions[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1924207-18-0
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Masse moléculaire 466.46
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Formule C23H23FN6O4
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SMILES
CN1C(C#N)=C2C(CN(C)C(C3=C([C@@H](C)OC4=C(N)N=CC2=C4)C=C(F)C=C3)=O)=N1.OC(C)=O
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Synonyms
PF-06463922 acetate
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (38)
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Journal Impact Factor
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Most Recent
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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 -
Cancer Discov
NVL-655 Is a Selective and Brain-Penetrant Inhibitor of Diverse ALK-Mutant Oncoproteins, Including Lorlatinib-Resistant Compound Mutations. [Abstract]2024 Sep 13:OF1-OF20. PMID: 39269178
Lorlatinib acetate purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2024 Sep 13:OF1-OF20. [Abstract]
Lorlatinib (10 mg/kg; oral; daily). Change in tumor volume over time plotted as mean ± SEM for models harboring ALK fusion with a WT kinase domain.
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Nat Cancer
Targeting the ALK-CDK9-Tyr19 kinase cascade sensitizes ovarian and breast tumors to PARP inhibition via destabilization of the P-TEFb complex. [Abstract]2022 Oct;3(10):1211-1227. PMID: 36253486
Lorlatinib acetate purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2022 Oct;3(10):1211-1227. [Abstract]
Representative images of clonogenic assay results in PARP inhibitor (PARPi)-resistant OVCA433 cell in the presence of the indicated inhibitor for 12 d. ALKi, ALK inhibitor; LOR, Lorlatinib (250-500 nM); TALA, Talazoparib (100-200 nM); Comb, combination of Lorlatinib and Talazoparib.
Lorlatinib acetate purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2022 Oct;3(10):1211-1227. [Abstract]
Representative images of RAD51 with EdU/DAPI staining in OVCA433 cell treated with 0.25 μM PARP inhibitor (PARPi; Talazoparib) or 0.5 μM ALK inhibitor (ALKi; Lorlatinib), either alone or in combination, for 48 h.
Lorlatinib acetate purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2022 Oct;3(10):1211-1227. [Abstract]
WB of indicated proteins in cells treated with or without 0.5 μM ALK inhibitor (Lorlatinib) for 24 h.
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Cancer Res
2022 Feb 1;82(3):484-496. PMID: 34853072 -
Nat Commun
Targeting NRAS via miR-1304-5p or farnesyltransferase inhibition confers sensitivity to ALK inhibitors in ALK-mutant neuroblastoma. [Abstract]2024 Apr 23;15(1):3422. PMID: 38653965 -
Nat Commun
Multi-dimensional genomic analysis of myoepithelial carcinoma identifies prevalent oncogenic gene fusions. [Abstract]2017 Oct 30;8(1):1197. PMID: 29084941
Lorlatinib acetate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2017 Oct 30;8(1):1197. [Abstract]
Lorlatinib (100 nM; 72 h). Representative photographs of soft agar colony formation assay.
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Leukemia
Unraveling the impact of crizotinib to promote megakaryopoiesis for alleviating thrombocytopenia in myelodysplastic neoplasms. [Abstract]2025 Aug 14. PMID: 40813622 -
J Exp Med
2024 Mar 4;221(3):e20232028. PMID: 38284990 -
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 -
EMBO Mol Med
Vulnerability of drug-resistant EML4-ALK rearranged lung cancer to transcriptional inhibition. [Abstract]2020 Jul 7;12(7):e11099. PMID: 32558295 -
Mol Syst Biol
Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]2024 Jan;20(1):28-55. PMID: 38177929 -
Oncogene
ALK fusion promotes metabolic reprogramming of cancer cells by transcriptionally upregulating PFKFB3. [Abstract]2022 Sep;41(40):4547-4559. PMID: 36064579 -
Oncogene
2022 May;41(20):2789-2797. PMID: 35411036 -
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 -
Mol Pharm
Dynamic Changes in Gastrointestinal Fluid Characteristics after Food Ingestion Are Important for Quantitatively Predicting the In Vivo Performance of Oral Solid Dosage Forms in Humans in the Fed State. [Abstract]2023 Jan 2;20(1):357-369. PMID: 36373973 -
Cancers (Basel)
A Zinc Finger Protein-Based Prognostic Model in Lung Adenocarcinoma Identifies FGD3 as a Marker Associated with Lorlatinib Resistance. [Abstract]2026 May 14;18(10):1591. PMID: 42192951 -
Cancers (Basel)
BRG1 and NPM-ALK Are Co-Regulated in Anaplastic Large-Cell Lymphoma; BRG1 Is a Potential Therapeutic Target in ALCL. [Abstract]2021 Dec 29;14(1):151. PMID: 35008316 -
iScience
ALK inhibitors suppress HCC and synergize with anti-PD-1 therapy and ABT-263 in preclinical models. [Abstract]2024 Apr 23;27(5):109800. PMID: 38741708 -
Sci Rep
Novel insight into mechanisms of ROS1 catalytic activation via loss of the extracellular domain. [Abstract]2024 Sep 27;14(1):22191. PMID: 39333184 -
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 -
Cancer Res Commun
SHP2 inhibition with TNO155 increases efficacy and overcomes resistance of ALK inhibitors in neuroblastoma. [Abstract]2023 Dec 27;3(12):2608-2622. PMID: 38032104 -
J Pharm Biomed Anal
To quantify the small-molecule kinase inhibitors ceritinib, dacomitinib, lorlatinib, and nintedanib in human plasma by liquid chromatography/triple-quadrupole mass spectrometry. [Abstract]2021 Jan 30;193:113733. PMID: 33217707 -
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 -
Mol Pharmacol
Influence of Tyrosine Kinase Inhibition on Organic Anion Transporting Polypeptide 1B3-Mediated Uptake. [Abstract]2022 Jun;101(6):381-389. PMID: 35383108 -
J Chromatogr B Analyt Technol Biomed Life Sci
Development of a validated and sensitive ultra-high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) method to simultaneous determination of crizotinib, alectinib and lorlatinib in human plasma. [Abstract]2025 Aug 28:1267:124770. PMID: 40902417 -
Fundam Clin Pharmacol
2021 Oct;35(5):919-929. PMID: 33523504 -
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 -
J Anal Methods Chem
Pharmacokinetic Study and Tissue Distribution of Lorlatinib in Mouse Serum and Tissue Samples by Liquid Chromatography-Mass Spectrometry. [Abstract]2019 Mar 4:2019:7574369. PMID: 30949374 -
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
Development and validation of an HPLC-MS/MS method to simultaneously quantify brigatinib, lorlatinib, pralsetinib and selpercatinib in human K2-EDTA plasma. [Abstract]2023 Jun;37(6):e5628. PMID: 36941218 -
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bioRxiv
2026 Jan 23:2026.01.21.700721. PMID: 41648424 -
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Pureté et documentation
Références
[1]. Zou HY, et al. PF-06463922, an ALK/ROS1 Inhibitor, Overcomes Resistance to First and Second Generation ALK Inhibitors in Preclinical Models. Cancer Cell. 2015 Jul 13;28(1):70-81. [Content Brief]
[2]. Johnson TW, et al. Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain exposure and broad-spectrum potency against ALK-resistant mutations. J Med Chem. 2014 Jun 12;57(11):4720-44. [Content Brief]
[3]. Zou HY, et al. PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking PF-02341066-resistant ROS1 mutations. Proc Natl Acad Sci U S A. 2015 Mar 17;112(11):3493-8 [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Lorlatinib acetate Related Classifications
HY-135509 Related Classifications
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