Art. -Nr.: HY-12215

Lorlatinib

(Synonyms: PF-06463922)

38 Cited Publications

Kundenbewertung

Based on 38 publication(s) in Google Scholar

Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib has K_is of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK^L1196M, respectively. Lorlatinib targets to EML4-ALK, and inhibits ALK phosphorylation with IC₅₀s of 15-43 nM (ALK^L1196), 14-80 nM (ALK^G1269A), 38-50 nM (ALK^1151Tins), 77-113 nM (ALK^G1202R), respectively.

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Reinheit: 99.99%
CAS. Nr.: 1454846-35-5
Formel: C₂₁H₁₉FN₆O₂
Molecular Weight:406.41

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Lorlatinib Chemical Structure

CAS. Nr.: 1454846-35-5

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (38)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 15-43 nM (ALK^L1196), 14-80 nM (ALK^G1269A), 38-50 nM (ALK^1151Tins), 77-113 nM (ALK^G1202R)^[3]
Ki: <0.07 nM (ALK^WT), 0.6 nM (ALK^L1996M), 0.9 nM (ALK^G1269A), 0.1 nM (ALK^1151Tins), <0.1 nM (ALK^L1152R), 0.2 nM (ALK^S1206Y), <0.1 nM (ALK^C1156Y), <0.1nM (ALK^F1174L)^[3]

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	1.2 nM Compound: 5	Antiproliferative activity against mouse BAF3 cells harboring CD74-ROS1 after 72 hrs by SRB or CCK8 assay Antiproliferative activity against mouse BAF3 cells harboring CD74-ROS1 after 72 hrs by SRB or CCK8 assay	[PMID: 29288940]
BaF3	IC₅₀	2.9 nM Compound: 5	Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK after 72 hrs by SRB or CCK8 assay Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK after 72 hrs by SRB or CCK8 assay	[PMID: 29288940]
BaF3	IC₅₀	200 nM Compound: 5	Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK G1202R mutant after 72 hrs by SRB or CCK8 assay Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK G1202R mutant after 72 hrs by SRB or CCK8 assay	[PMID: 29288940]
BaF3	IC₅₀	262 nM Compound: 5	Antiproliferative activity against mouse BAF3 cells harboring CD74-ROS1 G2032R mutant after 72 hrs by SRB or CCK8 assay Antiproliferative activity against mouse BAF3 cells harboring CD74-ROS1 G2032R mutant after 72 hrs by SRB or CCK8 assay	[PMID: 29288940]
BaF3	IC₅₀	42.4 nM Compound: 5	Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK L1196M mutant after 72 hrs by SRB or CCK8 assay Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK L1196M mutant after 72 hrs by SRB or CCK8 assay	[PMID: 29288940]
BaF3	IC₅₀	>1000 nM Compound: 5	Antiproliferative activity against IL3-stimulated mouse BAF3 cells after 72 hrs by SRB or CCK8 assay Antiproliferative activity against IL3-stimulated mouse BAF3 cells after 72 hrs by SRB or CCK8 assay	[PMID: 29288940]
HCC78	IC₅₀	357 nM Compound: 5	Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by SRB or CCK8 assay Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by SRB or CCK8 assay	[PMID: 29288940]
KARPAS-299	IC₅₀	3 nM Compound: 5	Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by SRB or CCK8 assay Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by SRB or CCK8 assay	[PMID: 29288940]
NCI-H3122	IC₅₀	7.8 nM Compound: 5	Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB or CCK8 assay Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB or CCK8 assay	[PMID: 29288940]
NIH3T3	IC₅₀	0.2 nM Compound: 8k, PF-06463922	Inhibition of human EML4-fused ALK F1174L mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA Inhibition of human EML4-fused ALK F1174L mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA	[PMID: 24819116]
NIH3T3	IC₅₀	1.3 nM Compound: 8k, PF-06463922	Inhibition of wild type human EML4-fused ALK expressed in mouse NIH-3T3 cells assessed as phosphorylated ALK level after 1 hr by sandwich ELISA Inhibition of wild type human EML4-fused ALK expressed in mouse NIH-3T3 cells assessed as phosphorylated ALK level after 1 hr by sandwich ELISA	[PMID: 24819116]
NIH3T3	IC₅₀	1.6 nM Compound: 8k, PF-06463922	Inhibition of human EML4-fused ALK C1156Y mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA Inhibition of human EML4-fused ALK C1156Y mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA	[PMID: 24819116]
NIH3T3	IC₅₀	15 nM Compound: 8k, PF-06463922	Inhibition of human EML4-fused ALK G1269A mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA Inhibition of human EML4-fused ALK G1269A mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA	[PMID: 24819116]
NIH3T3	IC₅₀	21 nM Compound: 8k, PF-06463922	Inhibition of human EML4-fused ALK L1196M mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA Inhibition of human EML4-fused ALK L1196M mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA	[PMID: 24819116]
NIH3T3	IC₅₀	38 nM Compound: 8k, PF-06463922	Inhibition of human EML4-fused ALK 1151Tins mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA Inhibition of human EML4-fused ALK 1151Tins mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA	[PMID: 24819116]
NIH3T3	IC₅₀	4.2 nM Compound: 8k, PF-06463922	Inhibition of human EML4-fused ALK S1206Y mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA Inhibition of human EML4-fused ALK S1206Y mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA	[PMID: 24819116]
NIH3T3	IC₅₀	77 nM Compound: 8k, PF-06463922	Inhibition of human EML4-fused ALK G1202R mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA Inhibition of human EML4-fused ALK G1202R mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA	[PMID: 24819116]
NIH3T3	IC₅₀	9 nM Compound: 8k, PF-06463922	Inhibition of human EML4-fused ALK L1152R mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA Inhibition of human EML4-fused ALK L1152R mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA	[PMID: 24819116]
SU-DHL-1	IC₅₀	4.9 nM Compound: 5	Antiproliferative activity against human SU-DHL1 cells harboring NPM-ALK after 72 hrs by SRB or CCK8 assay Antiproliferative activity against human SU-DHL1 cells harboring NPM-ALK after 72 hrs by SRB or CCK8 assay	[PMID: 29288940]

In Vitro

Lorlatinib (PF-06463922) 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 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 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.

In Vivo

In rats, Lorlatinib (PF-06463922) displays low plasma clearance, a moderate volume of distribution, a reasonable half-life, low propensity for p-glycoprotein 1-mediated efflux and a bioavailability of 100%^[1]. In vivo, Lorlatinib shows cytoreductive antitumor efficacy in the NIH3T3 xenograft models expressing human CD74-ROS1 and Fig-ROS1 via inhibition in ROS1 phosphorylation and the downstream signaling molecules, as well as inhibition of the cell cycle protein Cyclin D1 in tumors. Lorlatinib also demonstrates marked antitumor activity in mice bearing tumor xenografts expressing EML4-ALK, EML4-ALK-L1196M, EML4-ALK-G1269A, EML4-ALK-G1202R or NPM-ALK^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1454846-35-5
Appearance Solid
Molecular Weight 406.41
Formel C₂₁H₁₉FN₆O₂
Color White to off-white
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
Synonyms

PF-06463922
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (38)

All In Vivo Efficacy StudyCell Proliferation/Viability AssayCell Imaging/StainingWB

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Journal Impact Factor

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 Dec 2;14(12):2367-2386. PMID: 39269178

Lorlatinib purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2024 Dec 2;14(12):2367-2386. [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.
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 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 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 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.
Cancer Res

Mesenchymal-Type Neuroblastoma Cells Escape ALK Inhibitors. [Abstract]

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 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.
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
J Exp Med

EML4-ALK fusions drive lung adeno-to-squamous transition through JAK-STAT activation. [Abstract]

2024 Mar 4;221(3):e20232028. PMID: 38284990
Oncogene

ALK fusion promotes metabolic reprogramming of cancer cells by transcriptionally upregulating PFKFB3. [Abstract]

2022 Sep;41(40):4547-4559. PMID: 36064579
Oncogene

Novel TENM3-ALK fusion is an alternate mechanism for ALK activation in neuroblastoma. [Abstract]

2022 May;41(20):2789-2797. PMID: 35411036
Leukemia

Unraveling the impact of crizotinib to promote megakaryopoiesis for alleviating thrombocytopenia in myelodysplastic neoplasms. [Abstract]

2025 Aug 14. PMID: 40813622
EMBO Mol Med

Vulnerability of drug-resistant EML4-ALK rearranged lung cancer to transcriptional inhibition. [Abstract]

2020 Jul 7;12(7):e11099. PMID: 32558295
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 Syst Biol

Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]

2024 Jan;20(1):28-55. PMID: 38177929
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
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
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
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
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
Mol Pharmacol

Influence of Tyrosine Kinase Inhibition on Organic Anion Transporting Polypeptide 1B3-Mediated Uptake. [Abstract]

2022 Jun;101(6):381-389. PMID: 35383108
Fundam Clin Pharmacol

Inhibition of organic cation transporter 3 activity by tyrosine kinase inhibitors. [Abstract]

2021 Oct;35(5):919-929. PMID: 33523504
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 Dec 15:1267:124770. PMID: 40902417
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
bioRxiv

2026 Jan 27.
bioRxiv

Prevalence and Actionability of MTAP Loss in Oncogene-Driven Lung Cancer. [Abstract]

2026 Jan 23:2026.01.21.700721. PMID: 41648424
bioRxiv

2025 Dec 5.
Maastricht University

2023 Jun 1.
Universitat Autònoma de Barcelona

2022 Aug.
Uppsala University

2022 Feb.
bioRxiv

October 28, 2021.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 28 mg/mL (68.90 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4606 mL

12.3028 mL

24.6057 mL

5 mM

0.4921 mL

2.4606 mL

4.9211 mL

10 mM

0.2461 mL

1.2303 mL

2.4606 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.15 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (6.15 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.15 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 4

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 2.5 mg/mL (6.15 mM); Clear solution

Working Solution

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.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 5 mg/mL (12.30 mM); Clear solution; Need ultrasonic

Protocol 2

Add each solvent one by one: 0.5% CMC/saline water

Solubility: 1 mg/mL (2.46 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Cell Assay^[2]

Cells are seeded in 96-well plates in growth medium containing 10% FBS and are cultured overnight at 37°C. The following day, serial dilutions of Lorlatinib or appropriate controls are added to the designated wells, and cells are incubated at 37°C for 72 h. A CellTiter-Glo assay is performed to determine the relative cell numbers. IC₅₀ values are calculated by concentration-response curve fitting using a four-parameter analytical method.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[2]

De novoGBM tumorigenesis is initiated in LSL-FIG-ROS1;Cdkn2a−/−;LSL-Luc mice through intracranial stereotactic injections of Adeno-Cre as described previously. Tumor development is monitored using BLI as described below. Once tumors reach a given size (10⁷ p^-1·s^-1·cm^-2·sr^-1), animals are randomLy enrolled into vehicle control or 3-, 7-, or 14-d treatment with the indicated doses of Lorlatinib. Drug is administered through s.c. implanted Alzet osmotic pumps. After treatment, mice are killed, GBM tumors are microdissected, and tissues are flash-frozen in liquid N₂. The remaining brains are processed for histology.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4606 mL	12.3028 mL	24.6057 mL	61.5142 mL
	5 mM	0.4921 mL	2.4606 mL	4.9211 mL	12.3028 mL
	10 mM	0.2461 mL	1.2303 mL	2.4606 mL	6.1514 mL
	15 mM	0.1640 mL	0.8202 mL	1.6404 mL	4.1009 mL
	20 mM	0.1230 mL	0.6151 mL	1.2303 mL	3.0757 mL
	25 mM	0.0984 mL	0.4921 mL	0.9842 mL	2.4606 mL
	30 mM	0.0820 mL	0.4101 mL	0.8202 mL	2.0505 mL
	40 mM	0.0615 mL	0.3076 mL	0.6151 mL	1.5379 mL
	50 mM	0.0492 mL	0.2461 mL	0.4921 mL	1.2303 mL
	60 mM	0.0410 mL	0.2050 mL	0.4101 mL	1.0252 mL

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Lorlatinib

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