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Lorlatinib

Lorlatinib
Lorlatinib (PF-6463922) is an orally available, ATP-competitive inhibitor of the receptor tyrosine kinases, anaplastic lymphoma kinase (ALK) and C-ros oncogene 1 (Ros1), with potential antineoplastic activity.
Catalog No. T3061Cas No. 1454846-35-5
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Purity:99.93%
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Lorlatinib

Catalog No. T3061Cas No. 1454846-35-5
Lorlatinib (PF-6463922) is an orally available, ATP-competitive inhibitor of the receptor tyrosine kinases, anaplastic lymphoma kinase (ALK) and C-ros oncogene 1 (Ros1), with potential antineoplastic activity.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePriceAvailabilityQuantity
2 mg$35In Stock
5 mg$57In Stock
10 mg$87In Stock
25 mg$147In Stock
50 mg$237In Stock
100 mg$417In Stock
1 g$945In Stock
1 mL x 10 mM (in DMSO)$63In Stock
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Product Introduction

Bioactivity
Description
Lorlatinib (PF-6463922) is an orally available, ATP-competitive inhibitor of the receptor tyrosine kinases, anaplastic lymphoma kinase (ALK) and C-ros oncogene 1 (Ros1), with potential antineoplastic activity.
Targets&IC50
TYK1/LTK:2.7 nM, ALK (L1196M):0.07 nM(Ki), ROS1:<0.02 nM(Ki), ALK:<0.07 nM(Ki), FER:3.3 nM
In vitro
PF-06463922 effectively inhibits cell proliferation and induces apoptosis in HCC78 human NSCLC cells containing SLC34A2-ROS1 fusions and in BaF3-CD74-ROS1 cells expressing human CD74-ROS1. It also demonstrates this inhibitory action on cell proliferation and induces apoptosis in NSCLC cells with either non-mutated or mutated ALK fusions. PF-06463922 exhibits significant cellular activity against ALK and a wide range of ALK clinical mutations (IC50=0.2-77 nM).
In vivo
In NIH3T3 xenograft models expressing human CD74-ROS1 and Fig-ROS1, PF-06463922 inhibits cell proliferation by repressing ROS1 phosphorylation and downstream signaling molecules, including Cyclin D1. Furthermore, PF-06463922 demonstrates significant antitumor activity in mice bearing tumor grafts that overexpress EML4-ALK, EML4-ALK-L1196M, EML4-ALK-G1269A, EML4-ALK-G1202R, or NPM-ALK.
Kinase Assay
Recombinant human wild-type and mutant ALK kinase domain proteins (amino acids 1093–1411) are produced in-house using baculoviral expression, preactivated via autophosphorylation with MgATP, and assayed for kinase activity using a microfluidic mobility shift assay. The reactions contained 1.3 nM wild-type ALK or 0.5 nM mutant ALK (appropriate to produce 15-20% phosphorylation of peptide substrate after 1 h of reaction), 3 μM 5-FAM-KKSRGDYMTMQIG-CONH2), 5 mM MgCl2, and the Km level of ATP in 25 mM Hepes, pH 7.1. The inhibitors are shown to be ATP-competitive from kinetic and crystallographic studies. The Ki values are calculated by fitting the conversion (%) to a competitive inhibition equation. ROS1 enzyme is assayed as described above for ALK, except using 0.25 nM recombinant human ROS1 catalytic domain (amino acids 1883-2347). Kinase inhibitor selectivity is evaluated using a 206-kinase panel.
Cell Research
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 PF-06463922 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.
AliasPF-6463922, PF-06463922, Loratinib
Chemical Properties
Molecular Weight406.41
FormulaC21H19FN6O2
Cas No.1454846-35-5
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
Ethanol: 40.6 mg/mL (100 mM)
DMSO: 15 mg/mL (36.91 mM), Sonication is recommended.
Solution Preparation Table
DMSO/Ethanol
1mg5mg10mg50mg
1 mM2.4606 mL12.3028 mL24.6057 mL123.0285 mL
5 mM0.4921 mL2.4606 mL4.9211 mL24.6057 mL
10 mM0.2461 mL1.2303 mL2.4606 mL12.3028 mL
20 mM0.1230 mL0.6151 mL1.2303 mL6.1514 mL
Ethanol
1mg5mg10mg50mg
50 mM0.0492 mL0.2461 mL0.4921 mL2.4606 mL
100 mM0.0246 mL0.1230 mL0.2461 mL1.2303 mL

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