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PF-06463922 (Lorlatinib, CAS: 1454846-35-5) is for research use only. Condition of sample preparation and optimal sample dilution should be determined experimentally by the investigator.
Price/availability/specifications subject to change without notice. Unless otherwise indicated, our catalog and customized products are for research use only and not intended for human or animal diagnostic or therapeutic use.
Phone: 1-617-401-8149
Fax: 1-617-606-5019
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CAS No.: 1454846-35-5.
Molecular Formula: C25H19FN6O2 . 0.7xH2O.
Molecular Weight: 419.0.
Purity: >99.5% Chemical Purity (HPLC at 215 and 254 nm), 100% Optical Purity (by Chiral HPLC).
QC: HPLC-MS, Chiral HPLC and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO.
Storage: Store at 0oC (short term), -20oC (long term), Desiccated.
Background:
PF-06463922 (Lorlatinib, CAS: 1454846-35-5) is an orally bioavailable and blood-brain-barrier (BBB) penetrable dual ALK/ROS1 inhibitor, a cyclic small molecule engineered from Crizotinib. It is highly potent with Ki values of <0.02 nM, <0.07 nM, and 0.7 nM against ROS1, ALK (WT), and ALK (L1196M), respectively, and displays a broad-spectrum potency against ALK-Resistant Mutations (with IC50s at lower nM).
Reference about PF-06463922 (Lorlatinib, CAS number: 1454846-35-5):
1. 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. TW Johnson, et al, J Med Chem. 2014 Jun 12; 57(11):4720-44, doi: 10.1021/jm500261q. Epub 2014 Jun 3. PubMed PMID: 24819116.
Questions about PF-06463922 (Lorlatinib, CAS number: 1454846-35-5):
Question: What is the solubility of PF 06463922?
Answer: The solubility of PF 06463922 in DMSO is 5 mg/mL, in DMF: 5 mg/mL, in Ethanol: 1 mg/mL, and in Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/mL.
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