Product Name

Lorlatinib (PF-6463922)

General description

Lorlatinib is a potent, dual ALK/ROS1 inhibitor.

Synonym

(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

Purity

≥99.0%(HPLC)

CAS Number

1454846-35-5

Formula

C²¹H¹⁹FN⁶O²

Molecular Weight

406.41

Suitability

BioReagent,  suitable for cell culture, etc.

l  Physical and Chemical Information

Appearance

solid

Solubility(25℃)

DMSO

≥50mg/mL(warmed)

Ethanol

≥30mg/mL(warmed)

Water

Insoluble

l  Biological Information

Biochem/Physiol  Actions

Lorlatinib 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. Upon administration, lorlatinib binds to and inhibits both ALK and ROS1 kinases. The kinase inhibition leads to disruption of ALK- and ROS1-mediated signaling and eventually inhibits tumor cell growth in ALK- and ROS1-overexpressing tumor cells. In addition, PF-06463922 is able to ross the blood brain barrier. ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development; ALK dysregulation and gene rearrangements are associated with a series of tumors. ROS1, overexpressed in certain cancer cells, plays a key role in cell growth and survival of cancer cells.

PF-06463922 is a potent, dual ALK/ROS1 inhibitor with Ki of <0.02 nM, <0.07 nM, and 0.7 nM for ROS1, ALK (WT), and ALK (L1196M), respectively.

Application

Lorlatinib has been used in trials studying the basic science and treatment of Non-small Cell Lung Cancer and  ALK-positive Non Small Cell Lung Cancer (NSCLC) and ROS1-positive NSCLC.

l  Storage

Storage temp.

-20℃

l  Precautions and Disclaimer

This product is for R&D use only, not for drug, household, or other uses.

l  References

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov