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Substance Name: Lorlatinib [USAN:INN]
RN: 1454846-35-5
UNII: OSP71S83EU
InChIKey: IIXWYSCJSQVBQM-LLVKDONJSA-N

Note

  • Inhibits both anaplastic lymphoma kinase and c-ros oncogene 1 (ROS1) protein.

    NCI: 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, lorlatinib is able to cross 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. (NCI Thesaurus)

Molecular Formula

  • C21-H19-F-N6-O2

Molecular Weight

  • 406.4191
 

Classification Codes

  • Antineoplastic
  • Antineoplastic Agents
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Names and Synonyms

Name of Substance

  • Lorlatinib [USAN:INN]
  • PF-06463922

Synonyms

  • 2H-4,8-Methenopyrazolo(4,3-H)(2,5,11)benzoxadiazacyclotetradecine-3-carbonitrile, 7-amino-12-fluoro-10,15,16,17-tetrahydro-2,10,16-trimethyl-15-oxo-, (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
  • Loratinib
  • Lorlatinib
  • PF 06463922
  • PF-06463922
  • UNII-OSP71S83EU

Registry Numbers

CAS Registry Number

  • 1454846-35-5

FDA UNII

  • OSP71S83EU

System Generated Number

  • 1454846355

Structure Descriptors

InChI

1S/C21H19FN6O2/c1-11-15-7-13(22)4-5-14(15)21(29)27(2)10-16-19(17(8-23)28(3)26-16)12-6-18(30-11)20(24)25-9-12/h4-7,9,11H,10H2,1-3H3,(H2,24,25)/t11-/m1/s1

InChIKey

IIXWYSCJSQVBQM-LLVKDONJSA-N

Smiles

C[C@H]1Oc2cc(cnc2N)c3c(CN(C)C(=O)c4ccc(F)cc14)nn(C)c3C#N