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1454846-35-5,MFCD28144520
Catalog No.:AA001D0O

1454846-35-5 | Pf-06463922

Pack Size
Purity
Availability
Price(USD)
Quantity
  
1mg
98%
in stock  
$12.00   $8.00
- +
5mg
98%
in stock  
$25.00   $18.00
- +
100mg
98%
in stock  
$83.00   $58.00
- +
250mg
98%
in stock  
$159.00   $111.00
- +
  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
  • Request for Quotation
  • Download SDS
  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
Technical Information
Catalog Number:
AA001D0O
Chemical Name:
Pf-06463922
CAS Number:
1454846-35-5
Molecular Formula:
C21H19FN6O2
Molecular Weight:
406.4130
MDL Number:
MFCD28144520
SMILES:
N#Cc1n(C)nc2c1c1cnc(c(c1)O[C@H](C)c1c(C(=O)N(C2)C)ccc(c1)F)N
Properties
Computed Properties
 
Complexity:
700  
Covalently-Bonded Unit Count:
1  
Defined Atom Stereocenter Count:
1  
Heavy Atom Count:
30  
Hydrogen Bond Acceptor Count:
7  
Hydrogen Bond Donor Count:
1  
XLogP3:
1.5  

Downstream Synthesis Route

[1]CurrentPatentAssignee:PFIZERINC-WO2013/132376,2013,A1Locationinpatent:Page/Pagecolumn259-260

[2]Johnson,TedW.;Richardson,PaulF.;Bailey,Simon;Brooun,Alexei;Burke,BenjaminJ.;Collins,MichaelR.;Cui,J.Jean;Deal,JudithG.;Deng,Ya-Li;Dinh,Dac;Engstrom,LarsD.;He,Mingying;Hoffman,Jacqui;Hoffman,RobertL.;Huang,Qinhua;Kania,RobertS.;Kath,JohnC.;Lam,Hieu;Lam,JustineL.;Le,PhuongT.;Lingardo,Laura;Liu,Wei;McTigue,Michele;Palmer,CynthiaL.;Sach,NealW.;Smeal,Tod;Smith,GrahamL.;Stewart,AlbertE.;Timofeevski,Sergei;Zhu,Huichun;Zhu,Jinjiang;Zou,HelenY.;Edwards,MartinP.[JournalofMedicinalChemistry,2014,vol.57,#11,p.4720-4744]

[3]CurrentPatentAssignee:PFIZERINC-WO2014/207606,2014,A1Locationinpatent:Page/Pagecolumn37-38

[4]Elleraas,Jeff;Ewanicki,Jason;Johnson,TedW.;Sach,NealW.;Collins,MichaelR.;Richardson,PaulF.[AngewandteChemie-InternationalEdition,2016,vol.55,#11,p.3590-3595][Angew.Chem.,2016,vol.128,p.3654-3659,6]

[1]CurrentPatentAssignee:PFIZERINC-WO2014/207606,2014,A1Locationinpatent:Page/Pagecolumn60

[1]CurrentPatentAssignee:PFIZERINC-WO2014/207606,2014,A1

[1]CurrentPatentAssignee:PFIZERINC-WO2017/21823,2017,A1Locationinpatent:Page/Pagecolumn18

[2]CurrentPatentAssignee:PFIZERINC-WO2014/207606,2014,A1Locationinpatent:Page/Pagecolumn59-60

[3]Li,Bryan;Li,Ruizhi;Dorff,Peter;McWilliams,J.Christopher;Guinn,RobertM.;Guinness,StevenM.;Han,Lu;Wang,Ke;Yu,Shu[JournalofOrganicChemistry,2019,vol.84,#8,p.4846-4855]

[4]CurrentPatentAssignee:TEVAPHARMACEUTICALINDUSTRIESLTD.-WO2019/209633,2019,A1Locationinpatent:Paragraph00210;00236

[1]CurrentPatentAssignee:TELIGENE-WO2016/26423,2016,A1Locationinpatent:Paragraph0045;0046

[2]CurrentPatentAssignee:TELIGENE-US2017/216264,2017,A1Locationinpatent:Paragraph0064-0068

Literature

Title: Tackling ALK in non-small cell lung cancer: the role of novel inhibitors.

Journal: Translational lung cancer research 20160601

Title: Resistance: Crizotinib makes a comeback.

Journal: Nature reviews. Cancer 20160201

Title: Resensitization to Crizotinib by the Lorlatinib ALK Resistance Mutation L1198F.

Journal: The New England journal of medicine 20160107

Title: PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations.

Journal: Proceedings of the National Academy of Sciences of the United States of America 20150317

Title: 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.

Journal: Journal of medicinal chemistry 20140612

Title: 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,3-h,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.

Title: 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

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