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Synonyms: compound 1 (Table 1) [WO2012173521] | PF114
Compound class: Synthetic organic
Comment: PF-114 is a third generation BCR-ABL kinase inhibitor [2-3]. It was designed to target wild-type resistance mutations in BCR-ABL (including the T315I gatekeeper mutation) in order to overcome drug resistance in Philadelphia chromosome positive (Ph+) leukemias. The chemical strucure is claimed in patent WO2012173521 where it is the first compound listed in Table 1 of the patent . Off-targets identified by kinase profile screening include ABL2/ARG, DDR1, DDR2, FMS, FRK/PTK5, LCK, LYN, LYNB, PDGFRα and RET which had <10% residual activity when exposed to 100 nM of inhibitor .
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Chilov GG, Titov IY. (2016)
Protein kinase inhibitors (variants), use thereof in treating oncological diseases and a pharmaceutical composition based thereon.
Patent number: WO2012173521. Assignee: Fusion Pharma. Priority date: 16/06/2011. Publication date: 20/12/2016.
2. Mian A, Rafiei A, Metodieva A, Hebersbosch I, Zeifman A, Titov I, Stroylov V, Stroganov O, Novikov F, Ottman OG et al.. (2013)
PF-114, a Novel Selective Pan BCR/ABL Inhibitor Targets The T315I and Suppress Models Of Advanced Ph+ ALL.
Blood, 122: 3907 Meeting poster. DOI: 10.1182/blood.V122.21.3907.3907
3. Mian AA, Rafiei A, Haberbosch I, Zeifman A, Titov I, Stroylov V, Metodieva A, Stroganov O, Novikov F, Brill B et al.. (2015)
PF-114, a potent and selective inhibitor of native and mutated BCR/ABL is active against Philadelphia chromosome-positive (Ph+) leukemias harboring the T315I mutation.
Leukemia, 29 (5): 1104-14. [PMID:25394714]