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Pyridostatin TFA

Names

[ CAS No. ]:
1472611-44-1

[ Name ]:
Pyridostatin TFA

[Synonym ]:
4-(2-Aminoethoxy)-N,N'-bis[4-(2-aminoethoxy)-2-quinolinyl]-2,6-pyridinedicarboxamide trifluoroacetate (1:1)
RR82 trifluoroacetate salt
4-(2-Aminoethoxy)-N2,N6-bis[4-(2-aminoethoxy)-2-quinolinyl]-2,6-pyridinedicarboxamide trifluoroacetate salt
Acetic acid, 2,2,2-trifluoro-, compd. with 4-(2-aminoethoxy)-N2,N6-bis[4-(2-aminoethoxy)-2-quinolinyl]-2,6-pyridinedicarboxamide (1:1)
Pyridostatin Trifluoroacetate Salt
MFCD26142941

Biological Activity

[Description]:

Pyridostatin (RR82) TFA is a G-quadruplex DNA stabilizing agent (Kd=490 nM). Pyridostatin TFA promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin TFA targets the proto-oncogene Src. Pyridostatin TFA reduced SRC protein levels and SRC-dependent cellular motility in human breast cancer cells[1][2][3].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Cell Cycle/DNA Damage >> G-quadruplex

[In Vitro]

Pyridostatin (RR82) hydrochloride (10 μM; 48 hours) induces cell cycle arrest[1]. Pyridostatin TFA is a very selective G-quadruplex DNA-binding small molecule designed to form a complex with and stabilize G-quadruplex structure. Pyridostatin TFA causes neurite retraction, synaptic loss, and dose-dependent neuronal death. In cultured primary neurons, Pyridostatin TFA induces the formation of DNA DSBs. Remarkably, Pyridostatin TFA (1-5 μM, overnight) downregulates the BRCA1 protein, a protein that guards and repairs the neuronal genome, at the transcriptional level[3]. Cell Viability Assay[1] Cell Line: Over 60 different cancer cell lines Concentration: 10 μM Incubation Time: 48 hours Result: Predominantly accumulated in the G2 phase of the cell cycle over 60 different cancer cell lines.

[References]

[1]. Rodriguez R, et al. Small-molecule-induced DNA damage identifies alternative DNA structures in human genes. Nat Chem Biol. 2012;8(3):301-310. Published 2012 Feb 5.

[2]. Koirala D, et al. A single-molecule platform for investigation of interactions between G-quadruplexes and small-molecule ligands. Nat Chem. 2011;3(10):782-787. Published 2011 Aug 28.

[3]. Moruno-Manchon JF, et al. The G-quadruplex DNA stabilizing drug pyridostatin promotes DNA damage and downregulates transcription of Brca1 in neurons. Aging (Albany NY). 2017;9(9):1957-1970.

Chemical & Physical Properties

[ Molecular Formula ]:
C33H33F3N8O7

[ Molecular Weight ]:
710.660

[ Exact Mass ]:
710.242432

Related Compounds