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Pyridostatin Trifluoroacetate Salt

Cat. No. M9180
Pyridostatin Trifluoroacetate Salt Structure
Synonym:

Pyridostatin TFA salt; PDS; CAS# 1085412-37-8(free base)

Size Price Availability Quantity
5mg USD 97 In stock
10mg USD 167 In stock
50mg USD 547 In stock
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Quality Control
Biological Activity

Pyridostatin Trifluoroacetate Salt is a G-quadruplexe stabilizer, with a Kd of 490 nM. Pyridostatin stabilizes G-quadruplexes (G4s) in cells and elicits a DNA damage response by causing the formation of DNA double strand breaks (DSB). Pyridostatin promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin targets gene bodies containing clusters of sequences with a propensity for G-quadruplex formation. Pyridostatin (PDS) shows neurotoxic activity against primary cortical neurons at 0.01-5 μM, causes DNA double-strand breaks (DSBs) at 1 μM, downregulates BRCA1 in neurons at 1, 2 or 5 μM.

CAS# 1085412-37-8(free base)

Protocol
Cell Experiment
Cell lines MRC-5–SV40 cells and various cancer cell lines
Preparation method Cells are plated at equal confluence and are left either untreated or were treated with 2 μM pyridostatin continually during the indicated time before harvesting the cells. Cells from individual plates are trypsinized and counted in a Coulter counter. Graphs represent the total cell numbers at each time interval, and the error bars represent the s.e.m. Data represent three independent experiments.
Concentrations 10 μM
Incubation time 48 h
Animal Experiment
Animal models
Formulation
Dosages
Administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 938.72
Formula C37H35F9N8O11
CAS Number 1472611-44-1
Purity 99.87%
Solubility DMSO: ≥ 90 mg/mL
Storage at -20°C
References

Small-molecule-induced DNA damage identifies alternative DNA structures in human genes.
Rodriguez R, et al. Nat Chem Biol. 2012 Feb 5;8(3):301-10. PMID: 22306580.

A single-molecule platform for investigation of interactions between G-quadruplexes and small-molecule ligands.
Koirala D, et al. Nat Chem. 2011 Aug 28;3(10):782-7. PMID: 21941250.

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Keywords: Pyridostatin Trifluoroacetate Salt, Pyridostatin TFA salt; PDS; CAS# 1085412-37-8(free base) supplier, DNA/RNA Synthesis, inhibitors

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