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Cat.No. 6461 - PARPi-FL | C34H32BF3N6O3 | CAS No. 1380359-84-1
Description: Potent fluorescent PARP inhibitor; cell permeable
Chemical Name: (T-4)-[4-[[3-[[4-[3-[5-[(3,5-Dimethyl-2H-pyrrol-2-ylidene-κN)methyl]-1H-pyrrol-2-yl-κN-1-oxopropyl]-1-piperazinyl]carbonyl]-4-fluorophenyl]methyl]-1(2H)-phthalazinonato]difluoroboron
Purity: ≥90% (HPLC)
Literature (3)

Biological Activity

Fluorescent potent PARP inhibitor (IC50 = 12 nM). Composed of a PARP inhibitor conjugated to BDY FL, SE (Cat. No. 5465). Colocalizes with PARP immunostaining in multiple cancer cell lines in vivo and accumulates in tumor cells and tumor associated macrophages. Enables high temporal and subcellular spatial resolution of drug distribution. Emission max = 525 nm. Cell permeable.

Technical Data

M. Wt 640.46
Formula C34H32BF3N6O3
Storage Store at -20°C
Purity ≥90% (HPLC)
CAS Number 1380359-84-1
PubChem ID 70697686
Smiles CC1=CC(C)=[N+]2C1=CC3=CC=C(N3[B-]2(F)F)CCC(N4CCN(C(C5=CC(CC6=NNC(C7=CC=CC=C67)=O)=CC=C5F)=O)CC4)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 6.4 10

Preparing Stock Solutions

The following data is based on the product molecular weight 640.46. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.1 mM 15.61 mL 78.07 mL 156.14 mL
0.5 mM 3.12 mL 15.61 mL 31.23 mL
1 mM 1.56 mL 7.81 mL 15.61 mL
5 mM 0.31 mL 1.56 mL 3.12 mL

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References are publications that support the biological activity of the product.

Thurber et al (2013) Single-cell and subcellular pharmacokinetic imaging allows insight into drug action in vivo. Nat.Commun. 4 1504 PMID: 23422672

Thurber et al (2014) Effect of small-molecule modification on single-cell pharmacokinetics of PARP inhibitors. Mol.Cancer Ther. 13 986 PMID: 24552776

Dubach et al (2017) Quantitating drug-target engagement in single cells in vitro and in vivo. Nat.Chem.Biol. 13 168 PMID: 27918558

If you know of a relevant reference for PARPi-FL, please let us know.

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