Home DNA Damage/DNA Repair PARP inhibitor RBN012759 For research use only.

RBN012759

RBN012759 is a potent and selective inhibitor of PARP14 with IC50 of <3 nM and 5 nM for human catalytic domain and mouse catalytic domain, respectively. RBN012759 contributes to anti-tumor immune response.

RBN012759 Chemical Structure

RBN012759 Chemical Structure

CAS: 2360851-29-0

Purity & Quality Control

Batch: S899201 DMSO] 76 mg/mL] false] Ethanol] 5 mg/mL] false] Water] Insoluble] false Purity: 99.99%
99.99

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Biological Activity

Description RBN012759 is a potent and selective inhibitor of PARP14 with IC50 of <3 nM and 5 nM for human catalytic domain and mouse catalytic domain, respectively. RBN012759 contributes to anti-tumor immune response.
Targets
human PARP14 [2]
(Cell-free assay)		 mouse PARP14 [2]
(Cell-free assay)
<3 nM 5 nM
In vitro
In vitro

RBN012759 is a sufficiently soluble, highly permeable, low efflux and potent inhibitor of human and mouse PARP14 with high PARP family selectivity. RBN012759 treatment of human primary macrophages decreases the MAR/PAR signal corresponding to PARP14 self-MARylation and stabilizes PARP14 protein in a dose-dependent manner. Treatment of primary human macrophages with RBN012759 leads to decreased IL-4 driven M2-like gene expression, suggesting that PARP14 inhibition results in a less immunosuppressive phenotype. [2]
In Vivo
In vivo

RBN012759 has moderate clearance and oral bioavailability in mice. RBN012759 is well-tolerated in mice with repeat dosing up to 500 mg/kg BID (75-fold coverage of the PARP14 mouse). [2]

Chemical Information & Solubility

Molecular Weight 378.46 Formula

C19H23FN2O3S
CAS No. 2360851-29-0 SDF --
Smiles OC1CCC(CC1)SCC2=NC3=CC(=CC(=C3C(=O)N2)F)OCC4CC4
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 76 mg/mL ( (200.81 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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