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RBN012759 PARP inhibitor

Name: RBN012759
Brand: Selleck Chemicals
SKU: S8992
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S8992

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. This compound contributes to anti-tumor immune response.

Chemical Structure

Molecular Weight: 378.46

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

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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Chemical Information, Storage & Stability

Molecular Weight	378.46	Formula	C₁₉H₂₃FN₂O₃S	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	2360851-29-0	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	OC1CCC(CC1)SCC2=NC3=CC(=CC(=C3C(=O)N2)F)OCC4CC4

Solubility

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

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.900mg/ml (5.02mM)	Taking the 1 mL working solution as an example, add 50 μL of 38 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.630mg/ml (1.66mM)	Taking the 1 mL working solution as an example, add 50 μL of 12.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.

Mechanism of Action

Targets/IC₅₀/Ki	human PARP14 ^[2] (Cell-free assay) <3 nM mouse PARP14 ^[2] (Cell-free assay) 5 nM
In vitro	RBN012759 is a sufficiently soluble, highly permeable, low efflux and potent inhibitor of human and mouse PARP14 with high PARP family selectivity. Treatment of human primary macrophages with this compound 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 this inhibitor leads to decreased IL-4 driven M2-like gene expression, suggesting that PARP14 inhibition results in a less immunosuppressive phenotype. ^[2]
In vivo	RBN012759 has moderate clearance and oral bioavailability in mice. This compound is well-tolerated in mice with repeat dosing up to 500 mg/kg BID (75-fold coverage of the PARP14 mouse). ^[2]
References	https://cancerres.aacrjournals.org/content/80/16_Supplement/1038 https://ribontx.com/wp-content/uploads/2020/04/L.-SCHENKEL-2020_FINAL.pdf

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Handling Instructions

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