Atamparib (RBN-2397)

Catalog No.S8993

For research use only.

Atamparib (RBN-2397) is a potent, selective and orally active NAD+ competitive inhibitor PARP7 with IC50 of <3 nM and Kd of <0.001 μM. RBN-2397 has the potential for the research of tumor treatment.

Atamparib (RBN-2397) Chemical Structure

CAS No. 2381037-82-5

Purity & Quality Control

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Biological Activity

Description Atamparib (RBN-2397) is a potent, selective and orally active NAD+ competitive inhibitor PARP7 with IC50 of <3 nM and Kd of <0.001 μM. RBN-2397 has the potential for the research of tumor treatment.
Targets
PARP7 [1]
(Cell-free assay)
PARP7 [1]
(Cell-free assay)
<0.001 μM(Kd) <3 nM
In vitro

RBN-2397 restores cytosolic nucleic acid sensing and blocks cell proliferation in a human lung cancer cell line.[1]

In vivo

RBN-2397 causes complete regressions in human NSCLC NCI-H1373 xenografts and dose-dependent pharmacodynamic effects. RBN-2397 induces tumor-specific adaptive immune memory in CT26 syngeneic model with durable complete responses.[1]

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: NCI-H1373 human lung cancer cells
  • Concentrations: 0.4 nM to 1000 nM
  • Incubation Time: 24 h
  • Method:

    --

Animal Research:

[1]

  • Animal Models: CB17 SCID mice with NCI-H1373 xenografts, CT26 tumor-bearing BALB/c mice
  • Dosages: 300 mg/kg, 100 mg/kg, 30 mg/kg, 10 mg/kg, 3 mg/kg
  • Administration: Oral gavage

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(191.04 mM)
Water Insoluble
Ethanol '7 mg/mL

Chemical Information

Molecular Weight 523.43
Formula

C20H23F6N7O3

CAS No. 2381037-82-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(COCCC(=O)N1CCN(CC1)C2=NC=C(C=N2)C(F)(F)F)NC3=C(C(=O)NN=C3)C(F)(F)F

In vivo Formulation Calculator (Clear solution)

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

mg/kg g μL

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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05127590 Recruiting Drug: RBN-2397 Advanced Squamous Non-Small Cell Lung Carcinoma Ribon Therapeutics Inc. February 15 2022 Phase 1|Phase 2
NCT04053673 Recruiting Drug: RBN-2397 Solid Tumor Adult Ribon Therapeutics Inc. August 1 2019 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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