Atamparib (RBN-2397)

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

Atamparib (RBN-2397) Chemical Structure

CAS: 2381037-82-5

Purity & Quality Control

Batch: Purity: 99.80%
99.80

Atamparib (RBN-2397) Related Products

Signaling Pathway

Choose Selective PARP Inhibitors

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
In vitro

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

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

--

In Vivo
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]

Animal Research 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
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05127590 Active not recruiting
Advanced Squamous Non-Small Cell Lung Carcinoma
Ribon Therapeutics Inc.
March 15 2022 Phase 1|Phase 2
NCT04053673 Recruiting
Solid Tumor Adult
Ribon Therapeutics Inc.
August 1 2019 Phase 1

Chemical Information & Solubility

Molecular Weight 523.43 Formula

C20H23F6N7O3

CAS No. 2381037-82-5 SDF --
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
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (191.04 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 13 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.
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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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