Cat. No.: HY-136174

RBN-2397

17 Cited Publications

Customer Review

Based on 17 publication(s) in Google Scholar

RBN-2397 is a potent, accross species and orally active NAD⁺ competitive inhibitor of PARP7 (IC₅₀<3 nM). RBN-2397 selectively binds to PARP7 (K_d=0.001 μM) and restores IFN signaling. RBN-2397 has the potential for the study of advanced or metastatic solid tumors.

For research use only. We do not sell to patients.

Purity: 99.82%
CAS No.: 2381037-82-5
Formula: C₂₀H₂₃F₆N₇O₃
Molecular Weight:523.43

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

RBN-2397 Chemical Structure

CAS No.: 2381037-82-5

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (17)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[2]

PARP-7

3 nM (IC₅₀)

PARP-7

1 nM (Kd)

All PARP Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
AML12	IC₅₀	>50 μM Compound: RBN-2397	Cytotoxicity against mouse AML12 cells assessed as inhibition of cell growth measured after 6 days by MTT assay Cytotoxicity against mouse AML12 cells assessed as inhibition of cell growth measured after 6 days by MTT assay	[PMID: 36576395]
AML12	IC₅₀	>50 μM Compound: RBN-2397	Antiproliferative activity against mouse AML12 cells measured after 6 days incubation by MTT assay Antiproliferative activity against mouse AML12 cells measured after 6 days incubation by MTT assay	[PMID: 38059836]
CT26	IC₅₀	12.59 μM Compound: RBN-2397	Antiproliferative activity against mouse CT26 cells assessed as inhibition of cell growth measured after 6 days by MTT assay Antiproliferative activity against mouse CT26 cells assessed as inhibition of cell growth measured after 6 days by MTT assay	[PMID: 36576395]
CT26	IC₅₀	2.31 μM Compound: RBN-2397	Antiproliferative activity against mouse CT26 cells measured after 6 days incubation by CTG assay Antiproliferative activity against mouse CT26 cells measured after 6 days incubation by CTG assay	[PMID: 38059836]
CT26	IC₅₀	5.29 μM Compound: RBN-2397	Antiproliferative activity against mouse CT26 cells measured after 6 days incubation by MTT assay Antiproliferative activity against mouse CT26 cells measured after 6 days incubation by MTT assay	[PMID: 38059836]
CT26	IC₅₀	6.33 μM Compound: RBN-2397	Antiproliferative activity against mouse CT26 cells assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay Antiproliferative activity against mouse CT26 cells assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay	[PMID: 36576395]
MV4-11	IC₅₀	0.51 μM Compound: 6; RBN-2397	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 3 days in presence of vorinostat by celltiter-glo luminescent assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 3 days in presence of vorinostat by celltiter-glo luminescent assay	[PMID: 38456618]
MV4-11	IC₅₀	7.97 μM Compound: 6; RBN-2397	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 3 days by celltiter-glo luminescent assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 3 days by celltiter-glo luminescent assay	[PMID: 38456618]
NCI-H1373	IC₅₀	0.13 μM Compound: 6; RBN-2397	Antiproliferative activity against human NCI-H1373 cells assessed as inhibition of cell growth incubated for 6 days in presence of vorinostat by celltiter-glo luminescent assay Antiproliferative activity against human NCI-H1373 cells assessed as inhibition of cell growth incubated for 6 days in presence of vorinostat by celltiter-glo luminescent assay	[PMID: 38456618]
NCI-H1373	IC₅₀	0.18 μM Compound: 6; RBN-2397	Antiproliferative activity against human NCI-H1373 cells assessed as inhibition of cell growth incubated for 6 days by celltiter-glo luminescent assay Antiproliferative activity against human NCI-H1373 cells assessed as inhibition of cell growth incubated for 6 days by celltiter-glo luminescent assay	[PMID: 38456618]
NCI-H1373	IC₅₀	4.76 nM Compound: RBN-2397	Antiproliferative activity against human NCI-H1373 cells assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay Antiproliferative activity against human NCI-H1373 cells assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay	[PMID: 36576395]
NCI-H1373	IC₅₀	40 nM Compound: RBN-2397	Antiproliferative activity against human NCI-H1373 cells assessed as inhibition of cell viability incubated for 4 days by luminescence based assay Antiproliferative activity against human NCI-H1373 cells assessed as inhibition of cell viability incubated for 4 days by luminescence based assay	[PMID: 37826932]
NCI-H1373	IC₅₀	45.3 nM Compound: RBN-2397	Antiproliferative activity against human NCI-H1373 cells incubated for 4 days by luminescence cell viability assay Antiproliferative activity against human NCI-H1373 cells incubated for 4 days by luminescence cell viability assay	[PMID: 38277917]
U-937	IC₅₀	0.73 μM Compound: 6; RBN-2397	Antiproliferative activity against human U-937 cells assessed as inhibition of cell growth incubated for 3 days in presence of vorinostat by celltiter-glo luminescent assay Antiproliferative activity against human U-937 cells assessed as inhibition of cell growth incubated for 3 days in presence of vorinostat by celltiter-glo luminescent assay	[PMID: 38456618]
U-937	IC₅₀	20.79 μM Compound: 6; RBN-2397	Antiproliferative activity against human U-937 cells assessed as inhibition of cell growth incubated for 3 days by celltiter-glo luminescent assay Antiproliferative activity against human U-937 cells assessed as inhibition of cell growth incubated for 3 days by celltiter-glo luminescent assay	[PMID: 38456618]

In Vitro

RBN-2397 (0.0001-100 μM; 24 hours) inhibits cells proliferation with an IC₅₀ value of 20 nM in NCI-H1373 lung cancer cells^[2].
RBN-2397 (0.4 nM-1 μM; 24 hours) shows a restoration of type I IFN response by an increase in STAT1 phosphorylation as a dose-dependent manner in NCI-H1373 human lung cancer cells^[2].
RBN-2397 (0.0001-1 μM; 24 hours) inhibits cell MARylation in a cell biochemial assay with an EC₅₀ value of 1 nM^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[2]

Cell Line:

NCI-H1373 lung cancer cells
Concentration:

0.0001 μM; 0.001 μM; 0.001 μM; 0.1 μM; 1 μM; 10 μM; 100 μM
Incubation Time:

24 hours
Result:

Blocked cell proliferation.

Western Blot Analysis^[2]

Cell Line:

NCI-H1373 lung cancer cells
Concentration:

0.4 nM-1 μM
Incubation Time:

24 hours
Result:

Increased p-STAT1 protein expression.

In Vivo

RBN-2397 (oral administration; 3-100 mg/kg; once daily; 24-32 days) induces tumor-specific adaptive immune memory in CT26 syngeneic model with durable complete responses in CT26 tumor-bearing BALB/c mice^[2].
RBN-2397 (oral administration; 3-100 mg/kg; once daily; 32 days) causes complete regressions at the dose 100 mg/kg and exerts a dose-dependent effects on tumor growth at dose levels of ≥30 mg/kg^[2].
The half-life (t_1/2) of RBN-2397 in vivo is 325 mins^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

CB17 SCID mice with NCI-H1373 xenografts^[2]
Dosage:

3 mg/kg, 10mg/kg, 30 mg/kg, 100 mg/kg
Administration:

Oral administration; once daily; 24-32 days
Result:

Decreased tumor volume and exerted anti-tumor effects.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 2381037-82-5
Appearance Solid
Molecular Weight 523.43
Formula C₂₀H₂₃F₆N₇O₃
Color White to off-white
SMILES

O=C1C(C(F)(F)F)=C(N[C@@H](C)COCCC(N2CCN(C3=NC=C(C(F)(F)F)C=N3)CC2)=O)C=NN1
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (17)

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Journal Impact Factor

J Exp Med

PARP7 inhibits type I interferon signaling to prevent autoimmunity and lung disease. [Abstract]

2025 May 5;222(5):e20241184. PMID: 39969510
Proc Natl Acad Sci U S A

CRISPR screens and quantitative proteomics reveal remodeling of the aryl hydrocarbon receptor-driven proteome through PARP7 activity. [Abstract]

2025 Jun 17;122(24):e2424985122. PMID: 40493189
Proc Natl Acad Sci U S A

PARP7-mediated ADP-ribosylation of FRA1 promotes cancer cell growth by repressing IRF1- and IRF3-dependent apoptosis. [Abstract]

2023 Dec 5;120(49):e2309047120. PMID: 38011562
EMBO J

Ubiquitin pathway blockade reveals endogenous ADP-ribosylation marking PARP7 and AHR for degradation. [Abstract]

2026 Jan;45(1):261-277. PMID: 41326691
EMBO J

RNF114 and RNF166 exemplify reader-writer E3 ligases that extend K11 polyubiquitin onto sites of MARUbylation. [Abstract]

2025 Nov;44(21):5993-6018. PMID: 41039157
EMBO J

PARP7 is a proteotoxic stress sensor that labels proteins for degradation. [Abstract]

2025 Aug 20. PMID: 40836037
EMBO J

PARP14 and PARP9/DTX3L regulate interferon-induced ADP-ribosylation. [Abstract]

2024 Jul;43(14):2929-2953. PMID: 38834853
EMBO Mol Med

Thioparib inhibits homologous recombination repair, activates the type I IFN response, and overcomes olaparib resistance. [Abstract]

2023 Mar 8;15(3):e16235. PMID: 36652375
Biochem Pharmacol

Loss of aryl hydrocarbon receptor reduces pancreatic tumor growth by increasing immune cell infiltration. [Abstract]

2025 Jun:236:116872. PMID: 40090596
Mol Cancer Ther

PARP7 Inhibitors and AHR Agonists Act Synergistically across a Wide Range of Cancer Models. [Abstract]

2025 Jan 2;24(1):56-68. PMID: 39313957
Mol Cancer Ther

A Whole-Genome CRISPR Screen Identifies AHR Loss as a Mechanism of Resistance to a PARP7 Inhibitor. [Abstract]

2022 Jul 5;21(7):1076-1089. PMID: 35439318
Cells

PARP7 and Mono-ADP-Ribosylation Negatively Regulate Estrogen Receptor α Signaling in Human Breast Cancer Cells. [Abstract]

2021 Mar 11;10(3):623. PMID: 33799807
Cell Oncol (Dordr)

PARP7 and aryl hydrocarbon receptor differentially regulate mammary cancer cell proliferation and STING-induced type I interferon signalling. [Abstract]

2025 Dec 23;49(1):3. PMID: 41432900
Toxicol Sci

2,3,7,8-Tetrachlorodibenzo-p-Dioxin (TCDD)-Inducible Poly-ADP-Ribose Polymerase (TIPARP/PARP7) Catalytic Mutant Mice (TiparpH532A) Exhibit Increased Sensitivity to TCDD-Induced Hepatotoxicity and Lethality. [Abstract]

2021 Aug 30;183(1):154-169. PMID: 34129049
Res Sq

PARP7 Suppresses Radiation-induced Necroptosis and Abscopal Immunity. [Abstract]

2025 Nov 7:rs.3.rs-7881707. PMID: 41282221
Methods Mol Biol

Quantification of PARP7 Protein Levels and PARP7 Inhibitor Target Engagement in Cells Using a Split Nanoluciferase System. [Abstract]

2023:2609:387-395. PMID: 36515849
University of Oslo

2021 Aug.

Solvent & Solubility

In Vitro:

DMSO : 200 mg/mL (382.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9105 mL

9.5524 mL

19.1048 mL

5 mM

0.3821 mL

1.9105 mL

3.8210 mL

10 mM

0.1910 mL

0.9552 mL

1.9105 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.78 mM); Clear solution

Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (3.97 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (3.97 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 4

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (3.97 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 5

Add each solvent one by one: 1% DMSO 99% Saline

Solubility: ≥ 0.5 mg/mL (0.96 mM); Clear solution

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. RBN-2397-Inhibiting PARP7, a Key monoPARP Cancer Dependency

[2]. Melissa Vasbinder, et al. RBN-2397: A First-in-Class PARP7 Inhibitor Targeting a Newly Discovered Cancer Vulnerability in Stress-Signaling Pathways.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9105 mL	9.5524 mL	19.1048 mL	47.7619 mL
	5 mM	0.3821 mL	1.9105 mL	3.8210 mL	9.5524 mL
	10 mM	0.1910 mL	0.9552 mL	1.9105 mL	4.7762 mL
	15 mM	0.1274 mL	0.6368 mL	1.2737 mL	3.1841 mL
	20 mM	0.0955 mL	0.4776 mL	0.9552 mL	2.3881 mL
	25 mM	0.0764 mL	0.3821 mL	0.7642 mL	1.9105 mL
	30 mM	0.0637 mL	0.3184 mL	0.6368 mL	1.5921 mL
	40 mM	0.0478 mL	0.2388 mL	0.4776 mL	1.1940 mL
	50 mM	0.0382 mL	0.1910 mL	0.3821 mL	0.9552 mL
	60 mM	0.0318 mL	0.1592 mL	0.3184 mL	0.7960 mL
	80 mM	0.0239 mL	0.1194 mL	0.2388 mL	0.5970 mL
	100 mM	0.0191 mL	0.0955 mL	0.1910 mL	0.4776 mL

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RBN-2397

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) RBN-2397

All PARP Isoforms

Biological Activity

Chemical Information

Publications (17)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

RBN-2397

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) RBN-2397

All PARP Isoforms

Biological Activity

Chemical Information

Publications (17)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

RBN-2397 Related Classifications

Cat. No.: HY-136174