RBN-2397 New

Name: RBN-2397
Brand: Tocris Bioscience
SKU: 9003

Tocris Bioscience, part of Bio-Techne | Catalog # 9003

COA / SDS

Potent and selective PARP7 inhibitor; induces antitumor immunity.

Key Product Details

Description:	Potent and selective PARP7 inhibitor; induces antitumor immunity.
Chemical Name:	5-[[(1S)-1-Methyl-2-[3-oxo-3-[4-[5-(trifluoromethyl)-2-pyrimidinyl]-1-piperazinyl]propoxy]ethyl]amino]-4-(trifluoromethyl)-3(2H)-pyridazinone
Purity:	≥98% (HPLC)
Molecular Weight:	523.44

View Full Technical Details for RBN-2397

Technical Data
Citations

Biological Activity for RBN-2397

RBN-2397 is a potent and selective PARP7 inhibitor. RBN-2397 inhibits PARP7 with an IC₅₀< 3 nM and K_D = 0.22 nM in a probe displacement assay and IC₅₀= 1 nM in a NanoBRET assay. It displays >500-fold selectivity over PARP12 and >50-fold selectivity over all other PARPs.

RBN-2397 inhibits MARylation of multiple intracellular proteins in PARP7-overexpressing SK-MES-1 cells with an IC₅₀ = 2 nM, showing a 300-fold window over the inhibition of PARylation in PARP1-activated HeLa cells. It restores the Type I interferon (IFN) response in tumor cells and induces antitumor immunity dependent on Type I IFN and CD8 cells. Significantly increases the number of cells in the G₀/G₁ phase of the cell cycle, indicative of a cell-cycle arrest.

RBN-2397 inhibits tumor growth at all dose levels and schedules in CT26 tumor-bearing, immunocompetent BALB/c mice. It slows tumor growth (TGI: 49-67%) in most xenograft models, with complete tumor regression in the NCI-H1373 xenograft.

RBN-2397 is orally bioavailable.

Technical Data for RBN-2397

M. Wt	523.44
Formula	C₂₀H₂₃F₆N₇O₃
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	2381037-82-5
PubChem ID	146047148
InChi Key	UQZCQKXJAXKZQH-LBPRGKRZSA-N
Smiles	FC(F)(C1=C(C=NNC1=O)N[C@@H](C)COCCC(N2CCN(C3=NC=C(C(F)(F)F)C=N3)CC2)=O)F

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for RBN-2397

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	26.17	50
	ethanol	2.62	5

Preparing Stock Solutions for RBN-2397

The following data is based on the product molecular weight 523.44.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.5 mM	3.82 mL	19.10 mL	38.21 mL
2.5 mM	0.76 mL	3.82 mL	7.64 mL
5 mM	0.38 mL	1.91 mL	3.82 mL
25 mM	0.08 mL	0.38 mL	0.76 mL

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References for RBN-2397

References are publications that support the biological activity of the product.

Chen PARP7 inhibitors and AHR agonists act synergistically across a wide range of cancer models. Mol.Cancer.Ther 2025 PMID: 39313957
Yang Induction of PARP7 creates a vulnerability for growth inhibition by RBN2397 in prostate cancer cells. Cancer Res.Comm. 2023 PMID: 37077937
Gozgit PARP7 negatively regulates the type I interferon response in cancer cells and its inhibition triggers antitumor immunity. Cancer Cell 2021 PMID: 34375612