2. Cell Cycle/DNA Damage Epigenetics
  3. PARP
  4. RBN-2397

RBN-2397 is a potent, accross species and orally active NAD+ competitive inhibitor of PARP7 (IC50<3 nM). RBN-2397 selectively binds to PARP7 (Kd=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.

RBN-2397 Chemical Structure

RBN-2397 Chemical Structure

CAS No. : 2381037-82-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 461 In-stock
Solution
10 mM * 1 mL in DMSO USD 461 In-stock
Solid
1 mg USD 160 In-stock
5 mg USD 400 In-stock
10 mg USD 600 In-stock
25 mg USD 980 In-stock
50 mg USD 1300 In-stock
100 mg USD 1700 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 8 publication(s) in Google Scholar

RBN-2397 Related Antibodies

Top Publications Citing Use of Products

View All PARP Isoform Specific Products:

View All Isoforms
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

RBN-2397 is a potent, accross species and orally active NAD+ competitive inhibitor of PARP7 (IC50<3 nM). RBN-2397 selectively binds to PARP7 (Kd=0.001 μM) and restores IFN signaling. RBN-2397 has the potential for the study of advanced or metastatic solid tumors[1][2].

IC50 & Target[2]

PARP-7

3 nM (IC50)

PARP-7

1 nM (Kd)

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.

RBN-2397 Related Antibodies

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 (t1/2) 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
Molecular Weight

523.43

Formula

C20H23F6N7O3
CAS No.
Appearance

Solid

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
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9105 mL 9.5524 mL 19.1048 mL
5 mM 0.3821 mL 1.9105 mL 3.8210 mL
View the Complete Stock Solution Preparation Table

* 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

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.86%

COA (245 KB) LCMS (263 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* 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.

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 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RBN-23972381037-82-5RBN2397RBN 2397PARPpoly ADP ribose polymeraseovarianadvancedmetastaticsolidtumorlungcarcinomasquamouscellNSCLCInhibitorinhibitorinhibit

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