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

RBN-2397 

Cat. No.: HY-136174 Purity: 99.45%
Handling Instructions

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

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5 mg USD 500 In-stock
Estimated Time of Arrival: December 31
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100 mg USD 2750 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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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].

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 (t1/2) of RBN-2397 in vivo is 325 mins[2].

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.

2381037-82-5

SMILES

O=C1C(C(F)(F)F)=C(N[[email protected]@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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (477.62 mM; Need ultrasonic)

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
10 mM 0.1910 mL 0.9552 mL 1.9105 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    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

  • 2.

    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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References

Purity: 99.45%

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Keywords:

RBN-2397RBN2397RBN 2397PARPpoly ADP ribose polymeraseovarianadvancedmetastaticsolidtumorlungcarcinomasquamouscellNSCLCInhibitorinhibitorinhibit

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RBN-2397
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HY-136174
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