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RBN-2397

SKU: orb1309170

Description

RBN-2397 is a highly potent and selective, orally bioavailable PARP7 inhibitor that competes with NAD+ across multiple species, exhibiting an IC50 below 3 nM. It is a valuable research tool for studying PARP7's role in cancer biology and has demonstrated antitumor activity in both cellular assays and in vivo models.

Research Area

Epigenetics & Chromatin, Molecular Biology

Images & Validation

Key Properties

CAS Number2381037-82-5
MW523.43
Purity99.36%
FormulaC20H23F6N7O3
SMILESC[C@@H](COCCC(=O)N1CCN(CC1)c1ncc(cn1)C(F)(F)F)Nc1cn[nH]c(=O)c1C(F)(F)F
TargetPARP
Solubility10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (9.55 mM);DMSO:247 mg/mL (471.89 mM)

Bioactivity

Target IC50
PARP7:1 nM (Kd)|PARP7:3 nM (IC50)
In Vivo
RBN-2397 oral administration induces tumor-specific adaptive immune memory in CT26 syngeneic model with durable complete responses in CT26 tumor-bearing BALB/c mice.RBN-2397 oral administration 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.The half-life (t1/2) of RBN-2397 in vivo is 325 mins.
In Vitro
Inhibition of PARP7 with RBN-2397 can potently inhibit the growth of cancer cells and restore interferon signaling, effectively releasing the brake cancer uses to hide from the immune system and suppress both innate and adaptive immune mechanisms.RBN-2397 inhibits cells proliferation(IC50 value of 20 nM in NCI-H1373 lung cancer cells), 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,and inhibits cell MARylation in a cell biochemial assay with an EC50 value of 1 nM.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

cell, carcinoma, advanced, ovarian, NSCLC, metastatic, PARP, PARP7, PARP-7, lung, Inhibitor, inhibit, squamous, solid, RBN 2397, RBN2397, RBN-2397, poly ADP ribose polymerase, tumor

Similar Products

  • RBN-2397 [orb1220249]

    >98% (HPLC)

    2381037-82-5

    523.43

    C??H??F?N?O?

    5 mg, 10 mg, 25 mg, 100 mg, 500 mg, 1 g, 50 mg
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Key Properties

No computed properties available.

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RBN-2397 (orb1309170)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

1 mg
$ 140.00
2 mg
$ 190.00
5 mg
$ 280.00
1 ml x 10 mM (in DMSO)
$ 320.00
10 mg
$ 430.00
25 mg
$ 840.00
50 mg
$ 1,110.00
100 mg
$ 1,420.00
200 mg
$ 1,900.00
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