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  5. R&D Systems™ RBN-2397

R&D Systems™ RBN-2397
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Catalog No. RD10188005 Shop All Novus Products
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RD10188005 50 mg
RD10187997 10 mg
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Catalog No. RD10188005 Supplier R&D Systems™ Supplier No. 9003/50

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Description

A Tocris product, part of R&D Systems. Potent and selective PARP7 inhibitor; induces antitumor immunity

RBN-2397 is a potent and selective PARP7 inhibitor (IC50< 3 nM, KD = 0.22 nM in a probe displacement assay; 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 (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 proportion of cells in the G0/G1 phase of the cell cycle. In xenograft models, it slows tumor growth (TGI: 49-67%), with complete tumor regression in the NCI-H1373 xenograft. RBN-2397 is orally bioavailable.

Specifications

Chemical Name or Material 5-[[(1S)-1-Methyl-2-[3-oxo-3-[4-[5-(trifluoromethyl)-2-pyrimidinyl]-1-piperazinyl]propoxy]ethyl]amino]-4-(trifluoromethyl)-3(2H)-pyridazinone
CAS 2381037-82-5
Quantity 50 mg
Product Line Tocris
Target Poly(ADP-ribose) Polymerase Inhibitors
Molecular Formula C20H23F6N7O3
Purity 98%
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