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Background: BMN-673 is an orally bioavailable inhibitor of the nuclear enzyme poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity. PARP inhibitor BMN-673 selectively binds to PARP and prevents PARP-mediated DNA repair of single strand DNA breaks via the base-excision repair pathway. This enhances the accumulation of DNA strand breaks, promotes genomic instability and eventually leads to apoptosis. PARP catalyzes post-translational ADP-ribosylation of nuclear proteins that signal and recruit other proteins to repair damaged DNA and is activated by single-strand DNA breaks. BMN-673 has been proven to be highly active in mouse models of human cancer and also appears to be more selectively cytotoxic with a longer half-life and better bioavailability as compared to other compounds in development.
CAS Number: 1207456-00-5
Description: BMN 673 is a novel PARP inhibitor with IC50 of 0.58 nM(PARP1). It does not inhibit PARG and is highly sensitive to PTEN mutation. BMN-673 (8R,9S) is the (8R,9S) enantiomer of BMN-673.
Purity: ≥98% by HPLC
Solubility: Soluble in DMSO
Storage Stability: Store at or below -20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.
Target: PARP1
Biosafety Level: Not applicable (BSL-1)
References: 1. Shen Y, et al. Clin Cancer Res 2013; 19: 5003-5015.
2. Cardnell RJ, et al. Clin Cancer Res 2014; 20: 2237.
3. Murai J, et al. Mol Cancer Ther 2014; 13: 433-443.
4. Cardnell RJ, et al. Clin Cancer Res 2013; 19: 6322-6328.
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