产品名称 BMN-673 8R,9S - Inhibitors / Activators - PARP(s)
产品货号 27610-1
产品价格 现货询价,电话:010-67529703
产品规格 10 mg
产品品牌 bpsbioscience
产品概述
产品详情
MW: 380.4 Da
CAS Registry #: 1207456-00-5
Formula: C19H14F2N6O
Target: PARP1
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.
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.
Synonym(s):
(8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one
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.

Reference(s):
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.
Scientific Category:
PARP Inhibitor
Product Type:
Inhibitor
Data shown is lot-specific. Contact us for specific information on other lots.

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