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PARP-03
- Development stage
- Preclinical
- Lead developer
- Scienpharm
- Modality
- Small Molecules
01
Overview
PARP-03 is a small molecule poly(ADP-ribose) polymerase (PARP) inhibitor being developed by Fujian Boyue Pharmaceutical Technology (a subsidiary of Shanghai Scienpharm Biotechnology) for the treatment of cancer. Chemically known as 4-(3-(1,1-dioxothiomorpholine-4-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one, PARP-03 selectively and potently inhibits PARP1 and PARP2 enzyme activities. By blocking DNA single-strand damage repair, it causes the accumulation of DNA damage, ultimately leading to tumor cell death. In preclinical studies, PARP-03 demonstrated superior tumor growth inhibition compared to olaparib (AZD2281).
- Other names
- 4-(3-(1,1-dioxothiomorpholine-4-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one4-(3-(1,1-二氧代硫代吗啉-4-羰基)-4-氟苄基)酞嗪-1(2H)-酮
02
Targets
PARP1 (Poly (adp-ribose) polymerase 1)Pol II (RNA polymerase II elongation factors)
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