2925182-32-5
Chemical Structure
PROTAC PARP2 degrader-1
- CAS No.: 2925182-32-5
- Formula:C43H50ClFN6O6
- Molecular Weight:801.35
InChIKey: FFDCUOYHHZSVET-UHFFFAOYSA-N
SMILES: O=C1NN=C(CC2=CC=C(C(C(N3CCN(CC3)C(CCCCCCCCCNC(COC4=CC=C5C(CCCN5C(CCl)=O)=C4)=O)=O)=O)=C2)F)C6=C1C=CC=C6
Biological Activity: PROTAC PARP2 degrader-1 is an orally active PARP2 PROTAC degrader with a DC50 of 2 μM. PROTAC PARP2 degrader-1 potently inhibits the enzymatic activities of PARP1 (IC50 = 2.74 nM) and PARP2 (IC50 = 0.32 nM), with approximately 10-fold higher selectivity for PARP2. PROTAC PARP2 degrader-1 induces cell cycle arrest and apoptosis, and exhibits significant anti-tumor efficacy in mouse models. PROTAC PARP2 degrader-1 can be used for the research of triple-negative breast cancer[1].
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PROTAC PARP2 degrader-1 | 95.86% | PROTAC PARP2 degrader-1 is an orally active PARP2 PROTAC degrader with a DC50 of 2 μM. PROTAC PARP2 degrader-1 potently inhibits the enzymatic activities of PARP1 (IC50 = 2.74 nM) and PARP2 (IC50 = 0.32 nM), with approximately 10-fold higher selectivity for PARP2. PROTAC PARP2 degrader-1 induces cell cycle arrest and apoptosis, and exhibits significant anti-tumor efficacy in mouse models. PROTAC PARP2 degrader-1 can be used for the research of triple-negative breast cancer. | ||||||||||||||||||||
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Keywords
