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Lerzeparib

Chemical Structure : Lerzeparib

CAS No.: 2459693-01-5

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Lerzeparib (TQB-3823,TQB3823)

Catalog No.: PC-23088Not For Human Use, Lab Use Only.

Lerzeparib (TQB3823) is a novel, potent and selective PARP inhibitor with IC50 of  2.8/0.9/629.3 nM for PARP1/PARP2/Tankyrase 1, respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

Lerzeparib (TQB3823) is a novel, potent and selective PARP inhibitor with IC50 of  2.8/0.9/629.3 nM for PARP1/PARP2/Tankyrase 1, respectively.
Lerzeparib (TQB3823) inhibits proliferation of BRCA1 mutant MDA-MB-436 cell with IC50 of 9.6 nM, shows little anti-proliferative activity in BRCA-wild type MDA-MB-231 cell with IC50 >10 μM. 
Lerzeparib (TQB3823) demonstrated antitumor efficacy in dose dependent fashions with tumor regression was observed at 25 mg/kg in MDA-MB-436 CDX model. 

Physicochemical Properties

M.Wt 365.41
Formula C21H20FN3O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

8-Fluoro-1,3-dihydro-2-[4-[(2R)-2-methyl-2-pyrrolidinyl]phenyl]pyrrolo[4,3,2-ef][3,2]benzoxazepin-6(5H)-one

References

1. Hu Yanbin, et al. Cancer Res (2021) 81 (13_Supplement): 2054.

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