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PARP-1-IN-1

Catalog No. T61798

PARP-1-IN-1 is a highly selective and orally active inhibitor of the enzyme PARP-1, with an IC50 value of 0.96 nM. It exhibits excellent tolerance and demonstrates significant activity in a single dose in the MDA-MB-436 xenotransplantation model [1].

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
PARP-1-IN-1 Chemical Structure
PARP-1-IN-1, CAS N/A
Pack Size Availability Price/USD Quantity
25 mg 10-14 weeks $ 1,520.00
50 mg 10-14 weeks $ 1,980.00
100 mg 10-14 weeks $ 2,500.00
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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
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Biological Description
Chemical Properties
Storage & Solubility Information
Description PARP-1-IN-1 is a highly selective and orally active inhibitor of the enzyme PARP-1, with an IC50 value of 0.96 nM. It exhibits excellent tolerance and demonstrates significant activity in a single dose in the MDA-MB-436 xenotransplantation model [1].
In vitro PARP-1-IN-1 (compound Y49), over a 48-hour period, demonstrates effective inhibition of various cancer cells, with IC50 values of 9.64, 123.5, and 106.3 μM for MX-1, MCF7, and A548 cells, respectively. At concentrations ranging from 2.5 to 10 μM, it notably inhibits PARP-1 activity and decreases PAR production in A549 cells, exhibiting dose-dependent efficacy [1]. Western Blot Analysis confirms that PARP-1-IN-1, at 2.5 μM, 5 μM, and 10 μM concentrations and following a 48-hour incubation, successfully suppresses PARP-1 activity and lowers PAR levels in cancer cells, demonstrating its dose-dependent nature [1].
In vivo PARP-1-IN-1 (Compound Y49) administered orally at a dosage of 50 mg/kg/day for 18 days significantly inhibits the growth of MDA-MB-436 tumors in female athymic BALB/c nude mice without causing a significant change in the body weight of the treated mice. This finding highlights the compound's potential as a targeted therapy for this tumor model.
Molecular Weight 392.47
Formula C23H25FN4O

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

PARP-1-IN-1 inhibitor inhibit

 

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