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Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $1,520 | 10-14 weeks | |
50 mg | $1,980 | 10-14 weeks | |
100 mg | $2,500 | 10-14 weeks |
Description | PARP-1-IN-1 is a highly selective and orally active inhibitor of the enzyme PARP-1 with an IC50 of 0.96 nM, exhibiting excellent tolerance and significant activity in a single dose in the MDA-MB-436 xenotransplantation model [1]. |
In vitro | PARP-1-IN-1 (compound Y49) effectively inhibits various cancer cells over 48 hours, with IC50 values of 9.64, 123.5, and 106.3 μM for MX-1, MCF7, and A548 cells, respectively. At 2.5-10 μM concentrations, it significantly inhibits PARP-1 activity and reduces PAR production in A549 cells in a dose-dependent manner [1]. Western Blot Analysis confirms this, showing suppression of PARP-1 activity and decreased PAR levels at 2.5, 5, and 10 μM concentrations after 48-hour incubation [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 |
Cas No. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
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