Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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].
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
You can also refer to dose conversion for different animals. More
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