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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].
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 25 mg | $1,520 | 10-14 weeks | 10-14 weeks | |
| 50 mg | $1,980 | 10-14 weeks | 10-14 weeks | |
| 100 mg | $2,500 | 10-14 weeks | 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 |
| Smiles | #N/A |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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