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PDD00017273 is a radiosensitizing PARG) inhibitor with antitumor or activity for the study of epithelial ovaries.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | $75 | In Stock | In Stock | |
| 10 mg | $139 | In Stock | In Stock | |
| 25 mg | $298 | In Stock | In Stock | |
| 50 mg | $447 | In Stock | In Stock | |
| 100 mg | $645 | - | In Stock | |
| 500 mg | $1,330 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $88 | In Stock | In Stock |
| Description | PDD00017273 is a radiosensitizing PARG) inhibitor with antitumor or activity for the study of epithelial ovaries. |
| Targets&IC50 | PARG:1.45 nM (Kd), PARG:26 nM |
| In vitro | PDD 00017273 is an effective inhibitor of PARG with an IC50 of 26 nM and a KD of 1.45 nM. At 10 μM, PDD 00017273 does not inhibit five common cytochrome P450 enzymes. At 30 μM, it moderately increases phosphorylated H2AX (γH2AX) intensity. Additionally, PDD 00017273 reduces NAD/H through PARG inhibition after DNA damage. The compound inhibits ZR-75-1 cells carrying wild-type BRCA1 and BRCA2 and exhibits weaker activity against MDA-MB-436 cells carrying the 5396 + 1G>A mutation in BRCA1[2].At 0.3 μM, PDD 00017273 inhibits the degradation of PAR polymers in MCF7 cells. It also reduces the viability of BRCA1, BRCA2, PALB2, FAM175A, and BARD1-depleted cells. PDD 00017273 halts replication forks and induces DNA damage requiring homologous recombination (HR) for repair[1]. |
| Molecular Weight | 514.62 |
| Formula | C23H26N6O4S2 |
| Cas No. | 1945950-21-9 |
| Smiles | Cc1cc(Cn2c3ccc(cc3c(=O)n(Cc3cnc(C)s3)c2=O)S(=O)(=O)NC2(C)CC2)n(C)n1 |
| Relative Density. | 1.52 g/cm3 (Predicted) |
| Storage | keep away from moisture,store at low temperature | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 40.83 mg/mL (79.34 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.89 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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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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