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Polθ/PARP-IN-1 (compound 25d) is a potent dual inhibitor of DNA polymerase theta (Polθ) and PARP, with IC50 values of 45.6 nM and 5.4 nM, respectively. This compound exhibits antiproliferative activity, induces apoptosis and cell cycle arrest at the G2/M phase, leading to DNA damage, and demonstrates antitumor properties.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
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| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| Description | Polθ/PARP-IN-1 (compound 25d) is a potent dual inhibitor of DNA polymerase theta (Polθ) and PARP, with IC50 values of 45.6 nM and 5.4 nM, respectively. This compound exhibits antiproliferative activity, induces apoptosis and cell cycle arrest at the G2/M phase, leading to DNA damage, and demonstrates antitumor properties. |
| In vitro | Polθ/PARP-IN-1 (compound 25d) exhibits antiproliferative activity against HCC1937, MDA-MB-436, HCT116, SW48, SKOV-3, and MCF-10A cell lines with IC50 values of 20.9, 2.7, 8.9, 2.9, 18.9, and >80 µM, respectively. At a concentration of 2 µM over 3 days, this compound induces apoptosis and causes cell cycle arrest in the G2/M phase, leading to DNA damage. |
| In vivo | Polθ/PARP-IN-1, administered at doses of 20 or 40 mg/kg via intraperitoneal injection daily for 21 days, effectively inhibits tumor growth in the MDA-MB-436 xenograft model. |
| Formula | C38H33ClFN7O5S |
| 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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