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Pamiparib (BGB-290) is an orally active, potent, highly selective PARP inhibitor with IC50 values of 0.9 nM for PARP1 and 0.5 nM for PARP2. It exhibits strong PARP trapping, has the capability to penetrate the brain, and is used for researching various cancers, including solid tumors.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $30 | In Stock | In Stock | |
| 2 mg | $40 | In Stock | In Stock | |
| 5 mg | $50 | In Stock | In Stock | |
| 10 mg | $70 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $58 | In Stock | In Stock |
| Description | Pamiparib (BGB-290) is an orally active, potent, highly selective PARP inhibitor with IC50 values of 0.9 nM for PARP1 and 0.5 nM for PARP2. It exhibits strong PARP trapping, has the capability to penetrate the brain, and is used for researching various cancers, including solid tumors. |
| Targets&IC50 | PARP2:0.5 nM, PARP1:0.9 nM |
| In vivo | Pamiparib, an investigational Poly (ADP-ribose) polymerase (PARP) inhibitor in clinical development, demonstrates excellent selectivity for both PARP1 and PARP2, and superb anti-proliferation activities in tumor cell lines with BRCA1/2 mutations or HR pathway deficiency (HRD).?Pamiparib has good bioavailability and is 16-fold more potent than olaparib in an efficacy study using BRCA1 mutated MDA-MB-436 breast cancer xenograft model.?Pamiparib also shows strong anti-tumor synergy with temozolomide (TMZ), a DNA alkylating agent used to treat brain tumors.?Compared to other PARP inhibitors, pamiparib demonstrated improved penetration across the blood brain barrier (BBB) in mice.?Oral administration of pamiparib at a dose as low as 3 mg/kg is sufficient to abrogate PARylation in brain tumor tissues.?In SCLC-derived, TMZ-resistant H209 intracranial xenograft model, combination of pamiparib with TMZ overcomes its resistance and shows significant tumor inhibitory effects and prolonged life span[1]. |
| Synonyms | BGB-290 |
| Molecular Weight | 298.31 |
| Formula | C16H15FN4O |
| Cas No. | 1446261-44-4 |
| Smiles | C[C@]12CCCN1Cc1n[nH]c(=O)c3cc(F)cc4[nH]c2c1c34 |
| Relative Density. | 1.68 g/cm3 (Predicted) |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 62.5 mg/mL (209.51 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.7 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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